Comparative pharmacokinetics of selective serotonin reuptake inhibitors: a look behind the mirror

摘要: The presently available selective serotonin reuptake inhibitors (SSRIs) citalopram. fluoxetine. fluvoxamine, paroxetine and sertraline, despite their common mechanism of action, differ in chemical structure, metabolism pharmacokinetics. From a clinical point view, it is relevance that the potency to inhibit cytochrome P450 isozyme CYP2D6 gradually decreases from paroxetine, fluoxetine, norfluoxetine, desmethylcitalopram, fluvoxamine sertraline down citalopram, explaining great extent differences pharmacokinetic interactions between SSRIs tricyclic antidepressants, which are metabolized by this enzyme. Fluvoxamine interacts with these drugs involving inhibition CYP1A2, CYP3A4 CYP2CI9. Except for substrate CYP2D6, little known about enzymes implicated SSRIs. Fluoxetine citalopram used as racemic drugs. Data on stereoselectivity enantiomers (5-HT) uptake animal brain, also those kinetics humans, presented. It may be concluded routine therapeutic drug monitoring, plasma level measurement fluoxetine probably relevance. However, study structure-activity relationship cerebral 5-HT transporter, stereochemical should considered. In sense, could represent promising tool increase present knowledge.