The influence of mexidol (2-ethyl-6-methyl-3-oxypyridine) after a single peroral administration on the levels of 6beta-hydroxycortisol (6beta-OHC) and free cortisol (FC) in human urine has been evaluated. The 6beta-OHC/FC ratio is increased (approximately 2.96 +/- 0.76 times) against the basal 6beta-OHC/FC ratio during the first 24 hour after drug administration. Data analysis on the second and third day after mexidol administration did not show evident changes in 6beta-OHC/FC ratios. It is suggested that CYP3A4 activation after mexidol administration occurred only during active drug biotransformation and excretion and ceased after full excretion from the human body.
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The influence of mexidol (2-ethyl-6-methyl-3-oxypyridine) after a single peroral administration on the levels of 6beta-hydroxycortisol (6beta-OHC) and free cortisol (FC) in human urine has been evaluated. The 6beta-OHC/FC ratio is increased (approximately 2.96 +/- 0.
View Article and Find Full Text PDFPolychlorinated biphenyl (PCB) induction of CYP3A4 enzyme activity in healthy Faroese adults.
Toxicol Appl Pharmacol
October 2007
Institute of Public Health, Environmental Medicine, University of Southern Denmark, Winsløvparken 17, 5000 Odense C, Denmark.
The CYP3A4 enzyme is, along with other cytochrome P450 enzymes, involved in the metabolism of environmental pollutants and is highly inducible by these substances. A commercial polychlorinated biphenyl (PCB) mixture, 1,1,1,-trichloro-2-(o-chlorophenyl), 2-(p'-chlorophenyl)ethane (o,p'-DDT) and 1,1,-dichloro-2,2-bis (p-chlorophenyl)ethene (p,p'-DDE) are known to induce CYP3A4 activity through activation of nuclear receptors, such as the pregnane X receptor. However, this induction of CYP3A4 has not yet been investigated in humans.
View Article and Find Full Text PDFIle118Val genetic polymorphism of CYP3A4 and its effects on lipid-lowering efficacy of simvastatin in Chinese hyperlipidemic patients.
Eur J Clin Pharmacol
February 2005
Department of Health Toxicology, School of Public Health, Pharmacogenetics Research Institute, Central South University, Changsha, Hunan, 410078, China.
Objectives: To determine the frequencies of CYP3A4 alleles (CYP3A4*4,*5 and *6) in Chinese hyperlipidemic patients and to observe the impact of CYP3A4*4 (Ile118Val) genetic polymorphism on the lipid-lowering effects of simvastatin and on the activity of CYP3A4.
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