title: [Evaluation of pharmacokinetic interaction of aphobazole with CYP1A2 drug-substrate in experiments].
abstract: The effect of aphobazole on CYP1A2 (drug-marker caffeine) was studied in rats. Aphobazole was administered orally at doses 5 and 25 mg/kg, caffeine 50 mg/kg. The metabolic ratios (MR) for the caffeine metabolites (theobromine and paraxanthine) were accounted. After aphobazole administration at the effective, anxiolytic dose (5 mg/kg) for 4 days (3 times per day every 3 hours) neither the inhibiting nor the inducing effects on NOD1A2 was revealed. Increasing the aphobazole dose up to 25 mg/kg after 2 days repeated administrations of the drug made it possible to reveal a moderate inducing effect. Longer aphobazole administration (4 days), the inducing effect is amplified. Since the MR values on theobromine and paraxanthine after 2-day administration aphobazole exceed similar values in the control of 2.5 and 3.3 times, respectively. MR values after the 4-days aphobazole administration in dose 25 mg/kg exceed similar values in the control of 4.2 times for theobromine and in 6.1 times for paraxanthine.
authors.forename: Ia G
authors.initials: IaG
authors.lastname: Novitskaia
authors.forename: A A
authors.initials: AA
authors.lastname: Litvin
authors.forename: A O
authors.initials: AO
authors.lastname: Viglinskaia
authors.forename: V P
authors.initials: VP
authors.lastname: Zherdev
mesh_terms: D000284:Administration, Oral; D000818:Animals; D021461:Animals, Outbred Strains; D014151:Anti-Anxiety Agents / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D001562:Benzimidazoles / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D001711:Biotransformation; D002110:Caffeine / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D002849:Chromatography, Gas; D019388:Cytochrome P-450 CYP1A2; D003580:Cytochromes / Q000378:metabolism*; D004334:Drug Administration Schedule; D004347:Drug Interactions; D008297:Male; D009025:Morpholines / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D051381:Rats; D013805:Theobromine / Q000097:blood; D013806:Theophylline / Q000097:blood
chemical_list: C410924:2-((2-morpholino)ethylthio)-5-ethoxybenzimidazole; D014151:Anti-Anxiety Agents; D001562:Benzimidazoles; D003580:Cytochromes; D009025:Morpholines; D002110:Caffeine; D013806:Theophylline; C017170:Cyp1a2 protein, rat; D019388:Cytochrome P-450 CYP1A2; D013805:Theobromine; C021183:1,7-dimethylxanthine