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This information is not intended as a substitute for medical professional help or advice but is to be used only as a reference.

OK! = very likely to be safe for prolonged use by individuals with an acute porphyria, based on consistent evidence

OK? = probably safe for prolonged use by individuals with an acute porphyria, based on evidence that is either inconsistent or insufficient to be conclusive

BAD? = probably unsafe for prolonged use by individuals with an acute porphyria, based on evidence that is either inconsistent or insufficient to be conclusive

BAD! = very likely to be unsafe for prolonged use by individuals with an acute porphyria, based on consistent evidence

Class Type Generic name Brand name Conclusion References
721 records found
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- Levobunolol Betagan, others OK!
- Proparacaine Alcaine, Ophthetic, Ophthaine, others OK!
- Timolol Combigan, Timolide, Cosopt OK!
ANESTHETICS GENERAL Desflurane Suprane OK! www.drugs-porphyria.org: Probably Not Porphyrinogenic
ANESTHETICS GENERAL Etomidate Amidate BAD! www.porphyria-europe.com: Unsafeweb.uct.ac.za/depts/porphyria/: Avoidwww.uq.edu.au/porphyria/: Unsafe in animalsBr J Anaesth 1985;57:420. Unsafe in animals
ANESTHETICS GENERAL Isoflurane Forane OK! www.drugs-porphyria.org: Probably Not Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Use with Cautionwww.uq.edu.au/porphyria/: Unsafe in animals
ANESTHETICS GENERAL Ketamine Ketalar BAD! www.drugs-porphyria.org: Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Cautionwww.uq.edu.au/porphyria/: Probably safeBr J Anaesth 1985;57:420. Safe in animals
Anesthetics GENERAL Midazolam Versed OK? www.drugs-porphyria.org: Possibly Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Use with Cautionwww.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: safeweb.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/: Safe in patientsAnaesthesia 1992;47:355 SafeAnaesthesia 1988;43:1022. Safe in patients
ANESTHETICS GENERAL Sevoflurane Ultane OK! www.drugs-porphyria.org: Possibly Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with CautionPediat Anesthes 2005;15:426. SafeUSP 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: Porphyrinogenicwww.porphyria-europe.com: Unsafeweb.uct.ac.za/depts/porphyria/: AvoidSee Phenobarbital
ANESTHETICS LOCAL Benzocaine Many NO INFO
ANESTHETICS LOCAL Bupivacaine Many OK! www.drugs-porphyria.org: Probably Not Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/: Safe in animalsMedicine (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 Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/: Unsafe in patientsMedicine (Balt) 1992;71:1. Safe
ANESTHETICS LOCAL Procaine Many OK! www.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Usewww.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 Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/: Safe in animals
Anesthetics MUSCLE RELAXANTS Baclofen Many OK? www.drugs-porphyria.org: Probably Not Porphyrinogenichttp://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 PXRWilliams 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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Usewww.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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Caution
ANTI-INFECTIVES AMINOGLYCOSIDES Amikacin Amikin OK! www.drugs-porphyria.org: Not Porphyrinogenicweb.uct.ac.za/depts/porphyria/: UsePV Tishler MD clinical data: Safe
ANTI-INFECTIVES AMINOGLYCOSIDES Gentamicin Many OK! www.drugs-porphyria.org: Not Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Usewww.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: Safeweb.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/: Safewww.porphyriafoundation.com: Safe
ANTI-INFECTIVES AMINOGLYCOSIDES Tobramycin Many OK! www.drugs-porphyria.org: Not Porphyrinogenicweb.uct.ac.za/depts/porphyria/: UseS 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 Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Use with Cautionwww.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 Porphyrinogenicwww.rxlist.com: Metabolized by hydrolysis and N-acetylation
Anti-infectives ANTIFUNGALS Clotrimazole OK? www.drugs-porphyria.org: Probably Not /Possibly PorphyrinogenicComp 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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Extreme CautionInhibits Cyt3A,2C9, and pregnane X receptor. 3 Patient reports: Unsafe.
ANTI-INFECTIVES ANTIFUNGALS Flucytosine Ancobon OK! www.drugs-porphyria.org: Probably Not Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/: Safe in cell culturewww.porphyriafoundation.com: Safe
Anti-infectives ANTIFUNGALS Griseofulvin Many BAD! www.porphyria-europe.com: Unsafeweb.uct.ac.za/depts/porphyria/: Avoidwww.uq.edu.au/porphyria/: Unsafe in patientswww.porphyriafoundation.com: Unsafe. Induces CYP3A
Anti-infectives ANTIFUNGALS Itraconazole Sporanox BAD! www.drugs-porphyria.org: Probably Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Extreme CautionWilliams 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: Porphyrinogenicwww.porphyria-europe.com: Unsafeweb.uct.ac.za/depts/porphyria/: Avoidwww.uq.edu.au/porphyria/: Unsafe in cell cultureWilliams 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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Extreme Cautionwww.uq.edu.au/porphyria/: probably safeJ 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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Avoidwww.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 PorphyrinogenicWilliams 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 Porphyrinogenicwww.porphyria-europe.com: Safehttp://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: Safeweb.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/: Probably safeWilliams 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: Safeweb.uct.ac.za/depts/porphyria/: Usewww.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 inductionweb.uct.ac.za/depts/porphyria/: Use
ANTI-INFECTIVES ANTIMALARIALS Pyrimethamine Daraprim OK! www.porphyria-europe.com: Safeweb.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/: Usewww.uq.edu.au/porphyria/: Safe in patientsS Afr Med J 1988;74:321. Safe in patientsWilliams 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
ANTI-INFECTIVES ANTIMYCOBACTERIAL AGENTS Ethambutol Myambutol OK! www.drugs-porphyria.org: Probably Not Porphyrinogenicwww.porphyria-europe.com: Safeweb.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 useweb.uct.ac.za/depts/porphyria/: Use with Extreme Cautionwww.uq.edu.au/porphyria/: Probably unsafe
ANTI-INFECTIVES ANTIMYCOBACTERIAL AGENTS Pyrazinamide Many BAD! www.porphyria-europe.com: Unsafeweb.uct.ac.za/depts/porphyria/: Avoidwww.uq.edu.au/porphyria/: unsafe in patientswww.porphyriafoundation.com: Unsafe
Anti-infectives ANTIMYCOBACTERIAL AGENTS Rifabutin Mycobutin BAD! www.drugs-porphyria.org: Probably Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Extreme CautionSubstrate 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 CautionWilliams 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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Caution
Anti-infectives ANTIPARASITICS Praziquantel Many BAD! web.uct.ac.za/depts/porphyria/: Use with Extreme CautionWilliams 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 PorphyrinogenicUSP 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 PorphyrinogenicWilliams 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 PorphyrinogenicMetab 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: Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Extreme CautionWilliams 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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Extreme Cautionwww.drugs.com: 70% excreted as unchanged drug in urine
Anti-infectives ANTIRETROVIRALS Lopinavir/Ritonavir Kaletra BAD! Lopinavirwww.drugs-porphyria.org: Probably PorphyrinogenicUSP 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 CYP3A4Ritonavirwww.drugs-porphyria.org: Porphyrinogenicweb.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 PorphyrinogenicWilliams 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 PorphyrinogenicUSP DI? Drug Info. for the Health Care Pro. - 26th Ed: 70-80% eliminated as unchanged drughttp://redpoll.pharmacy.ualberta.ca/drugbank/: Not substrate of CYP3A4 or CYP2C9
ANTI-INFECTIVES ANTIRETROVIRALS Zalcitabine Hivid OK! www.drugs-porphyria.org: Probably Not Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Use
ANTI-INFECTIVES ANTIRETROVIRALS Zidovudine Retrovir BAD? www.drugs-porphyria.org: Probably Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Extreme Cautionwww.uq.edu.au/porphyria/: Safe in patients
ANTI-INFECTIVES ANTIVIRALS Acyclovir Acyclovir OK! www.drugs-porphyria.org: Not Porphyrinogenicwww.porphyria-europe.com: Safewww.uq.edu.au/porphyria/: Safe in cell culturePatient report: Safe
ANTI-INFECTIVES ANTIVIRALS Adefovir Hepsera OK! www.drugs-porphyria.org: Probably Not Porphyrinogenichttp://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 metabolizedwww.rxlist.com: Primarily secreted as unchanged drug
ANTI-INFECTIVES ANTIVIRALS Famciclovir Famvir OK! www.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Use
ANTI-INFECTIVES ANTIVIRALS Ganciclovir Cytovene OK! www.porphyria-europe.com: Safeweb.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 PorphyrinogenicNot 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 PorphyrinogenicUSP DI? Drug Info. for the Health Care Pro. - 26th Ed: not p450 substratewww.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 Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Usepatient report: safe
ANTI-INFECTIVES ANTIVIRALS Zanamivir Relenza OK! www.drugs-porphyria.org: Not Porphyrinogenichttp://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 Porphyrinogenicweb.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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Caution
Anti-infectives CEPHALOSPORINS Cefpodoxime Proxetil Vantin OK! www.drugs-porphyria.org: Probably Not Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Caution. Patient report: safe
Anti-infectives CEPHALOSPORINS Ceftazidime Fortaz OK! www.drugs-porphyria.org: Probably Not Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Caution. Patient report: safe
ANTI-INFECTIVES CEPHALOSPORINS Ceftriaxone Rocephin OK! www.drugs-porphyria.org: Probably Not Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Caution
ANTI-INFECTIVES CEPHALOSPORINS Cefuroxime Zinacef OK! www.drugs-porphyria.org: Probably Not Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Caution
ANTI-INFECTIVES CEPHALOSPORINS Cephalexin Keflex OK! www.drugs-porphyria.org: Probably Not Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with CautionPatient 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 PorphyrinogenicUSP 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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Extreme Cautionwww.uq.edu.au/porphyria/: Safe in PatientsPV Tishler MD clinical data & patient reports: SafeJ 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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Extreme Cautionwww.uq.edu.au/porphyria/: Safe in cell cultureJ Appl Toxicol 2005;25:339. Inhibits CYP3A
Anti-infectives MACROLIDES Azithromycin Zithromax OK? www.drugs-porphyria.org: Probably Not Porphyrinogenicwww.porphyria-europe.com: Safe. 2 patient reports: safeweb.uct.ac.za/depts/porphyria/: Use with Extreme CautionUSP DI? Drug Info. for the Health Care Pro. - 26th Ed. (2006): Metabolized in liver, but 50% in bile unchanged & 35% metabolized by demethylationPatient 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 Cautionwww.uspharmacist.com: Inhibitor of CYP3A4Williams 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 CYP3A4Sinz: Cur Drug Metab 2006; 7:375: no human pregnane X receptor activation
Anti-infectives MACROLIDES Erythromycin Many BAD! www.drugs-porphyria.org: Porphyrinogenicwww.porphyria-europe.com: Unsafeweb.uct.ac.za/depts/porphyria/: Avoidwww.uq.edu.au/porphyria/: Unsafe in patientsWilliams 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 Porphyrinogenichttp://redpoll.pharmacy.ualberta.ca/drugbank/: Metabolized via hydrolysis
ANTI-INFECTIVES MISCELLANEOUS Bacitracin Many OK?
Anti-infectives MISCELLANEOUS Chloramphenicol Many BAD! www.drugs-porphyria.org: Porphyrinogenicwww.porphyria-europe.com: Unsafeweb.uct.ac.za/depts/porphyria/: Avoidwww.uq.edu.au/porphyria/: Unsafe in patientsWilliams 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: Porphyrinogenicweb.uct.ac.za/depts/porphyria/: AvoidWilliams 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 CYP3A4Patient report: Safe
Anti-infectives MISCELLANEOUS Dapsone Leprostatic BAD! www.porphyria-europe.com: Unsafeweb.uct.ac.za/depts/porphyria/: Avoidwww.uq.edu.au/porphyria/: Unsafe in patientsWilliams 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 Porphyrinogenicwww.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 Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/: Safe in patientsBr 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 Porphyrinogenicwww.rxlist.com: Does not appear to undergo hepatic metabolism
Anti-infectives PENEM ANTIBIOTICS Imipenem/Cilastatin Primaxin OK! www.drugs-porphyria.org: Probably Not PorphyrinogenicUSP 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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/: Safe in patientsPV Tishler MD clinical data & patient reports: SafePregnane X receptor inducer.
Anti-infectives PENICILLINS Amoxicillin/ Clavulanate Augmentin OK! patient report: safe
ANTI-INFECTIVES PENICILLINS Ampicillin Many OK! www.drugs-porphyria.org: Not Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Usewww.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/: Usewww.uq.edu.au/porphyria/: Safe in patientsPatient report: Safe
Anti-infectives PENICILLINS Piperacillin Zosyn, etc. OK! www.drugs-porphyria.org: Not Porphyrinogenicweb.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: Unsafewww.uq.edu.au/porphyria/: Unsafe in patientswww.porphyriafoundation.com: UnsafeMedicine (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: Unsafewww.uq.edu.au/porphyria/: Unsafe in patientswww.porphyriafoundation.com: UnsafeMedicine (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/: Avoid2 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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Usepatient report: safe
Anti-infectives URINARY ANTI-INFECTIVES Nitrofurantoin Macrodantin, Macrobid BAD! www.drugs-porphyria.org: Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Extreme Cautionwww.uq.edu.au/porphyria/: Probably Unsafe
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 Cautionwww.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 - Deferoxamine Desferal OK! www.drugs-porphyria.org: Not Porphyrinogenicwww.rxlist.com: Mostly metabolized by plasma enzymes
ANTIDOTES - Dimercaprol BAL OK! web.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/: Safe
ANTIDOTES - Edetate Many OK!
ANTIDOTES - Ipecac Many OK?
Antidotes - 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 Porphyrinogenicweb.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: Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Extreme Cautionwww.uq.edu.au/porphyria/: Safe in patientsMetab 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 Porphyrinogenicweb.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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Cautionwww.uq.edu.au/porphyria/: Unsafe in animalsS Afr Med J 1984;65:924. Safe in patientsXenobiotica 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 PorphyrinogenicMetab 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 Porphyrinogenicwww.uq.edu.au/porphyria/: Safe in patientsExtensively 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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Cautionwww.uq.edu.au/porphyria/: Unsafe in animalsS Afr Med J 1984;65:924. Safe in patientsMainly 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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Extreme CautionWilliams 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 Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/: Safe in patientsDoes 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 CautionS 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 Porphyrinogenicwww.uq.edu.au/porphyria/: Safe in animals
ANTINEOPLASTICS (Cancer Therapies) ANTIBIOTICS Bleomycin Blenoxane OK! www.drugs-porphyria.org: Not Porphyrinogenichttp://redpoll.pharmacy.ualberta.ca/drugbank/: Metabolized by CYP1A1
Antineoplastics (Cancer Therapies) ANTIBIOTICS Idarubicin Idamycin BAD? www.drugs-porphyria.org: Probably Not Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Extreme Caution
ANTINEOPLASTICS (Cancer Therapies) ANTIBIOTICS Mitomycin Mutamycin BAD? www.drugs-porphyria.org: Possibly Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Extreme CautionInsufficient 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 Porphyrinogenichttp://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 Porphyrinogenichttp://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 Porphyrinogenichttp://redpoll.pharmacy.ualberta.ca/drugbank/: Not P450 substrate
Antineoplastics (Cancer Therapies) ANTIMETABOLITES Cytarabine Alexan, Cytarabin, Cytocin, others OK! www.drugs-porphyria.org: Probably Not Porphyrinogenicwww.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 Porphyrinogenicwww.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 Porphyrinogenicweb.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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with CautionUSP DI? Drug Info. for the Health Care Pro. - 26th Ed: Liver metabolism is minor pathwayhttp://medicine.iupui.edu/flockhart/table.htm: Inhibitor of CYP1A2
ANTINEOPLASTICS (Cancer Therapies) MISC. Interferon Alfa-2B Intron A OK! www.drugs-porphyria.org: Not Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Cautionhttp://medicine.iupui.edu/flockhart/table.htm: Inhibitor of CYP1A2
ANTINEOPLASTICS (Cancer Therapies) MISC. Interferon Gamma-1B Actimmune OK! www.drugs-porphyria.org: Not Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Cautionhttp://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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Extreme Cautionwww.uq.edu.au/porphyria/: Probably safe in cell cultureExtensively 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 Cautionwww.uq.edu.au/porphyria/: Probably safe in cell cultureS Afr Med J 1984;65:924. Safe in patientsUSP 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/: Avoidwww.uq.edu.au/porphyria/: Unsafe in animals
Antineoplastics (Cancer Therapies) NITROGEN MUSTARDS Ifosfamide Ifex BAD? www.drugs-porphyria.org: Probably Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Extreme CautionSubstrate 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: Safeweb.uct.ac.za/depts/porphyria/: Use with Cautionwww.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 Porphyrinogenichttp://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 PorphyrinogenicWilliams DA: Op. Cit.: Substrate of CYP3A4
Antineoplastics (Cancer Therapies) Thyroid Cancer-Specific Radioactive Iodine (I-131) -- OK! Patient experience
ANTINEOPLASTICS (Cancer Therapies) URINARY TRACT PROTECTIVE AGENTS Amifostine Ethyol OK! www.drugs-porphyria.org: Not Porphyrinogenichttp://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
Arthritis Abatacept Orencia OK! Protein. Not metab by CYPs (PDR 63:921,2009)
Arthritis adalimumab Humira OK! Protein. Not metab by CYPs(PDR 63:442,2009)
Arthritis 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 Certolizumab Pegol Cimzia OK! Protein + polyethylene glycol. Not metab by CYPs (PDR 63:3127,2009)
Arthritis etanercept Enbrel OK! Protein. Not metab by CYPs(PDR 63:569,2009)
Arthritis Golimumab Simponi OK! Protein. No CYP metabolism
Arthritis Leflunomide Arava No info Prob metab by CYPs (www.clinicalpharmacology-ip.com)
Arthritis - Allopurinol Zyloprim OK! www.drugs-porphyria.org: Probably Not Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/: Safe in animalsPatient reports: Safe
Arthritis - Auranofin Ridaura OK? www.drugs-porphyria.org: Possibly Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Extreme Caution www.uq.edu.au/porphyria/: Unsafe in patients
Arthritis - Aurothioglucose Solganal OK! www.drugs-porphyria.org: Not Porphyrinogenic
Arthritis - Colchicine Colsalide OK! www.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/: Safe in patientsInt 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 - Gold Sodium Thiomalate Myochrysin BAD! www.drugs-porphyria.org: Possibly Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Extreme Cautionwww.uq.edu.au/porphyria/: Unsafe in animals
Arthritis - Penicillamine Cuprimine OK! www.drugs-porphyria.org: Not Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: usewww.uq.edu.au/porphyria/: Safe in patients
Arthritis - Probenecid Benemid BAD? www.drugs-porphyria.org: Probably Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Extreme Cautionwww.uq.edu.au/porphyria/: Probably unsafeLittle 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 - Sulfinpyrazone Many BAD! web.uct.ac.za/depts/porphyria/: Use with Extreme Cautionwww.uq.edu.au/porphyria/: Unsafe in cell cultureMajor metabolism by CYP3A4,2C9. Induces CYP3A4 via transactivation ofpregnane 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 PorphyrinogenicUSP 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 Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/: Safe in cell culture
BLOOD RELATED THERAPY ANTICOAGULANTS Enoxaparin Lovenox OK! www.drugs-porphyria.org: Not Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Use
Blood related therapy ANTICOAGULANTS Eptifibatide Integrilin OK! www.drugs-porphyria.org: Not PorphyrinogenicClin Ther 1998;20:307. Polypeptide; deamidation probably via hydrolysis, not inlving P450
BLOOD RELATED THERAPY ANTICOAGULANTS Heparin Many OK! www.drugs-porphyria.org: Not Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Usewww.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 Porphyrinogenichttp://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 Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/: Safe in patientsWilliams 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 PorphyrinogenicPV Tishler, MD clinical data: Safe
BLOOD RELATED THERAPY HEMATOPOIETICS Epoetin Alfa Epogen OK! www.drugs-porphyria.org: Not Porphyrinogenicwww.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/: Usewww.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 metabolizedPatient reports: safe
Bones Bisphosphonates Ibandronate Boniva OK? Bisphosphonates are not metabolized.
BONES BISPHOSPHONATES Zoledronic Acid Zometa OK! www.drugs-porphyria.org: Not PorphyrinogenicUSP 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 Porphyrinogenic2 Patient reports: SafeNo transactivation of pregnane X receptor (Curr Drug Metab 6:375,2006)
Cardiovascular ACE INHIBITORS Lisinopril Prinivil OK! www.drugs-porphyria.org: Not PorphyrinogenicP4 atient reports: SafeNo transactivation of pregnane X receptor (Curr Drug Metab 6:375,2006)
Cardiovascular ACE INHIBITORS Ramipril Altace OK! www.drugs-porphyria.org: Probably Not PorphyrinogenicPatient reports: Safe
Cardiovascular ANGIOTENSIN II RECEPTOR ANTAGONISTS Candesartan Cilexetil Atacand OK! www.drugs-porphyria.org: Not Porphyrinogenicwww.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 PorphyrinogenicUSP 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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with CautionPV Tishler MD clinical data: SafeBr 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 - safeMainly 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 Porphyrinogenicweb.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 Porphyrinogenicwww.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 - safeweb.uct.ac.za/depts/porphyria/: Use with Extreme Cautionwww.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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/: Safe in patientspatient report: safe
Cardiovascular BETA BLOCKERS (includes some ophthalmic preparations) Metoprolol Lopressor OK! web.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/: Safe in patientsPV Tishler MD clinical data & patient report: SafeMedicine (Balt)1992;71:1. Safe. Induces CYP3A.
Cardiovascular CALCIUM CHANNEL BLOCKERS Amlodipine Norvasc OK? www.drugs-porphyria.org: Probably Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Extreme CautionNot 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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Cautionwww.uq.edu.au/porphyria/: Probably unsafeSubstrate 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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Extreme CautionSubstrate 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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Extreme Cautionwww.uq.edu.au/porphyria/: Unsafe in patientswww.porphyriafoundation.com: UnsafeMedicine (Balt) 1992;71:1. SafeClin Sci (Lond) 1985;69:581. Unsafe in cell cultureSubstrate 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 Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Use with Cautionwww.uq.edu.au/porphyria/: Unsafe in patientsPV Tishler MD clinical data & patient reports: SafeMedicine (Balt) 1992;71:1. Safe
Cardiovascular DIURETICS Spironolactone Aldactone BAD? www.drugs-porphyria.org: Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Cautionwww.uq.edu.au/porphyria/: Unsafe in animalsSafe (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 PorphyrinogenicMajor 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: safeNo 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 PorphyrinogenicMostly 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 Porphyrinogenicwww.porphyria-europe.com: Unsafeweb.uct.ac.za/depts/porphyria/: Avoidwww.uq.edu.au/porphyria/: Unsafe in patients and cell culture
Cardiovascular agents ANTIADRENERGICS Methyldopa Aldomet BAD! www.drugs-porphyria.org: Porphyrinogenicwww.porphyria-europe.com: Unsafeweb.uct.ac.za/depts/porphyria/: AvoidPatient report: Unsafe
Cardiovascular agents ANTIADRENERGICS Prazosin Minipress OK! www.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/: Probably safe Medicine (Balti) 1992:71:1. Safe
Cardiovascular agents ANTIADRENERGICS Terazosin Hytrin OK! www.drugs-porphyria.org: Probably Not Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with CautionNo 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 Porphyrinogenicweb.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 PorphyrinogenicUSP 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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Avoidwww.uq.edu.au/porphyria/: Unsafe in cell cultureGen Pharmacol 1999;32:259. SafeProbably 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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Cautionwww.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 PorphyrinogenicCirculation 1998;97:493. Metabolic pathway does not seem to involve CYP3A4 or CYP2D6
Cardiovascular agents ANTIARRHYTHMICS Lidocaine Xylocaine OK? www.drugs-porphyria.org: Porphyrinogenicmetab 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: Safeweb.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/: Safe in cell culture
Cardiovascular agents ANTIARRHYTHMICS Propafenone Rhthmol BAD? www.drugs-porphyria.org: Possibly PorphyrinogenicMetabolized 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 PorphyrinogenicSubstrate 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: Safeweb.uct.ac.za/depts/porphyria/: Use with Cautionwww.uq.edu.au/porphyria/: Safe in cell culture
Cardiovascular agents ANTIHYPERLIPIDEMIC AGENTS Ezetimibe Zetia, Vitorin OK! www.drugs-porphyria.org: Probably Not PorphyrinogenicUSP 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 Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Use with CautionMetab 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/: UseMedicine (Balt)1992; 71:1. Safebiocomp.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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/ safe in patientsPV Tishler MD clinical data & patient reports: SafeMedicine (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 Porphyrinogenicweb.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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use
Cardiovascular agents BETA BLOCKERS (includes some ophthalmic preparations) Propranolol Inderal OK! www.drugs-porphyria.org: Not Porphyrinogenicweb.uct.ac.za/depts/porphyria/: UsePV Tishler MD clinical data & patient report: SafeSafe (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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: UseMedicine (Balt) 1992;71:1. Safe
Cardiovascular agents BETA BLOCKERS (includes some ophthalmic preparations) Timolol Blocadren OK! www.drugs-porphyria.org: Not Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/: Safe in cell cultureMedicine (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 cultureWilliams 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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Extreme CautionSubstrate 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 Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Use with Cautionwww.uq.edu.au/porphyria/: Safe in patientsMedicine (Balt) 1992;71:1. Safe
Cardiovascular agents DIURETICS Acetazolamide Diamox OK! web.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/: Safe in patients & cell culture
Cardiovascular agents DIURETICS Amiloride Midamor, Moduretic, others OK! www.drugs-porphyria.org: Not Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/: Safe in patients
Cardiovascular agents DIURETICS Bumetanide Bumex OK! www.drugs-porphyria.org: Probably Not Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/: Safe in patientsPatient 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 patientshttp://www.emedicine.com/MED/topic1880.htm: Safe in porphyria
Cardiovascular agents DIURETICS Hydrochlorothiazide Many OK! www.drugs-porphyria.org: Probably Not Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Use with Cautionwww.uq.edu.au/porphyria/: Safe in patientsPV 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: Safeweb.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: Safeweb.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/: Safe in cell culture
Cardiovascular agents MISC. Tolazoline Priscoline OK! www.uq.edu.au/porphyria/: Safe in patientshttp://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 Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Use with Caution
Cardiovascular agents THROMBOLYTIC ENZYMES Streptokinase Many OK! www.drugs-porphyria.org: Not Porphyrinogenicwww.porphyria-europe.com: Safeweb.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: Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Extreme Cautionwww.uq.edu.au/porphyria/: Unsafe in patients
Cardiovascular agents VASODILATORS Minoxidil Many BAD? www.drugs-porphyria.org: Possibly Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Extreme Caution
Cardiovascular agents VASODILATORS Nitroprusside Nipride OK? web.uct.ac.za/depts/porphyria/: Use with CautionRedox Rep 2004;9:360: No P450 metabolism
Cardiovascular agents VASOPRESSORS Dobutamine Dobutrex, others OK! www.drugs-porphyria.org: Not Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Use
Cardiovascular agents VASOPRESSORS Dopamine Intropin, others OK! www.drugs-porphyria.org: Not Porphyrinogenicwww.porphyria-europe.com: Safeweb.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: Porphyrinogenicwww.porphyria-europe.com: unsafeweb.uct.ac.za/depts/porphyria/: Avoidwww.uq.edu.au/porphyria/: Unsafe in patientsUnsafe/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 Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: UsePV Tishler MD clinical data & patient reports: SafeNot 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: Porphyrinogenicwww.porphyria-europe.com: Unsafeweb.uct.ac.za/depts/porphyria/: Avoidwww.uq.edu.au/porphyria/: Unsafe in patientsUnsafe 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: Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Avoidwww.porphyriafoundation.com: UnsafeLargely 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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Cautionwww.uq.edu.au/porphyria/: Unsafe in cell cultureMainly 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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Cautionwww.uq.edu.au/porphyria/: Unsafe in patientsMedicine (Balt) 1992;71:1. SafeSubstrate 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: Safeweb.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/: Safe in patientsSubstrate 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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/: Safe in animalsMedicine (Balt) 1992;71:1. SafeSubstrate 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: Safewww.uq.edu.au/porphyria/: Safe in patientsPeter V. Tishler, MD, clinical experience: safepatient 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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Caution2 patient reports: safe
Central nervous system NARCOTICS (Pain Therapies) Fentanyl Duragesic OK? www.drugs-porphyria.org: Probably Not Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/: Safe in animalsSubstrate 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 Porphyrinogenicwww.porphyria-europe.com: safeweb.uct.ac.za/depts/porphyria/: UseMetab 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: SafePV Tishler MD clinical data & patient reports: SafeInduces 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 Porphyrinogenicwww.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 Porphyrinogenicwww.porphyria-europe.com: safeweb.uct.ac.za/depts/porphyria/: Use with Cautionwww.uq.edu.au/porphyria/: Probably unsafewww.porphyriafoundation.com: unsafeEpilepsia 1992;33:108. porphyrogenic but safe in lose dosagesNeurology 1982;32:1409. safe in low dosagesGreatly 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 Porphyrinogenicwww.porphyria-europe.com: Unsafeweb.uct.ac.za/depts/porphyria/: Use with Extreme Cautionwww.uq.edu.au/porphyria/: Unsafe in patientswww.porphyriafoundation.com: UnsafeUnsafe 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 Porphyrinogenicwww.porphyriafoundation.com: UnsafeMetab 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: PorphyrinogenicMetab 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 Porphyrinogenicwww.porphyria-europe.com: SafeNot 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 patientsNeurology 1981;31:480. Unsafe in animals
Central nervous system agents ANTICONVULSANTS Oxcarbazepine Trileptal BAD! www.drugs-porphyria.org: Probably Porphyrinogenicwww.porphyria-europe.com: Unsafeweb.uct.ac.za/depts/porphyria/: AvoidInduces 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: Porphyrinogenicwww.porphyria-europe.com: Unsafeweb.uct.ac.za/depts/porphyria/: Avoidwww.uq.edu.au/porphyria/: Unsafe in patientswww.porphyriafoundation.com: UnsafeNeurology 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 Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Use
Central nervous system agents ANTIMYASTHENIC AGENTS Pyridostigmine Mestinon OK! www.drugs-porphyria.org: Probably Not Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Caution. Patient report: safe
Central nervous system agents ANTIPARKINSON AGENTS Amantadine Symmetrel OK! www.porphyria-europe.com: Safeweb.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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Extreme Cautionwww.uq.edu.au/porphyria/: Unsafe in cell cultureMetab 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 Porphyrinogenicwww.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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Extreme CautionMetab by CYP2B6, which may involve pregnane X receptor
Central nervous system agents ANTIPARKINSON AGENTS Trihexyphenidyl Artane BAD? www.drugs-porphyria.org: Possibly Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Avoid
Central nervous system agents BENZODIAZEPINES Chlordiazepoxide Librium BAD! web.uct.ac.za/depts/porphyria/: Use with Extreme Cautionwww.uq.edu.au/porphyria/: Unsafe in patientsMedicine (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: SafeMetab. 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 Cautionwww.uq.edu.au/porphyria/: Unsafe in patients
Central nervous system agents BENZODIAZEPINES Lorazepam Ativan OK! www.drugs-porphyria.org: Probably Not Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/: Probably safeNot metab by CYPs (Curr Drug Metab 9:827,2008)PV Tishler MD clinical data: SafeMedicine (Balt) 1992;7:1. Safe
Central nervous system agents BENZODIAZEPINES Oxazepam Serax OK! www.drugs-porphyria.org: Probably Not Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Cautionwww.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: UnsafePatient report: UnsafeSee 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: UnsafeInduces CYP3A4 (Arch Toxicol 82:667,2008)See Phenobarbital
Central nervous system agents HYPNOTICS (Sleeping Medications) Zaleplon Sonata BAD! www.drugs-porphyria.org: Possibly PorphyrinogenicMetabolized 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: Unsafeweb.uct.ac.za/depts/porphyria/: Avoidwww.uq.edu.au/porphyria/: Unsafe in patientswww.porphyriafoundation.com: UnsafeSubstrate 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 PorphyrinogenicNo 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 Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: UseSubstrate 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 Porphyrinogenicwww.porphyria-europe.com: Safewww.uq.edu.au/porphyria/: Safe in patientsPV Tishler MD clinical data: SafeAnn Fr Anesth Reanim 1989;8:525. SafeSubstrate 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 Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/: Safe in patientsPV Tishler MD clinical data & patient report: SafeSubstrate 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: SafeJAMA 1965;194:1037. Safe in patients
Central nervous system agents NARCOTICS (Pain Therapies) Morphine Many OK! www.drugs-porphyria.org: Not Porphyrinogenicwww.porphyria-europe.com: safeweb.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/: Safe in patientsPV Tishler MD clinical data: Safe
Central nervous system agents NARCOTICS (Pain Therapies) Nalbuphine Nubain OK! www.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Use
Central nervous system agents NARCOTICS (Pain Therapies) Oxycodone Oxycontin, Percocet, Percodan, others OK! www.drugs-porphyria.org: Possibly Porphyrinogenicwww.uq.edu.au/porphyria/: Unsafe in animalsPV Tishler MD clinical data & patient reports: Safe
Central nervous system agents NARCOTICS (Pain Therapies) Pentazocine Talwin BAD! web.uct.ac.za/depts/porphyria/: Avoidwww.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 Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/: Safe in patientswww.porphyriafoundation.com: SafePV 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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Extreme Cautionwww.uq.edu.au/porphyria/: Unsafe in patientswww.porphyriafoundation.com: UnsafePV Tishler MD clinical data: SafeBiomed Pharmacother 43:135,1989 - Unsafe in cell cultureLimited 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/: Usewww.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 Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Use with CautionProbably not metab by CYPsPV 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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Extreme CautionEksp 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 Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/: Safe in patients and animals20-40% 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 Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/: Safe in animalsMinimal CYP2D9 metab (Drug Metab Disp 33:1567,2005)
CONTRAST MEDIA - Diatrizoate Meglumine Hypaque OK!
CONTRAST MEDIA - Ethiodized Oil Ethiodol OK!
CONTRAST MEDIA - Ferumoxides Endorem OK!
CONTRAST MEDIA - Gadopentetate Dimeglumine Magnevist OK!
CONTRAST MEDIA - Iodipamide Meglumine Chlorografin, Sinografin OK!
Contrast media - Iodixanol Visipaque OK! www.drugs-porphyria.org: Not Porphyrinogenic www.fda.gov/medwatch/SAFETY/ 2003/03DEC_PI/Visipaque_PI.pdf: No metabolism
CONTRAST MEDIA - Iohexol Omnipaque OK! www.drugs-porphyria.org: Not Porphyrinogenic
CONTRAST MEDIA - Iopanoic Acid Telepaque OK!
CONTRAST MEDIA - 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 CautionSubstrate 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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Extreme Caution
Dermatologicals Dermatosis, allergy, psoriasis desoximetasone topicort OK? Topical corticosteroid. 1 patinet report: safe
Diagnostic - Methacholine Provocholine, others OK!
Diagnostic Imaging Gadobutrol Gadavist OK! MRI contrast agent that is not metabolized
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 patientsPatient 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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Cautionwww.uq.edu.au/porphyria/: Probably unsafeClin Chim Acta 1995;234:171. Safe in patientsAnn Int Med 2005; 143:694. Safe and possibly therapeutic during acute attack.PV Tishler, MD clinical data & patient reports: SafeSubstrate % 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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Cautionwww.uq.edu.au/porphyria/: Safe in patientsPatient reports: Safe
Gastrointestinal H-2 ANTAGONISTS, PPIs (Reflux, Ulcer Therapies) Omeprazole Prilosec OK! www.drugs-porphyria.org: Possibly Porphyrinogenicwww.porphyria-europe.com: Safeweb.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 PorphyrinogenicMajor 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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Cautionwww.uq.edu.au/porphyria/: Probably unsafewww.porphyriafoundation.com: SafePV Tishler MD clinical data: Safe
Gastrointestinal LAXATIVES Bisacodyl Dulcolax OK! www.drugs-porphyria.org: Probably Not Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Use with CautionPV 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 PorphyrinogenicProtein; 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 Porphyrinogenicmetab to mesalamine which has no CYP metab
GASTROINTESTINAL THERAPIES ANTIDIARRHEAL AGENTS Diphenoxylate Lomotil OK! www.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/: Safe in patients
GASTROINTESTINAL THERAPIES ANTIDIARRHEAL AGENTS Kaolin-Pectin Kaopectate OK! web.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/: Safe in patients
GASTROINTESTINAL THERAPIES ANTIDIARRHEAL AGENTS Loperamide Imodium OK! www.drugs-porphyria.org: Probably Not Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/: Safe in cell culturePatient report: Safe
Gastrointestinal therapies ANTIEMETICS (Vomiting Therapies) Cyclizine Merezine OK! www.drugs-porphyria.org: Probably Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/: Safe in patients
Gastrointestinal therapies ANTIEMETICS (Vomiting Therapies) Dimenhydrinate Dramamine BAD! www.porphyria-europe.com: unsafeweb.uct.ac.za/depts/porphyria/: Avoidwww.uq.edu.au/porphyria/: Unsafe in patients
Gastrointestinal therapies ANTIEMETICS (Vomiting Therapies) Ondansetron Zofran OK! www.drugs-porphyria.org: Probably Not Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Use with CautionPV Tishler MD clinical data & patient reports: SafeSubstrate 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 Porphyrinogenicweb.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 Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/: Safe in patientswww.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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Cautionwww.uq.edu.au/porphyria/: Probably unsafewww.porphyriafoundation.com: UnsafeLancet 1981;2:91 Not safeHowever, 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 Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Usewww.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 PorphyrinogenicNot metab by and does not affect CYPs (www.clinicalpharmacology-ip.com)
Hormones CORTICOSTEROIDS Dexamethasone Decadron OK? www.drugs-porphyria.org: Possibly Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: UseSubstrate 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 Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: UseSubstrate & 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 Cautionwww.uq.edu.au/porphyria/: Probably safePV Tishler MD clinical data & patient report: SafeHorm Metab Res 1995;27:379. Safe in patientsMass. 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 Cautionwww.uq.edu.au/porphyria/: Unsafe in patientswww.porphyriafoundation.com: UnsafeSubstrate 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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Extreme Caution. Metab by CYP3A4.
Hormones PROGESTINS Norethindrone Loestrin No info JAMA 1965;194:1037. Safe in patientsUSP 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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Extreme Cautionwww.porphyriafoundation.com: UnsafePatient report: unsafe. Induces CYP3A, pregnane X receptor
Hormones, hormone-like ANDROGENS Danazol Danocrine BAD! www.drugs-porphyria.org: Probably Porphyrinogenicwww.porphyria-europe.com: Unsafeweb.uct.ac.za/depts/porphyria/: Avoidwww.uq.edu.au/porphyria/: Unsafe in patientswww.porphyriafoundation.com: UnsafeJ Clin Endocrinol Metab 1981;52:549. Exacerbates acute porphyriaJ 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: Porphyrinogenicwww.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: PorphyrinogenicSubstrate 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 Porphyrinogenicweb.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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Caution
Hormones, hormone-like CORTICOSTEROIDS Hydrocortisone Many OK! www.drugs-porphyria.org: Probably Not Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/: Probably safeSubstrate 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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: UseSubstrate 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 Porphyrinogenicweb.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 Porphyrinogenicwww.porphyria-europe.com: Safe
HORMONES, HORMONE-LIKE OVULATION STIMULANTS Clomiphene Clomid OK! web.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/: Safe in patients
Hormones, hormone-like PARATHYROID Calcitonin Miacelcin, Calcimar, Fortical OK! www.drugs-porphyria.org: Probably Not Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Usewww.porphyria-europe.com: SafePatient 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 Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Usewww.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: Porphyrinogenicweb.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 Porphyrinogenicwww.porphyria-europe.com: Safeweb.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 Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: UsePV 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 Porphyrinogenicwww.porphyria-europe.com: safeweb.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/: Safe in patients
Immunologic IMMUNOSUPPRESSIVE AGENTS Sirolimus Rapamune BAD? www.drugs-porphyria.org: Possibly Porphyrinogenicmetab 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 OK?
IMMUNOLOGIC AGENTS ANTIMICROBIAL VACCINES Haemophilus B OK?
IMMUNOLOGIC AGENTS ANTIMICROBIAL VACCINES Hepatitis A OK? www.drugs-porphyria.org: Not Porphyrinogenic
IMMUNOLOGIC AGENTS ANTIMICROBIAL VACCINES Hepatitis B OK! www.drugs-porphyria.org: Not Porphyrinogenic
IMMUNOLOGIC AGENTS ANTIMICROBIAL VACCINES Influenza OK! www.drugs-porphyria.org: Not Porphyrinogenic
IMMUNOLOGIC AGENTS ANTIMICROBIAL VACCINES Japanese Encephalitis OK?
IMMUNOLOGIC AGENTS ANTIMICROBIAL VACCINES Measles, Mumps & Rubella OK! www.drugs-porphyria.org: Not Porphyrinogenic
IMMUNOLOGIC AGENTS ANTIMICROBIAL VACCINES Meningococcal OK?
IMMUNOLOGIC AGENTS ANTIMICROBIAL VACCINES Mumps OK!
IMMUNOLOGIC AGENTS ANTIMICROBIAL VACCINES Pneumococcal OK!
IMMUNOLOGIC AGENTS ANTIMICROBIAL VACCINES Polio OK!
IMMUNOLOGIC AGENTS ANTIMICROBIAL VACCINES Rabies OK?
IMMUNOLOGIC AGENTS ANTIMICROBIAL VACCINES Typhoid OK? www.drugs-porphyria.org: Not Porphyrinogenic
IMMUNOLOGIC AGENTS ANTIMICROBIAL VACCINES Typhoid VI Polysaccharide OK? www.drugs-porphyria.org: Not Porphyrinogenic
IMMUNOLOGIC AGENTS ANTIMICROBIAL VACCINES Varicella OK! www.drugs-porphyria.org: Not Porphyrinogenic
IMMUNOLOGIC AGENTS ANTIMICROBIAL VACCINES Yellow Fever OK? www.drugs-porphyria.org: Not Porphyrinogenic
IMMUNOLOGIC AGENTS ANTIVENINS Antivenin Crotalidae Polyvalent AntiveninPolyvalent OK?
IMMUNOLOGIC AGENTS ANTIVENINS Antivenin Latrodectus Mactans OK?
IMMUNOLOGIC AGENTS ANTIVENINS Antivenin Micrurus Fulvius OK?
IMMUNOLOGIC AGENTS ANTIVIRAL MONOCLONAL ANTIBODIES Palivizumab Synagis OK? www.drugs-porphyria.org: Not Porphyrinogenic
IMMUNOLOGIC AGENTS IMMUNE GLOBULINS Cytomegalovirus OK? (web.uct.ac.za/depts/porphyria/: Use)
IMMUNOLOGIC AGENTS IMMUNE GLOBULINS Hepatitis B OK? (web.uct.ac.za/depts/porphyria/: Use)www.drugs-porphyria.org: Not Porphyrinogenic
IMMUNOLOGIC AGENTS IMMUNE GLOBULINS Immune Globulin IV OK? (web.uct.ac.za/depts/porphyria/: Use)www.drugs-porphyria.org: Not Porphyrinogenic
IMMUNOLOGIC AGENTS IMMUNE GLOBULINS Rabies OK? (web.uct.ac.za/depts/porphyria/: Use)
IMMUNOLOGIC AGENTS IMMUNE GLOBULINS Tetanus 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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/: Safe in animalsJ Clin Pharmacol 2001;41:113. SafeNot metab by CYPs (www.clinicalpharmacology-ip.com)
Immunologic agents IMMUNOSUPPRESSIVE AGENTS Cyclosporine Sandimmune OK? www.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Use with Extreme Cautionwww.uq.edu.au/porphyria/: Unsafe in animalsJ Clin Pharmacol 2001;41:113. SafeMajor 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. Safe85% 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 PorphyrinogenicJ Clin Pharmacol 2001;41:113. SafeMajor 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.
NARCOTIC ANTAGONISTS - Naloxone Narcan OK! www.drugs-porphyria.org: Possibly Porphyrinogenic. Opioid derivative metabolised by a series of CYPs, mainly 3A4. Two references: Usewww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Use
OPHTHALMIC AGENTS (intraocular) - Acetylcholine Miochol OK!
OPHTHALMIC AGENTS (intraocular) - Apraclonidine Iopidine OK! www.drugs-porphyria.org: Not Porphyrinogenic
OPHTHALMIC AGENTS (intraocular) - Betaxolol Many OK!
OPHTHALMIC AGENTS (intraocular) - Bimatoprost Lumigan OK!
OPHTHALMIC AGENTS (intraocular) - Brimonidine Alphagan OK! www.drugs-porphyria.org: Not Porphyrinogenic
OPHTHALMIC AGENTS (intraocular) - Cyclopentolate Cyclogyl OK! www.drugs-porphyria.org: Probably Not Porphyrinogenic
OPHTHALMIC AGENTS (intraocular) - Dapiprazole Rev-Eyes OK!
OPHTHALMIC AGENTS (intraocular) - Dorzolamide Trusopt OK! www.drugs-porphyria.org: Probably Not Porphyrinogenicwww.drugs.com: excreted primarily as unchanged drug
OPHTHALMIC AGENTS (intraocular) - Fluorescein Many OK! www.drugs-porphyria.org: Not Porphyrinogenic
OPHTHALMIC AGENTS (intraocular) - Homatropine Many OK!
OPHTHALMIC AGENTS (intraocular) - Latanoprost Xalatan OK! www.drugs-porphyria.org: Not Porphyrinogenic
OPHTHALMIC AGENTS (intraocular) - Naphazoline Many OK! www.drugs-porphyria.org: Probably Not Porphyrinogenic
OPHTHALMIC AGENTS (intraocular) - Pilocarpine Many OK! www.drugs-porphyria.org: Probably Not Porphyrinogenic
OPHTHALMIC AGENTS (intraocular) - Travoprost Travatan OK! www.drugs-porphyria.org: Not Porphyrinogenic
OPHTHALMIC AGENTS (intraocular) - Trifluridine Viroptic OK!
OPHTHALMIC AGENTS (intraocular) - 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 Cautionwww.uq.edu.au/porphyria/: Unsafe in animalsSubstrate 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 Porphyrinogenic1/3 metabolized by CYP3A4 (www.rxlist.com; J Clin Psychopharm 23:229,2003)
Psychiatric PHENOTHIAZINES Chlorpromazine Thorazine OK! www.drugs-porphyria.org: Not Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/: Safe in patientsPV Tishler MD clinical data: SafeJAMA 1965;194:1042. Safe in patientsSubstrate 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 Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Use with Cautionwww.uq.edu.au/porphyria/: Safe in patientsSubstrate 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 Porphyrinogenicweb.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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Extreme Cautionwww.uq.edu.au/porphyria/: Probably unsafeSubstrate 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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Extreme Cautionwww.uq.edu.au/porphyria/: Probably unsafeMetab 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 PorphyrinogenicEur J Clin Chem Clin Biochem 1997;35:427. Safe in patientsMajor 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 Porphyrinogenicwww.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 Porphyrinogenicwww.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 Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Usewww.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 Cautionwww.uq.edu.au/porphyria/: Unsafe in animals
PSYCHIATRIC MEDICATIONS PHENOTHIAZINES Fluphenazine Prolixin OK! www.drugs-porphyria.org: Not Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Use
PSYCHIATRIC MEDICATIONS PHENOTHIAZINES Perphenazine Trilafon OK! www.drugs-porphyria.org: Probably Not Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Caution
Psychiatric medications PHENOTHIAZINES Prochlorperazine Compazine, Compro, Combid, others OK! www.drugs-porphyria.org: Not Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/: Safe in patientsPV Tishler MD clinical data: Safe
Psychiatric medications PHENOTHIAZINES Thioridazine Mellaril OK! www.drugs-porphyria.org: Possibly Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Cautionwww.uq.edu.au/porphyria/: Safe in patientsPolish 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 PorphyrinogenicSubstrate 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. SafePatient report: Safe
Psychiatric medications TRICYCLICS Nortriptyline Aventyl OK? www.drugs-porphyria.org: Probably Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Extreme Cautionwww.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 PorphyrinogenicPV Tishler MD clinical data & patient report: SafeMetab by CYP3A
Respiratory ANTIASTHMATIC AND BRONCHODILATOR AGENTS Fluticasone Flovent OK! www.drugs-porphyria.org: Not PorphyrinogenicPV Tishler MD clinical data & patient reports: SafeSubstrate 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 PorphyrinogenicSubstrate 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 patientsMetab 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: Safeweb.uct.ac.za/depts/porphyria/: UsePatient reports: Safe
Respiratory ANTIHISTAMINES Fexofenadine Allegra OK! www.drugs-porphyria.org: Probably Not PorphyrinogenicUSP 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 Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Use with CautionSubstrate 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: Safeweb.uct.ac.za/depts/porphyria/: UseMetab 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 Porphyrinogenicweb.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 patientsPV 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 PorphyrinogenicSubstrate 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 PorphyrinogenicEur. J. Clin. Pharmacol. 1993;45 :483. No metabolism in liver
Respiratory agents ANTIASTHMATIC AND BRONCHODILATOR AGENTS Theophylline Many BAD? www.drugs-porphyria.org: Probably Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Extreme Cautionwww.uq.edu.au/porphyria/: Unsafe in patientsMedicine (Balt) 1992;71:1. SafeSubstrate 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: Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Extreme Cautionwww.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 Porphyrinogenicwww.porphyria-europe.com: Safeweb.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/: Probably unsafeCurr 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 CYP3A4Patient 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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: UsePV Tishler MD clinical data: SafeEur 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 Porphyrinogenicwww.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: Safeweb.uct.ac.za/depts/porphyria/: Usewww.uq.edu.au/porphyria/: Safe in patientsPatient 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 Porphyrinogenicweb.uct.ac.za/depts/porphyria/: Use with Extreme Cautionwww.drugs.com: Metabolized primarily in liver by CYP3A4Substrate 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)

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