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SSRI pharmacokinetics

SSRI pharmacokinetics
Drug Time to peak serum concentration (Tmax) Elimination half-life (parent drug, unless noted)* Metabolism Active metabolites Protein binding
Citalopram 4 hours 35 hours Liver (CYPs 2C19, 2D6, 3A4) Desmethylcitalopram, didesmethylcitalopram (weakly active) 80%
Escitalopram 5 hours 27 to 32 hours Liver (CYPs 2C19, 2D6, 3A4) S-desmethylcitalopram, S-didesmethylcitalopram (weakly active) 56%
Fluoxetine 6 to 8 hours

Parent: 2 to 6 days

Metabolite: 7 to 10 days
Liver (CYPs 1A2, 2B6, 2C19, 2C9, 2D6, 2E1, 3A4) Norfluoxetine 94.5%
Fluvoxamine 3 to 8 hours 14 to 16 hours Liver (CYPs 1A2, 2D6) None 80%
Paroxetine

IR: 5.2 to 8.1 hours

CR: 6 to 10 hours
15 to 21 hours Liver (CYP2D6) None 95%
Sertraline 4.5 to 8.4 hours

Parent: 26 hours

Metabolite: 62 to 104 hours
Liver (CYPs 2B6, 2C19, 2C9, 2D6, 3A4) Desmethylsertraline (weakly active) 98%

CR: controlled-release; CYP: cytochrome P450; IR: immediate-release; SSRI: selective serotonin reuptake inhibitor.

* Elimination half-life may be prolonged in patients with liver impairment, older adults, and with chronic use. During overdose, elimination time may also be prolonged due to saturation of metabolic enzymes and delayed absorption.

¶ CYP isoenzymes in bold indicate a major metabolic pathway of the SSRI.
Graphic 67511 Version 5.0

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