Amiodarone biokinetics, the formation of its major oxidative metabolite and neurotoxicity after acute and repeated exposure of brain cell cultures

G Pomponio, MG Zurich, L Schultz, DG Weiss… - Toxicology in vitro, 2015 - Elsevier
The difficulty in mimicking nervous system complexity and cell–cell interactions as well as
the lack of kinetics information has limited the use of in vitro neurotoxicity data. Here, we …

Prediction of the dose range for adverse neurological effects of amiodarone in patients from an in vitro toxicity test by in vitro–in vivo extrapolation

EAH Algharably, E Di Consiglio, E Testai, R Kreutz… - Archives of …, 2021 - Springer
Amiodarone is an antiarrhythmic agent inducing adverse effects on the nervous system,
among others. We applied physiologically based pharmacokinetic (PBPK) modeling …

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 …

Integrating distribution kinetics and toxicodynamics to assess repeat dose neurotoxicity in vitro using human BrainSpheres: a case study on amiodarone

C Nunes, S Proença, G Ambrosini, D Pamies… - Frontiers in …, 2023 - frontiersin.org
For ethical, economical, and scientific reasons, animal experimentation, used to evaluate the
potential neurotoxicity of chemicals before their release in the market, needs to be replaced …

A physiologically based pharmacokinetic model of amiodarone and its metabolite desethylamiodarone in rats: pooled analysis of published data

JT Lu, Y Cai, F Chen, WW Jia, ZY Hu… - European journal of drug …, 2016 - Springer
Abstract Background and Objective Amiodarone (AMD) is one of the most effective drugs for
rhythm control of atrial fibrillation. The use of AMD is also associated with adverse effects in …

Cell type-specific expression and localization of cytochrome P450 isoforms in tridimensional aggregating rat brain cell cultures

S Vichi, JS Von Tobel, S Gemma, S Stanzel… - Toxicology in Vitro, 2015 - Elsevier
Abstract Within the Predict-IV FP7 project a strategy for measurement of in vitro biokinetics
was developed, requiring the characterization of the cellular model used, especially …

Metabolite identification studies on amiodarone in in vitro (rat liver microsomes, rat and human liver S9 fractions) and in vivo (rat feces, urine, plasma) matrices by …

NR Varkhede, S Jhajra, DS Ahire… - … in Mass Spectrometry, 2014 - Wiley Online Library
RATIONALE Several mechanisms have been anticipated for the toxicity of amiodarone, such
as oxidative stress, lipid peroxidation, phospholipidosis, free radical generation, etc …

A Rapid Procedure for the Monitoring of Amiodarone and N-Desethylamiodarone by HPLC-UV Detection

JEM Juenke, PI Brown, GA McMillin… - Journal of analytical …, 2004 - academic.oup.com
This article describes a rapid isocratic high-performance liquid chromatographic (HPLC)
method for the simultaneous measurement of the antiarrhythmic drug amiodarone and its …

A rapid HPLC method for the simultaneous determination of amiodarone and its major metabolite in rat plasma and tissues: a useful tool for pharmacokinetic studies

M Rodrigues, G Alves, A Ferreira… - Journal of …, 2013 - academic.oup.com
A rapid and sensitive high-performance liquid chromatography (HPLC) method was
developed and validated in rat plasma and tissue (heart, liver, kidney and lung) …

Detection of glutathione conjugates of amiodarone and its reactive diquinone metabolites in rat bile using mass spectrometry tools

KR Parmar, S Jhajra, S Singh - Rapid Communications in Mass …, 2016 - Wiley Online Library
Rationale Amiodarone is reported to cause hepato and pulmonary toxicity in humans, which
has been envisaged to be due to formation of its reactive metabolites, essentially based on …