A study of the potential effect of sertraline on the pharmacokinetics and protein binding of tolbutamide.

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Tremaine LM, Wilner KD, Preskorn SH

A study of the potential effect of sertraline on the pharmacokinetics and protein binding of tolbutamide.

Clin Pharmacokinet. 1997;32 Suppl 1:31-6.

PubMed ID

9068933 [ View in PubMed

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Abstract

The effect of the selective serotonin reuptake inhibitor (SSRI) sertraline 200 mg/day on the metabolism of intravenously administered tolbutamide was examined in a randomised nonblinded parallel-group study in 25 healthy male volunteers. There was a small but statistically significant decrease (16%) in the clearance of tolbutamide in patients receiving the maximum recommended dosage of sertraline. The terminal elimination rate constant was also significantly reduced, corresponding to the increase in the terminal elimination half-life (from 6.9 to 8.6 hours). The decrease in clearance was not associated with any significant changes in plasma protein binding or in the apparent volume of distribution of tolbutamide. This suggests that the change in tolbutamide clearance may be due to a slight inhibition of the cytochrome P450 (CYP) isoenzyme CYP2C9/10 when sertraline was administered in its maximum recommended dosage. However, the small changes in the volume of distribution and plasma binding of tolbutamide after sertraline treatment indicate that there is a minimal interaction between sertraline and tolbutamide.

DrugBank Data that Cites this Article

Drug Enzymes

Drug	Enzyme	Kind	Organism	Pharmacological Action	Actions
Sertraline	Cytochrome P450 2C9	Protein	Humans	Unknown	Substrate Inhibitor	Details