Clinical Pharmacokinetics of Sertraline

  title={Clinical Pharmacokinetics of Sertraline},
  author={C. Lindsay De Vane and Heidi L. Liston and John Seth Markowitz},
  journal={Clinical Pharmacokinetics},
Sertraline is a naphthalenamine derivative with the predominant pharmacological action of inhibiting presynaptic reuptake of serotonin from the synaptic cleft. It was initially marketed for the treatment of major depressive disorder and is now approved for the management of panic disorder, obsessive-compulsive disorder and post-traumatic stress disorder.Sertraline is slowly absorbed following oral administration and undergoes extensive first-pass oxidation to form N-desmethyl-sertraline, a… 
Sertraline in the treatment of depression in the elderly
Sertraline selectively inhibits the CNS neuronal reuptake of serotonin, with a steady-state plasma concentration reached after approximately 1 week and taking 2–3 weeks longer in older adults.
Plasma Risperidone Concentrations During Combined Treatment with Sertraline
Findings indicate that sertraline at dosages up to 100 mg/d is not associated with clinically significant changes in plasma risperidone concentrations, however, higher doses of sertRALine may elevate plasma ris peridone levels, presumably as a result of a dose-dependent inhibitory effect of sERTraline on CYP2D6-mediated 9-hydroxylation of risperodone.
Effects of sertraline on the pharmacokinetics of bupropion and its major metabolite, hydroxybupropion, in mice
This is the first study, to the authors' knowledge, that reports a mild pharmacokinetic drug–drug interaction between bupropion and sertraline in mice, and it is unknown whether these quantitative changes in enzyme activity and consequent drug exposure would equate to significant pharmacodynamic changes observed in the clinic.
Sertraline concentrations in pregnant women are steady and the drug transfer to their infants is low
Placental passage of sertraline to the infant is low, however, the interindividual variation in maternal concentrations during pregnancy is huge, why therapeutic drug monitoring might assist in finding the poor metabolizers at risk for adversity and increase the safety of the treatment.
Comparison of Duloxetine, Escitalopram, and Sertraline Effects on Cytochrome P450 2D6 Function in Healthy Volunteers
This study is the first to directly compare the relative effects of duloxetine, escitalopram, and sertraline on the functional activity of the drug-metabolizing cytochrome P450 2D6 enzyme as assessed
Solid-state characterization of sertraline base-β-cyclodextrin inclusion complex.
Time course of the effects of the serotonin-selective reuptake inhibitor sertraline on central and peripheral serotonin neurochemistry in the rhesus monkey
The results suggest that response latency for SSRIs in depression is not due to gradually increasing brain extracellular fluid 5-HT levels and tend not to support theories that posit SSRI response latency as being due to autoreceptor desensitization, transporter downregulation, or drug accumulation.
Drug interaction study between bupropion and ticlopidine in male CF-1 mice.
There was a strong trend in both plasma and brain data towards greater bupropion levels and smaller hydroxybupropion levels in ticlopidine treated mice, and this is the first study to document an in vivo drug interaction between these drugs in mice.


Clinical implications of the pharmacology of sertraline.
Sertraline does not impair psychomotor performance, including simulated car driving, and overall seems neither stimulating nor sedating: an increase in critical flicker fusion threshold suggests a slight alerting effect, whereas subjective tests indicate an increased in perceived sedation at doses of 100 mg or more.
Sertraline: a new antidepressant.
Sertraline exhibits acute antidepressant effects in the dose range 50 to 200 mg/day; in the same dose range it prevents recurrence of depression and its side-effect profile is similar to that of drugs of the same class (dry mouth, nausea, and diarrhea being the most prominent).
Effect of sertraline on plasma nortriptyline levels in depressed elderly.
Overall, a modest effect of sertraline was observed on nortriptyline metabolism in these elderly depressed patients, consistent with prior reports of a weak inhibition of CYP2D6 by sERTraline in vitro and in young healthy volunteers.
Hemodialyzability of sertraline.
Smaller doses of sertraline may be required in ESRD patients, yet post-hemodialysis supplementation is unnecessary, yet impaired clearance is suggested.
Comparison of desmethylsertraline with sertraline as a monoamine uptake inhibitor in vivo
Influence of liver cirrhosis on sertraline pharmacokinetics.
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.
Pharmacokinetics of selective serotonin reuptake inhibitors.
Distribution of sertraline in postmortem cases.
Sertraline is a potent inhibitor of serotonin reuptake in the central nervous system and is used clinically to treat depression and obsessive-compulsive behavior and one similarity with tricyclic antidepressants is the high liver concentrations of drug and metabolite relative to the blood.
A Study of the Potential Effect of Sertraline on the Pharmacokinetics and Protein Binding of Tolbutamide
There was a small but statistically significant decrease in the clearance of tolbutamide in patients receiving the maximum recommended dosage of sertraline, which suggests that the change in tol butamide clearance may be due to a slight inhibition of the cytochrome P450 (CYP) isoenzyme CYP2C9/10 when sERTraline was administered in its maximum recommended dose.