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- W2118569857 abstract "Enantiomerically pure drugs and genotyping are promising approaches to achieve optimization in antidepressant therapy. Mirtazapine is a mixed noradrenergic serotoninergic antidepressant used as a racemate. We analyzed pharmacokinetics of its enantiomers in relation to CYP2D6 genotype and in relation to its adverse effects. Mirtazapine was enantioselectively absorbed from the gut with a rate constant of 0.2 min−1 for S(+), but 0.08 min−1 for R(−) mirtazapine. Kinetics of R(−) mirtazapine was only marginally dependent on CYP2D6 genotype, but total clearance of the S(+) enantiomer were 1.3, 2.3, and 3.4 L min−1 in poor, extensive, and ultrarapid metabolizers of CYP2D6 substrates with apparent substantial first-pass metabolism in rapid and ultrarapid metabolizers. Mirtazapine effects on heart rate and blood pressure correlated much more strongly with R(−) then with S(+) concentrations, whereas sedation correlated similarly with both enantiomers. At least concerning some adverse effects, it might be worthwhile to study further mirtazapine enantiospecifically. Clinical Pharmacology & Therapeutics (2007) 81, 699–707. doi:10.1038/sj.clpt.6100116; published online 28 February 2007." @default.
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- W2118569857 date "2007-02-28" @default.
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- W2118569857 title "Pharmacokinetics of Mirtazapine: Enantioselective Effects of the CYP2D6 Ultra Rapid Metabolizer Genotype and Correlation with Adverse Effects" @default.
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- W2118569857 doi "https://doi.org/10.1038/sj.clpt.6100116" @default.
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