Influence of liver cirrhosis on sertraline pharmacokinetics.
Sertraline is a serotonin reuptake inhibitor. The enhancement of serotoninergic transmission is associated with antidepressant activity. In order to determine the pharmacokinetics of sertraline in patients with chronic stable hepatic insufficiency, 10 patients were matched (age, weight, sex) with 10 healthy subjects in an open study. Each participant received a single capsule containing the equivalent of 100 mg sertraline base. Blood samples were taken during 264 h after administration for measurement of plasma concentrations of sertraline. The results confirm that the oral clearance of sertraline is reduced with a 1.7-fold increase in Cmax and a significant prolongation in elimination half-life in hepatically impaired patients.
Démolis
J L
JL
Clinical Pharmacology Unit, Saint-Antoine University Hospital, Paris, France.
Angebaud
P
P
Grangé
J D
JD
Coates
P
P
Funck-Brentano
C
C
Jaillon
P
P
D015057:1-Naphthylamine / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D000328:Adult; D000368:Aged; D000928:Antidepressive Agents / Q000493:pharmacokinetics*; D005260:Female; D006801:Humans; D008103:Liver Cirrhosis / Q000378:metabolism*; D008297:Male; D008875:Middle Aged; D017367:Selective Serotonin Reuptake Inhibitors / Q000493:pharmacokinetics*; D020280:Sertraline
D015057:1-Naphthylamine; D000928:Antidepressive Agents; D017367:Selective Serotonin Reuptake Inhibitors; D020280:Sertraline