Pharmacokinetics of Citalopram in Relation to the Sparteine and the Mephenytoin Oxidation Polymorphisms

Pharmacogenetics, Drug-Metabolizing Enzymes, and Clinical Practice

“…Likewise, citalopram is metabolized to a less active metabolite (desmethylcitalopram) mainly by CYP2C19 and 3A4 (ϳ35% each in EMs) and thence to didesmethylcitalopram (less active again) by CYP2D6 (Sindrup et al, 1993;Kobayashi et al, 1997;von Moltke et al, 1999von Moltke et al, , 2001Herrlin et al, 2003). The AUC of racemic or S-citalopram (active enantiomer) does not vary appreciably with CYP2D6 status (Sindrup et al, 1993;Herrlin et al, 2003).…”

“…CYP2C19 PMs have significantly higher concentrations of citalopram (Sindrup et al, 1993;Herrlin et al, 2003), fluoxetine , and sertraline (Wang et al, 2001). Citalopram (racemic and the active S-enantiomer) concentrations are ϳ1.7-fold higher in PMs at steady state (Sindrup et al, 1993;Herrlin et al, 2003), although no significant difference was seen after a single dose (Yu et al, 2003). The AUC of sertraline was 1.4-fold higher after a single dose in Chinese volunteers (Wang et al, 2001).…”

Treatment of Comorbid Tuberculosis and Depression

“…As in the case of isoniazid, the metabolic pathways of SSRIs have not been firmly established. In vivo data have indicated that CYP2C19 is the major isoenzyme involved in the first step of citalopram metabolism, 31,32 while an in vitro study implicated CYP3A4 as the primary isoenzyme with CYP2C19 having a secondary role. 33 This discrepancy was accounted for by genetic differences in the populations studied.…”

Impact of CYP2C19 phenotypes on escitalopram metabolism and an evaluation of pupillometry as a serotonergic biomarker

“…Previous studies have shown that racemic citalopram is mainly metabolised by cytochrome P450 2C19 (CYP2C19) [5]. Up to 5% of Blacks and Caucasians are phenotyped as poor metabolisers (PM), whereas up to 20% of Asians are PM [6].…”