Monograph
C01BD01 - Amiodarone |
Probably porphyrinogenic |
PRP |
Rationale
Inhibitor of CYP 2C9, 2D6. Mechanism-based inhibitior of CYP 3A4. Conflicting references, but three lists warn strictly against use of the drug.
Therapeutic characteristics
Antiarrythmic benzofurane derivative. Dose: 200-600 mg/d.
Metabolism and pharmacokinetics
Liver metabolism is extensive and encompasses multiple pathways, including hepatic CYP3A-mediated N-deethylation. The terminal elimination half-life is about 50 days with a range of about 20 to 100 days due to its extensive tissue distribution. On stopping prolonged amiodarone therapy a pharmacological effect is evident for a month or more.
Preclinical data
Amiodarone has been studied in mice and non-porphyric patients. Neither the activities of the heme enzymes, nor the levels of precursors and porphyrins in urine and plasma were altered. The authors wrongly conclude that amiodarone is a safe drug in porphyria.(Mendez M et al). Amiodarone is a mechanism based inhibitor of CYP3A4 (Larry D et al).
Personal communication
None.
Published experience
None.
IPNet drug reports
Uneventful use reported in 1 patient with acute porphyria.
References
| # |
Citation details |
PMID |
|---|
| * | Scientific articles |
| 1. |
Formation of an inactive cytochrome P-450Fe(II)-metabolite complex after administration of amiodarone in rats, mice and hamsters.
Larrey D, Tinel M, Letteron P, Geneve J, Descatoire V, Pessayre D. Biochem Pharmacol. 1986 Jul 1;35(13):2213-20. |
|
| 2. |
Amiodarone is a pharmacologically safe drug for porphyrias. General Pharmacology 1999; 32(2):259-263.
Mendez M, Parera V, Enriquez dS, Batlle A. |
10188629 |
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