Finn Bradley
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In vitro study.Caffeine undergoes 3-N-demethylation pain relief via CYP1A2, as well as 1-N-demethylation, 7-N-demethylation and 8-hydroxylation, which may involve other CYP isoenzymes. Desipramine decreased the rates of 1-N-, 3-N- and 7-N-demethylations, and 8-hydroxylation of caffeine (Ki 23.3, 36.6, 23.3 and pain relief 63.3 microM, respectively), drugstore usa online the effect on 1-N- and 7-N-demethylation being the most pronounced. In contrast to the above-tested antidepressants, Mirtazapine ( Remeron ) did not decrease significantly the antidepressants oxidation rates of 3-N-demethylation or 8-hydroxylation (Ki 264 and 455 microM, respectively) and had no effect on other oxidation pathways of caffeine. carisoprodol The tested antidepressants (with an exception of Mirtazapine ( Remeron )) may lead to drug-drug metabolic interactions at a level of a few CYP isoforms. Dixon analysis sleeping pills of caffeine metabolism carried out in the control liver microsomes, in the absence and presence of the peyote drugs sho that desipramine sleeping pills and clomipramine exerted the most potent inhibitory effect on caffeine metabolism. Sertraline HCL ( Zoloft )decreased significantly the rate of 1-N- and 3-N-demethylation cialis and 8-hydroxylation (Ki 37.3, 69.3 and 64 microM, respectively), while its effect on 7-N-demethylation of caffeine was less pronounced (Ki 92.1 microM). The obtained results sho that all the investigated antidepressants, with an exception of Mirtazapine ( Remeron ), added in vitro to liver microsomes had an inhibitory effect on caffeine metabolism (via competitive or mixed mechanism), though their potency towards particular metabolic pathways was different. The aim of the present study was to investigate the influence of clomipramine, desipramine, Sertraline HCL ( Zoloft ), nefazodone and Mirtazapine ( Remeron ) on cytochrome P-450 activity measured by caffeine oxidation in rat liver microsomes. Clomipramine sho distinct inibition of 1-N- and 3-N-demethylation and 8-hydroxylation of caffeine, the effects on N-demethylations being the most pronounced (Ki 38.6, 34.8, 45.6 microM, respectively). Its effect on 7-N-demethylation was rather weak (Ki 97.8 microM). In summary, we have observed intra- and inter-drug differences in the inhibitory effects of the antidepressants on the four oxidation pathways of caffeine in rat liver microsomes. Effects of classic and newer antidepressants on the oxidation pathways of caffeine in rat liver. The obtained results provide further indirect evidence that apart from CYP1A2, other CYP isoforms are also important for the metabolism of caffeine.. Nefazodone displayed clear effect on 3-N- and 7-N-demethylation (Ki 68.8 and 66.4 microM, respectively), but was weak in inhibiting 1-N-demethylation and 8-hydroxylation of caffeine (Ki 110 and 186 microM, respectively).
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