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.
Similar drugs
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 |
Tradenames
Amiodaron 
Amiodarone · Cordarone 
Amiodarona · Trangorex 
Amiodaron · Cordarone 
Amiodar · Amiodarone · Cordarone 
Amiodarona · Cordarone 
Amiodar · Amiodaron · Amiodarone · Cordarone 
Amiodarone · Amyben · Cordarone X · Cordarone X 100 · Cordarone X 200 · Darmil 
Amiodaron · Amiodaronhydrochlorid · Cordan · Cordarone 
Amiodaron · Amiodarone · Cordarone 
Amiodaron · Amiokordin · Cordarone · Opacorden 
Amiodarona · Cordarone 
Amiodarone 
Amiodarone · Cordarone 
Cordarone 
Amiodaron · Cordarone 
Amiodaron · Amiodarona · Amiodarone · Amiokordin · Cordarone 
Amiokordin 
Amiokordin · Cordarone 
Amiodaron · Cordarone 
Amiodaron · Amiodaronijev · Amiokordin · Amjodaron · Amjodaronijev · Cordarone 
Amiodarona 
Amiodarone