Assessment of cytochrome P4502E1 induction in alcoholic patients by chlorzoxazone pharmacokinetics
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2024, American Journal of MedicinePrediction of inter-individual variability on the pharmacokinetics of CYP1A2 substrates in non-smoking healthy volunteers
2016, Drug Metabolism and PharmacokineticsCitation Excerpt :To estimate the CV of CLint,h,2E1, the AUC/D and its CV for chlorzoxazone, a CYP2E1 specific substrate, were collected from literature. The data in 5 populations with a total of 80 subjects for chlorzoxazone were collected from literature on healthy volunteers [39,42–45], and the WM of AUC/D and its CV were calculated as 3.93 min/l and 45.6%, respectively. Then, the CV of AUC/D was simulated using an arbitrary CV for CLint,h,2E1 ranging from 0% to 100%.
Ultrasensitive quantification of the CYP2E1 probe chlorzoxazone and its main metabolite 6-hydroxychlorzoxazone in human plasma using ultra performance liquid chromatography coupled to tandem mass spectrometry after chlorzoxazone microdosing
2016, Journal of Chromatography B: Analytical Technologies in the Biomedical and Life SciencesCitation Excerpt :Conversely, isoniazid acts as an inducer of CYP2E1 (ligand stabilisator), thus promoting acetaminophen toxicity [7,8]. While alcohol acutely inhibits this enzyme [9], chronic alcohol abuse induces CYP2E1 [10], thus precipitating NAPQI and rifampicin toxicity [2,11]. Finally CYP2E1 may also foster the formation of reactive oxidative species in alcoholic liver disease, liver fibrosis, and carcinogenesis [12,13].
Methodology to assay CYP2E1 mixed function oxidase catalytic activity and its induction
2014, Redox BiologyCitation Excerpt :With respect to exogenous compounds, CYP2E1 metabolizes a wide variety of hydrophobic compounds such as solvents, aromatic hydrocarbons, alcohols, halogenated anesthetics, nitrosamines, and drugs such as acetaminophen and chlorzoxazone (Table 1). Of interest, the ratio of 6-hydroxychlorzoxazone/chlorzoxazone can be used to estimate levels of CYP2E1 in humans, including alcoholics [28]. Similar to other CYPs, CYP2E1 can be induced by its substrates such as ethanol, pyrazole, 4-methylpyrazole, benzene, imidazole, pyridine, acetone and isoniazid [6–8].
Hepatocyte growth factor protects hepatocytes against oxidative injury induced by ethanol metabolism
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