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HOME >> API >> API List 3 >> Sertraline Hcl >> Interaction

INTERACTION
Sertraline Hcl CAS Registry Number 79559-97-0

Potential Effects of Coadministration of Drugs Highly Bound to Plasma Proteins-Because sertraline is tightly bound to plasma protein, the administration of Sertraline  (sertraline hydrochloride) to a patient taking another drug which is tightly bound to protein (e.g., warfarin, digitoxin) may cause a shift in plasma concentrations potentially resulting in an adverse effect. Conversely, adverse effects may result from displacement of protein bound Sertraline  by other tightly bound drugs.Cimetidine-In a study assessing disposition of Sertraline  (100 mg) on the second of 8 days of cimetidine administration (800 mg daily), there were significant increases in Sertraline  mean AUC (50%), Cmax (24%) and half-life (26%) compared to the placebo group. The clinical significance of these changes is unknown.CNS Active Drugs-In a study comparing the disposition of intravenously administered diazepam before and after 21 days of dosing with either Sertraline  (50 to 200 mg/day escalating dose) or placebo, there was a 32% decrease relative to baseline in diazepam clearance for the Sertraline  group compared to a 19% decrease relative to baseline for the placebo group (p < 0.03). There was a 23% increase in Tmax for desmethyldiazepam in the Sertraline  group compared to a 20% decrease in the placebo group (p < 0.03).

The clinical significance of these changes is unknown.Drugs Metabolized by P450 3A4-In three separate in vivo interaction studies, sertraline was co- administered with cytochrome P450 3A4 substrates, terfenadine, carbamazepine, or cisapride under steady-state conditions. The results of these studies indicated that sertraline did not increase plasma concentrations of terfenadine, carbamazepine, or cisapride. These data indicate that sertraline's extent of inhibition of P450 3A4 activity is not likely to be of clinical significance. Results of the interaction study with cisapride indicate that sertraline 200 mg (q.d.) induces the metabolism of cisapride (cisapride AUC and Cmax were reduced by about 35%).Serotonergic Drugs: Based on the mechanism of action of SNRIs and SSRIs, including Sertraline , and the potential for serotonin syndrome, caution is advised when SNRIs and SSRIs, including Sertraline , are coadministered with other drugs that may affect the serotonergic neutrotransmitter systems, such as triptans, linezolid (an antibiotic which is a reversible non-selective MAOI), lithium, tramadol,riptans:

There have been rare post marketing reports of serotonin syndrome with use of an SNRI or an SSRI and a triptan. If concomitant treatment of SNRIs and SSRIs, including Sertraline , with a triptan is clinically warranted, careful observation of the patient is advised, particularly during treatment initiation and dose increasesSumatriptan-There have been rare post marketing reports describing patients with weakness, hyperreflexia, and incoordination following the use of a selective serotonin reuptake inhibitor (SSRI) and sumatriptan. If concomitant treatment with sumatriptan and an SSRI (e.g., citalopram, fluoxetine, fluvoxamine, paroxetine, sertraline) is clinically warranted, appropriate observation of the patient is advised.

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