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 …

The role of CYP 3A4 and 1A1 in amiodarone-induced hepatocellular toxicity

Q Wu, B Ning, J Xuan, Z Ren, L Guo, MS Bryant - Toxicology letters, 2016 - Elsevier
Amiodarone is a widely used potent antiarrhythmic for the treatment of cardiac disease;
however, its use is often discontinued due to numerous adverse effects, including …

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 …

The effect of β-naphthoflavone on the metabolism of amiodarone by hepatic and extra-hepatic microsomes

ME Elsherbiny, AOS El-Kadi, DR Brocks - Toxicology letters, 2010 - Elsevier
Amiodarone is a potent antiarrhythmic drug with several limiting side effects, some of which
have been correlated with increased levels of its more toxic metabolite …

Establishment of a mouse model for amiodarone‐induced liver injury and analyses of its hepatotoxic mechanism

S Takai, S Oda, K Tsuneyama, T Fukami… - Journal of Applied …, 2016 - Wiley Online Library
Drug‐induced liver injury (DILI) is the most frequent cause of post‐marketing warnings and
withdrawals. Amiodarone (AMD), an antiarrhythmic, presents a risk of liver injury in humans …

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 …

Role of oxidative stress in amiodarone-induced toxicity

JSM Sarma, H Pei… - Journal of Cardiovascular …, 1997 - journals.sagepub.com
Background: The clinical usefulness of amiodarone for the treatment of cardiac arrhythmias
is limited by multiorgan toxicity, especially pulmonary and hepatic. There are conflicting …

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 …

In vitro kinetics of amiodarone and its major metabolite in two human liver cell models after acute and repeated treatments

G Pomponio, CC Savary, C Parmentier, F Bois… - Toxicology in Vitro, 2015 - Elsevier
The limited value of in vitro toxicity data for the in vivo extrapolation has been often attributed
to the lack of kinetic data. Here the in vitro kinetics of amiodarone (AMI) and its mono-N …

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 …