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In summary, CYP1A2 was distinctly inhibited by imipramine and Amitriptyline ( Elavil ), CYP3A generic skinoren clonidine cyproheptadine by imipramine and Fluoxetine ( Prozac ), while other CYP isoenzymes (CYP2B and/or 2E1) by imipramine and Fluoxetine ( Prozac ).. In contrast to the rozerem generic tested tricyclic antidepressants, Fluoxetine ( Prozac ) did not exert any considerable effect generic skinoren on the 3-N- or 1-N-demethylation of caffeine (Ki 152 and 196 microM, respectively), which indicates its low affinity for CYP1A2. The contraceptive pills for women aim of the present study names of was to investigate the influence of imipramine, Amitriptyline ( Elavil ) and Fluoxetine ( Prozac ) on cytochrome P-450 activity measured by caffeine micardis hct oxidation in rat liver microsomes.
Fluoxetine ( Prozac ) diminished markedly the 8-hydroxylation of the marker drug; as reflected by Ki values, the potency of inhibition cephalexin of rat CYP3A by Fluoxetine ( Prozac ) was similar to that of imipramine (Ki 40 and 45 microM, respectively). The influence of Amitriptyline ( Elavil yasmin generic ) on 8-hydroxylation and especially on 7-N-demethylation of caffeine was weaker (Ki 108 and 190 pM, respectively) than on 3-N- or 1-N-demethylation, suggesting ticlid a narrower spectrum of cytochrome P-450 inhibition by Amitriptyline ( Elavil ) than by imipramine, involving mainly the subfamily CYP1A2, and--to a lesser degree--CYP3A. Imipramine decreased the rate of 3-N-, 1-N- and 7-N-demethylations, and 8-hydroxylation of caffeine, the effect on 3-N-demethylation being most pronounced (Ki 33 microM). Moreover, it is also a relatively specific substrate of CYP3A (8-hydroxylation).
The obtained results sho that imipramine exerted a most potent inhibitory effect on caffeine metabolism. Effects of antidepressant drugs on the activity of cytochrome P-450 measured by caffeine oxidation in rat liver microsomes.Caffeine is a marker drug for testing the activity of CYP1A2 (3-N-demethylation) in humans and rats. Amitriptyline ( Elavil ) sho distinct inhibition of 3-N- and 1-N-demethylation of caffeine, though its effect was less potent than in the jordan of imipramine (Ki 57 and 61 pM, respectively). In the jefferson of 1-N- and in particular 7-N-demethylation of caffeine, apart from CYP1A2, other cytochrome P-450 isoenzymes play a considerable role.
However, Fluoxetine ( Prozac ) displayed a clear inhibitory effect on caffeine 7-N-demethylation (Ki 72 microM), the reaction which is catalyzed mainly by other than CYP1A2 isoenzymes.
