P450-based drug-drug interactions of amiodarone and its metabolites: diversity of inhibitory mechanisms

MG McDonald, NT Au, AE Rettie - Drug Metabolism and Disposition, 2015 - ASPET
In this study, IC50 shift and time-dependent inhibition (TDI) experiments were carried out to
measure the ability of amiodarone (AMIO), and its circulating human metabolites, to …

Inhibitory effects of amiodarone and its N‐deethylated metabolite on human cytochrome P450 activities: Prediction of in vivo drug interactions

K Ohyama, M Nakajima, M Suzuki… - British journal of …, 2000 - Wiley Online Library
Aims To predict the drug interactions of amiodarone and other drugs, the inhibitory effects
and inactivation potential for human cytochrome P450 (CYP) enzymes by amiodarone and …

Metabolism of amiodarone (part I): identification of a new hydroxylated metabolite of amiodarone

HR Ha, L Bigler, M Binder, P Kozlik, B Stieger… - Drug metabolism and …, 2001 - ASPET
Amiodarone (AMI) is a potent antiarrhythmic drug, but its metabolism has not yet been fully
documented. Mono-N-desethylamiodarone (MDEA) is its only known metabolite. Our …

Determination of the enzyme (s) involved in the metabolism of amiodarone in liver and intestine of rat: the contribution of cytochrome P450 3A isoforms

A Shayeganpour, AOS El-Kadi, DR Brocks - Drug metabolism and …, 2006 - ASPET
In humans, cytochrome P450 3A (CYP3A4) is a major enzyme involved in the metabolism of
amiodarone (AM) to its major metabolite, desethylamiodarone (DEA). In rat, a commonly …

The metabolism of amiodarone by various CYP isoenzymes of human and rat, and the inhibitory influence of ketoconazole

ME Elsherbiny, AOS El-Kadi… - Journal of Pharmacy & …, 2008 - journals.library.ualberta.ca
PURPOSE. To evaluate the metabolism of amiodarone (AM) to desethylamiodarone (DEA)
by selected human and rat cytochrome P450, and the inhibitory effect of ketoconazole (KTZ) …

A significant role of human cytochrome P450 2C8 in amiodarone N-deethylation: an approach to predict the contribution with relative activity factor

K Ohyama, M Nakajima, S Nakamura… - Drug Metabolism and …, 2000 - ASPET
Human cytochrome P450 (CYP) isoforms involved in amiodarone N-deethylation were
identified, and the relative contributions of these CYP isoforms were evaluated in different …

Identification and quantitation of novel metabolites of amiodarone in plasma of treated patients

HR Ha, L Bigler, B Wendt, M Maggiorini… - European journal of …, 2005 - Elsevier
In mammals, mono-N-desethylamiodarone (MDEA) is the only known metabolite of
amiodarone. Our previous experiments demonstrated that in vitro MDEA may be …

The role of CYP3A4 in amiodarone-associated toxicity on HepG2 cells

A Zahno, K Brecht, R Morand, S Maseneni… - Biochemical …, 2011 - Elsevier
Amiodarone is a class III antiarrhythmic drug with potentially life-threatening hepatotoxicity.
Recent in vitro investigations suggested that the mono-N-desethyl (MDEA) and di-N …

Identification of amiodarone metabolites in human bile by ultraperformance liquid chromatography/quadrupole time-of-flight mass spectrometry

P Deng, T You, X Chen, T Yuan, H Huang… - Drug metabolism and …, 2011 - ASPET
Amiodarone is recognized as an effective drug in the treatment of arrhythmias. Previous
experiments demonstrated that mono-N-desethylamiodarone (MDEA) was the major …

Metabolism of amiodarone (Part III): identification of rabbit cytochrome P450 isoforms involved in the hydroxylation of mono-N-desethylamiodarone

P Kozlik, HR Ha, B Stieger, L Bigler, F Follath - Xenobiotica, 2001 - Taylor & Francis
1. Amiodarone (AMI) is a potent anti-arrhythmic drug and mono-N-desethylamiodarone
(MDEA) is its only known metabolite. It was found recently that in rabbit liver microsomes …