displayName: DESCRIPTION SECTION
FDA Article Code: 34089-3
Sertraline hydrochloride is a selective serotonin reuptake inhibitor (SSRI) for oral administration. It has a molecular weight of 342.7. Sertraline hydrochloride has the following chemical name: (1S-cis)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-naphthalenamine hydrochloride. The empirical formula C17H17NCl2•HCl is represented by the following structural formula:
Sertraline hydrochloride is a white to off white crystalline powder that is sparingly soluble in methanol and dimethyl formamide.
Sertraline hydrochloride is supplied for oral administration as film-coated tablets containing sertraline hydrochloride equivalent to 25, 50 and 100 mg of sertraline and the following inactive ingredients: D & C Yellow #10 (in 25 mg tablet), dibasic calcium phosphate anhydrous, FD & C Blue #1 (in 25 mg tablet), FD & C Blue #2 (in 50 mg tablet), FD & C Red #40 (in 25 mg tablet), hydroxypropyl cellulose, hypromellose, iron oxide yellow (in 100 mg tablet), magnesium stearate, microcrystalline cellulose, polyethylene glycol, polysorbate 80, sodium starch glycolate and titanium dioxide.
displayName: DRUG INTERACTIONS SECTION
FDA Article Code: 34073-7
Potential Effects of Coadministration of Drugs Highly Bound to Plasma Proteins
Because sertraline is tightly bound to plasma protein, the administration of 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.
In a study comparing prothrombin time AUC (0 to 120 hr) following dosing with warfarin (0.75 mg/kg) before and after 21 days of dosing with either sertraline (50 to 200 mg/day) or placebo, there was a mean increase in prothrombin time of 8% relative to baseline for sertraline compared to a 1% decrease for placebo (p<0.02). The normalization of prothrombin time for the sertraline group was delayed compared to the placebo group. The clinical significance of this change is unknown. Accordingly, prothrombin time should be carefully monitored when sertraline therapy is initiated or stopped.
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.
In a placebo-controlled trial in normal volunteers, the administration of two doses of sertraline did not significantly alter steady-state lithium levels or the renal clearance of lithium.
Nonetheless, at this time, it is recommended that plasma lithium levels be monitored following initiation of sertraline therapy with appropriate adjustments to the lithium dose.
In a controlled study of a single dose (2 mg) of pimozide, 200 mg sertraline (q.d.) co- administration to steady state was associated with a mean increase in pimozide AUC and Cmax of about 40%, but was not associated with any changes in EKG. Since the highest recommended pimozide dose (10 mg) has not been evaluated in combination with sertraline, the effect on QT interval and PK parameters at doses higher than 2 mg at this time are not known. While the mechanism of this interaction is unknown, due to the narrow therapeutic index of pimozide and due to the interaction noted at a low dose of pimozide, concomitant administration of sertraline and pimozide should be contraindicated (see
Results of a placebo-controlled trial in normal volunteers suggest that chronic administration of sertraline 200 mg/day does not produce clinically important inhibition of phenytoin metabolism. Nonetheless, at this time, it is recommended that plasma phenytoin concentrations be monitored following initiation of sertraline therapy with appropriate adjustments to the phenytoin dose, particularly in patients with multiple underlying medical conditions and/or those receiving multiple concomitant medications.
The effect of sertraline on valproate levels has not been evaluated in clinical trials. In the absence of such data, it is recommended that plasma valproate levels be monitored following initiation of sertraline therapy with appropriate adjustments to the valproate dose.
The risk of using sertraline in combination with other CNS active drugs has not been systematically evaluated. Consequently, caution is advised if the concomitant administration of sertraline and such drugs is required.
There is limited controlled experience regarding the optimal timing of switching from other drugs effective in the treatment of major depressive disorder, obsessive-compulsive disorder, panic disorder, posttraumatic stress disorder, premenstrual dysphoric disorder and social anxiety disorder to sertraline. Care and prudent medical judgment should be exercised when switching, particularly from long-acting agents. The duration of an appropriate washout period which should intervene before switching from one selective serotonin reuptake inhibitor (SSRI) to another has not been established.
displayName: HOW SUPPLIED SECTION
FDA Article Code: 34069-5
Sertraline capsule-shaped, film-coated tablets, containing sertraline hydrochloride equivalent to 100 mg of sertraline, are packaged in bottles as well as unit dose blisters.
Sertraline Tablets USP, 100 mg: yellow colored, capsule shaped, biconvex, film-coated tablets, debossed with ‘L’ & ‘U’ on either side of the breakline on one side and ‘D03’ on the other side.
NDC 33261-0346-30 Bottles of 30
NDC 33261-0346-60 Bottles of 60
NDC 33261-0346-90 Bottles of 90
Store at 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature].
PACKAGE LABEL.PRINCIPAL DISPLAY PANEL
displayName: PACKAGE LABEL.PRINCIPAL DISPLAY PANEL
FDA Article Code: 51945-4
Sertraline Tablets USP, 100 mg
Each film-coated tablet contains sertraline hydrochloride USP equivalent to 100 mg of sertraline.