Amiodarone N‐Deethylation by CYP2C8 and its Variants, CYP2C8*3 and CYP2C8 P404A
A Soyama, N Hanioka, Y Saito… - Pharmacology & …, 2002 - Wiley Online Library
Amiodarone is a potent Class III antiarrhythmic drug. The N‐deethylation of amiodarone to
desethylamiodarone is known to be catalyzed by cytochrome P450 (CYP) 2C8. In the …
desethylamiodarone is known to be catalyzed by cytochrome P450 (CYP) 2C8. In the …
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 …
identified, and the relative contributions of these CYP isoforms were evaluated in different …
Evidence for CYP3A-mediated N-deethylation of amiodarone in human liver microsomal fractions.
G Fabre, B Julian, B Saint-Aubert, H Joyeux… - Drug Metabolism and …, 1993 - ASPET
Metabolism of amiodarone to its N-deethylated derivative was investigated on a bank of
human hepatic microsomal fractions, two of them lacking the CYP2D6 isozyme. Michaelis …
human hepatic microsomal fractions, two of them lacking the CYP2D6 isozyme. Michaelis …
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 …
Recent in vitro investigations suggested that the mono-N-desethyl (MDEA) and di-N …
Functional characterization of 21 CYP3A4 variants on amiodarone metabolism in vitro
CC Yang, X Zheng, TH Liu, CC Wang, PF Tang… - Xenobiotica, 2019 - Taylor & Francis
Cytochrome P450 3A4 (CYP3A4) is an important member of the cytochrome P450 enzyme
superfamily, with 33 allelic variants reported previously. Genetic polymorphisms of CYP3A4 …
superfamily, with 33 allelic variants reported previously. Genetic polymorphisms of CYP3A4 …
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) …
by selected human and rat cytochrome P450, and the inhibitory effect of ketoconazole (KTZ) …
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 …
and inactivation potential for human cytochrome P450 (CYP) enzymes by amiodarone and …
Amiodarone N-deethylation in human liver microsomes: involvement of cytochrome P450 3A enzymes (first report)
JM Trivier, C Libersa, C Belloc, M Lhermitte - Life sciences, 1993 - Elsevier
Experiments were conducted on three different human liver samples to identify the
cytochrome P450 isozyme which is involved in the biotransformation of the class III …
cytochrome P450 isozyme which is involved in the biotransformation of the class III …
Amiodarone analog-dependent effects on CYP2C9-mediated metabolism and kinetic profiles
CYP2C9 substrates can exhibit both hyperbolic and atypical kinetic profiles, and their
metabolism can be activated or inhibited depending on the effector studied. CYP2C9 …
metabolism can be activated or inhibited depending on the effector studied. CYP2C9 …
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 …
measure the ability of amiodarone (AMIO), and its circulating human metabolites, to …