Clinical Pharmacokinetics of SSRIs

Pierre Baumann, Chin B Eap and Pierre Voirol

Citalopram,1 fluoxetine,2,3 fluvoxamine,4 paroxetine5 and sertraline6 are the five antidepressants which are known as selective serotonin reuptake inhibitors (SSRIs) (Fig. 2.1). Their clinical efficacy, good tolerance and safety have been demonstrated in many studies7,8 and some of them may also be prescribed successfully for the treatment of obsessive compulsive disorder, bulimia or panic attacks. Despite their common pharmacological properties, the SSRIs differ in their metabolism by cytochrome P450 and in their interaction profile with other drugs which are also substrates of this enzyme system. Sensitive and selective (including stereoselective) methods, using high performance liquid chromatography or gas chromatography, have been introduced for their quantitative analysis in blood samples.9 These have enabled studies of their pharmacokinetics as well as investigations of the relationship between plasma concentration and clinical efficacy. This review summarizes our present knowledge of the metabolism, pharmacokinetics and pharmacogenetics of this group of antidepressants.

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