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[Evaluation of pharmacokinetic interaction of aphobazole with CYP1A2 drug-substrate in experiments].

Authors :
Novitskaia IaG
Litvin AA
Viglinskaia AO
Zherdev VP
Source :
Eksperimental'naia i klinicheskaia farmakologiia [Eksp Klin Farmakol] 2013; Vol. 76 (6), pp. 30-3.
Publication Year :
2013

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.

Details

Language :
Russian
ISSN :
0869-2092
Volume :
76
Issue :
6
Database :
MEDLINE
Journal :
Eksperimental'naia i klinicheskaia farmakologiia
Publication Type :
Academic Journal
Accession number :
24003488