| Anesthetics |
GENERAL |
Desflurane |
Suprane |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic |
| ANESTHETICS |
GENERAL |
Etomidate |
Amidate |
BAD! |
www.porphyria-europe.com: Unsafe
web.uct.ac.za/depts/porphyria/: Avoid
www.uq.edu.au/porphyria/: Unsafe in animals
Br J Anaesth 1985;57:420. Unsafe in animals |
| ANESTHETICS |
GENERAL |
Isoflurane |
Forane |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use with Caution
www.uq.edu.au/porphyria/: Unsafe in animals |
| ANESTHETICS |
GENERAL |
Ketamine |
Ketalar |
BAD! |
www.drugs-porphyria.org: Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Caution
www.uq.edu.au/porphyria/: Probably safe
Br J Anaesth 1985;57:420. Safe in animals |
| Anesthetics |
GENERAL |
Midazolam |
Versed |
OK? |
www.drugs-porphyria.org: Possibly Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use with Caution
www.uq.edu.au/porphyria/: Cell culture - Safe
Substrate of CYP3A4. Transactivates pregnane X receptor, but low probability of CYP3A4 induction (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; Curr Drug Metab 7:375,2006; Curr Drug Metab 9:827,2008) |
| ANESTHETICS |
GENERAL |
Propofol |
Diprivan |
OK! |
www.porphyria-europe.com: safe
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in patients
Anaesthesia 1992;47:355 Safe
Anaesthesia 1988;43:1022. Safe in patients |
| ANESTHETICS |
GENERAL |
Sevoflurane |
Ultane |
OK! |
www.drugs-porphyria.org: Possibly Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Caution
Pediat Anesthes 2005;15:426. Safe
USP DI? Drug Info. for the Health Care Pro. - 26th Ed. (2006): Only 5% is metabolized, primarily by CYP2E1 (not CYP3A or 2C9) |
| Anesthetics |
General |
Thiamylal |
Surital |
BAD! |
Barbiturate drug |
| Anesthetics |
GENERAL |
Thiopental |
Pentothal |
BAD! |
www.drugs-porphyria.org: Porphyrinogenic
www.porphyria-europe.com: Unsafe
web.uct.ac.za/depts/porphyria/: Avoid
See Phenobarbital |
| ANESTHETICS |
LOCAL |
Benzocaine |
Many |
NO INFO |
|
| ANESTHETICS |
LOCAL |
Bupivacaine |
Many |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in animals
Medicine (Balt) 1992;71:1. Safe |
| ANESTHETICS |
LOCAL |
Chloroprocaine |
Nesacaine |
NO INFO |
|
| ANESTHETICS |
LOCAL |
Dibucaine |
Nupercainal |
NO INFO |
|
| ANESTHETICS |
LOCAL |
Ethyl chloride |
Ethyl Chloride |
OK! |
|
| ANESTHETICS |
LOCAL |
Prilocaine |
Citanest |
OK! |
www.drugs-porphyria.org: Possibly Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Unsafe in patients
Medicine (Balt) 1992;71:1. Safe |
| ANESTHETICS |
LOCAL |
Procaine |
Many |
OK! |
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in patients |
| ANESTHETICS |
LOCAL |
Ropivacaine |
Naropin |
OK? |
www.drugs-porphyria.org: Possibly Porphyrinogenic. Substrate of CYP 1A. Use with care in doses >2 mL (of 10 mg/mL solution)
Clin Pharmacol Ther 1998;64:484. Mostly metabolized by CYP1A2 |
| ANESTHETICS |
LOCAL |
Tetracaine |
Many |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in animals |
| Anesthetics |
MUSCLE RELAXANTS |
Baclofen |
Many |
OK? |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
http://www.bio.net/bionet/hypermail/neur-sci/2005-July/060879.html: Ca. 85% is excreted unchanged, and ca. 15% of the dose is metabolized primarily by deamination |
| Anesthetics |
MUSCLE RELAXANTS |
Cyclobenzaprine |
Flexeril |
BAD? |
www.drugs.com: Metabolized by CYP3A4; forms ligand with PXR
Williams DA. Drug metabolism. In: Foye?s Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007. Substrate of CYP3A4 |
| ANESTHETICS |
MUSCLE RELAXANTS |
Doxacurium |
Nuromax |
NO INFO |
|
| ANESTHETICS |
MUSCLE RELAXANTS |
Pancuronium |
Pavulon |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Probably safe |
| ANESTHETICS |
MUSCLE RELAXANTS |
Succinylcholine |
Anectine |
OK? |
Patient report: Safe |
| ANESTHETICS |
MUSCLE RELAXANTS |
Vecuronium |
Norcuron |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Caution |
| ANTI-INFECTIVES |
AMINOGLYCOSIDES |
Amikacin |
Amikin |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use
PV Tishler MD clinical data: Safe |
| ANTI-INFECTIVES |
AMINOGLYCOSIDES |
Gentamicin |
Many |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in patients and animals |
| ANTI-INFECTIVES |
AMINOGLYCOSIDES |
Neomycin |
Many |
OK? |
|
| ANTI-INFECTIVES |
AMINOGLYCOSIDES |
Streptomycin |
Many |
OK! |
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe
www.porphyriafoundation.com: Safe |
| ANTI-INFECTIVES |
AMINOGLYCOSIDES |
Tobramycin |
Many |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use
S Afr Med J 1984;65:924. Safe in patients |
| Anti-infectives |
Animycobacterial agents |
Rifapentine |
Priftin |
BAD! |
Induces CyP3A, 2C9, ALA synthase (analogous to rifampicin) |
| Anti-infectives |
anthelmintics |
albendazole |
multiple |
BAD? |
poorly absorbed from GI tract; but signif metabolsim by CyP3A4. Poor data.(Eur. J. Clin Pharm 71:528, 2011) |
| Anti-infectives |
anthelmintics |
mebendazole |
multiple |
No info |
Poorly absorbed from GI tract. Probably metabolised by P450. |
| ANTI-INFECTIVES |
ANTIFUNGALS |
Amphotericin B |
Amphotec |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic/Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use with Caution
www.uq.edu.au/porphyria/: Safe in cell culture |
| ANTI-INFECTIVES |
ANTIFUNGALS |
Carbamide Peroxide |
Debrox |
OK? |
www.drugs-porphyria.org: Not Porphyrinogenic |
| ANTI-INFECTIVES |
ANTIFUNGALS |
Caspofungin |
Cancidas |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
www.rxlist.com: Metabolized by hydrolysis and N-acetylation |
| Anti-infectives |
ANTIFUNGALS |
Clotrimazole |
none |
OK? |
www.drugs-porphyria.org: Probably Not /Possibly Porphyrinogenic
Comp Biochem Physiol C Toxicol Pharmacol 2005;140:403. Induces CYP3A. Did not affect expression of PXR and MDR1 in zebrafish. Inhibits constituitive androstene receptor. |
| Anti-infectives |
ANTIFUNGALS |
Fluconazole |
Diflucan |
BAD! |
www.drugs-porphyria.org: Probably Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
Inhibits Cyt3A,2C9, and pregnane X receptor. 3 Patient reports: Unsafe. |
| ANTI-INFECTIVES |
ANTIFUNGALS |
Flucytosine |
Ancobon |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in cell culture
www.porphyriafoundation.com: Safe |
| Anti-infectives |
ANTIFUNGALS |
Griseofulvin |
Many |
BAD! |
www.porphyria-europe.com: Unsafe
web.uct.ac.za/depts/porphyria/: Avoid
www.uq.edu.au/porphyria/: Unsafe in patients
www.porphyriafoundation.com: Unsafe. Induces CYP3A |
| Anti-infectives |
ANTIFUNGALS |
Itraconazole |
Sporanox |
BAD! |
www.drugs-porphyria.org: Probably Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007. substrate & inhibitor of CYP3A4 |
| Anti-infectives |
ANTIFUNGALS |
Ketoconazole |
Many |
BAD! |
www.drugs-porphyria.org: Porphyrinogenic
www.porphyria-europe.com: Unsafe
web.uct.ac.za/depts/porphyria/: Avoid
www.uq.edu.au/porphyria/: Unsafe in cell culture
Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007. Substrate & inhibitor of CYP3A4. Inhibitor of pregnane X receptor & constit. androstene receptor. |
| Anti-infectives |
ANTIFUNGALS |
Metronidazole |
Flagyl |
BAD? |
www.drugs-porphyria.org: Probably Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
www.uq.edu.au/porphyria/: probably safe
J Neurol Neurosurg Psychiat 1997;62:421.
Sinz: Cur Drug Metab 2006; 7:375: no human pregnane X receptor activation.
Unsafe in patients. 1 patient: safe |
| Anti-infectives |
ANTIFUNGALS |
Micafungin |
Mycamine |
OK? |
Metab by and weakely inhibits CYP3A. 3A is not major path. |
| Anti-infectives |
ANTIFUNGALS |
Miconazole |
Monistat, others |
BAD? |
www.drugs-porphyria.org: Probably Not Porphyrinogenic/Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Avoid
www.uq.edu.au/porphyria/: Unsafe in cell culture |
| Anti-infectives |
ANTIFUNGALS |
Nystatin |
Many |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
USP DI? Drug Info. for the Health Care Pro. - 26th Ed. (2006): No P450 metabolism |
| ANTI-INFECTIVES |
ANTIFUNGALS |
Posaconazole |
Noxafil |
NO INFO |
|
| Anti-infectives |
ANTIFUNGALS |
Terbinafine |
Lamisil |
BAD? |
www.drugs-porphyria.org: Oral -Probably Porphyrinogenic. Topical - ok.
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution.
Vickers, Drug Metab Disp 1999; 27:1029: Main metab via CYP2C9, 1A2, 3A4.
Sinz M. Cur Drug Metab 2006; 7:375: High activation of pregnane X receptor but low prediction of clinical induction.
(This is given over a ca. 3 month period, so acute experimental data may not be relevant.) |
| Anti-infectives |
ANTIFUNGALS |
Terconazole |
Terazol |
No info |
Induces pregnane X receptor. |
| Anti-infectives |
ANTIFUNGALS |
Voriconazole |
Vfend |
BAD! |
www.drugs-porphyria.org: Probably Porphyrinogenic
Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007. Substrate of & inhibits CYP3A4 & 2C9. |
| ANTI-INFECTIVES |
ANTIMALARIALS |
Atovaquone |
Mepron |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
www.porphyria-europe.com: Safe
http://www.pharmgkb.org/: Not much is metabolized |
| Anti-infectives |
ANTIMALARIALS |
Chloroquine |
Many |
OK? |
www.drugs-porphyria.org: Possibly Porphyrinogenic, Compare the 8-aminoquioline primaquine: Inducer of CYPs 1A1, 1A2 and 1B1. No data pointing to clinically significant CYP-inducing properties. Conflicting references. One report of possible porphyrinogenicity.
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Probably safe
Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007. Substrate of CYP3A4 |
| ANTI-INFECTIVES |
ANTIMALARIALS |
Hydroxychloroquine |
Plaquenil |
OK? |
www.drugs-porphyria.org: Possibly Porphyrinogenic. Partly CYP-metabolized. Compare the 8-aminoquinoline primaquine: Inducer of CYPs 1A1, 1A2 and 1B1 |
| ANTI-INFECTIVES |
ANTIMALARIALS |
Mefloquine |
Lariam |
OK! |
www.drugs-porphyria.org: Possibly Porphyrinogenic. Substrate for CYP 3A4. No clinical observations pointing to CYP-induction. Compare the other methanolquinoline quinine: Inducer of CYPs 1A1, 1A2 and 2C9. Activator/stimulator of CYP 3A4. Inhibitor of CYPs e.g. 1A1 (potent). |
| ANTI-INFECTIVES |
ANTIMALARIALS |
Primaquine |
Primaquine |
OK! |
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in patients |
| Anti-infectives |
ANTIMALARIALS |
Proguanil |
Malarone (also contains atovaquone) |
OK! |
www.drugs-porphyria.org: Possibly Porphyrinogenic, substrate of CYP2C19, 1A2, 3A4; no clinical observations pointing to CYP induction
web.uct.ac.za/depts/porphyria/: Use |
| ANTI-INFECTIVES |
ANTIMALARIALS |
Pyrimethamine |
Daraprim |
OK! |
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use |
| Anti-infectives |
ANTIMALARIALS |
Quinine Sulfate |
Many |
OK? |
www.drugs-porphyria.org: Possibly Porphyrinogenic. Metab. by CYP3A. Inducer of 2C9. Possible activator/stimulator of CYP 3A4. 1Aweb.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in patients
S Afr Med J 1988;74:321. Safe in patients
Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007. Substrate of CYP3A4 |
| Anti-infectives |
antimycobacterial |
rifampicin |
none |
|
|
| ANTI-INFECTIVES |
ANTIMYCOBACTERIAL AGENTS |
Ethambutol |
Myambutol |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use |
| ANTI-INFECTIVES |
ANTIMYCOBACTERIAL AGENTS |
Isoniazid |
Many |
BAD! |
www.drugs-porphyria.org: Probably Porphyrinogenic. Inhibitor of CYP 1A2, 2A6, 2C19, 3A4. Several references warn against its use
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
www.uq.edu.au/porphyria/: Probably unsafe |
| ANTI-INFECTIVES |
ANTIMYCOBACTERIAL AGENTS |
Pyrazinamide |
Many |
BAD! |
www.porphyria-europe.com: Unsafe
web.uct.ac.za/depts/porphyria/: Avoid
www.uq.edu.au/porphyria/: unsafe in patients
www.porphyriafoundation.com: Unsafe |
| Anti-infectives |
ANTIMYCOBACTERIAL AGENTS |
Rifabutin |
Mycobutin |
BAD! |
www.drugs-porphyria.org: Probably Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
Substrate of CYP3A4. Induces CYP3A4 via pregnane X receptor transactivation (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; Arch Toxicol 82:667,2008; Cur Drug Metab 7:375,2006) |
| Anti-infectives |
ANTIMYCOBACTERIAL AGENTS |
Rifampin |
Rifadin |
BAD! |
Substrate of CYP3A4. Induces CYP3A4 via transactivation of pregnane X receptor (Cur Drug Metab 7:375,2006; Arch Toxicol 82:667,2008) |
| Anti-infectives |
ANTIPARASITICS |
Albendazole |
Many |
OK? |
web.uct.ac.za/depts/porphyria/: Use with Caution
Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007. Substrate of CYP3A4 |
| ANTI-INFECTIVES |
ANTIPARASITICS |
Iodoquinol |
Yodoxin |
NO INFO |
|
| ANTI-INFECTIVES |
ANTIPARASITICS |
Ivermectin |
Stromectol |
BAD? |
Xenabiotica 1998; 28: 313. Metabolized extensively by CYP3A4 |
| Anti-infectives |
ANTIPARASITICS |
Mebendazole |
Vermox |
OK? |
www.drugs-porphyria.org: Possibly Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Caution |
| Anti-infectives |
ANTIPARASITICS |
Praziquantel |
Many |
BAD! |
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007. Substrate of CYP3A4 |
| Anti-infectives |
ANTIPARASITICS |
Tinidazole |
Tindamax |
BAD? |
~75% metab by CYP3A4. Porphyrinogenic in vitro (Eur J Clin Pharmacol 59:429,2003) |
| Anti-infectives |
antiretroviral |
Telbivudine |
Tyzeka |
OK? |
Not metabolized; no P450 interaction (Medical Letter 49:11, 2007; Micromedex |
| ANTI-INFECTIVES |
ANTIRETROVIRALS |
Abacavir |
Ziagen |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
USP DI? Drug Info. for the Health Care Pro. - 26th Ed. (2006): No P450 metabolism |
| Anti-infectives |
ANTIRETROVIRALS |
Amprenavir |
Agenerase |
BAD! |
www.drugs-porphyria.org: Probably Porphyrinogenic. Substrate of CYP3A4. Induces CYP3A4 via transactivation of pregnane X receptor
(Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; Arch Toxicol 82:667,2008) |
| Anti-infectives |
ANTIRETROVIRALS |
Atazanavir |
Reyataz |
BAD? |
USP DI? Drug Info. for the Health Care Pro. - 26th Ed: Extensively metabolized by CYP3A4
Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007. Substrate of CYP3A4 |
| Anti-infectives |
ANTIRETROVIRALS |
Delavirdine |
Rescriptor |
BAD! |
www.drugs-porphyria.org: Probably Porphyrinogenic
Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007. Substrate of CYP3A4 |
| ANTI-INFECTIVES |
ANTIRETROVIRALS |
Didanosine |
Videx |
OK? |
www.drugs-porphyria.org: Probably Not Porphyrinogenic |
| Anti-infectives |
ANTIRETROVIRALS |
Efavirenz |
Sustiva |
BAD? |
www.drugs-porphyria.org: Probably Porphyrinogenic
Metab mainly by CYP2B6, with minor role for CYP3A4. Induces CYP2B6,3A4 via transactivation of constitutive androstane rerceptor & pregnane X receptor (Pharmacogenet Genomics 19:300, 2009; Arch Toxicol 82:667,2008; J Pharmacol Exp Therap 320:72,2007; Clin. Pharmacol. Ther. 91: 475, 2012). |
| Anti-infectives |
ANTIRETROVIRALS |
Emtricitabine |
Emtriva, Truvada |
OK? |
Blum MR: C Clin Pharm 2007; 47:751 - Primarily eliminated via renal excretion; 60-70% recovered unchanged. |
| ANTI-INFECTIVES |
ANTIRETROVIRALS |
Enfuvirtide |
Fuzeon |
OK? |
|
| Anti-infectives |
ANTIRETROVIRALS |
Indinavir |
Crixivan |
BAD! |
www.drugs-porphyria.org: Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007. Substrate,inducer and inhibitor of CYP3A4; pregnane X receptor inducer |
| ANTI-INFECTIVES |
ANTIRETROVIRALS |
Lamivudine |
Epivir |
OK? |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
www.drugs.com: 70% excreted as unchanged drug in urine |
| Anti-infectives |
ANTIRETROVIRALS |
Lopinavir/Ritonavir |
Kaletra |
BAD! |
Lopinavir
www.drugs-porphyria.org: Probably Porphyrinogenic
USP DI? Drug Info. for the Health Care Pro. - 26th Ed. (2006): Metabolized mainly by CYP3A, but metabolized by CYP2D6 if used with ritonavir.
Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007. Substrate of CYP3A4
Ritonavir
www.drugs-porphyria.org: Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution. Substrate of & inhibits CYP3A via human pregnane X receptor transactivation
(Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T CYP2C9, pregnane X receptor
Combination: Induces CYP2C9 |
| Anti-infectives |
ANTIRETROVIRALS |
Maraviroc |
Selzentry |
OK? |
~50% meetab but does not induce CYP3A4 (Brit J Clin Pharmacol 65S:5,2008; and 66:498,2008) |
| Anti-infectives |
ANTIRETROVIRALS |
Nelfinavir |
Viracept |
BAD? |
www.drugs-porphyria.org: Probably Porphyrinogenic
Williams DA: Op. Cit.: Substrate & inducer of CYP3A4, 2C9 |
| Anti-infectives |
ANTIRETROVIRALS |
Nevirapine |
Viramune |
BAD! |
www.drugs-porphyria.org: Probably Porphyrinogenic. >80% metab, by CYP3A4; also metab by CYP2B6. Induces CYP3A4 & 2B6 via transactivation of constitutive androstane receptor (Arch Toxicol 82:667,2008; Drug Metab Disp 8:895,1999; J Pharmacol Exp Therap 320:72,2007) |
| Anti-infectives |
ANTIRETROVIRALS |
Nilotinib |
Tasigna |
No info |
~30% metab by CYP3A4 (Clin Therapeutics 30:1956,2008) |
| Anti-infectives |
ANTIRETROVIRALS |
Raltegravir |
Isentress |
OK? |
No CYP meetabolism or induction (Drug Metab Disp 35:1657,2007) |
| Anti-infectives |
ANTIRETROVIRALS |
Ritonavir |
Norvir |
BAD! |
www.drugs-porphyria.org: Porphyrinogenic.
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution. Substrate of, induces and inhibits CYP3A via human pregnane X receptor transactivation(Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; Cur Drug Metab 7:375,2006; Arch Toxicol 82:667,2008) |
| ANTI-INFECTIVES |
ANTIRETROVIRALS |
Saquinavir |
Fortovase |
BAD! |
www.drugs-porphyria.org: Possibly Porphyrinogenic. CYP 3A4-metabolized. Inhibitor of CYP 3A4, seemingly not potent.
Williams DA. Drug metabolism. In: Foye?s Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007. Substrate of CYP3A4 |
| ANTI-INFECTIVES |
ANTIRETROVIRALS |
Stavudine |
Zerit |
NO INFO |
www.drugs-porphyria.org: Possibly Porphyrinogenic. Furanosyl pyrimidine derivative. No P450 metabolism |
| Anti-infectives |
ANTIRETROVIRALS |
Tenofovir |
Viread, Truvada |
OK? |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
USP DI? Drug Info. for the Health Care Pro. - 26th Ed: 70-80% eliminated as unchanged drug
http://redpoll.pharmacy.ualberta.ca/drugbank/: Not substrate of CYP3A4 or CYP2C9 |
| ANTI-INFECTIVES |
ANTIRETROVIRALS |
Zalcitabine |
Hivid |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use |
| ANTI-INFECTIVES |
ANTIRETROVIRALS |
Zidovudine |
Retrovir |
BAD? |
www.drugs-porphyria.org: Probably Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
www.uq.edu.au/porphyria/: Safe in patients |
| ANTI-INFECTIVES |
ANTIVIRALS |
Acyclovir |
Acyclovir |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
www.porphyria-europe.com: Safe
www.uq.edu.au/porphyria/: Safe in cell culture
Patient report: Safe |
| ANTI-INFECTIVES |
ANTIVIRALS |
Adefovir |
Hepsera |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
http://redpoll.pharmacy.ualberta.ca/drugbank/: Not a P450 substrate |
| ANTI-INFECTIVES |
ANTIVIRALS |
Amantidine |
Many |
NO INFO |
USP DI? Drug Info. for the Health Care Pro. - 26th Ed: not metabolized
www.rxlist.com: Primarily secreted as unchanged drug |
| ANTI-INFECTIVES |
ANTIVIRALS |
Famciclovir |
Famvir |
OK! |
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use |
| ANTI-INFECTIVES |
ANTIVIRALS |
Ganciclovir |
Cytovene |
OK! |
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use |
| ANTI-INFECTIVES |
ANTIVIRALS |
Interferon alfa-2B/Ribavirin |
Rebetron |
OK! |
??? |
| Anti-infectives |
ANTIVIRALS |
Oseltamivir |
Tamiflu |
OK? |
www.drugs-porphyria.org: Not Porphyrinogenic
Not a P450 substrate (USP DI? Drug Info. for the Health Care Pro. - 26th Ed; http://redpoll.pharmacy.ualberta.ca/drugbank/)
patient report: safe |
| Anti-infectives |
ANTIVIRALS |
Ribavirin |
Pegetron (also contains peginterferon) |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
USP DI? Drug Info. for the Health Care Pro. - 26th Ed: not p450 substrate
www.rxlist.com: Two pathways of metabolism: (i) reversible phosphorylation in nucleated cells; (ii) degradation via deribosylation and amide hydrolysis to yield a triazole carboxylic acid. Should not involve CYP3A4 or CYP2C9 |
| Anti-infectives |
ANTIVIRALS |
Valacyclovir |
Valtrex |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use
patient report: safe |
| ANTI-INFECTIVES |
ANTIVIRALS |
Zanamivir |
Relenza |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
http://redpoll.pharmacy.ualberta.ca/drugbank/: Not metabolized |
| Anti-infectives |
CEPHALOSPORIN |
Ceftaroline Fosamil |
Teflaro |
No info |
Incomplete information re metabolism (Drugs 69:809, 2009) |
| ANTI-INFECTIVES |
CEPHALOSPORINS |
Cefaclor |
Ceclor |
OK! |
web.uct.ac.za/depts/porphyria/: Use with Caution |
| ANTI-INFECTIVES |
CEPHALOSPORINS |
Cefazolin |
Ancef |
OK! |
web.uct.ac.za/depts/porphyria/: Use with Caution |
| ANTI-INFECTIVES |
CEPHALOSPORINS |
Cefepime |
Maxipime |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Caution |
| Anti-infectives |
CEPHALOSPORINS |
Cefotaxime |
Claforan |
OK? |
Probably not metab by CYP |
| ANTI-INFECTIVES |
CEPHALOSPORINS |
Cefotetan |
Cefotan |
OK! |
USP DI? Drug Info. for the Health Care Pro. - 26th Ed. (2006): Not metabolized by P450 |
| ANTI-INFECTIVES |
CEPHALOSPORINS |
Cefoxitin |
Mefoxin |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Caution |
| Anti-infectives |
CEPHALOSPORINS |
Cefpodoxime Proxetil |
Vantin |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Caution. Patient report: safe |
| Anti-infectives |
CEPHALOSPORINS |
Ceftazidime |
Fortaz |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Caution. Patient report: safe |
| ANTI-INFECTIVES |
CEPHALOSPORINS |
Ceftriaxone |
Rocephin |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Caution |
| ANTI-INFECTIVES |
CEPHALOSPORINS |
Cefuroxime |
Zinacef |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Caution |
| ANTI-INFECTIVES |
CEPHALOSPORINS |
Cephalexin |
Keflex |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Caution
Patient reports: Safe |
| ANTI-INFECTIVES |
CMV AGENTS |
Cidofovir |
Vistide |
OK? |
|
| ANTI-INFECTIVES |
CMV AGENTS |
Fosamprenavir |
Lexiva |
BAD? |
|
| ANTI-INFECTIVES |
CMV AGENTS |
Foscarnet |
Foscavir |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
USP DI? Drug Info. for the Health Care Pro. - 26th Ed. (2006): No P450 metabolism |
| ANTI-INFECTIVES |
CMV AGENTS |
Valganciclovir |
Valcyte |
OK! |
USP DI? Drug Info. for the Health Care Pro. - 26th Ed. (2006): Undergoes hydrolysis |
| Anti-infectives |
FLUOROQUINOLONES |
Ciprofloxacin |
Cipro |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
www.uq.edu.au/porphyria/: Safe in Patients
PV Tishler MD clinical data & patient reports: Safe
J Appl Toxicol 2005;25:339. Inhibits CYP3A |
| Anti-infectives |
FLUOROQUINOLONES |
Levofloxacin |
Levaquin |
OK? |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
PV Tishler MD clinical data & patient report: Safe
Drug Metab Disp 1996;24:1134. Undergoes limited metabolism
http://biocomp.health.unm.edu/ p450/metabP450diseasep3.pdf: Substrate of CYP1 family |
| ANTI-INFECTIVES |
FLUOROQUINOLONES |
Moxifloxacin |
Avelox |
OK? |
www.drugs-porphyria.org: Probably Not Porphyrinogenic |
| Anti-infectives |
FLUOROQUINOLONES |
Norfloxacin |
Noroxin |
OK? |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
www.uq.edu.au/porphyria/: Safe in cell culture
J Appl Toxicol 2005;25:339. Inhibits CYP3A |
| Anti-infectives |
MACROLIDES |
Azithromycin |
Zithromax |
OK? |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
www.porphyria-europe.com: Safe. 2 patient reports: safe
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
USP DI? Drug Info. for the Health Care Pro. - 26th Ed. (2006): Metabolized in liver, but 50% in bile unchanged & 35% metabolized by demethylation
Patient reports: safe |
| Anti-infectives |
MACROLIDES |
Clarithromycin |
Biaxin |
OK? |
www.drugs-porphyria.org: Possibly Porphyrinogenic. Inhibitor of CYP3A4 but forms irreversible complexes less readily than erythromycin. Some clinical experience of non-porphyrinogenicity. Two references state non- porphyrinogenicity.
web.uct.ac.za/depts/porphyria/: Use with Caution
www.uspharmacist.com: Inhibitor of CYP3A4
Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007: Substrate & inhibitor of CYP3A4
Sinz: Cur Drug Metab 2006; 7:375: no human pregnane X receptor activation |
| Anti-infectives |
MACROLIDES |
Erythromycin |
Many |
BAD! |
www.drugs-porphyria.org: Porphyrinogenic
www.porphyria-europe.com: Unsafe
web.uct.ac.za/depts/porphyria/: Avoid
www.uq.edu.au/porphyria/: Unsafe in patients
Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007: Substrate of, induces & inhibits CYP3A4.
Patient report: Unsafe |
| ANTI-INFECTIVES |
MISCELLANEOUS |
Aztreonam |
Azactam |
OK? |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
http://redpoll.pharmacy.ualberta.ca/drugbank/: Metabolized via hydrolysis |
| ANTI-INFECTIVES |
MISCELLANEOUS |
Bacitracin |
Many |
OK? |
|
| Anti-infectives |
MISCELLANEOUS |
Chloramphenicol |
Many |
BAD! |
www.drugs-porphyria.org: Porphyrinogenic
www.porphyria-europe.com: Unsafe
web.uct.ac.za/depts/porphyria/: Avoid
www.uq.edu.au/porphyria/: Unsafe in patients
Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007. Substrate of CYP2C9 |
| Anti-infectives |
MISCELLANEOUS |
Clindamycin |
Cleocin |
BAD? |
www.drugs-porphyria.org: Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Avoid
Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007. Substrate of & induces CYP3A4
Patient report: Safe |
| Anti-infectives |
MISCELLANEOUS |
Dapsone |
Leprostatic |
BAD! |
www.porphyria-europe.com: Unsafe
web.uct.ac.za/depts/porphyria/: Avoid
www.uq.edu.au/porphyria/: Unsafe in patients
Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007. Substrate of CYP3A4 & CYP2C9 |
| ANTI-INFECTIVES |
MISCELLANEOUS |
Daptomycin |
Cubicin |
NO INFO |
|
| Anti-infectives |
MISCELLANEOUS |
Fosfomycin |
Monurol |
OK? |
Mainly not metabolized (Ann Pharmacother 32:215,1998)
patient report: safe |
| ANTI-INFECTIVES |
MISCELLANEOUS |
Linezolid |
Zyvox |
OK? |
www.drugs-porphyria.org: Possibly Porphyrinogenic; insufficient data on metabolism but no indications for P450 interaction in vivo.
USP DI? Drug Info. for the Health Care Pro. - 26th Ed. (2006): Not metabolized by P450 |
| Anti-infectives |
MISCELLANEOUS |
Meropenem |
Meronem |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
www.rxlist.com: 70% excreted as unchanged drug |
| ANTI-INFECTIVES |
MISCELLANEOUS |
Mupirocin |
Bactroban |
OK? |
www.drugs-porphyria.org: Possibly Porphyrinogenic. Probably not significantly absorbed. Probably not metabolized by P450 |
| ANTI-INFECTIVES |
MISCELLANEOUS |
Polymyxin B |
Many |
OK? |
|
| ANTI-INFECTIVES |
MISCELLANEOUS |
Tigecycline |
Tygacil |
NO INFO |
|
| Anti-infectives |
MISCELLANEOUS |
Vancomycin |
Vancocin, Others |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in patients
Br J Clin Pharmacol 1990;29:273. Safe |
| Anti-infectives |
PENEM ANTIBIOTICS |
Doripenem |
Doribax |
OK! |
Not a CYP substrate (Clin Therapeut 31:42,2009) |
| Anti-infectives |
PENEM ANTIBIOTICS |
Ertapenem |
Invanz |
OK? |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
www.rxlist.com: Does not appear to undergo hepatic metabolism |
| Anti-infectives |
PENEM ANTIBIOTICS |
Imipenem/Cilastatin |
Primaxin |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
USP DI? Drug Info. for the Health Care Pro. - 26th Ed. (2006): Not metabolized by P450 |
| Anti-infectives |
PENICILLINS |
Amoxicillin |
Many |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in patients
PV Tishler MD clinical data & patient reports: Safe
Pregnane X receptor inducer. |
| Anti-infectives |
PENICILLINS |
Amoxicillin/ Clavulanate |
Augmentin |
OK! |
patient report: safe |
| ANTI-INFECTIVES |
PENICILLINS |
Ampicillin |
Many |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in patients |
| ANTI-INFECTIVES |
PENICILLINS |
Ampicillin/Sulbactam |
Unasyn |
NO INFO |
|
| ANTI-INFECTIVES |
PENICILLINS |
Carbenicillin |
Geopen |
NO INFO |
|
| Anti-infectives |
PENICILLINS |
Dicloxacillin |
Many |
OK? |
www.drugs-porphyria.org: Not Porphyrinogenic. Induces CYP3A. |
| Anti-infectives |
Penicillins |
flucloxacillin |
Floxapen, etc. |
BAD? |
Not metabolizd by or inhibits CYP3A, 2C9, but induces CYP3A, PXR |
| Anti-infectives |
PENICILLINS |
Nafcillin |
Many |
OK? |
http://medicine.iupui.edu/flockhart/table.htm: CYP3A inducer. |
| ANTI-INFECTIVES |
PENICILLINS |
Oxacillin |
Many |
OK? |
http://www.rxlist.com/cgi/generic3/oxacillin_cp.htm: Rapidly excreted as unchanged drug |
| ANTI-INFECTIVES |
PENICILLINS |
Penicillin |
Many |
OK! |
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in patients
Patient report: Safe |
| Anti-infectives |
PENICILLINS |
Piperacillin |
Zosyn, etc. |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use. Patient report: safe |
| ANTI-INFECTIVES |
PENICILLINS |
Ticarcillin |
Ticar |
OK! |
www.uq.edu.au/porphyria/: Safe in patients |
| ANTI-INFECTIVES |
SEPSIS SYNDROME AGENTS - NON-ANTIBIOTIC |
Drotrecogin alfa |
Xigris |
OK? |
www.drugs-porphyria.org: Not Porphyrinogenic |
| ANTI-INFECTIVES |
SULFONAMIDES |
Sulfadiazine |
Many |
BAD! |
www.porphyria-europe.com: Unsafe
www.uq.edu.au/porphyria/: Unsafe in patients
www.porphyriafoundation.com: Unsafe
Medicine (Balt) 1992;71:1. Unsafe |
| Anti-infectives |
SULFONAMIDES |
Sulfamethoxazole/ Trimethoprim |
Bactrim |
BAD! |
www.porphyria-europe.com: Unsafe
www.uq.edu.au/porphyria/: Unsafe in patients
www.porphyriafoundation.com: Unsafe
Medicine (Balt) 1992;71:1. Unsafe.
CYP2C9 substrate. Pregnane X receptor inducer. |
| ANTI-INFECTIVES |
SULFONAMIDES |
Sulfasalazine |
Azulfidine |
BAD! |
www.porphyria-europe.com: Unsafe
www.uq.edu.au/porphyria/: Unsafe in patients
www.porphyriafoundation.com: Unsafe
Medicine (Balt) 1992;71:1. Unsafe |
| ANTI-INFECTIVES |
TETRACYCLINES |
Demeclocycline |
Declomycin |
NO INFO |
www.drugs-porphyria.org: Probably Porphyrinogenic |
| Anti-infectives |
TETRACYCLINES |
Doxycycline |
Vibramycin, others |
OK? |
www.drugs-porphyria.org: Possibly Porphyrinogenic/Probably Not Porphyrinogenic. Induces Pgrenane X receptor.
web.uct.ac.za/depts/porphyria/: Avoid
2 patient reports: safe 1 patient report: unsafe |
| Anti-infectives |
TETRACYCLINES |
Minocycline |
Dynacin, Minocin |
No info |
www.uq.edu.au/porphyria/: Safe in cell culture |
| Anti-infectives |
TETRACYCLINES |
Tetracycline |
Many |
OK? |
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution. Induces CYP3A. 1 patient report: safe |
| Anti-infectives |
URINARY ANTI-INFECTIVES |
Methenamine Mandelate |
Many |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use
patient report: safe |
| Anti-infectives |
URINARY ANTI-INFECTIVES |
Nitrofurantoin |
Macrodantin, Macrobid |
BAD! |
www.drugs-porphyria.org: Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
www.uq.edu.au/porphyria/: Probably Unsafe |
| Anti-infectives |
ANTIRETROVIRALS |
nirmatrelvir tablets and ritonavir tablets |
PAXLOVID |
BAD! |
PAXLOVID ( nirmatrelvir tablets; ritonavir tablets
has not been approved, but has been authorized for emergency use by FDA under an EUA, for the treatment of mild-to-moderate COVID-19 in adults and pediatric patients (12 years of age and older weighing at least 40 kg) with positive results of direct SARS-CoV-2 viral testing, and who are at high risk for progression to severe COVID-19, including hospitalization or death. see comments on ritonavir in the drug database.
|
| Antidiabetics |
Biguanides |
Metformin |
Glucophage, others |
OK! |
www.drugs-porphyria.org: Not porphyrinogenic. www.porphyria-europe.com: Safe. web.uct.ac.za/depts/porphyria/: Use. www.uq.edu/au/porphyria/: Safe in animals. Excreted largely unchanged; no hepatic metab (www.clinicalpharmacology-ip.com).
Inhibits pregnane X receptor |
| Antidiabetics |
Dopamine Agonist |
Bromocriptine |
Cycloset |
BAD! |
See Bromocriptine, brand name Parlodel, in Central Nervous System Agents, Antiparkinson agents. |
| Antidiabetics |
DPP-4 Inhibitor |
Linagliptin |
Tradjenta, Jentadueto |
OK? |
>75% excreted unchanged. Major meteabolite created via CYP3A4, which is not induced (Drug Metab Disp 2010; 38:667). |
| Antidiabetics |
DPP-4 Inhibitors |
Saxagliptin |
Onglyza, Kombiglyze XR |
No info |
Primarily metab. by CYP3A4/5 (Clin Pharmacokinet 49:573, 2010) |
| Antidiabetics |
DPP-4 Inhibitors |
Sitagliptin |
Januvia |
OK? |
~80% not metab; rest mainly by CYP3A4 (Drug Metab Disp 35:523,2007) |
| Antidiabetics |
DPP-4 Inhibitors/ Biguanides |
Saxagliptin/ Metformin |
Kombiglyze XR |
No info |
See Saxagliptin |
| Antidiabetics |
DPP-4 Inhibitors/ Biguanidess |
Sitagliptin/ Metformin |
Janumet |
OK? |
See Sitagliptin |
| Antidiabetics |
GLP-1 Receptor Agonist |
Exenatide |
Byetta |
OK? |
Drug is a peptide, with peptide metabolism. Physicians' Desk Reference 2010; 64:648 |
| Antidiabetics |
GLP-1 Receptor Agonist |
Liraglutide |
Victoza |
OK? |
Polypeptide-fatty acid, metabolized enzymatically. Drug Metab Disp 2010; 38:1944. |
| Antidiabetics |
Insulin |
Insulin detmir |
Levemir |
OK! |
Insulin analog; insulins are ok. |
| Antidiabetics |
Insulins |
Insulins |
Insulin |
OK! |
www.drugs-porphyria.org: Not porphyrinogenic. www.porphyria-europe.com: Safe. web.uct.ac.za/depts/porphyria/: Use. www.uq.au/porphyria/: Safe in patients |
| Antidiabetics |
Meglitinides |
Repaglinide |
Prandin |
OK? |
Metab mainly by CYP2C8, less by CYP3A4. No evidence of inducing CYPs (Clin Pharmacol Therap 77:341,2005; Med Letter 51:41,2009) |
| Antidiabetics |
Meglitinides/ Biguanides |
Repaglinide/ Metformin |
PrandiMet |
OK? |
See Repaglinide |
| Antidiabetics |
Sulfonylureas |
Glimepiride |
Amaryl |
BAD? |
www.drugs-porphyria.org: Possibly porphyrinogenic. Substrate of CYP2C9. Significantly transactivates pregnane X receptor but has a low probability of inducing CYP3A4 (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; Curr Drug Meetab 7:375,2006) |
| Antidiabetics |
Sulfonylureas |
Glipizide |
Glucotrol |
BAD? |
www.drugs-porphyria.org: Possibly porphyrinogenic. www.porphyria-europe.com:Safe. web.uct.ac.za/depts/porphyria/: Use with Caution
www.uq.edu.au/porphyria/ : Unsafe in patients.
Metab by CYP2C9(Pharmacogenetics 9:71,1999) |
| Antidiabetics |
Sulfonylureas |
Glyburide |
Micronase, Diabeta, others |
OK? |
Medicine (Balt) 71:1,1992 - Safe. Major metab by CYP2C9, minor metab by CYP3A4. No evidence for CYP induction (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed Lemke T and Williams TA. Baltimore, Williams & Wilkins, 6th ed, 2007; Clin Pharm Therap 85:78,2008) |
| Antidiabetics |
Sulfonylureas/ Biguanides |
Glipizide/ Metformin |
Metaglip |
BAD? |
See Glipizide |
| Antidiabetics |
Sulfonylureas/ Biguanides |
Glyburide/ Metformin |
Glucovance |
OK? |
See Glyburide |
| Antidiabetics |
Thiazolidinediones |
Pioglitazone |
Actos |
BAD? |
www.drugs-porphyria.org: Probably porphyrinogenic. USP DI Drug Info. for the Health Care Pro. - 26th ED: Extensively metab by CYP2C8 & 3A4. Induces CYP3A4 & transactivates pregnane X receptor but at concns. higher than usual (Drug Metab Disp 31:439,2003;Curr Drug Metab 7:375,2006; Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; Drug Metab Dispos 31:439,2003; Mol Pharmavcol 80:518, 2011) |
| Antidiabetics |
Thiazolidinediones |
Rosiglitazone |
Avandia |
BAD? |
www.drugs-porphyria.org: Probably porphyrinogenic. Metab by CYP2C9, CYP2C8. Induces CYP3A4 & 2B6, & does transactivate pregnane X receptor (Pharmaceutical Res 23:1089,2006; Eur J Pharm Sci 11:185,2000; Drug Metab Disp 31:439,2003; Curr Drug Metab 7:375,2006) Patient report: Safe |
| Antidiabetics |
Thiazolidinediones/ Biguanides |
Pioglitazone/ Metformin |
Actoplus Met |
BAD? |
See Pioglitazone |
| Antidiabetics |
Thiazolidinediones/ Biguanides |
Rosiglitazone/ Metformin |
Avandamet |
BAD? |
See Rosiglitazone |
| ANTIDOTES |
n/a |
Deferoxamine |
Desferal |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
www.rxlist.com: Mostly metabolized by plasma enzymes |
| ANTIDOTES |
n/a |
Dimercaprol |
BAL |
OK! |
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe |
| ANTIDOTES |
n/a |
Edetate |
Many |
OK! |
|
| ANTIDOTES |
n/a |
Ipecac |
Many |
OK? |
|
| Antidotes |
n/a |
Physostigmine |
Antilirium, others |
OK? |
|
| Antidotes |
SMOKING CESSATION |
Varenicline |
Chantix |
OK? |
J Clin Pharmacol 2006; 46:991: not a human P450 substrate; mostly excreted unchanged in animals. |
| Antineoplastics |
ALKYLATING AGENTS |
Carboplatin |
Paraplatin |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Caution
No P450 metabolism. Does not induce CYP3A4 or transactivate pregnane X receptor (USP DI? Drug Info. for the Health Care Pro. - 26th Ed. (2006); Cancer Chemother Pharmacol 64:35,2009). Publ report: safe (Exp Opin Drug Saf 2008; 7:159) |
| Antineoplastics |
ANTIESTROGENS |
Tamoxifen |
Nolvadex |
BAD? |
www.drugs-porphyria.org: Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
www.uq.edu.au/porphyria/: Safe in patients
Metab by CYP3A4,2B6,2C9,2D6. Minimally to modestly transactivates pregnane X receptor; inhibits CYP (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; Curr Drug Metab 7:375,2006; Clin Therapeutics 30:1385,2008; Cancer Chemother Pharmacol 64:35,2009; Curr Drug Metab 9:598,2008) |
| Antineoplastics |
ANTIMETABOLITES |
Fluorouracil, 5-Fluorouracil |
Many |
OK? |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Caution. Safe in patients. Does not induce CYP3A4 or transactivate pregnane X receptor (S Afr Med J 65:924,1984; Cancer Chemother Pharmacol 64:35,2009). Pub rpt: safe (Exp Opin Drug Saf 2008; 7:159). Patient report:as skin cream, safe |
| Antineoplastics |
ANTIMETABOLITES |
Methotrexate |
Trexall, Rheumatrex, others |
OK? |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Caution
www.uq.edu.au/porphyria/: Unsafe in animals
S Afr Med J 1984;65:924. Safe in patients
Xenobiotica 1996;26:503. Limited or no interaction with CYP2C9 and CYP3A4 except for inhibition of Cyp3A. No effect on pregnane X receptor (Curr Drug Metab 7:375,2006; Drug Metab Dispos 32:348,2004) |
| Antineoplastics |
ENZYME INHIBITORS |
Imatinib |
Gleevac |
OK? |
www.drugs-porphyria.org: Possibly Porphyrinogenic
Metab by CYP3A4, less by 2C9; induces and inhibits both. Does not transactivate pregnane X receptor (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; Cancer Chemother Pharmacol 64:35,2009) |
| Antineoplastics |
MISC. |
Denosumab |
Xgeva |
OK! |
Antibody for skeletal mets., osteoporosis. |
| Antineoplastics |
MITOTIC INHIBITORS |
Docetaxel |
Taxotere, etc. |
OK? |
www.drugs-porphyria.org: Probably Porphyrinogenic.
Metab mainly by CYP3A4. Does not induce CYP3A, 2C9; weakly inhibits 3A. No to minimal transactivation of human pregnane X receptor (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; Pharmacogenetics 8:391,1998; Cur Drug Metab 7:375,2006; Cancer Chemother Pharmacol 64:35,2009. pt report pupblished: safe (Expert Opin Druf Saf 2008; 7:159.
Patient report: safe. |
| Antineoplastics |
MITOTIC INHIBITORS |
Etoposide |
Eposin, Etopophos, Vepesid |
BAD? |
www.drugs-porphyria.org: Probably Porphyrinogenic
www.uq.edu.au/porphyria/: Safe in patients
Extensively metab by & induces CYP3A4. Transactivates pregnane X receptor & induces CYP3A4 in several studies, but not in one study (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; Mol Pharmacol 2002;62:439; Clin Therapeutics 30; 1385,2008; Cancer Chemother Pharmacol 64:35,2009) |
| Antineoplastics |
Mitotic Inhibitors |
Gefitinib |
Iressa |
OK? |
Well absorbed. Metabolized by CYP3A. Does not induce/inhibit CYP3a, 2C9. |
| Antineoplastics |
MITOTIC INHIBITORS |
Paclitaxel |
Taxol |
BAD? |
www.drugs-porphyria.org: Probably Porphyrinogenic. Minor metabolism by,& induces CYP3A4. Transactivates and induces pregnane X receptor (Pharmacogenomics 8:803,2007; Clin Cancer Res 11: 6359,2005;
Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; Cancer Chemother Pharmacol 64:35,2009) |
| Antineoplastics |
NITROGEN MUSTARDS |
Cyclophosphamide |
Cytoxan |
OK? |
www.drugs-porphyria.org: Probably Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Caution
www.uq.edu.au/porphyria/: Unsafe in animals
S Afr Med J 1984;65:924. Safe in patients
Mainly metab by CYP2B6,~10% by CYP3A4. Minimally/moderately transactivates pregnane X receptor; strong constitutive androstane receptor activator. Does not induce CYP3A4, but does induce CYP2C9, CYP2B6 (Biochem Pharmacol 59:961,2000; Cancer Chemother Pharmacol 64:35,2009; Curr Drug Metab 9:598,2008; J Pharmacol Exp Therap 320:72, 2007)
Patient report: Safe |
| Antineoplastics |
TOPOISOMERASE I INHIBITORS |
Topotecan |
Hycamtin |
BAD? |
www.drugs-porphyria.org: Probably Porphyrinogenic. Does induce CYP3A4 and transactivate pregnane X receptor (Cancer Chemother Pharmacol 64:35,2009) |
| Antineoplastics |
TOPOSIOMERASE INHIBITORS |
irinotecan |
Camptosar |
BAD? |
Major metab by & inhibits CYP3A4, also by CYP2B6. Strongly induces both CYPs in some studies, but neither induces CYP3A4 or transactivates pregnane X receptor in another study (Clin Cancer Res 7:2182,2001; Clin Therapeutics 30:1385,2008; Cancer Chemother Pharmacol 64:35,2009) |
| Antineoplastics |
TROPOISOMERASE INHIBITORS |
Doxorubicin |
Doxil, Adriamycin |
OK! |
Does not induce CYPs or transactivate pregnane X receptor(Canad J Physiol Pharmacol 77:589,1999; Cancer Chemother Pharmacol 64:35,2009). Publ. report: safe (Exp Opin Drug Saf 2008; 7:159) |
| Antineoplastics (Cancer Therapies) |
ALKYLATING AGENTS |
Busulfan |
Myleran |
BAD! |
www.drugs-porphyria.org: Probably Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007. Substrate of CYP3A4 |
| Antineoplastics (Cancer Therapies) |
ALKYLATING AGENTS |
Cisplatin |
Platinol, Blastolem, others |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in patients
Does not induce CYP3A4 or trnasactivate pregnane X receptor (Cancer Chemother Pharmacol 64:35,2009). |
| ANTINEOPLASTICS (Cancer Therapies) |
ALKYLATING AGENTS |
Procarbazine |
Natulan |
BAD! |
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
S Afr Med J 1984;65:924. Safe in patients |
| ANTINEOPLASTICS (Cancer Therapies) |
ALKYLATING AGENTS |
Thiotepa |
Thioplex |
NO INFO |
|
| ANTINEOPLASTICS (Cancer Therapies) |
ANGIOGENESIS INHIBITORS |
Bevacizumab |
Avastin |
OK? |
|
| Antineoplastics (Cancer Therapies) |
ANTIANDROGENS |
Flutamide |
Eulexin |
BAD! |
www.drugs-porphyria.org: Possibly Porphyrinogenic. Possibly metabolised by P450. Possibly ALAS-inducer.
Metabolized by CYP3A or CYP2C9. Modestly transactivates pregnane X receptor and markedly induces CYP3A4 (J Gastroenterol 2006;41:231; Cancer Chemother Pharmacol 64:35,2009)
Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007. Substrate of CYP3A4 |
| Antineoplastics (Cancer Therapies) |
ANTIBIOTICS |
Actinomycin D or Dactinomycin |
Cosmegen |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
www.uq.edu.au/porphyria/: Safe in animals |
| ANTINEOPLASTICS (Cancer Therapies) |
ANTIBIOTICS |
Bleomycin |
Blenoxane |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
http://redpoll.pharmacy.ualberta.ca/drugbank/: Metabolized by CYP1A1 |
| Antineoplastics (Cancer Therapies) |
ANTIBIOTICS |
Idarubicin |
Idamycin |
BAD? |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution |
| ANTINEOPLASTICS (Cancer Therapies) |
ANTIBIOTICS |
Mitomycin |
Mutamycin |
BAD? |
www.drugs-porphyria.org: Possibly Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
Insufficient data on metabolism. Little systemic resorption; probably safe for intravesical installation |
| ANTINEOPLASTICS (Cancer Therapies) |
ANTIBIOTICS |
Mitoxantrone |
Novantrone |
BAD? |
www.drugs-porphyria.org: Possibly Porphyrinogenic. Insufficient data on metabolism Largely unmetabolized.
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution |
| ANTINEOPLASTICS (Cancer Therapies) |
ANTIBIOTICS |
Plicamycin |
Mithracin |
NO INFO |
|
| ANTINEOPLASTICS (Cancer Therapies) |
ANTIBODIES |
Alemtuzumab |
Campath |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
http://redpoll.pharmacy.ualberta.ca/drugbank/: Not metabolized |
| ANTINEOPLASTICS (Cancer Therapies) |
ANTIBODIES |
Cetuximab |
Erbitux |
OK? |
|
| ANTINEOPLASTICS (Cancer Therapies) |
ANTIBODIES |
Rituximab |
Rituxan |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
http://redpoll.pharmacy.ualberta.ca/drugbank/: No liver metabolism |
| ANTINEOPLASTICS (Cancer Therapies) |
ANTIESTROGENS |
Megestrol |
Megace |
BAD! |
|
| ANTINEOPLASTICS (Cancer Therapies) |
ANTIMETABOLITES |
Azacitidine |
Vidaza |
NO INFO |
|
| Antineoplastics (Cancer Therapies) |
ANTIMETABOLITES |
Capecitabine |
Xeloda |
OK? |
Not metab by CYP. Metab to 5-fluorouracil, which does not induce CYPs (Drug Metab Disp 32:762,2004; Canad J Physiol Pharmacol 74:150,1996) |
| ANTINEOPLASTICS (Cancer Therapies) |
ANTIMETABOLITES |
Capecitabine |
Xeloda |
NO INFO |
|
| ANTINEOPLASTICS (Cancer Therapies) |
ANTIMETABOLITES |
Cladribine |
Leustatin |
OK? |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
http://redpoll.pharmacy.ualberta.ca/drugbank/: Not P450 substrate |
| Antineoplastics (Cancer Therapies) |
ANTIMETABOLITES |
Cytarabine |
Alexan, Cytarabin, Cytocin, others |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
www.rxlist.com: Not P450 substrate |
| ANTINEOPLASTICS (Cancer Therapies) |
ANTIMETABOLITES |
Floxuridine |
FUDR |
OK? |
|
| Antineoplastics (Cancer Therapies) |
ANTIMETABOLITES |
Fludarabine |
Fludara, others |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
www.rxlist.com: Not P450 substrate |
| ANTINEOPLASTICS (Cancer Therapies) |
ANTIMETABOLITES |
Pemetrexed |
Alimta |
NO INFO |
|
| ANTINEOPLASTICS (Cancer Therapies) |
ANTIMETABOLITES |
Thioguanine |
Lanvis |
OK! |
S Afr Med J 1984;65:924. Safe in patients |
| Antineoplastics (Cancer Therapies) |
AROMATASE INHIBITORS |
Letrozole |
Femara |
BAD? |
www.drugs-porphyria.org: Possibly Porphyrinogenic. Administered in rather low dose.
CYP 3A4 and 2A6-mediated metabolism. Not an inhibitor of CYP19.
(Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007) |
| Antineoplastics (Cancer Therapies) |
ENZYME INHIBITORS |
Erlotinib |
Tarceva |
OK? |
Williams DA. ~70% metab by CYP3A4. Modestly transactivates pregnane X receptor but does not induce CYP3A4 (Eur J Clin Pharmacol 64:31,2008; Cancer Chemother Pharmacol 64:35,2009) |
| Antineoplastics (Cancer Therapies) |
ENZYME INHIBITORS |
Lapatinib |
Tykerb |
OK? |
Metab mainly by CYP3A4,3A5. No evidence for CYP induction (Drugs 67:2101,2007) |
| Antineoplastics (Cancer Therapies) |
ENZYME INHIBITORS |
Sorafenib |
Nexavar |
No info |
~50% metab by CYP3A4, ~50% not metab (PDR 63:784,2009) |
| Antineoplastics (Cancer Therapies) |
ENZYME INHIBITORS |
Sunitinib |
Sutent |
OK? |
~30% metab by CYP3A4, ~40% not metab (PDR 63:2540,2009; Medical Letter 49:18,2007). Does not induce CYPs (Clin Therapeutics 30:1385,2008) |
| ANTINEOPLASTICS (Cancer Therapies) |
ENZYMES |
Asparaginase |
Elspar |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Caution |
| ANTINEOPLASTICS (Cancer Therapies) |
HORMONAL AGENTS |
Diethylstilbestrol |
Many |
NO INFO |
|
| ANTINEOPLASTICS (Cancer Therapies) |
HORMONAL AGENTS |
Estramustine |
Emcyt |
BAD? |
www.drugs-porphyria.org: Probably Porphyrinogenic |
| ANTINEOPLASTICS (Cancer Therapies) |
HORMONAL AGENTS |
Testolactone |
Teslac |
NO INFO |
|
| Antineoplastics (Cancer Therapies) |
IMMUNOMODULATORS |
Levamisole |
Ergamisol |
No info |
|
| ANTINEOPLASTICS (Cancer Therapies) |
INTERLEUKINS |
Aldesleukin |
Proleukin |
OK? |
|
| ANTINEOPLASTICS (Cancer Therapies) |
KERATINOCYTE GROWTH FACTOR |
Palifermin |
Kepivance |
OK? |
|
| ANTINEOPLASTICS (Cancer Therapies) |
MISC. |
Arsenic Trioxide |
Trisenox |
NO INFO |
|
| ANTINEOPLASTICS (Cancer Therapies) |
MISC. |
Dacarbazine |
Dtic-Dome |
BAD? |
www.drugs-porphyria.org: Possibly Porphyrinogenic. Not porphyrinogenic in chick embryo model. Like chloroambucil, melphalan, may be safer than other alkylating agents. |
| ANTINEOPLASTICS (Cancer Therapies) |
MISC. |
Hydroxyurea |
Hydrea |
OK? |
S Afr Med J 1984;65:924. Safe in patients |
| ANTINEOPLASTICS (Cancer Therapies) |
MISC. |
Interferon Alfa-2A |
Roferon-A |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Caution
USP DI? Drug Info. for the Health Care Pro. - 26th Ed: Liver metabolism is minor pathway
http://medicine.iupui.edu/flockhart/table.htm: Inhibitor of CYP1A2 |
| ANTINEOPLASTICS (Cancer Therapies) |
MISC. |
Interferon Alfa-2B |
Intron A |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Caution
http://medicine.iupui.edu/flockhart/table.htm: Inhibitor of CYP1A2 |
| ANTINEOPLASTICS (Cancer Therapies) |
MISC. |
Interferon Gamma-1B |
Actimmune |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Caution
http://medicine.iupui.edu/flockhart/table.htm: Inhibitor of CYP1A2 |
| Antineoplastics (Cancer Therapies) |
MISC. |
Ixabepilone |
Ixempra |
BAD? |
Highly metab by and induces CYP3A4; weakly transactivates pregnane X receptor (Clin Cancer Res 14:2701,2008; S Mani, pers commun) |
| Antineoplastics (Cancer Therapies) |
MISC. |
oxaliplatin |
Eloxatin |
OK? |
No evidence for CYP metabolism (PDR 63:2731,2009) |
| ANTINEOPLASTICS (Cancer Therapies) |
MISC. |
Pentostatin |
Nipent |
NO INFO |
|
| Antineoplastics (Cancer Therapies) |
MITOTIC INHIBITORS |
Vinblastine |
Velban |
BAD? |
www.drugs-porphyria.org: Possibly Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
www.uq.edu.au/porphyria/: Probably safe in cell culture
Extensively metab by CYP3A4. Does not induce CYP3A4 or transactivate pregnane X receptor (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; Cancer Chemother Pharmacol 64:35,2009) |
| Antineoplastics (Cancer Therapies) |
MITOTIC INHIBITORS |
Vincristine |
Oncovin |
OK? |
www.drugs-porphyria.org: Possibly Porphyrinogenic. Porphyrinogenic in vitro. Administered in low weekly dose, probably insignificant hepatic exposure. Some clinical reports of non-porphyrinogenicity.
web.uct.ac.za/depts/porphyria/: Use with Caution
www.uq.edu.au/porphyria/: Probably safe in cell culture
S Afr Med J 1984;65:924. Safe in patients
USP DI? Drug Info. for the Health Care Pro. - 26th Ed. (2006): Metabolized by CYP3A4. Does not induce CYP3A4 or transactivate pregnane X receptor (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; Cancer Chemother Pharmacol 64:35,2009) |
| ANTINEOPLASTICS (Cancer Therapies) |
MITOTIC INHIBITORS |
Vinorelbine |
Navelbine |
BAD? |
www.drugs-porphyria.org: Possibly Porphyrinogenic. Substrate for CYP 3A4. No reports of CYP-induction in humans. Other vinca alkaloids have shown to be porphyrinogenic in vitro.
Drug Metab Dispos 2000;28:1121. Major interaction with CYP3A4 |
| ANTINEOPLASTICS (Cancer Therapies) |
NITROGEN MUSTARDS |
Chlorambucil |
Leukeran |
BAD! |
www.drugs-porphyria.org: Possibly Porphyrinogenic. Insufficient data on metabolism. Conflicting references. Considered better tolerated than other alkylating agents generally avoided. One case report of uneventful use in a 54 yr old patient with IAP.
web.uct.ac.za/depts/porphyria/: Avoid
www.uq.edu.au/porphyria/: Unsafe in animals |
| Antineoplastics (Cancer Therapies) |
NITROGEN MUSTARDS |
Ifosfamide |
Ifex |
BAD? |
www.drugs-porphyria.org: Probably Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
Substrate of CYP3A4. Modestly transactivates pregnane X receptor. Does not induce CYP3A4 but does induce CYP2B6(Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; Cancer Chemother Pharmacol 64:35,2009; Curr Drug Mdetab 9:598,2008) |
| ANTINEOPLASTICS (Cancer Therapies) |
NITROGEN MUSTARDS |
Mechlorethamine |
Mustargen |
NO INFO |
|
| ANTINEOPLASTICS (Cancer Therapies) |
NITROGEN MUSTARDS |
Melphalan |
Alkeran |
OK? |
www.drugs-porphyria.org: Possibly Porphyrinogenic. Not porphyrinogenic in experimental rat and chicken systems. Two references safe/probably safe.
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use with Caution
www.uq.edu.au/porphyria/: Probably safe |
| ANTINEOPLASTICS (Cancer Therapies) |
NITROSOUREAS |
Carmustine |
Bicnu |
NO INFO |
|
| ANTINEOPLASTICS (Cancer Therapies) |
NITROSOUREAS |
Lomustine |
Ceenu |
BAD! |
www.drugs-porphyria.org: Probably Porphyrinogenic
http://redpoll.pharmacy.ualberta.ca/drugbank: CYP3A4 substrate |
| ANTINEOPLASTICS (Cancer Therapies) |
NITROSOUREAS |
Streptozocin |
Zanosar |
NO INFO |
|
| ANTINEOPLASTICS (Cancer Therapies) |
RETINOIDS |
Tretinoin |
Retin-A |
OK? |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
Williams DA: Op. Cit.: Substrate of CYP3A4 |
| Antineoplastics (Cancer Therapies) |
Thyroid Cancer-Specific |
Radioactive Iodine (I-131) |
none |
OK! |
Patient experience |
| ANTINEOPLASTICS (Cancer Therapies) |
URINARY TRACT PROTECTIVE AGENTS |
Amifostine |
Ethyol |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
http://redpoll.pharmacy.ualberta.ca/drugbank/: No P450 metabolism |
| ANTINEOPLASTICS (Cancer Therapies) |
URINARY TRACT PROTECTIVE AGENTS |
Mesna |
Mesnex |
OK? |
www.drugs-porphyria.org: Probably Not Porphyrinogenic |
| Arthritis |
n/a |
none |
none |
|
|
| Arthritis |
n/a |
Abatacept |
Orencia |
OK! |
Protein. Not metab by CYPs (PDR 63:921,2009) |
| Arthritis |
n/a |
adalimumab |
Humira |
OK! |
Protein. Not metab by CYPs
(PDR 63:442,2009) |
| Arthritis |
n/a |
Celecoxib |
Celebrex |
BAD? |
www.drugs-porphyria.org: Possibly porphyrinogenic. Metab.~80% by CYP2D9, <25% by CYP3A4; transactivates pregnane X receptor & induces CYP3A4 (Clin Pharmacokinetics 42:283, 2003; Durg Metab Disp 33:1567,2005; Clin Pharm Therap 80:298,2006) |
| Arthritis |
n/a |
Certolizumab Pegol |
Cimzia |
OK! |
Protein + polyethylene glycol. Not metab by CYPs (PDR 63:3127,2009) |
| Arthritis |
n/a |
etanercept |
Enbrel |
OK! |
Protein. Not metab by CYPs
(PDR 63:569,2009) |
| Arthritis |
n/a |
Golimumab |
Simponi |
OK! |
Protein. No CYP metabolism |
| Arthritis |
n/a |
Leflunomide |
Arava |
No info |
Prob metab by CYPs (www.clinicalpharmacology-ip.com) |
| Arthritis |
n/a |
Allopurinol |
Zyloprim |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in animals
Patient reports: Safe |
| Arthritis |
n/a |
Auranofin |
Ridaura |
OK? |
www.drugs-porphyria.org: Possibly Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
www.uq.edu.au/porphyria/: Unsafe in patients |
| Arthritis |
n/a |
Aurothioglucose |
Solganal |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic |
| Arthritis |
n/a |
Colchicine |
Colsalide |
OK! |
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in patients
Int J Biochem 1985;17:937. Safe in patients
Substrate of CYP3A4 (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007) |
| Arthritis |
n/a |
Gold Sodium Thiomalate |
Myochrysin |
BAD! |
www.drugs-porphyria.org: Possibly Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
www.uq.edu.au/porphyria/: Unsafe in animals |
| Arthritis |
n/a |
Penicillamine |
Cuprimine |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: use
www.uq.edu.au/porphyria/: Safe in patients |
| Arthritis |
n/a |
Probenecid |
Benemid |
BAD? |
www.drugs-porphyria.org: Probably Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
www.uq.edu.au/porphyria/: Probably unsafe
Little to no induction of CYPs and no transactivation of pregnane X receptor (Curr Drug Metab 7:375,2006; Drug Metab Dispos 32:348,2004) |
| Arthritis |
n/a |
Sulfinpyrazone |
Many |
BAD! |
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
www.uq.edu.au/porphyria/: Unsafe in cell culture
Major metabolism by CYP3A4,2C9. Induces CYP3A4 via transactivation of
pregnane X receptor (Drug Metab Disp 29:701,2001; Arch toxicol 82:667,2008; Cur Drug Metab 7:375,2006). Inhibits CYP2C9. |
| Arthritis |
Gout Treatment |
Pegloticase |
Krystexxa |
OK! |
Protein enzyme, with no metabolic problem |
| Blood related |
ANTICOAGULANTS |
Dabigatran |
Pradaxa |
OK! |
No appreciable P450 metab. (Drug Metab Disp 36:386, 2008) |
| Blood related |
ANTICOAGULANTS |
Fondaparinux |
Arixtra |
OK? |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
USP DI? Drug Info. for the Health Care Pro. - 26th Ed: 77% eliminated unchanged. Patient report: safe |
| Blood related |
Bleeding retardant |
Tranexamic acid |
Lystela, etc. |
OK! |
Mostly excreted unchanged |
| Blood related |
Plasma Replacement |
Hydroxyethyl starch |
Voluven |
OK! |
Not metabolized in any injurious way. |
| BLOOD RELATED THERAPY |
ANTICOAGULANTS |
Abciximab |
Reopro |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic |
| BLOOD RELATED THERAPY |
ANTICOAGULANTS |
Argatroban |
Argatroban |
OK? |
USP DI? Drug Info. for the Health Care Pro. - 26th Ed: CYP3A4/5 is not an important elimination pathway |
| BLOOD RELATED THERAPY |
ANTICOAGULANTS |
Bivalirudin |
Angiomax |
OK? |
USP DI? Drug Info. for the Health Care Pro. - 26th Ed: Clearance from plasma does not seem to involve liver |
| Blood related therapy |
ANTICOAGULANTS |
Clopidogrel |
Plavix |
OK? |
Metab by a number of CYPs. CYP3A4 and 2C19 are probably the most important, but their relative contributions are unknown. Does not induce CYP3A4 (Drug Metab Pharmacokinet 23:412,2008; Drug Metab Rev 37:99,2005; WC Lau, Pers Commun; MP Knadler, Pers Commun) |
| BLOOD RELATED THERAPY |
ANTICOAGULANTS |
Dalteparin |
Fragmin |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic |
| BLOOD RELATED THERAPY |
ANTICOAGULANTS |
Dipyridamole |
Persantine |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in cell culture |
| BLOOD RELATED THERAPY |
ANTICOAGULANTS |
Enoxaparin |
Lovenox |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use |
| Blood related therapy |
ANTICOAGULANTS |
Eptifibatide |
Integrilin |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
Clin Ther 1998;20:307. Polypeptide; deamidation probably via hydrolysis, not inlving P450 |
| BLOOD RELATED THERAPY |
ANTICOAGULANTS |
Heparin |
Many |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in patients |
| Blood related therapy |
ANTICOAGULANTS |
Lepirudin |
Refludan |
OK! |
Polypeptide. Not metab by CYPs |
| BLOOD RELATED THERAPY |
ANTICOAGULANTS |
Protamine |
Protamine |
OK! |
|
| Blood related therapy |
ANTICOAGULANTS |
Ticlopidine |
Ticlid |
OK? |
www.drugs-porphyria.org: Probably Porphyrinogenic
http://medicine.iupui.edu/flockhart/table.htm: Similar to (and see discussion of) clopidogrel |
| BLOOD RELATED THERAPY |
ANTICOAGULANTS |
Warfarin |
Coumadin |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in patients
Williams DA. Drug metabolism. In: Foye?s Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007. Substrate of CYP3A4 & 2C9 |
| BLOOD RELATED THERAPY |
HEMATOPOIETICS |
Cyanocobalamin |
Vitamin B12 |
OK! |
www.drugs-porphyria.org: Probably Porphyrinogenic
PV Tishler, MD clinical data: Safe |
| BLOOD RELATED THERAPY |
HEMATOPOIETICS |
Epoetin Alfa |
Epogen |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
www.porphyria-europe.com: Safe |
| Blood related therapy |
HEMATOPOIETICS |
Filgrastim (G-CSF) |
Neupogen |
OK! |
(G-C web.uct.ac.za/depts/porphyria/)
www.drugs-porphyria.org: Not Porphyrinogenic |
| BLOOD RELATED THERAPY |
HEMATOPOIETICS |
Multivitamins |
Many |
OK! |
|
| BLOOD RELATED THERAPY |
HEMOSTATICS |
Aminocaproic Acid |
Amicar |
OK! |
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in patients |
| BLOOD RELATED THERAPY |
HEMOSTATICS |
Aprotinin |
Trasylol |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic |
| BONES |
BISPHOSPHONATES |
Alendronate |
Fosamax |
OK! |
USP DI? Drug Info. for the Health Care Pro. - 26th Ed. (2006): Not metabolized
Patient reports: safe |
| Bones |
Bisphosphonates |
Ibandronate |
Boniva |
OK? |
Bisphosphonates are not metabolized. |
| BONES |
BISPHOSPHONATES |
Zoledronic Acid |
Zometa |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
USP DI? Drug Info. for the Health Care Pro. - 26th Ed: No P450 inhibition in vitro |
| Bones |
Bisphosponates |
Risedronate |
Actonel |
OK? |
Bisphosphonates are not metabolized |
| Cardiovascular |
ACE INHIBITORS |
Enalapril (Enalaprilat) |
Vasotec |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
2 Patient reports: Safe
No transactivation of pregnane X receptor (Curr Drug Metab 6:375,2006) |
| Cardiovascular |
ACE INHIBITORS |
Lisinopril |
Prinivil |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
P4 atient reports: Safe
No transactivation of pregnane X receptor (Curr Drug Metab 6:375,2006) |
| Cardiovascular |
ACE INHIBITORS |
Ramipril |
Altace |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
Patient reports: Safe |
| Cardiovascular |
ANGIOTENSIN II RECEPTOR ANTAGONISTS |
Candesartan Cilexetil |
Atacand |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
www.porphyria-europe.com: Safe, Metab by CYP2C9. |
| Cardiovascular |
ANGIOTENSIN II RECEPTOR ANTAGONISTS |
Losartan |
Cozaar |
OK! |
www.drugs-porphyria.org: Possibly Porphyrinogenic.
>2 clinical reports: safe. Substrate of mainly CYP2C9, lesser of CYPs 3A4, 3A5. No data pointing to CYP induction. Safe in cell culture.
(Biochem Pharmacol 1999;58:887;Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007) |
| Cardiovascular |
ANGIOTENSIN II RECEPTOR ANTAGONISTS |
Olmesartan |
Benicar |
OK! |
Virtually not metabolized (PDR 63:1009,2009). 1 patient report: safe |
| Cardiovascular |
ANGIOTENSIN II RECEPTOR ANTAGONISTS |
Valsartan |
Diovan |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
USP DI? Drug Info. for the Health Care Pro. - 26th Ed: Some metabolism by CYP2C9.
Patient reports: Safe |
| Cardiovascular |
ANGIOTENSIN RECEPTOR ANTAGONISTS |
Eprosartan |
Teveten |
OK! |
98% excreted unchanged, 2% as glucuronide. |
| Cardiovascular |
ANTIADRENERGICS |
Doxazosin |
Cardura |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Caution
PV Tishler MD clinical data: Safe
Br J Clin Pharmacol 1997;43:339. Safe at <10mg/d.
patient report: safe (5 yrs) |
| Cardiovascular |
ANTIHYPERLIPIDEMIC AGENTS |
Atorvastatin |
Lipitor |
OK? |
www.drugs-porphyria.org: Patient report - safe
Mainly metab by CYP3A4, but very low likelihood of CYP3A4 induction (Clin Pharmacol Therap 80:565,2006; Curr Drug Metab 7:375,2006)
4 patient reports: Safe |
| Cardiovascular |
ANTIHYPERLIPIDEMIC AGENTS |
Colestipol |
Colestid |
OK! |
Not absorbed. Patient reports: safe |
| Cardiovascular |
ANTIHYPERLIPIDEMIC AGENTS |
Fluvastatin |
Lescol |
OK? |
Mainly metab by CYP2C9, also 3A4. Minimal transactivation of pregnane X receptor (Clin Pharmacol Therap 80:565,2006; Curr Drug Metab 7:375,2006) |
| Cardiovascular |
Antihyperlipidemic Agents |
Lovastatin |
Mevacor, etc |
BAD? |
Readily absorbed by liver. Metabolized by & induces CYP3A, 2C9. Induces PXR. |
| Cardiovascular |
ANTIHYPERLIPIDEMIC AGENTS |
Pravastatin |
Pravachol |
OK? |
www.drugs-porphyria.org: Possibly Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution. Substrate of CYP3A, but excreted mostly unchanged, and does not induce CYPs (Mol Pharmacol 65:1302,2004;Clin Pharm Therap 80:565,2006)
Experience of P. Tishler, MD and others - safe |
| Cardiovascular |
ANTIHYPERLIPIDEMIC AGENTS |
Rosuvastatin |
Crestor |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
www.porphyria-europe.com: Safe. Metab by CYP2C9; not metab. by CYP3A4,5.
patient report: safe |
| Cardiovascular |
ANTIHYPERLIPIDEMIC AGENTS |
Simvastatin |
Zocor, others |
OK? |
www.drugs-porphyria.org: Patient experience - safe
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
www.uq.edu.au/porphyria/: Unsafe in animals Unsafe in cell culture (Biomed Pharmacother 43:135,1989). Mainly metab by CYP3A4,but very low likelihood of CYP3A4 induction (Clin Pharm Therap 80:565,2006;Curr Drug Metab 7:375,2006); strong pregnane xenobiotic activator (J Pharm Exp Therap 320:72, 2007).
Patient reports: Safe |
| Cardiovascular |
ANTIOGENSIN RECEPTOR ANTAGONISTS |
Telmisartan |
Micardis |
OK! |
Only metabolite is glucuronide (J Clin Pharm 2000: 40 (12 pt 1), 1312. |
| Cardiovascular |
BETA BLOCKERS (includes some ophthalmic preparations) |
Labetalol |
Normodyne, Trandate |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in patients
patient report: safe |
| Cardiovascular |
BETA BLOCKERS (includes some ophthalmic preparations) |
Metoprolol |
Lopressor |
OK! |
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in patients
PV Tishler MD clinical data & patient report: Safe
Medicine (Balt)1992;71:1. Safe. Induces CYP3A. |
| Cardiovascular |
CALCIUM CHANNEL BLOCKERS |
Amlodipine |
Norvasc |
OK? |
www.drugs-porphyria.org: Probably Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
Not safe in patients (Ann Pharmacother 1997;31:253)
Safe at <10mg/d (Br J Clin Pharmacol 1997;43:339)
Substrate of & induces CYP3A4 (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007. Induces pregnane X receptor.
4 patient reports: Safe, certainly at 5 mg/day. |
| Cardiovascular |
CALCIUM CHANNEL BLOCKERS |
Diltiazem |
Cardizem |
BAD? |
www.drugs-porphyria.org: Probably Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Caution
www.uq.edu.au/porphyria/: Probably unsafe
Substrate of & inhibitor of CYP3A4. Modest transactivation of pregnane X receptor, but low probability of CYP3A4 induction (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; http://medicine.iupui.edu/clinpharm/ddis/; Curr Drug Metab 7:375,2006) |
| Cardiovascular |
CALCIUM CHANNEL BLOCKERS |
Felodipine |
Plendil |
BAD? |
www.drugs-porphyria.org: Probably Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
Substrate of & inducer of CYP3A4. Modest transactivator of pregnane X receptor, metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; Curr Drug Metab 7:375,2006) |
| Cardiovascular |
CALCIUM CHANNEL BLOCKERS |
Nicardipine |
Cardene |
BAD! |
Induces CYP3A4, 2C9; inhibits 3A. Transactivates pregnane X receptor (Drug Metab Disp 29:1325,2001) |
| Cardiovascular |
CALCIUM CHANNEL BLOCKERS |
Nifedipine |
Procardia, Adalat |
BAD! |
www.drugs-porphyria.org: Probably Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
www.uq.edu.au/porphyria/: Unsafe in patients
www.porphyriafoundation.com: Unsafe
Medicine (Balt) 1992;71:1. Safe
Clin Sci (Lond) 1985;69:581. Unsafe in cell culture
Substrate of CYP3A4. Induces CYP3A4, 2C9 via transactivation of pregnane X receptor (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; Drug Metab Disp 29:1325,2001)
Patient report: safe |
| Cardiovascular |
CALCIUM CHANNEL BLOCKERS |
Verapamil |
Verapamil, Tarka |
OK? |
Metab by & inhibits induction of CYP3A4.(http://medicine.iupui.edu/clinpharm/ddis/; Amer J Therap 16:155, 2009; Curr Drug Metab 5:543,2004) |
| Cardiovascular |
DIURETICS |
Furosemide |
Lasix |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use with Caution
www.uq.edu.au/porphyria/: Unsafe in patients
PV Tishler MD clinical data & patient reports: Safe
Medicine (Balt) 1992;71:1. Safe |
| Cardiovascular |
DIURETICS |
Spironolactone |
Aldactone |
BAD? |
www.drugs-porphyria.org: Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Caution
www.uq.edu.au/porphyria/: Unsafe in animals
Safe (Medicine (Balt) 1992;71:1, 1992). Induces CYP3A. Transactivates pregnane X receptor (Expert Opin Drug Metab Toxicol 4:895,2008) |
| Cardiovascular |
DIURETICS |
Torsemide |
Demadex, others |
OK? |
~75% metab, mostly by CYP2C9 (Br J Clin Pharm 50:573,2000; Clin Pharmacol Therap 76:557,2004). 2 Patient reports: safe |
| Cardiovascular |
IMPOTENCE AGENTS |
Sildenafil |
Viagra |
BAD? |
www.drugs-porphyria.org: Possibly Porphyrinogenic
Major metab by CYP3A4, less by CYP2C9; weak inhibitors of both (Drug Metab Disp 36:986,2008). Patient report: Safe |
| Cardiovascular agents |
ACE INHIBITORS |
Benazepril |
Lotensin |
OK! |
Patient report: safe |
| Cardiovascular agents |
ACE INHIBITORS |
Captopril |
Capoten |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic. Patient report: safe
No transactivation of pregnane X receptor (Curr Drug Metab 6:375,2006) |
| Cardiovascular agents |
ACE INHIBITORS |
Trandolapril |
Mavik |
OK! |
|
| Cardiovascular agents |
ANGIOTENSIN II RECEPTOR ANTAGONISTS |
Irbesartan |
Avapro, Avalide |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
Mostly not metab by CYPs. Some metab by CYP2C9, but doessnot induce any CYP (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; PDr 63:892,2009) |
| Cardiovascular agents |
ANTIADRENERGICS |
Clonidine |
Catapres |
BAD! |
www.drugs-porphyria.org: Probably Porphyrinogenic
www.porphyria-europe.com: Unsafe
web.uct.ac.za/depts/porphyria/: Avoid
www.uq.edu.au/porphyria/: Unsafe in patients and cell culture |
| Cardiovascular agents |
ANTIADRENERGICS |
Methyldopa |
Aldomet |
BAD! |
www.drugs-porphyria.org: Porphyrinogenic
www.porphyria-europe.com: Unsafe
web.uct.ac.za/depts/porphyria/: Avoid
Patient report: Unsafe |
| Cardiovascular agents |
ANTIADRENERGICS |
Prazosin |
Minipress |
OK! |
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Probably safe
Medicine (Balti) 1992:71:1. Safe |
| Cardiovascular agents |
ANTIADRENERGICS |
Terazosin |
Hytrin |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Caution
No transactivation of pregnane X receptor (Curr Drug Metab 6:375,2009) |
| Cardiovascular agents |
ANTIANGINAL AGENTS |
Isosorbide Dinitrate |
Imdur |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Caution |
| Cardiovascular agents |
ANTIANGINAL AGENTS |
Nitroglycerin |
Many |
OK? |
Not a CYP substrate (Biochem. J 1993; 292:545) |
| Cardiovascular agents |
ANTIARRHYTHMICS |
Adenosine |
Many |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
USP DI? Drug Info. for the Health Care Pro. - 26th Ed. (2006): Not metabolized by P450 |
| Cardiovascular agents |
ANTIARRHYTHMICS |
Amiodarone |
Many |
BAD? |
www.drugs-porphyria.org: Probably Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Avoid
www.uq.edu.au/porphyria/: Unsafe in cell culture
Gen Pharmacol 1999;32:259. Safe
Probably mostly metab by CYP3A4. Induces but more strongly inhibits CYP3A4 (J Pharm Pharm Sci 11:147,2008; Clin Pharm Therap 77:63, 2005) |
| Cardiovascular agents |
ANTIARRHYTHMICS |
Bretylium |
Bretylol |
OK? |
|
| Cardiovascular agents |
ANTIARRHYTHMICS |
Disopyramide |
Norpace |
BAD? |
www.drugs-porphyria.org: Probably Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Caution
www.uq.edu.au/porphyria/: Probably safe |
| Cardiovascular agents |
ANTIARRHYTHMICS |
Flecainide |
Tambocor, others |
OK! |
www.drugs-porphyria.org: Possibly Porphyrinogenic. Metabolized by CYP2D6. No data pointing to CYP-induction (http://medicine.iupui.edu/clinpharm/ddis/) |
| Cardiovascular agents |
ANTIARRHYTHMICS |
Ibutilide |
Corvert |
OK? |
www.drugs-porphyria.org: Possibly Porphyrinogenic
Circulation 1998;97:493. Metabolic pathway does not seem to involve CYP3A4 or CYP2D6 |
| Cardiovascular agents |
ANTIARRHYTHMICS |
Lidocaine |
Xylocaine |
OK? |
www.drugs-porphyria.org: Porphyrinogenic
metab by CYP3A4, 1A2. May ihibit its metab (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007: Pharmacol 1990; 255:1385; Curr Drug Metab 5:543, 2004) |
| Cardiovascular agents |
ANTIARRHYTHMICS |
Mexiletine |
Mexitil |
OK? |
www.drugs-porphyria.org: Possibly Porphyrinogenic. Metabolized by CYP2D6, 1A2. No data pointing to CYP-induction (Clin Pharmacokinet 46:985,2007) |
| Cardiovascular agents |
ANTIARRHYTHMICS |
Moricizine |
Ethmozine |
No info |
|
| Cardiovascular agents |
ANTIARRHYTHMICS |
Procainamide |
Pronestyl |
OK! |
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in cell culture |
| Cardiovascular agents |
ANTIARRHYTHMICS |
Propafenone |
Rhthmol |
BAD? |
www.drugs-porphyria.org: Possibly Porphyrinogenic
Metabolized by CYP2D6, 3A4, others; relative importances not known (Curr Drug Metab 5:543,2004; Clin Pharmacokinet 46:985,2007) |
| Cardiovascular agents |
ANTIARRHYTHMICS |
Quinidine |
Many |
OK? |
www.drugs-porphyria.org: Probably Porphyrinogenic
Substrate of CYP3A4. Minimal transactivation of pregnane X receptor (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; Curr Drug Metab 7:375,2006) |
| Cardiovascular agents |
ANTIARRHYTHMICS |
Tocainide |
Tonocard |
No info |
|
| Cardiovascular agents |
ANTIHYPERLIPIDEMIC AGENTS |
Cholestyramine |
Questran |
OK! |
Not absorbed from GI tract |
| Cardiovascular agents |
ANTIHYPERLIPIDEMIC AGENTS |
Clofibrate |
Atromid-S |
OK! |
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use with Caution
www.uq.edu.au/porphyria/: Safe in cell culture |
| Cardiovascular agents |
ANTIHYPERLIPIDEMIC AGENTS |
Ezetimibe |
Zetia, Vitorin |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
USP DI? Drug Info. for the Health Care Pro. - 26th Ed. (2006): Undergoes minimal oxidation. Extensively metabolized but not by CYP (PDR 63:2149,2009)
Patient report: Safe |
| Cardiovascular agents |
ANTIHYPERLIPIDEMIC AGENTS |
Gemfibrozil |
Lopid |
OK? |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use with Caution
Metab by CYP2C8. Minimally transactivates pregnane X receptor (Drug Metab Disp 34:191,2006; Curr Drug Metab 7:375,2006) |
| Cardiovascular agents |
ANTIHYPERLIPIDEMIC AGENTS |
Niacin |
Many |
No info |
USP DI? Drug Info. for the Health Care Pro. - 26th Ed: Not P450 substrate |
| Cardiovascular agents |
ANTIHYPERTENSIVE - RENIN INHIBITOR |
Aliskiren |
Tekturna |
OK? |
~20% metab, mainly by CYP3A4; does not induce CYP3A4 (Pharmacol Rpts 60:623,2008; J clin Pharmacol 48:1323,2008) |
| Cardiovascular agents |
ANTIHYPERTENSIVE- DUAL AGENT |
Aliskiren/ Amlodipine |
Tekamlo |
BAD? |
See individual drug listings. |
| Cardiovascular agents |
BETA BLOCKERS |
Nebivolol |
Bystolic |
OK? |
Extensively metab by CYP2D6 (Med Letter 50:17,2008). Patient experience: safe |
| Cardiovascular agents |
BETA BLOCKERS (includes some ophthalmic preparations) |
Acebutolol |
Many |
OK! |
web.uct.ac.za/depts/porphyria/: Use
Medicine (Balt)1992; 71:1. Safe
biocomp.health.unm.edu/p450/metabP450diseasep4.pdf: Substrate/inhibitor of CYP2D6 |
| Cardiovascular agents |
BETA BLOCKERS (includes some ophthalmic preparations) |
Atenolol |
Tenormin |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/ safe in patients
PV Tishler MD clinical data & patient reports: Safe
Medicine (Balt) 1992;71:1. Safe |
| Cardiovascular agents |
BETA BLOCKERS (includes some ophthalmic preparations) |
Betaxolol |
Many |
OK! |
www.drugs-porphyria.org: Possibly Porphyrinogenic |
| Cardiovascular agents |
BETA BLOCKERS (includes some ophthalmic preparations) |
Carteolol |
Many |
OK! |
web.uct.ac.za/depts/porphyria/: Use |
| Cardiovascular agents |
BETA BLOCKERS (includes some ophthalmic preparations) |
Esmolol |
Brevibloc |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use |
| Cardiovascular agents |
BETA BLOCKERS (includes some ophthalmic preparations) |
Nadolol |
Corgard |
OK! |
web.uct.ac.za/depts/porphyria/: Use |
| Cardiovascular agents |
BETA BLOCKERS (includes some ophthalmic preparations) |
Pindolol |
Visken |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use |
| Cardiovascular agents |
BETA BLOCKERS (includes some ophthalmic preparations) |
Propranolol |
Inderal |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use
PV Tishler MD clinical data & patient report: Safe
Safe (Br J Clin Pharmacol 1997;43:339)
Safe (Medicine (Balt) 1992;71:1)
Substrate of CYP3A4 & other CYPs. Does not transactivate pregnane X receptor (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; Curr Drug Metab 7:375,2006; http://medicine.iupui.edu/clinpharm/ddis/) |
| Cardiovascular agents |
BETA BLOCKERS (includes some ophthalmic preparations) |
Sotalol |
Betapace, others |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use
Medicine (Balt) 1992;71:1. Safe |
| Cardiovascular agents |
BETA BLOCKERS (includes some ophthalmic preparations) |
Timolol |
Blocadren |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in cell culture
Medicine (Balt)1992;71:1. Safe |
| Cardiovascular agents |
CALCIUM CHANNEL BLOCKERS |
Amlodipine/ olmesartan |
Azor |
BAD? |
See amlodipine |
| Cardiovascular agents |
CALCIUM CHANNEL BLOCKERS |
Bepridil |
Vascor |
BAD! |
www.uq.edu.au/porphyria/: Unsafe in cell culture
Williams DA: Op. Cit.: Substrate of CYP3A4 |
| Cardiovascular agents |
CALCIUM CHANNEL BLOCKERS |
Clevidipine |
Cleviprex |
OK? |
Unlikely inducer of CYPs at therapeutic doses (Drug Metab Disp 34:734,2006) |
| Cardiovascular agents |
CALCIUM CHANNEL BLOCKERS |
Nimodipine |
Nimotop |
BAD! |
www.drugs-porphyria.org: Probably Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
Substrate of CYP3A4 (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007) |
| Cardiovascular agents |
CARDIAC GLYCOSIDES |
Digoxin |
Lanoxin |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use with Caution
www.uq.edu.au/porphyria/: Safe in patients
Medicine (Balt) 1992;71:1. Safe |
| Cardiovascular agents |
DIURETICS |
Acetazolamide |
Diamox |
OK! |
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in patients & cell culture |
| Cardiovascular agents |
DIURETICS |
Amiloride |
Midamor, Moduretic, others |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in patients |
| Cardiovascular agents |
DIURETICS |
Bumetanide |
Bumex |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in patients
Patient report: Safe |
| Cardiovascular agents |
DIURETICS |
Eplerenone |
Inspra |
BAD? |
~95% metab, mainly by CYP3A4. (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; J Clin Pharmacol 45:810,2005; Am J Therapeutics 16:255,2009) |
| Cardiovascular agents |
DIURETICS |
Ethacrynic Acid |
Edecrin |
OK! |
www.uq.edu.au/porphyria/: Safe in patients
http://www.emedicine.com/MED/topic1880.htm: Safe in porphyria |
| Cardiovascular agents |
DIURETICS |
Hydrochlorothiazide |
Many |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use with Caution
www.uq.edu.au/porphyria/: Safe in patients
PV Tishler MD clinical data & patient reports: Safe |
| Cardiovascular agents |
DIURETICS |
Metolazone |
Zaroxolyn |
BAD? |
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution |
| CARDIOVASCULAR AGENTS |
DIURETICS |
Triamterene |
Dyrenium |
OK! |
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use |
| Cardiovascular agents |
DOPAMINE D1 RECEPTOR AGONISTS |
Fenoldopam |
Corlopam |
No info |
|
| Cardiovascular agents |
IMPOTENCE AGENTS |
Tadalafil |
Cialis |
OK? |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
www.premiumdrugs.com/globalcart/ html/media/docs/cialis-pi-us.pdf: metabolized primarily by CYP3A4 |
| Cardiovascular agents |
IMPOTENCE AGENTS |
Vardenafil |
Levitra |
No info |
Major metab by CYP3A4, 3A5 (Drug Metab Disp 36:986,2008) |
| Cardiovascular agents |
MISC. |
Diazoxide |
Hyperstat |
OK! |
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in cell culture |
| Cardiovascular agents |
MISC. |
Tolazoline |
Priscoline |
OK! |
www.uq.edu.au/porphyria/: Safe in patients
http://www.emedicine.com/MED/topic1880.htm: Safe in porphyria |
| Cardiovascular agents |
PHOSPHODIESTERASE INHIBITORS |
Milrinone |
Primacor |
No info |
|
| Cardiovascular agents |
THROMBOLYTIC ENZYMES |
Alteplase |
Activase |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use with Caution |
| Cardiovascular agents |
THROMBOLYTIC ENZYMES |
Streptokinase |
Many |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use |
| Cardiovascular agents |
THROMBOLYTIC ENZYMES |
Tenecteplase |
Tnkase |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic |
| Cardiovascular agents |
VASODILATORS |
Hydralazine |
Apresoline |
BAD! |
www.drugs-porphyria.org: Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
www.uq.edu.au/porphyria/: Unsafe in patients |
| Cardiovascular agents |
VASODILATORS |
Minoxidil |
Many |
BAD? |
www.drugs-porphyria.org: Possibly Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution |
| Cardiovascular agents |
VASODILATORS |
Nitroprusside |
Nipride |
OK? |
web.uct.ac.za/depts/porphyria/: Use with Caution
Redox Rep 2004;9:360: No P450 metabolism |
| Cardiovascular agents |
VASOPRESSORS |
Dobutamine |
Dobutrex, others |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use |
| Cardiovascular agents |
VASOPRESSORS |
Dopamine |
Intropin, others |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use |
| Cardiovascular agents |
VASOPRESSORS |
Ephedrine |
Many |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic |
| Central nervous system |
ANTICONVULSANTS |
Carbamazepine |
Tegretol |
BAD! |
www.drugs-porphyria.org: Porphyrinogenic
www.porphyria-europe.com: unsafe
web.uct.ac.za/depts/porphyria/: Avoid
www.uq.edu.au/porphyria/: Unsafe in patients
Unsafe/risky in patients (Epilepsia 33:108,1992; Neurology 32:1409,1982; Neurology 45:1216,1995). Major metab by CYP3A4. Induces CYP3A4 via transactivation of constitutive androstane receptor & kpregnane X receptor. Also induces CYP2C9, other CYPs. (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; Arch toxicol 82:667,2008; Clin Therapeutics 30:1385,2008)
Patient report: Safe (low dose) |
| Central nervous system |
ANTICONVULSANTS |
Gabapentin |
Neurontin |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use
PV Tishler MD clinical data & patient reports: Safe
Not a substrate for & does not induce CYPs (Fundam Clin Pharmacol 14:301,2000; Clin Therapeutics 30:1385,2008) |
| Central nervous system |
ANTICONVULSANTS |
Phenytoin |
Dilantin |
BAD! |
www.drugs-porphyria.org: Porphyrinogenic
www.porphyria-europe.com: Unsafe
web.uct.ac.za/depts/porphyria/: Avoid
www.uq.edu.au/porphyria/: Unsafe in patients
Unsafe in patients (Neurology 45:1216,1995; Epilepsia 33:108,1992)
Substrate & inducer of CYP3A4 & CYP2C9. Strongly activates constitutive androstane receptor & pregnane X receptor, & induces CYP3A4. (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; JBC 279:29295,2004; Arch Toxicol 82:667,2008)
1 Patient report: Safe. 1 patinet report: unsafe |
| Central nervous system |
ANTICONVULSANTS |
Pregabalin |
Lyrica |
OK! |
>90% non-metabolized (PDR 63:2527,2009). Patient reports: safe |
| Central nervous system |
ANTICONVULSANTS |
Topiramate |
Topomax |
BAD? |
www.drugs-porphyria.org: Probably porphyrinogenic.
www.porphyria.uct.ac.za: Use only with extreme caution. 30-40% metabolized, some by CYP2C9; metab by CYP3A4 probably minimal, but induces CYP3A4 via transactivation of pregnane X receptor (Pharmacokinet 45:1061,2006; Epilepsia 46:378,2005; Arch Toxicol 82:667,2008; Clin Therapeutics 30:1385,2008)
1 patient report: safe |
| Central nervous system |
ANTICONVULSANTS |
Valproic Acid |
Depakene, Stavzor |
OK? |
www.drugs-porphyria.org: Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Avoid
www.porphyriafoundation.com: Unsafe
Largely not CYP metab; some metab by multiple CYP2C9 but not CYP3A4. Induces CYP3A. Does not transactivate pregnane X receptor. (Clin Therapeutics 30:1385,2008; Curr Drug Metab 7:375,2006) |
| Central nervous system |
ANTIPARKINSON AGENTS |
Ropinirole |
Roquid |
OK? |
~90% metab by CYP1A2, small amt by CYP3A (Clin Pharmacokinet 39:243,2000). 1 patient report: safe. |
| Central nervous system |
Antispasmodic |
Trospium |
Sanctura |
OK! |
Ester hydrolysis, with probably littel/no P450 metabolism. 1 patient report: safe. |
| Central nervous system |
BENZODIAZEPINES |
Alprazolam |
Xanax |
OK? |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Caution
www.uq.edu.au/porphyria/: Unsafe in cell culture
Mainly metab by CYP3A4, but does not transactivate pregnane X receptor (USP DI? Drug Info. for the Health Care Pro. - 26th Ed;
Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; Curr Drug Metrab 7:375,2006)
>1Patient reports: Safe |
| Central nervous system |
BENZODIAZEPINES |
Diazepam |
Valium |
OK? |
www.drugs-porphyria.org: Probably Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Caution
www.uq.edu.au/porphyria/: Unsafe in patients
Medicine (Balt) 1992;71:1. Safe
Substrate of CYP3A4,2B6,2C9. Modest transactivator of pregnane X receptor, but low prediction of CYP3A4 inducibility (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; Curr Drug Metab 7:375,2006; Curr Drug Metab 9:598,2008)
2 Patient reports: Safe |
| Central nervous system |
BENZODIAZEPINES |
Temazepam |
Restoril |
OK! |
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in patients
Substrate of CYP3A4 (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007)
2 Patient reports: Safe |
| Central nervous system |
BENZODIAZEPINES |
Triazolam |
Halcion |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in animals
Medicine (Balt) 1992;71:1. Safe
Substrate of CYP3A4 (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007). 1 patientreport: safe. |
| Central nervous system |
HYPNOTICS (Sleeping Medications) |
Chloral Hydrate |
Many |
OK! |
www.porphyria-europe.com: Safe
www.uq.edu.au/porphyria/: Safe in patients
Peter V. Tishler, MD, clinical experience: safe
patient report: safe |
| Central nervous system |
HYPNOTICS (Sleeping Medications) |
Zolpidem |
Ambien, Edluar, Intermezzo, Zolpimist |
OK! |
www.drugs-porphyria.org: Possibly Porphyrinogenic
CYP3A substrate. Moderate transactivator of pregnane X receptor, but low prediction of CYP3A4 inducibility (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007;http://medicine.iupui.edu/flockhart/table.htm; Curr Drug Metab 7:375,2006)
6 Patient reports: safe |
| Central nervous system |
MIGRAINE THERAPY |
Sumatriptan |
Imitrex |
OK? |
www.drugs-porphyria.org: Possibly Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Caution
2 patient reports: safe |
| Central nervous system |
NARCOTICS (Pain Therapies) |
Fentanyl |
Duragesic |
OK? |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in animals
Substrate of & induces CYP3A4 (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007).Induces pregnane X receptor
Patient reports: Safe |
| Central nervous system |
NARCOTICS (Pain Therapies) |
Methadone |
Many |
OK! |
www.drugs-porphyria.org: Possibly Porphyrinogenic
www.porphyria-europe.com: safe
web.uct.ac.za/depts/porphyria/: Use
Metab by CYP3A, less by 2C9. |
| Central nervous system |
NARCOTICS (Pain Therapies) |
Tramadol |
Ultram, Ultracet, Ryzolt, etc. |
No info |
Largely metab by CYP3A4,2D6 (Eur J Clin Pharm 62:513,2006). Patient report: safe |
| Central nervous system |
NONSTEROIDAL ANTI-INFLAMMATORY AGENTS -NSAIDs (Pain, Arthritis Therapies, etc.) |
Acetaminophen |
Tylenol |
OK! |
www.porphyriafoundation.com: Safe
PV Tishler MD clinical data & patient reports: Safe
Induces constitutive androstene receptor. |
| Central nervous system |
NONSTEROIDAL ANTI-INFLAMMATORY AGENTS -NSAIDs (Pain, Arthritis Therapies, etc.) |
Ibuprofen |
Advil, Motrin |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
www.porphyria-europe.com: Safe. Metab by CYP2C9,2C8.
PV Tishler MD clinical data & patient reports: Safe at low dose used intermittently, BUT one acute attack at high, prolonged dose (Drug Metab Disp 33:1567, 2005)
patient reports: safe |
| Central nervous system agents |
AMPHETAMINES |
Dextroamphetamine |
Dexedrine |
OK? |
|
| Central nervous system agents |
Anti-Glaucoma |
Brinzolamide/ Brimonidine |
Simbrinza |
BAD! |
Brinzolamide is a sulfonamide, and thus this is contraindicated |
| Central nervous system agents |
ANTICONVULSANTS |
Clonazepam |
Klonopin |
BAD! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
www.porphyria-europe.com: safe
web.uct.ac.za/depts/porphyria/: Use with Caution
www.uq.edu.au/porphyria/: Probably unsafe
www.porphyriafoundation.com: unsafe
Epilepsia 1992;33:108. porphyrogenic but safe in lose dosages
Neurology 1982;32:1409. safe in low dosages
Greatly induces CYP2B. Substrate of but does not induce CYP3A or 2C9
(Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; Drug Metab Dispos 25:750,1997) |
| Central nervous system agents |
ANTICONVULSANTS |
Divalproex |
Depakote |
OK? |
Dimer of valproic acid. See Valproic acid. |
| Central nervous system agents |
ANTICONVULSANTS |
Ethosuximide |
Zarontin |
BAD? |
www.drugs-porphyria.org: Probably Porphyrinogenic
www.porphyria-europe.com: Unsafe
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
www.uq.edu.au/porphyria/: Unsafe in patients
www.porphyriafoundation.com: Unsafe
Unsafe in animals (Neurology 1981;31:480)
Substrate of CYP3A4, but does not transactivate pregnane X receptor. Minor metab by CYP2C9, other CYPs (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; Curr Drug Metab 7:375, 2006; Clin Therapeutics 30:1385,2008) |
| Central nervous system agents |
ANTICONVULSANTS |
Felbamate |
Felbatol |
BAD! |
www.drugs-porphyria.org: Probably Porphyrinogenic
www.porphyriafoundation.com: Unsafe
Metab mainly by CYP3A4, also 2C9, others. Induces CYP3A4 but does not transactivate pregnane X receptor (Fundam Clin Pharmacol 14:301,2000; Curr Drug Metab 7:375,2006; Clin Therapeutics 30:1385,2008) |
| Central nervous system agents |
ANTICONVULSANTS |
Fosphenytoin |
Cerebyx |
BAD! |
www.drugs-porphyria.org: Porphyrinogenic
Metab mainly by CYP2C9, also CYP3A4, others. Induces CYP2C9,3A4 (Clin Therapeutics 30:1385,2008. Same as Phenytoin. |
| Central nervous system agents |
ANTICONVULSANTS |
Levetiracetam |
Keppra |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
www.porphyria-europe.com: Safe
Not a substrate for & does not induce CYPs (Fundam Clin Pharmacol 14:301,2000; Clin Therapeutics 30:1385,2008) |
| Central nervous system agents |
ANTICONVULSANTS |
Methsuximide |
Celontin |
BAD! |
www.uq.edu.au/porphyria/: Unsafe in patients
Neurology 1981;31:480. Unsafe in animals |
| Central nervous system agents |
ANTICONVULSANTS |
Oxcarbazepine |
Trileptal |
BAD! |
www.drugs-porphyria.org: Probably Porphyrinogenic
www.porphyria-europe.com: Unsafe
web.uct.ac.za/depts/porphyria/: Avoid
Induces CYP3A4 (Fundam Clin Pharmacol 14:301,2000) |
| Central nervous system agents |
ANTICONVULSANTS |
Phenobarbital |
Luminal |
BAD! |
www.drugs-porphyria.org: Porphyrinogenic
www.porphyria-europe.com: Unsafe
web.uct.ac.za/depts/porphyria/: Avoid
Strongly activates constitutive androstane receptor, pregnane X receptor, & induces CYP3A4 (BBRC 277:1, 2000; Arch Toxicol 82:667,2008) |
| Central nervous system agents |
ANTICONVULSANTS |
Primidone |
Mysoline |
BAD! |
www.drugs-porphyria.org: Porphyrinogenic
www.porphyria-europe.com: Unsafe
web.uct.ac.za/depts/porphyria/: Avoid
www.uq.edu.au/porphyria/: Unsafe in patients
www.porphyriafoundation.com: Unsafe
Neurology 1981;31:480. Unsafe in animals. Metab by CYP3A4 to phenobarbital (BAD!!); induces CYP3A4 (Clin Therapeutics 30:1385,2008) |
| Central nervous system agents |
ANTICONVULSANTS |
Zonisamide |
Zonegran |
BAD? |
Major metab by CYP3A4; also CYP2C19. (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; Clin Therapeutics 30:1385,2008) |
| Central nervous system agents |
ANTIMYASTHENIC AGENTS |
Ambenonium |
Mytelase |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic |
| Central nervous system agents |
ANTIMYASTHENIC AGENTS |
Edrophonium |
Tensilon |
OK! |
|
| Central nervous system agents |
ANTIMYASTHENIC AGENTS |
Guanidine |
Guanidine |
NO INFO |
|
| Central nervous system agents |
ANTIMYASTHENIC AGENTS |
Neostigmine |
Prostigmine |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use |
| Central nervous system agents |
ANTIMYASTHENIC AGENTS |
Pyridostigmine |
Mestinon |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Caution.
Patient report: safe |
| Central nervous system agents |
ANTIPARKINSON AGENTS |
Amantadine |
Symmetrel |
OK! |
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use |
| Central nervous system agents |
ANTIPARKINSON AGENTS |
Benztropine |
Cogentin |
NO INFO |
|
| Central nervous system agents |
ANTIPARKINSON AGENTS |
Bromocriptine |
Parlodel |
BAD! |
www.drugs-porphyria.org: Probably Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
www.uq.edu.au/porphyria/: Unsafe in cell culture
Metab by CYP3A4 (Clin Therapeutics 28:1065,2006) |
| Central nervous system agents |
ANTIPARKINSON AGENTS |
Entacapone |
Comtan, Stalevo |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic. Not metab by CYPs (PDR 63:2208, 2009) |
| Central nervous system agents |
ANTIPARKINSON AGENTS |
Levodopa |
Many |
OK! |
web.uct.ac.za/depts/porphyria/: Use with Caution
USP DI? Drug Info. for the Health Care Pro. - 26th Ed: Not P450 substrate
http://www.ukmi.nhs.uk/NewMaterial/ html/docs/entacapo.pdf: Main metabolic pathway does not involve P450 |
| Central nervous system agents |
ANTIPARKINSON AGENTS |
Levodopa/ Carbidopa |
Sinemet |
OK! |
|
| Central nervous system agents |
ANTIPARKINSON AGENTS |
Pergolide |
Permax |
No info |
metab by CYP3A4 (Clin Therapeutics 28:2065,2006) |
| Central nervous system agents |
ANTIPARKINSON AGENTS |
Pramipexole |
Mirapex |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
www.rxlist.com: ~90% excreted unchanged. No CYP metab (Eur J Neurol 7 Suppl 1:15,2000) |
| Central nervous system agents |
ANTIPARKINSON AGENTS |
Rotigotine |
Neupro (patch) |
OK? |
Metab by multiple CYPs. Does not induce CYP3A4, 2C9 (PDR 63:3149,2009) |
| Central nervous system agents |
ANTIPARKINSON AGENTS |
Selegiline |
Emsam, Eldepryl, Zelapar |
BAD? |
www.drugs-porphyria.org: Probably Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
Metab by CYP2B6, which may involve pregnane X receptor |
| Central nervous system agents |
ANTIPARKINSON AGENTS |
Trihexyphenidyl |
Artane |
BAD? |
www.drugs-porphyria.org: Possibly Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Avoid |
| Central nervous system agents |
BENZODIAZEPINES |
Chlordiazepoxide |
Librium |
BAD! |
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
www.uq.edu.au/porphyria/: Unsafe in patients
Medicine (Balt) 1992;71:1. Safe |
| Central nervous system agents |
BENZODIAZEPINES |
Estazolam |
Prosom |
OK? |
www.uq.edu.au/porphyria/: Cell cuture - probably safe
PV Tishler MD clinical data: Safe
Metab. almost exclusively by CYP3A4
(https://online.epocrates.com/front_porch/; Xenobiotica 35:455,2005) |
| Central nervous system agents |
BENZODIAZEPINES |
Flurazepam |
Dalmane |
BAD! |
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
www.uq.edu.au/porphyria/: Unsafe in patients |
| Central nervous system agents |
BENZODIAZEPINES |
Lorazepam |
Ativan |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Probably safe
Not metab by CYPs (Curr Drug Metab 9:827,2008)
PV Tishler MD clinical data: Safe
Medicine (Balt) 1992;7:1. Safe |
| Central nervous system agents |
BENZODIAZEPINES |
Oxazepam |
Serax |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Caution
www.uq.edu.au/porphyria/: Probably unsafe. Not metab by CYPs (Curr Drug Metab 9:827,2008) |
| Central nervous system agents |
HYPNOTICS (Sleeping Medications) |
Butabarbital |
Butisol |
BAD! |
www.porphyria-europe.com: Unsafe.
See phenobarbital |
| Central nervous system agents |
HYPNOTICS (Sleeping Medications) |
Butalbital |
Fiorinal |
BAD! |
See phenobarbital |
| Central nervous system agents |
HYPNOTICS (Sleeping Medications) |
Eszopiclone |
Lunesta |
OK? |
Substrate of CYP3A4 (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007) |
| Central nervous system agents |
HYPNOTICS (Sleeping Medications) |
Ethchlorvynol |
Placidyl |
BAD! |
|
| Central nervous system agents |
HYPNOTICS (Sleeping Medications) |
Pentobarbital |
Nembutal |
BAD! |
www.porphyria-europe.com: Unsafe
Patient report: Unsafe
See Phenobarbital |
| Central nervous system agents |
HYPNOTICS (Sleeping Medications) |
Ramelteon |
Rozerem |
BAD? |
Patient report - bad. Minor metab. by CYP3A4. |
| Central nervous system agents |
HYPNOTICS (Sleeping Medications) |
Secobarbital |
Seconal |
BAD! |
www.porphyria-europe.com: Unsafe
Induces CYP3A4 (Arch Toxicol 82:667,2008)
See Phenobarbital |
| Central nervous system agents |
HYPNOTICS (Sleeping Medications) |
Zaleplon |
Sonata |
BAD! |
www.drugs-porphyria.org: Possibly Porphyrinogenic
Metabolized by CYP3A4
(Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; Xenobiotica 2002;32:835)
Patient reports: Safe |
| Central nervous system agents |
MIGRAINE THERAPY |
Ergotamine |
Cafergot |
BAD! |
www.porphyria-europe.com: Unsafe
web.uct.ac.za/depts/porphyria/: Avoid
www.uq.edu.au/porphyria/: Unsafe in patients
www.porphyriafoundation.com: Unsafe
Substrate of CYP3A4 (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007) |
| Central nervous system agents |
MIGRAINE THERAPY |
Isometheptene/ Dichloralphenazone |
Midrin, others |
BAD? |
Isometheptene
www.uq.edu.au/porphyria/: Unsafe in animals
Dichloralphenazone
www.uq.edu.au/porphyria/: Unsafe in patients |
| Central nervous system agents |
MIGRAINE THERAPY |
Naratriptan |
Amerge |
NO INFO |
www.drugs-porphyria.org: Possibly Porphyrinogenic |
| Central nervous system agents |
MIGRAINE THERAPY |
Rizatriptan |
Maxalt |
OK? |
www.drugs-porphyria.org: Possibly Porphyrinogenic
No significant interaction with CYPs. Primary metabolism does not involve CYPs (PDR 63:2056,2009; www.cbg-meb.nl/uk/docs/nieuws/par-maxalt.pdf) |
| Central nervous system agents |
MIGRAINE THERAPY |
Zolmitriptan |
Zomig |
OK? |
www.drugs-porphyria.org: Possibly Porphyrinogenic. Insufficient data on metabolism. One report (Swedish) of tolerance.
Xenobiotica 1999;29:847. Metabolized almost entirely by CYP1A2.
Sinz M: Cur Drug Metab 2006; 7:375. No activation of pregnane X receptor. |
| Central nervous system agents |
NARCOTICS (Pain Therapies) |
Alfentanil |
Alfenta |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use
Substrate ~equally of CYP3A4, 3A5 (Williams DA. Drug metabolism. In: Foye?s Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; Drug Metab Disp 33:303,2005) |
| Central nervous system agents |
NARCOTICS (Pain Therapies) |
Buprenorphine |
Buprenex, Suboxone, Subutex |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
www.porphyria-europe.com: Safe
www.uq.edu.au/porphyria/: Safe in patients
PV Tishler MD clinical data: Safe
Ann Fr Anesth Reanim 1989;8:525. Safe
Substrate of CYP3A4 (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007) |
| Central nervous system agents |
NARCOTICS (Pain Therapies) |
Butorphanol |
Stadol |
OK! |
|
| Central nervous system agents |
NARCOTICS (Pain Therapies) |
Codeine |
Many |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in patients
PV Tishler MD clinical data & patient report: Safe
Substrate of CYP3A4 (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007) |
| Central nervous system agents |
NARCOTICS (Pain Therapies) |
Hydrocodone |
Vicodin, others |
OK! |
see Respiratory Agents/antitussive Agents |
| Central nervous system agents |
NARCOTICS (Pain Therapies) |
Hydromorphone |
Dilaudid |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic |
| Central nervous system agents |
NARCOTICS (Pain Therapies) |
Meperidine |
Demerol |
OK! |
PV Tishler MD clinical data: Safe
JAMA 1965;194:1037. Safe in patients |
| Central nervous system agents |
NARCOTICS (Pain Therapies) |
Morphine |
Many |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
www.porphyria-europe.com: safe
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in patients
PV Tishler MD clinical data: Safe |
| Central nervous system agents |
NARCOTICS (Pain Therapies) |
Nalbuphine |
Nubain |
OK! |
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use |
| Central nervous system agents |
NARCOTICS (Pain Therapies) |
Oxycodone |
Oxycontin, Percocet, Percodan, others |
OK! |
www.drugs-porphyria.org: Possibly Porphyrinogenic
www.uq.edu.au/porphyria/: Unsafe in animals
PV Tishler MD clinical data & patient reports: Safe |
| Central nervous system agents |
NARCOTICS (Pain Therapies) |
Pentazocine |
Talwin |
BAD! |
web.uct.ac.za/depts/porphyria/: Avoid
www.uq.edu.au/porphyria/: Unsafe in patients |
| Central nervous system agents |
NONSTEROIDAL ANTI-INFLAMMATORY AGENTS -NSAIDs (Pain, Arthritis Therapies, etc.) |
Aspirin |
Many |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in patients
www.porphyriafoundation.com: Safe
PV Tishler MD clinical data & patient reports: Safe |
| Central nervous system agents |
NONSTEROIDAL ANTI-INFLAMMATORY AGENTS -NSAIDs (Pain, Arthritis Therapies, etc.) |
Diclofenac |
Voltaren |
BAD? |
www.drugs-porphyria.org: Probably Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
www.uq.edu.au/porphyria/: Unsafe in patients
www.porphyriafoundation.com: Unsafe
PV Tishler MD clinical data: Safe
Biomed Pharmacother 43:135,1989 - Unsafe in cell culture
Limited metab by CYP2C9, ?2C8 (Drug Metab Disp 33:1567, 2005) |
| Central nervous system agents |
NONSTEROIDAL ANTI-INFLAMMATORY AGENTS -NSAIDs (Pain, Arthritis Therapies, etc.) |
Indomethacin |
Indocin |
OK! |
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Probably safe. ~50% metab by CYP2C9 (Drug Metab Disp 33:1567, 2005).
Medicine (Balt) 71:1, 1992 - Safe in some, not safe in others |
| Central nervous system agents |
NONSTEROIDAL ANTI-INFLAMMATORY AGENTS -NSAIDs (Pain, Arthritis Therapies, etc.) |
Ketoprofen |
Orudis, Oruvail, others |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use with Caution
Probably not metab by CYPs
PV Tishler MD clinical data: Safe (Drug Metab Disp 33:1567,2005) |
| Central nervous system agents |
NONSTEROIDAL ANTI-INFLAMMATORY AGENTS -NSAIDs (Pain, Arthritis Therapies, etc.) |
Ketorolac Tromethamine |
Toradol |
BAD! |
www.drugs-porphyria.org: Possibly Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
Eksp Klin Farmakol. 2005;68:56. CYP2C substrate |
| Central nervous system agents |
NONSTEROIDAL ANTI-INFLAMMATORY AGENTS -NSAIDs (Pain, Arthritis Therapies, etc.) |
Naproxen |
Naprosyn, Aleve |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in patients and animals
20-40% metab by CYP2C9 (<50% of this), other CYPs
Patient reports: Safe (Drug Metab Disp 33:1567,2005) |
| Central nervous system agents |
NONSTEROIDAL ANTI-INFLAMMATORY AGENTS -NSAIDs (Pain, Arthritis Therapies, etc.) |
Sulindac |
Clinoril |
OK! |
www.drugs-porphyria.org: Possibly Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in animals
Minimal CYP2D9 metab (Drug Metab Disp 33:1567,2005) |
| CONTRAST MEDIA |
n/a |
Diatrizoate Meglumine |
Hypaque |
OK! |
|
| CONTRAST MEDIA |
n/a |
Ethiodized Oil |
Ethiodol |
OK! |
|
| CONTRAST MEDIA |
n/a |
Ferumoxides |
Endorem |
OK! |
|
| CONTRAST MEDIA |
n/a |
Gadopentetate Dimeglumine |
Magnevist |
OK! |
|
| CONTRAST MEDIA |
n/a |
Iodipamide Meglumine |
Chlorografin, Sinografin |
OK! |
|
| Contrast media |
n/a |
Iodixanol |
Visipaque |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
www.fda.gov/medwatch/SAFETY/ 2003/03DEC_PI/Visipaque_PI.pdf: No metabolism |
| CONTRAST MEDIA |
n/a |
Iohexol |
Omnipaque |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic |
| CONTRAST MEDIA |
n/a |
Iopanoic Acid |
Telepaque |
OK! |
|
| CONTRAST MEDIA |
n/a |
Iopromide |
Ultravist |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic |
| Dermatologicals |
ACNE |
Isotretinoin |
Accutane, Sotret, Amnesteem, Claravis |
BAD? |
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
Substrate of CYP3A4. Minimally transactivates pregnane X receptor, and has low proability of inducing CYP3A4 (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; Curr Drug Metab 7:375,2006) |
| Dermatologicals |
ANTIPSORIATICS - SYSTEMIC |
Acitretin |
Soriatane |
BAD? |
www.drugs-porphyria.org: Possibly Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution |
| Dermatologicals |
Dermatosis, allergy, psoriasis |
desoximetasone |
topicort |
OK? |
Topical corticosteroid. 1 patinet report: safe |
| Diagnostic |
n/a |
Methacholine |
Provocholine, others |
OK! |
|
| Diagnostic |
Imaging |
Gadobutrol |
Gadavist |
OK! |
MRI contrast agent that is not metabolized |
| Diagnostic drugs |
|
Thyrotropin |
THYROTROPIN ALFA inj pdr |
OK! |
|
| Gastrointestinal |
ANTIDIARRHEAL AGENTS |
Rifaximin |
Xifaxan |
OK! |
>99% excreted in feces unabsorbed/unchanged (PDR 65:2911, 2011). Induces pregnane X receptor. |
| Gastrointestinal |
ANTIEMETICS (Vomiting Therapies) |
Dronabinol |
Marinol |
BAD? |
Major metab by CYP3A4 & 2C9 (Williams DA. Induces pregnane X receptor. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007) |
| Gastrointestinal |
ANTIEMETICS (Vomiting Therapies) |
Meclizine |
Antivert, Bonine |
OK! |
>3 patient reports: safe. Induces & inhibits constitutive androstene receptor. |
| Gastrointestinal |
ANTISPASMODICS |
Dicyclomine |
Bental, others |
OK! |
www.uq.edu.au/porphyria/: Safe in patients
Patient reports: Safe |
| Gastrointestinal |
ANTISPASMODICS |
Hyoscyamine |
Levsin, others |
OK! |
3 patient reports: safe |
| Gastrointestinal |
H-2 ANTAGONISTS, PPIs (Reflux, Ulcer Therapies) |
Cimetidine |
Tagamet |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Caution
www.uq.edu.au/porphyria/: Probably unsafe
Clin Chim Acta 1995;234:171. Safe in patients
Ann Int Med 2005; 143:694. Safe and possibly therapeutic during acute attack.
PV Tishler, MD clinical data & patient reports: Safe
Substrate % inhibitor of CYP3A4 but does not transactivate pregnane X receptor (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; Curr Drug Metab 7:375,2006) |
| Gastrointestinal |
H-2 ANTAGONISTS, PPIs (Reflux, Ulcer Therapies) |
Famotidine |
Pepcid |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Caution
www.uq.edu.au/porphyria/: Safe in patients
Patient reports: Safe |
| Gastrointestinal |
H-2 ANTAGONISTS, PPIs (Reflux, Ulcer Therapies) |
Omeprazole |
Prilosec |
OK! |
www.drugs-porphyria.org: Possibly Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Substrate & inducer of CYP3A4. Significantly transactivates pregnane X receptor, but has low probability of inducing CYP3A4 (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; Curr Drug Metab 7:375, 2006; Drug Safety 29:769, 2006)
7 patient reports: safe |
| Gastrointestinal |
H-2 ANTAGONISTS, PPIs (Reflux, Ulcer Therapies) |
Rabeprazole |
Aciphex |
OK? |
www.drugs-porphyria.org: Probably Porphyrinogenic
Major metab is nonenzymatic. Minor metab via CYP2C19,3A4. Modestly transactivates pregnane X receptor, but has low probability of inducing CYP3A4 (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; Curr Drug Metab 7:375,2006; Drug Safety 29:769, 2006). 1 patient report: safe |
| Gastrointestinal |
H-2 ANTAGONISTS, PPIs (Reflux, Ulcer Therapies) |
Ranitidine |
Zantac |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Caution
www.uq.edu.au/porphyria/: Probably unsafe
www.porphyriafoundation.com: Safe
PV Tishler MD clinical data: Safe |
| Gastrointestinal |
LAXATIVES |
Bisacodyl |
Dulcolax |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use with Caution
PV Tishler MD clinical data: Safe |
| Gastrointestinal |
POTASSIUM REMOVING RESINS |
Sodium Polystyrene Sulfonate |
Kayexalate |
OK! |
patient report: safe |
| Gastrointestinal therapies |
ANTI-INFLAMMATORY AGENTS |
Infliximab |
Remicade |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
Protein; no CYP metab |
| Gastrointestinal therapies |
ANTI-INFLAMMATORY AGENTS |
Mesalamine |
Rowasa, Pentasa, Asacol, others |
OK! |
<30% absorbed; not metab by CYPs |
| Gastrointestinal therapies |
ANTI-INFLAMMATORY AGENTS |
Olsalazine |
Dipentum |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
metab to mesalamine which has no CYP metab |
| GASTROINTESTINAL THERAPIES |
ANTIDIARRHEAL AGENTS |
Diphenoxylate |
Lomotil |
OK! |
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in patients |
| GASTROINTESTINAL THERAPIES |
ANTIDIARRHEAL AGENTS |
Kaolin-Pectin |
Kaopectate |
OK! |
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in patients |
| GASTROINTESTINAL THERAPIES |
ANTIDIARRHEAL AGENTS |
Loperamide |
Imodium |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in cell culture
Patient report: Safe |
| Gastrointestinal therapies |
ANTIEMETICS (Vomiting Therapies) |
Cyclizine |
Merezine |
OK! |
www.drugs-porphyria.org: Probably Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in patients |
| Gastrointestinal therapies |
ANTIEMETICS (Vomiting Therapies) |
Dimenhydrinate |
Dramamine |
BAD! |
www.porphyria-europe.com: unsafe
web.uct.ac.za/depts/porphyria/: Avoid
www.uq.edu.au/porphyria/: Unsafe in patients |
| Gastrointestinal therapies |
ANTIEMETICS (Vomiting Therapies) |
Ondansetron |
Zofran |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use with Caution
PV Tishler MD clinical data & patient reports: Safe
Substrate of CYP3A4. Modestly transactivates pregnane X receptor but has a low probability of inducing CYP3A4 (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; Curr Drug Metab 7:375,2006) |
| Gastrointestinal therapies |
ANTIEMETICS (Vomiting Therapies) |
Palonosetron |
Aloxi |
OK? |
|
| Gastrointestinal therapies |
ANTIEMETICS (Vomiting Therapies) |
Scopolamine |
Transderm-Scop, Scopace, Meldemar, others |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use |
| Gastrointestinal therapies |
ANTIEMETICS (Vomiting Therapies) |
Thiethylperazine |
Torecan |
OK? |
www.drugs-porphyria.org: Probably Not Porphyrinogenic |
| Gastrointestinal therapies |
ANTIEMETICS (Vomiting Therapies) |
Trimethobenzamide |
Tigan |
No info |
|
| GASTROINTESTINAL THERAPIES |
ANTISPASMODICS |
Atropine |
Many |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in patients
www.porphyriafoundation.com: Safe |
| GASTROINTESTINAL THERAPIES |
ANTISPASMODICS |
Belladonna Alkaloids |
Many |
BAD? |
web.uct.ac.za/depts/porphyria/: Avoid |
| Gastrointestinal therapies |
GASTROINTESTINAL MOTILITY STIMULANTS |
Alvimopan |
Entereg |
OK? |
Hepatic/CYP metab unlikely (Clin Pharmacol Therap 83:770,2008; PDR 63:3293,2009; pkg insert) |
| Gastrointestinal therapies |
GASTROINTESTINAL MOTILITY STIMULANTS |
Lubiprostone |
Amitiza |
OK? |
No CYP metabolism or induction (PDR 63:3082,2007) |
| Gastrointestinal therapies |
GASTROINTESTINAL MOTILITY STIMULANTS |
Metoclopramide |
Reglan |
OK? |
www.drugs-porphyria.org: Probably Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Caution
www.uq.edu.au/porphyria/: Probably unsafe
www.porphyriafoundation.com: Unsafe
Lancet 1981;2:91 Not safe
However, ~80% not metab by CYP (www.clinicalpharmacology-ip.com) |
| Gastrointestinal therapies |
H-2 ANTAGONISTS, PPIs (Reflux, Ulcer Therapies) |
Esomeprazole |
Nexium |
OK! |
www.drugs-porphyria.org: Possibly Porphyrinogenic.
www.porphyria.uct.ac.za: Use with extreme caution.
PV Tishler MD clinical data & patient report: Safe.
Major metabolic path via CYP2C19, minor via CYP3A4 (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007)
. |
| Gastrointestinal therapies |
H-2 Antagonists, PPIs (Reflux, Ulcer Therapies) |
Lansoprazole |
Pravacid |
OK? |
www.drugs-porphyria.org: Probably porphyrinogenic.
www.porphyria.uct.ac.za: Use but with caution.
Metabolsim mainly via CYP2C19.
Sinz M: Cur Drug Metab 2006; 7:375: Moderate activation of pregnane X receptor but low prediction of clinical induction. |
| Gastrointestinal therapies |
H-2 ANTAGONISTS, PPIs (Reflux, Ulcer Therapies) |
Pantoprazole |
Protonix |
OK! |
www.drugs-porphyria.org: Possibly Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Caution
Metabolized by CYP2C19, 3A4. No evidence for CYP3A4 inducibility (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; Drug Safety 29:769,2006)
2 Patient reports: Safe |
| GASTROINTESTINAL THERAPIES |
LAXATIVES |
Senna |
Senokot |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in patients |
| GASTROINTESTINAL THERAPIES |
PHOSPHATE BINDER AGENTS |
Sevelamer |
Renagel |
OK? |
www.drugs-porphyria.org: Not Porphyrinogenic |
| Gastrointestinal therapies |
PROSTAGLANDINS |
Misoprostol |
Cytotec |
OK? |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
Not metab by and does not affect CYPs (www.clinicalpharmacology-ip.com) |
| Hormones |
CORTICOSTEROIDS |
Dexamethasone |
Decadron |
OK? |
www.drugs-porphyria.org: Possibly Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use
Substrate of CYP3A4. Induces CYP3A4, 2C9 via transactivation of pregnane X receptor (modest). Patient report: Safe. MAY BE UNSAFE if used for prolonged periods. (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; Arch Toxicol 82:667,2008) |
| Hormones |
CORTICOSTEROIDS |
Methylprednisolone |
Medrol,others |
OK? |
www.drugs-porphyria.org: Possibly Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use
Substrate & inhibitor of CYP3A4. Induces CYP3A4 via transactivation of pregnane X receptor. Patient report: Safe. MAY BE UNSAFE if used for prolonged periods. (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; Arch Toxicol 82:667,2008) |
| Hormones |
ESTROGENS |
Ethinyl Estradiol |
Many |
OK? |
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
www.uq.edu.au/porphyria/: Probably safe
PV Tishler MD clinical data & patient report: Safe
Horm Metab Res 1995;27:379. Safe in patients
Mass. College of Pharmacy databse: Substrate & inhibitor of CYP3A4. Inducer of pregnane X receptor. |
| Hormones |
ORAL CONTRACEPTIVES |
Birth Control Pills |
Many |
BAD! |
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
www.uq.edu.au/porphyria/: Unsafe in patients
www.porphyriafoundation.com: Unsafe
Substrate of CYP3A4 (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007)
1Patient report: Safe. 3 patient reports: unsafe -
ethinyl estradiol/drospirenone (Yasmin), ethinyl estradiol-desogestrel (Orthocoept), ethinyl estradiol-norgestimate (Orcho Cyclen) unsafe |
| Hormones |
PROGESTINS |
Levonorgestrel |
Many |
BAD! |
www.drugs-porphyria.org: Possibly Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution. Metab by CYP3A4. |
| Hormones |
PROGESTINS |
Norethindrone |
Loestrin |
No info |
JAMA 1965;194:1037. Safe in patients
USP DI? Drug Info. for the Health Care Pro. - 26th Ed. (2006): Undergoes reduction in liver; induces CYP2C9. |
| Hormones |
PROGESTINS |
Progesterone |
Many |
BAD! |
www.drugs-porphyria.org: Probably Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
www.porphyriafoundation.com: Unsafe
Patient report: unsafe. Induces CYP3A, pregnane X receptor |
| Hormones, hormone-like |
ANDROGENS |
Danazol |
Danocrine |
BAD! |
www.drugs-porphyria.org: Probably Porphyrinogenic
www.porphyria-europe.com: Unsafe
web.uct.ac.za/depts/porphyria/: Avoid
www.uq.edu.au/porphyria/: Unsafe in patients
www.porphyriafoundation.com: Unsafe
J Clin Endocrinol Metab 1981;52:549. Exacerbates acute porphyria
J Clin Endocrinol Metab 1979;48:123. Unsafe in patients |
| HORMONES, HORMONE-LIKE |
ANDROGENS |
Methyltestosterone |
Many |
BAD! |
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution |
| HORMONES, HORMONE-LIKE |
ANDROGENS |
Nandrolone |
Deca-Durabolin |
BAD! |
www.drugs-porphyria.org: Porphyrinogenic
www.uq.edu.au/porphyria/: Probably unsafe |
| HORMONES, HORMONE-LIKE |
ANDROGENS |
Oxandrolone |
Oxandrin |
BAD? |
|
| HORMONES, HORMONE-LIKE |
ANDROGENS |
Stanozolol |
Winstrol |
BAD? |
www.drugs-porphyria.org: Not Porphyrinogenic |
| Hormones, hormone-like |
ANDROGENS |
Testosterone |
Many |
BAD! |
www.drugs-porphyria.org: Porphyrinogenic
Substrate of CYP3A4 & CYP2C9. Modestly transactivates pregnane X receptor (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; Curr Drug Metab 7:375,2006) |
| HORMONES, HORMONE-LIKE |
CORTICOSTEROIDS |
Betamethasone |
Many |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Caution |
| HORMONES, HORMONE-LIKE |
CORTICOSTEROIDS |
Cortisone |
Many |
OK! |
|
| HORMONES, HORMONE-LIKE |
CORTICOSTEROIDS |
Fludrocortisone |
Florinef |
OK! |
www.drugs-porphyria.org: Possibly Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Caution |
| Hormones, hormone-like |
CORTICOSTEROIDS |
Hydrocortisone |
Many |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Probably safe
Substrate of CYP3A4 (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007) |
| Hormones, hormone-like |
CORTICOSTEROIDS |
Prednisolone |
Many |
OK? |
Substrate of CYP3A4. Induces CYP3A4 via transactivation of pregnane X receptor. Patient report: Safe. MAY BE UNSAFE if used for prolonged periods. (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; Arch Toxicol 82:667,2008) |
| Hormones, hormone-like |
CORTICOSTEROIDS |
Prednisone |
Many |
OK! |
www.drugs-porphyria.org: Possibly Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use
Substrate of CYP3A4. Weakly transactivates pregnane X receptor (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; Curr Drug Metab 7:375, 2006)
Patient reports: Safe |
| HORMONES, HORMONE-LIKE |
CORTICOSTEROIDS |
Triamcinolone |
Aristocort |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Caution |
| HORMONES, HORMONE-LIKE |
ESTROGENS |
Estrogens, Conjugated |
Many |
OK! |
www.drugs-porphyria.org: Possibly Porphyrinogenic |
| Hormones, hormone-like |
ESTROGENS |
Estropipate |
Ogen, Ortho-est |
No info |
|
| HORMONES, HORMONE-LIKE |
LHRH/GNRH AGONISTS |
Goserelin |
Zoladex |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic |
| HORMONES, HORMONE-LIKE |
LHRH/GNRH AGONISTS |
Leuprolide |
Lupron |
OK? |
Protein, metabolized by proteolysis |
| HORMONES, HORMONE-LIKE |
LHRH/GNRH AGONISTS |
Nafarelin |
Synarel |
OK! |
www.drugs-porphyria.org: Possibly Porphyrinogenic
www.porphyria-europe.com: Safe |
| HORMONES, HORMONE-LIKE |
OVULATION STIMULANTS |
Clomiphene |
Clomid |
OK! |
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in patients |
| Hormones, hormone-like |
PARATHYROID |
Calcitonin |
Miacelcin, Calcimar, Fortical |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use
www.porphyria-europe.com: Safe
Patient report: Safe |
| HORMONES, HORMONE-LIKE |
PITUITARY |
Chorionic Gonadotropin |
Pregnyl |
OK! |
www.drugs-porphyria.org: Possibly Porphyrinogenic |
| HORMONES, HORMONE-LIKE |
PITUITARY |
Desmopressin |
DDAVP |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic |
| HORMONES, HORMONE-LIKE |
PITUITARY |
Ergonovine |
Ergotrate |
OK! |
|
| HORMONES, HORMONE-LIKE |
PITUITARY |
Menotropins |
Repronex |
OK! |
|
| HORMONES, HORMONE-LIKE |
PITUITARY |
Methylergonovine |
Methergine |
OK! |
|
| HORMONES, HORMONE-LIKE |
PITUITARY |
Oxytocin |
Pitocin |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in patients |
| HORMONES, HORMONE-LIKE |
PITUITARY |
Urofollitropin |
Fertinorm |
OK! |
|
| HORMONES, HORMONE-LIKE |
PITUITARY |
Vasopressin |
Pitressin |
OK! |
|
| HORMONES, HORMONE-LIKE |
PROGESTINS |
Medroxyprogesterone |
Provera |
BAD! |
www.drugs-porphyria.org: Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution |
| Hormones, hormone-like |
SELECTIVE ESTROGEN RECEPTOR MODULATORS (SERMs) |
Raloxifene |
Evista |
BAD? |
www.drugs-porphyria.org: Probably Porphyrinogenic.
Chang: Drug Metab Disp 2006; 34:2073: bound to P-gycoprotein & activated by CYP3A4.
Sinz M: Cur Drug Metab 2006; 7:375: Little activation of human pregnane X receptor & low prediction of clinical induction. |
| HORMONES, HORMONE-LIKE |
SOMATOSTATIC AGENTS |
Octreotide |
Sandostatin |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use |
| HORMONES, HORMONE-LIKE |
SPERMICIDES (VAGINAL) |
Nonoxynol-9 |
Many |
NO INFO |
|
| HORMONES, HORMONE-LIKE |
THYROID |
Levothyroxine |
Levoxyl, Synthroid |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use
PV Tishler MD clinical data & patient reports: Safe |
| HORMONES, HORMONE-LIKE |
THYROID |
Liothyronine |
Cytomel |
OK! |
web.uct.ac.za/depts/porphyria/: Use |
| Hormones, hormone-like |
THYROID |
Methimazole |
Tapazole |
No info |
Metab by liver, presumably by CYPs; inhibits several CYPs also (Drug Metab Dispos 1997;25:390) |
| Hormones, hormone-like |
THYROID |
Propylthiouracil (PTU) |
Procasil, Propacil, others |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
www.porphyria-europe.com: safe
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in patients |
| Immunologic |
IMMUNOSUPPRESSIVE AGENTS |
Sirolimus |
Rapamune |
BAD? |
www.drugs-porphyria.org: Possibly Porphyrinogenic
metab mainly by & induces CYP3A4, also CYP3A5 (Drug Metab Disp 35:350,2007. Induces pregnane X receptor. |
| IMMUNOLOGIC AGENTS |
ANTIMICROBIAL VACCINES |
Anti-Thymocyte Globulin, Lymphocyte Immune Globulin |
none |
OK? |
|
| IMMUNOLOGIC AGENTS |
ANTIMICROBIAL VACCINES |
Haemophilus B |
none |
OK? |
|
| IMMUNOLOGIC AGENTS |
ANTIMICROBIAL VACCINES |
Hepatitis A |
none |
OK? |
www.drugs-porphyria.org: Not Porphyrinogenic |
| IMMUNOLOGIC AGENTS |
ANTIMICROBIAL VACCINES |
Hepatitis B |
none |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic |
| IMMUNOLOGIC AGENTS |
ANTIMICROBIAL VACCINES |
Influenza |
none |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic |
| IMMUNOLOGIC AGENTS |
ANTIMICROBIAL VACCINES |
Japanese Encephalitis |
none |
OK? |
|
| IMMUNOLOGIC AGENTS |
ANTIMICROBIAL VACCINES |
Measles, Mumps & Rubella |
none |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic |
| IMMUNOLOGIC AGENTS |
ANTIMICROBIAL VACCINES |
Meningococcal |
none |
OK? |
|
| IMMUNOLOGIC AGENTS |
ANTIMICROBIAL VACCINES |
Mumps |
none |
OK! |
|
| IMMUNOLOGIC AGENTS |
ANTIMICROBIAL VACCINES |
Pneumococcal |
none |
OK! |
|
| IMMUNOLOGIC AGENTS |
ANTIMICROBIAL VACCINES |
Polio |
none |
OK! |
|
| IMMUNOLOGIC AGENTS |
ANTIMICROBIAL VACCINES |
Rabies |
none |
OK? |
|
| IMMUNOLOGIC AGENTS |
ANTIMICROBIAL VACCINES |
Typhoid |
none |
OK? |
www.drugs-porphyria.org: Not Porphyrinogenic |
| IMMUNOLOGIC AGENTS |
ANTIMICROBIAL VACCINES |
Typhoid VI Polysaccharide |
none |
OK? |
www.drugs-porphyria.org: Not Porphyrinogenic |
| IMMUNOLOGIC AGENTS |
ANTIMICROBIAL VACCINES |
Varicella |
none |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic |
| IMMUNOLOGIC AGENTS |
ANTIMICROBIAL VACCINES |
Yellow Fever |
none |
OK? |
www.drugs-porphyria.org: Not Porphyrinogenic |
| IMMUNOLOGIC AGENTS |
ANTIVENINS |
Antivenin Crotalidae Polyvalent |
AntiveninPolyvalent |
OK? |
|
| IMMUNOLOGIC AGENTS |
ANTIVENINS |
Antivenin Latrodectus Mactans |
none |
OK? |
|
| IMMUNOLOGIC AGENTS |
ANTIVENINS |
Antivenin Micrurus Fulvius |
none |
OK? |
|
| IMMUNOLOGIC AGENTS |
ANTIVIRAL MONOCLONAL ANTIBODIES |
Palivizumab |
Synagis |
OK? |
www.drugs-porphyria.org: Not Porphyrinogenic |
| IMMUNOLOGIC AGENTS |
IMMUNE GLOBULINS |
Cytomegalovirus |
none |
OK? |
(web.uct.ac.za/depts/porphyria/: Use) |
| IMMUNOLOGIC AGENTS |
IMMUNE GLOBULINS |
Hepatitis B |
none |
OK? |
(web.uct.ac.za/depts/porphyria/: Use)
www.drugs-porphyria.org: Not Porphyrinogenic |
| IMMUNOLOGIC AGENTS |
IMMUNE GLOBULINS |
Immune Globulin IV |
none |
OK? |
(web.uct.ac.za/depts/porphyria/: Use)
www.drugs-porphyria.org: Not Porphyrinogenic |
| IMMUNOLOGIC AGENTS |
IMMUNE GLOBULINS |
Rabies |
none |
OK? |
(web.uct.ac.za/depts/porphyria/: Use) |
| IMMUNOLOGIC AGENTS |
IMMUNE GLOBULINS |
Tetanus |
none |
OK? |
(web.uct.ac.za/depts/porphyria/: Use) |
| IMMUNOLOGIC AGENTS |
IMMUNOMODULATORS |
Thalidomide |
Thalomid |
NO INFO |
|
| Immunologic agents |
IMMUNOSUPPRESSIVE AGENTS |
Azathioprine |
Imuran |
OK? |
www.drugs-porphyria.org: Probably Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in animals
J Clin Pharmacol 2001;41:113. Safe
Not metab by CYPs (www.clinicalpharmacology-ip.com) |
| Immunologic agents |
IMMUNOSUPPRESSIVE AGENTS |
Cyclosporine |
Sandimmune |
OK? |
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
www.uq.edu.au/porphyria/: Unsafe in animals
J Clin Pharmacol 2001;41:113. Safe
Major metab by CYP3A4,3A5. Does not transactivate pregnene X receptor (Biochem Pharmacol 68:1889,2004; Curr Drug Metab 7:375,2006) |
| Immunologic agents |
IMMUNOSUPPRESSIVE AGENTS |
Mycophenolate Mofetil |
CellCept |
OK? |
J Clin Pharmacol 2001;41:113. Safe
~85% nonmetab by CYP, with minor contribution of CYP3A4/5 (Clin Pharmacokinet 46:13,2007; Therapeutic Drug Monitor 26:600,2004) |
| Immunologic agents |
IMMUNOSUPPRESSIVE AGENTS |
Tacrolimus |
Prograf, Protopic |
BAD? |
www.drugs-porphyria.org: Possibly Porphyrinogenic
J Clin Pharmacol 2001;41:113. Safe
Major metab by CYP3A4, 3A5 (Pharmacogenetics & Genomics 19:458,2009) |
| Immunologic agents |
TOXOIDS |
Diphtheria + Tetanus Toxoids & Acellular Pertussis Adsorbed, Hepatitis B (recombinant) & Inactivated Polioviruis Vaccine Combined |
Pediatrix |
OK! |
All component parts of this vaccine are safe individually as well. |
| n/a |
n/a |
Levobunolol |
Betagan, others |
OK! |
|
| n/a |
n/a |
Proparacaine |
Alcaine, Ophthetic, Ophthaine, others |
OK! |
|
| n/a |
n/a |
Timolol |
Combigan, Timolide, Cosopt |
OK! |
|
| NARCOTIC ANTAGONISTS |
n/a |
Naloxone |
Narcan |
OK! |
www.drugs-porphyria.org: Possibly Porphyrinogenic. Opioid derivative metabolised by a series of CYPs, mainly 3A4. Two references: Use
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use |
| OPHTHALMIC AGENTS (intraocular) |
n/a |
Acetylcholine |
Miochol |
OK! |
|
| OPHTHALMIC AGENTS (intraocular) |
n/a |
Apraclonidine |
Iopidine |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic |
| OPHTHALMIC AGENTS (intraocular) |
n/a |
Betaxolol |
Many |
OK! |
|
| OPHTHALMIC AGENTS (intraocular) |
n/a |
Bimatoprost |
Lumigan |
OK! |
|
| OPHTHALMIC AGENTS (intraocular) |
n/a |
Brimonidine |
Alphagan |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic |
| OPHTHALMIC AGENTS (intraocular) |
n/a |
Cyclopentolate |
Cyclogyl |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic |
| OPHTHALMIC AGENTS (intraocular) |
n/a |
Dapiprazole |
Rev-Eyes |
OK! |
|
| OPHTHALMIC AGENTS (intraocular) |
n/a |
Dorzolamide |
Trusopt |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
www.drugs.com: excreted primarily as unchanged drug |
| OPHTHALMIC AGENTS (intraocular) |
n/a |
Fluorescein |
Many |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic |
| OPHTHALMIC AGENTS (intraocular) |
n/a |
Homatropine |
Many |
OK! |
|
| OPHTHALMIC AGENTS (intraocular) |
n/a |
Latanoprost |
Xalatan |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic |
| OPHTHALMIC AGENTS (intraocular) |
n/a |
Naphazoline |
Many |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic |
| OPHTHALMIC AGENTS (intraocular) |
n/a |
Pilocarpine |
Many |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic |
| OPHTHALMIC AGENTS (intraocular) |
n/a |
Travoprost |
Travatan |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic |
| OPHTHALMIC AGENTS (intraocular) |
n/a |
Trifluridine |
Viroptic |
OK! |
|
| OPHTHALMIC AGENTS (intraocular) |
n/a |
Tropicamide |
Mydriacyl |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic |
| Psychiatric |
ANTI-DEPRESSANT |
Desvenlafaxine |
Pristiq |
OK? |
<5% metab by CYP3A4 (PDR 63:3247,2009). No CyP3A4 inhibition.
(CNS Drugs 2012:26:39) |
| Psychiatric |
ANTI-DEPRESSANT |
Duloxetine |
Cymbalta |
OK? |
~97% metab by CYP1A2, 2D6 (Drug Metab Disp 31:1142,2003). No effect on activity of CyP3A4 or 2C9 (CNS Drugs 2012; 26:39) 2 Patient reports:safe. Report of questionable patient: unsafe. |
| Psychiatric |
ANTI-DEPRESSANT |
Mirtazapine |
Remeron |
OK! |
www.drugs-porphyria.org: Possibly Porphyrinogenic.
1/4 not metab, 1/3 metab by CYP2D6, rest by CYP3A4, 1A2.
Moderate activation of pregnane X receptor but low prediction of clinical induction (Clin Pharmacogenet 38:461,2000; Cur Drug Metab 7:375,2006). Patient reports: safe |
| Psychiatric |
ANTI-DEPRESSANT |
Venlafaxine |
Effexor |
OK? |
www.drugs-porphyria.org: Possibly porphyrinogenic.
www.porphyria.uct.ac.za: Use only with extreme caution.
Fogelman SM: Neuropsychopharm 1999; 20:480: Major metabolism via CYP2D6 (90%), 2C19 (9%); or also CYP3A4 (CNS Drugs 2012; 26:39).
Sinz M: Cur Drug Metab 2006; 7:375: No activation of pregnane X receptor. |
| Psychiatric |
MISC. |
Asenapine |
Saphris |
No info |
Metab by CYPs; proportion by CYP3A4 unknown (Drug Metab Disp 39:580, 2011) |
| Psychiatric |
MISC. |
Bupropion |
Wellbutrin, Zyban |
OK? |
www.drugs-porphyria.org: Unlikely Porphyrinogenic.
USP DI? Drug Info. for the Health Care Pro. - 26th Ed: Metabolized primarily by CYP2B6 (also CNS Drugs 2012; 26:39) & CYP2D6; Moderately transactivates pregnane X receptor but has low probability of inducing CYP3A4 (Curr Drug Metab 9:598,2008; http://medicine.iupui.edu/clinpharm/ddis/) |
| Psychiatric |
MISC. |
Clozapine |
Clozaril |
OK? |
www.drugs-porphyria.org: Probably Not Porphyrinogenic. Metab. mainly by CYP1A2, to lesser extent by CYP3A & other CYPs. Induces CYP 3A, 2C9. Minimal transactivation of pregnane X receptor (Eur J Pharm Sci 20:451, 2003; Curr Drug Metab 11:516, 2010; Toxicol Lett 82:203, 2011) |
| Psychiatric |
MISC. |
Dexmedetomidine |
Precedex |
OK? |
~14% metab. by CYP2A6, remainder by glucuronidation. |
| Psychiatric |
MISC. |
Iloperidone |
Fenapt |
No info |
99% metab, mainly by CYP2D6, less so by CYP3A4 (Curr Drug Metab 11:516, 2010) |
| Psychiatric |
Misc. |
Olanzapine |
Zyprexa |
OK? |
www.drugs-porphyria.org: Probably not porphyrinogenic.
www.porphyria_europe.com: Safe. Minor metab. by CYP1A2, 2D6 ?3A4.
Moderate activation of pregnane X receptor & low prediction of clinical induction (Basic Clin Pharmacol Toxicol 100:4,2007; Cur Drug Metab 7:375,2006; Curr Drug Metab 11:516,2010) |
| Psychiatric |
Misc. |
Quetiapine |
Seroquel |
BAD? |
www.drugs-porphyria.org: Possibly Porphyrinogenic.
Metab. mainly by CYP3A4. No evidence for its induction. (http://medicine.iupui.edu/clinpharm/ddis/; Basic Clin Pharmacol Toxicol 100:4,2007)
Patient report: safe |
| Psychiatric |
Misc. |
resperidone |
Resperdal, etc. |
OK? |
Major metab via CyP2D6. Weak inhibition of Cyp3A, PXR. |
| Psychiatric |
MISC. |
Risperidone |
Risperdal |
OK? |
www.drugs-porphyria.org: Probably Porphyrinogenic.
Spina E: Basic Clin Pharmacol Toxicol 2007; 100:4: Substrate mainly of CYP2D6, less of 3A4. Sinz M. Cur Durg Metab 2006; 7:375: No activation of pregnane X rerceptor. Toxicol Lett 203:82, 2011: modest activation of pregnane X receptor (1/5 that of rifampin). |
| Psychiatric |
MISC. |
Trazodone |
Desyrel |
BAD? |
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
www.uq.edu.au/porphyria/: Unsafe in animals
Substrate of CYP3A4 (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; http://medicine.iupui.edu/clinpharm/ddis/) |
| Psychiatric |
MISC. |
Ziprasidone |
Geodon |
BAD? |
www.drugs-porphyria.org: Possibly Porphyrinogenic
1/3 metabolized by CYP3A4 (www.rxlist.com; J Clin Psychopharm 23:229,2003) |
| Psychiatric |
PHENOTHIAZINES |
Chlorpromazine |
Thorazine |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in patients
PV Tishler MD clinical data: Safe
JAMA 1965;194:1042. Safe in patients
Substrate of CYP3A4. Does not or does moderately transactivate pregnane X receptor. and does transactivate constitutive androgen receptor (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; Curr Drug Metab 7:375,2006; Xenobiotica 37:1196,2007; J Pharmacol Exp Therap 320:72, 2007) |
| Psychiatric |
SELECTIVE SEROTONIN REUPTAKE INHIBITORS (SSRIs) |
Citalopram |
Celexa |
OK? |
www.drugs-porphyria.org: Possibly Porphyrinogenic. Substrate of CYP3A. web.uct.ac.za/depts/porphyria/: Use with Caution.
1 Patient report: safe. 1 patient report: unsafe |
| Psychiatric |
SELECTIVE SEROTONIN REUPTAKE INHIBITORS (SSRIs) |
Escitalopram |
Lexapro |
No info |
Major metabolism by CYP2C19, CYP3A4; no inhibition of CYP3A4 (CNS Drugs 2012; 26:39) |
| Psychiatric |
SELECTIVE SEROTONIN REUPTAKE INHIBITORS (SSRIs) |
Fluoxetine |
Prozac |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use with Caution
www.uq.edu.au/porphyria/: Safe in patients
Substrate of CYP2C9 (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007)
Does not induce pregnane X receptor (Toxicol Lett 203:82, 2011)
Patient reports: safe |
| Psychiatric |
SELECTIVE SEROTONIN REUPTAKE INHIBITORS (SSRIs) |
Paroxetine |
Paxil |
OK? |
www.drugs-porphyria.org: Probably Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Caution Does not induce pregnane-X-receptor (Toxicol Lett 203:82, 2011). |
| Psychiatric |
SSELECTIVE SEROTONIN REUPTAKE INHIBITORS (SSRIs) |
Fluvoxamine |
Luvox |
OK? |
Prob ~65% metab by CYP2D6 + alcohol dehydrogenase (Xenobiotica 37:169,2007). Inhibits CYP3A4. |
| Psychiatric |
TRICYCLICS |
Amitriptyline |
Elavil |
OK! |
www.drugs-porphyria.org: Probably Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
www.uq.edu.au/porphyria/: Probably unsafe
Substrate of many CYPs, including CYP3A4, but does not transactivate pregnane X receptor (http://medicine.iupui.edu/clinpharm/ddis/; Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; Curr Drug Metab 7:375, 2006)
patient reports: safe |
| Psychiatric |
TRICYCLICS |
Imipramine |
Tofranil |
OK? |
www.drugs-porphyria.org: Probably Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
www.uq.edu.au/porphyria/: Probably unsafe
Metab by CYP2C19, 2D6, 3A4.
(http://medicine.iupui.edu/clinpharm/ddis/; Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007) |
| Psychiatric medications |
AGENTS FOR CHEMICAL DEPENDENCY |
Disulfiram |
Antabuse |
OK? |
www.drugs-porphyria.org: Probably Porphyrinogenic
Eur J Clin Chem Clin Biochem 1997;35:427. Safe in patients
Major metabolism by CYP3A4/3A5. Inhibits but probably does not induce CYPs (Alcohol Clin Exp Res 22:1212,1998; Arch Toxicol 82:667,2008) |
| Psychiatric medications |
AGENTS FOR CHEMICAL DEPENDENCY |
Naltrexone |
Vivitrol |
OK? |
No CYP metabolism (PDR 63:988, 2009) |
| Psychiatric medications |
ANTIDEMENTIA AGENTS |
Donepezil |
Aricept |
OK? |
www.drugs-porphyria.org: Possibly Porphyrinogenic
www.drugs.com: ~80% metab via CYP2D6, 3A4
(www.clinicalpharmacology-ip.com; Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007) |
| Psychiatric medications |
ANTIDEMENTIA AGENTS |
Memantine |
Namenda |
OK? |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
www.rxlist.com: ca. 50% excreted unchanged; no significant metabolic role for CYPs |
| Psychiatric medications |
MISC. |
Aripiprazole |
Abilify |
No info |
Metab mainly by CYP3A4,2D6 (Curr Drug Metab 9:410,2008) |
| Psychiatric medications |
MISC. |
Dextroamphetamine |
Dexedrine |
BAD? |
Substrate of CYP3A4 (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007) |
| Psychiatric medications |
MISC. |
Haloperidol |
Haldol |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic.
www.porphyria-europe.com: Safe.
web.uct.ac.za/depts/porphyria/: Use.
www.uq.edu.au/porphyria/: Probably unsafe.
Substrate mainly of 3A4, also 3A5, 3A7. Moderate activation of human pregnane X receptor & low prediction of clinical induction.
(Chem Res Toxicol 2006; 19:914; Cur Drug Metab 2006; 7:375) |
| Psychiatric medications |
MISC. |
Lithium |
Eskalith, Lithobid |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in patients |
| PSYCHIATRIC MEDICATIONS |
MISC. |
Methylphenidate |
Ritalin |
OK? |
www.drugs.com: Major metabolic route probably does not involve P450 |
| Psychiatric medications |
MISC. |
Paliperidone |
Invega |
OK? |
60% excreted unchanged. Small amt metab by CYP2D6,?other CYPs (Drug Metab Disp 36:769,2008) |
| PSYCHIATRIC MEDICATIONS |
MISC. |
Phenelzine |
Nardil |
BAD! |
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
www.uq.edu.au/porphyria/: Unsafe in animals |
| PSYCHIATRIC MEDICATIONS |
PHENOTHIAZINES |
Fluphenazine |
Prolixin |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use |
| PSYCHIATRIC MEDICATIONS |
PHENOTHIAZINES |
Perphenazine |
Trilafon |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Caution |
| Psychiatric medications |
PHENOTHIAZINES |
Prochlorperazine |
Compazine, Compro, Combid, others |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in patients
PV Tishler MD clinical data: Safe |
| Psychiatric medications |
PHENOTHIAZINES |
Thioridazine |
Mellaril |
OK! |
www.drugs-porphyria.org: Possibly Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Caution
www.uq.edu.au/porphyria/: Safe in patients
Polish J Pharmacol 2001;53:615. Metabolized by CYP2D6;inhibits CYP1A2 and CYP3A2 |
| Psychiatric medications |
SELECTIVE SEROTONIN REUPTAKE INHIBITORS (SSRIs) |
Sertraline |
Zoloft |
OK? |
www.drugs-porphyria.org: Possibly Porphyrinogenic
Substrate of CYP3A4 but minimially transactivates pregnane X receptor (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; Curr Drug Metab 7:375,2006. |
| Psychiatric medications |
TRICYCLICS |
Doxepin |
Sinequan, Adepin, others |
OK? |
Medicine (Balt)1992;71:1. Safe
Patient report: Safe |
| Psychiatric medications |
TRICYCLICS |
Nortriptyline |
Aventyl |
OK? |
www.drugs-porphyria.org: Probably Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
www.uq.edu.au/porphyria/: Probably unsafe.
Metab by CYP2D6. Does not transactivate pregnane X receptor (http://medicine.iupui.edu/clinpharm/ddis/; Curr Drukg Metab 7:375,2006) |
| Respiratory |
ANTIASTHMATIC AND BRONCHODILATOR AGENTS |
Albuterol |
Ventolin, Proventil, others |
OK! |
PV Tishler MD clinical data, 3 patient reports: Safe
https://online.epocrates.com/front_porch/: Metabolized extensively by P450. Does not transactivate pregnane X receptor (Curr Drug Metab 7:375,2006) |
| Respiratory |
ANTIASTHMATIC AND BRONCHODILATOR AGENTS |
Budesonide |
Pulmicort, Rhinocort, Entocort |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
PV Tishler MD clinical data & patient report: Safe
Metab by CYP3A |
| Respiratory |
ANTIASTHMATIC AND BRONCHODILATOR AGENTS |
Fluticasone |
Flovent |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
PV Tishler MD clinical data & patient reports: Safe
Substrate of CYP3A4 (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007) |
| Respiratory |
ANTIASTHMATIC AND BRONCHODILATOR AGENTS |
Formoterol |
Foradil, Perforomist |
OK? |
Secondary metab via 4 CYPs (PDR 63:1025,2009), inc. CYP2C9 |
| Respiratory |
ANTIASTHMATIC AND BRONCHODILATOR AGENTS |
Montelukast |
Singulair |
OK! |
www.drugs-porphyria.org: Possibly Porphyrinogenic
Substrate of CYP3A4 & CYP2C9. No inhibition of CYP2C9, 3A4. Moderate transactivation of pregnane X receptor but low prediction of CYP3A4 induction (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; Curr Drug Metab 7:375, 2006)
Patient report: Safe |
| Respiratory |
ANTIASTHMATIC AND BRONCHODILATOR AGENTS |
Zafirlukast |
Accolate |
BAD? |
Substrate of CYP2C9. Induces pregnane X receptor. (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007) |
| Respiratory |
ANTIHISTAMINES |
Cetirizine |
Zyrtec |
OK! |
Mainly excreted unchanged. Does not induce CYPs (Cur Med Therap 15:2193,2008; Med Letter 49:97,2007). 1 patient report: safe. |
| Respiratory |
ANTIHISTAMINES |
Chlorpheniramine |
Chlor-Trimeton, others |
OK! |
www.uq.edu.au/porphyria/: Safe in patients
Metab by CYP2D6, CYP3A4, 2D9 (Pharmacogenetics 1999;9:71; J Pharm Pharmacol 49:257,1997)
Patient report: Safe |
| Respiratory |
ANTIHISTAMINES |
Diphenhydramine |
Benadryl |
OK! |
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use
Patient reports: Safe |
| Respiratory |
ANTIHISTAMINES |
Fexofenadine |
Allegra |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
USP DI? Drug Info. for the Health Care Pro. - 26th Ed. (2006): Ca. 1% metabolized by P450, ~5% total. Patient reports: Safe |
| Respiratory |
ANTIHISTAMINES |
Loratadine |
Claritin |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use with Caution
Substrate of CYP3A4, 2C9. Moderate transactivator of pregnane X receptor, but low probability of inducing CYP3A4 (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; Curr Drug Mertab 7:375,2006)
3 Patient reports: safe |
| Respiratory |
ANTITUSSIVES (Cough Therapies) |
Benzonatate |
Tessalon, etc. |
OK? |
patient report: safe |
| Respiratory |
ANTITUSSIVES (Cough Therapies) |
Dextromethorphan |
Many |
OK! |
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use
Metab by CYP3A4. |
| Respiratory |
Asthma Treatment |
Fluticasone |
Advair |
OK? |
fluticasone = corticosteroid; salmeterol, brochodilator, metab via CYP3A. Used by inhalation. 1 patient report: safe. |
| RESPIRATORY AGENTS |
ANTIASTHMATIC AND BRONCHODILATOR AGENTS |
Aminophylline |
Many |
BAD! |
www.drugs-porphyria.org: Probably Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Avoid |
| Respiratory agents |
ANTIASTHMATIC AND BRONCHODILATOR AGENTS |
Arformoterol |
Brovana |
OK? |
Secondary metab via 4 CYPs (PDR 63:2990,2009) |
| Respiratory agents |
ANTIASTHMATIC AND BRONCHODILATOR AGENTS |
Beclomethasone (Inhalant) |
Beclovent, Vanceril, others |
OK! |
www.uq.edu.au/porphyria/: Safe in patients
PV Tishler MD clinical data: Safe |
| Respiratory agents |
ANTIASTHMATIC AND BRONCHODILATOR AGENTS |
Cromolyn |
Intal, others |
OK? |
|
| Respiratory agents |
ANTIASTHMATIC AND BRONCHODILATOR AGENTS |
Flunisolide (Inhalant) |
Aerobid, Nasalide, Nasarel |
No info |
|
| Respiratory agents |
ANTIASTHMATIC AND BRONCHODILATOR AGENTS |
Ipratropium |
Atrovent |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
http://www.bidocs.com/renetnt:/Prescribing+ Information/PIs/Atrovent+Nasal+03/ATR03.pdf: Metabolized via hydrolysis patient report: safe |
| Respiratory agents |
ANTIASTHMATIC AND BRONCHODILATOR AGENTS |
Salmeterol |
Serevent |
OK? |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
Substrate of CYP3A4 (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007) |
| RESPIRATORY AGENTS |
ANTIASTHMATIC AND BRONCHODILATOR AGENTS |
Terbutaline |
Brethine |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
Eur. J. Clin. Pharmacol. 1993;45 :483. No metabolism in liver |
| Respiratory agents |
ANTIASTHMATIC AND BRONCHODILATOR AGENTS |
Theophylline |
Many |
BAD? |
www.drugs-porphyria.org: Probably Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
www.uq.edu.au/porphyria/: Unsafe in patients
Medicine (Balt) 1992;71:1. Safe
Substrate of CYP3A4, but does not transactivate pregnane X receptor (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007; Curr Drug Metab 7:375,2006) |
| Respiratory agents |
ANTIHISTAMINES |
Azatadine |
Optimine, Trinalin, others |
No info |
|
| RESPIRATORY AGENTS |
ANTIHISTAMINES |
Cyproheptadine |
Periactin |
OK! |
www.drugs-porphyria.org: Possibly Porphyrinogenic |
| Respiratory agents |
ANTIHISTAMINES |
Hydroxyzine |
Atarax, Vistaril |
BAD! |
www.drugs-porphyria.org: Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
www.uq.edu.au/porphyria/: Unsafe in patients |
| Respiratory agents |
ANTIHISTAMINES |
Levocetirizine |
Xyzal |
OK! |
Mainly excreted unchanged. Does not induce CYPs (Curr Med Therap 15:2193, 2008; Med Letter 49:97,2007) |
| RESPIRATORY AGENTS |
ANTIHISTAMINES |
Promethazine |
Phenergan |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Probably unsafe
Curr Drug Metab 2003;4:105. Metabolized by CYP2D6 |
| Respiratory agents |
ANTITUSSIVES (Cough Therapies) |
Hydrocodone |
Many |
OK! |
Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007. Substrate of CYP3A4
Patient reports: Safe |
| Respiratory agents |
EXPECTORANTS |
Guaifenesin |
Robitussin |
OK! |
www.drugs-porphyria.org: Possibly Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
PV Tishler MD clinical data & patient report: Safe |
| RESPIRATORY AGENTS |
MUCOLYTICS |
Acetylcysteine |
Mucomyst |
OK! |
www.drugs-porphyria.org: Not Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use
PV Tishler MD clinical data: Safe
Eur J Clin Chem Clin Biochem 1997;35:427. Safe |
| RESPIRATORY AGENTS |
NASAL AGENTS - SYSTEMIC AND TOPICAL |
Oxymetazoline |
Afrin |
OK? |
www.drugs-porphyria.org: Probably Not Porphyrinogenic
www.uq.edu.au/porphyria/: Unsafe in patients |
| RESPIRATORY AGENTS |
NASAL AGENTS - SYSTEMIC AND TOPICAL |
Phenylephrine |
Many |
OK! |
www.drugs-porphyria.org: Probably Not Porphyrinogenic |
| RESPIRATORY AGENTS |
NASAL AGENTS - SYSTEMIC AND TOPICAL |
Pseudoephedrine |
Sudafed |
OK! |
www.porphyria-europe.com: Safe
web.uct.ac.za/depts/porphyria/: Use
www.uq.edu.au/porphyria/: Safe in patients
Patient reports: Safe |
| URINARY TRACT |
ANALGESICS |
Phenazopyridine |
Pyridium |
NO INFO |
|
| URINARY TRACT |
ANTISPASMODICS |
Bethanechol |
Urecholine |
NO INFO |
|
| Urinary tract |
ANTISPASMODICS |
Darifenacin |
Enablex |
BAD? |
Significantly metab by CYP3A4, 2D6. No evidence of CYP induction (Clin Pharmacokinet 45:325,2006) |
| Urinary tract |
ANTISPASMODICS |
Oxybutynin |
Oxytrol, Ditropan |
BAD! |
www.drugs-porphyria.org: Possibly Porphyrinogenic
web.uct.ac.za/depts/porphyria/: Use with Extreme Caution
www.drugs.com: Metabolized primarily in liver by CYP3A4
Substrate of CYP3A4 (Williams DA. Drug metabolism. In: Foye's Principles of Medicinal Chemistry, ed. Lemke T and Williams DA. Baltimore, Williams & Wilkins, 6th ed., 2007) |
| Urinary tract |
ANTISPASMODICS |
Solifenacin |
Vesicare |
OK? |
Metab primarily by CYP3A4. No evidence of any CYP induction (Br J Clin Pharmacol 59:647,2004) |
| Urinary tract |
ANTISPASMODICS |
Tolterodine |
Detrol |
OK? |
www.drugs-porphyria.org: Safe in one patient, but possibly porphyrinogenic. Metab by CYP2D6,3A4; CYP3A4 may be increased in CYP2D6 poor metabolizers (Drug Metab Disp 26:289,1998)
Patient report to Peter Tishler, MD - safe |
| Urinary tract |
PROSTATIC HYPERTROPHY |
Dutasteride |
Avodart |
BAD? |
Extensively metab by CYP3A4,3A5 (PDR 63:1359,2009). 2 patient reports: unsafe |
| Urinary tract |
PROSTATIC HYPERTROPHY |
Tamsulosin |
Flomax |
BAD? |
Extensively metab by CYP3A4,2D6 (Xenobiotica 28:909, 1998; PDR 63:848,2009). |
| Urinary tract |
PROSTATIC HYPERTROPHY (also Baldness) |
Finasteride |
Proscar, Propecia |
OK! |
www.drugs-porphyria.org:Possibly porphyrinogenic.
www.porphyria.uct.ac.za: Use only with extreme caution.
Metab mainly by CYP3A4. Little activation of pregnane X receptor (Huskey SW: Drug Metab Disp 1996; 24:695; Sinz M. Cur Drug Metab 2006; 7:375) |
