[Effect of mexidol on 6beta/free hydroxycortisol ratio. Possibility of CYP3A4 activation].
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.
P A
PA
Baranov
S A
SA
Appolonova
G M
GM
Rodchenkov
A K
AK
Sariev
V P
VP
Zherdev
D000328:Adult; D000975:Antioxidants / Q000008:administration & dosage / Q000493:pharmacokinetics; D001711:Biotransformation; D051544:Cytochrome P-450 CYP3A / Q000378:metabolism*; D004789:Enzyme Activation / Q000187:drug effects; D020536:Enzyme Activators / Q000008:administration & dosage / Q000493:pharmacokinetics; D005260:Female; D006801:Humans; D006854:Hydrocortisone / Q000031:analogs & derivatives* / Q000652:urine*; D008297:Male; D010847:Picolines / Q000008:administration & dosage / Q000493:pharmacokinetics
D000975:Antioxidants; D020536:Enzyme Activators; D010847:Picolines; C070020:emoxypine succinate; C001380:6 beta-hydroxycortisol; D051544:Cytochrome P-450 CYP3A; C510163:CYP3A4 protein, human; D006854:Hydrocortisone