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[Evaluation of pharmacokinetic interaction of aphobazole with CYP1A2 drug-substrate in experiments].
- 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.
- Subjects :
- Administration, Oral
Animals
Animals, Outbred Strains
Anti-Anxiety Agents administration & dosage
Anti-Anxiety Agents blood
Benzimidazoles administration & dosage
Benzimidazoles blood
Biotransformation
Caffeine administration & dosage
Caffeine blood
Chromatography, Gas
Cytochrome P-450 CYP1A2
Drug Administration Schedule
Drug Interactions
Male
Morpholines administration & dosage
Morpholines blood
Rats
Theobromine blood
Theophylline blood
Anti-Anxiety Agents pharmacokinetics
Benzimidazoles pharmacokinetics
Caffeine pharmacokinetics
Cytochromes metabolism
Morpholines pharmacokinetics
Subjects
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