Monograph

C01BD01 - Amiodarone

Probably porphyrinogenic

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.

Similar drugs

Explore alternative drugs in similar therapeutic classes C01B / C01BD or go back.

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

Citation details

PMID

Scientific articles

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.

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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