Overview
DESCRIPTION Sertraline hydrochloride is a selective serotonin reuptake inhibitor (SSRI) for oral administration. It has a molecular weight of 342.7. Sertraline hydrochloride, USP has the following chemical name: (1S-cis)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-naphthalenamine hydrochloride.
Mechanism of Action
CLINICAL PHARMACOLOGY Pharmacodynamics The mechanism of action of sertraline is presumed to be linked to its inhibition of CNS neuronal uptake of serotonin (5HT). Studies at clinically relevant doses in man have demonstrated that sertraline blocks the uptake of serotonin into human platelets. In vitro studies in animals also suggest that sertraline is a potent and selective inhibitor of neuronal serotonin reuptake and has only very weak effects on norepinephrine and dopamine neuronal reuptake. In vitro studies have shown that sertraline has no significant affinity for adrenergic (alpha 1 , alpha 2 , beta), cholinergic, GABA, dopaminergic, histaminergic, serotonergic (5HT 1A , 5HT 1B , 5H T2 ), or benzodiazepine receptors; antagonism of such receptors has been hypothesized to be associated...
Indications
- INDICATIONS AND USAGE Major Depressive Disorder – Sertraline hydrochloride is indicated for the treatment of major depressive disorder in adults. The efficacy of Sertraline hydrochloride in the treatment of a major depressive episode was established in six to eight week controlled trials of adult outpatients whose diagnoses corresponded most closely to the DSM-III category of major depressive disorder (see Clinical Trials under CLINICAL PHARMACOLOGY ).
Common Doses
- 50 mg
- 200 mg
- 150 mg
- 100 mg
Dosage
DOSAGE AND ADMINISTRATION Initial Treatment Dosage for Adults Major Depressive Disorder –Sertraline hydrochloride treatment should be administered at a dose of 50 mg once daily. While a relationship between dose and effect has not been established for major depressive disorder, OCD, panic disorder, PTSD or social anxiety disorder, patients were dosed in a range of 50-200 mg/day in the clinical trials demonstrating the effectiveness of Sertraline hydrochloride for the treatment of this indication.
Black Box Warning
BOXED WARNING Suicidality and Antidepressant Drugs Antidepressants increased the risk compared to placebo of suicidal thinking and behavior (suicidality) in children, adolescents, and young adults in short-term studies of major depressive disorder (MDD) and other psychiatric disorders. Anyone considering the use of Sertraline hydrochloride or any other antidepressant in a child, adolescent, or young adult must balance this risk with the clinical need.
Contraindications
- CONTRAINDICATIONS All Dosage Forms of Sertraline: The use of MAOIs intended to treat psychiatric disorders with Sertraline hydrochloride or within 14 days of stopping treatment with Sertraline hydrochloride is contraindicated because of an because of an increased risk if serotonin syndrome. The use of Sertraline hydrochloride within 14 days of stopping an MAOI intended to treat psychiatric disorders is also contraindicated (see WARNINGS and DOSAGE AND ADMINISTRATION ).
Side Effects
- ADVERSE REACTIONS During its premarketing assessment, multiple doses of sertraline hydrochloride were administered to over 4000 adult subjects as of February 18, 2000. The conditions and duration of exposure to sertraline hydrochloride varied greatly, and included (in overlapping categories) clinical pharmacology studies, open and double-blind studies, uncontrolled and controlled studies, inpatient and outpatient studies, fixed-dose and titration studies, and studies for multiple indications, including major depressive disorder and PMDD.
Interactions
- Drug Interactions 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 hydrochloride by other tightly bound drugs. In a study comparing prothrombin time AUC (0-120 hr) following dosing with warfarin (0.