Sertraline is a prescription selective serotonin reuptake inhibitor (SSRI), a class of antidepressant medication. It is used to treat major depressive disorder, obsessive-compulsive disorder (OCD), and several anxiety-related conditions. It is taken orally and is marketed under the brand name Zoloft, among other products. (medlineplus.gov)
Mechanism and pharmacokinetics
Sertraline inhibits the reuptake of serotonin, a neurotransmitter, into neurons, enhancing serotonergic activity in the central nervous system. Its effects on norepinephrine and dopamine reuptake are comparatively weak. It does not inhibit monoamine oxidase. (dailymed.nlm.nih.gov)
Its average elimination half-life is approximately 26 hours, and steady-state blood concentrations are reached after about one week of daily administration. Sertraline undergoes extensive metabolism; its principal metabolite, N-desmethylsertraline, is substantially less pharmacologically active. These pharmacokinetic properties support once-daily administration. (dailymed.nlm.nih.gov)
The full therapeutic benefit may take several weeks or longer to develop. (medlineplus.gov)
Clinical uses and formulations
In addition to major depressive disorder and OCD, U.S. indications include panic disorder, post-traumatic stress disorder, social anxiety disorder, and premenstrual dysphoric disorder (PMDD). PMDD treatment may involve continuous daily administration or administration during a specified portion of the menstrual cycle. (medlineplus.gov)
U.S. labeling establishes safety and effectiveness for OCD in children and adolescents aged 6–17. It does not establish pediatric safety and effectiveness for other indications or for OCD below age six. (dailymed.nlm.nih.gov)
Zoloft formulations include tablets and an oral concentrate containing sertraline hydrochloride. The concentrate requires dilution before administration and contains alcohol; its concurrent use with disulfiram is contraindicated. (dailymed.nlm.nih.gov)
Adverse effects and safety
Common adverse effects include nausea, diarrhea, tremor, indigestion, decreased appetite, and excessive sweating. Sexual adverse effects include reduced libido, delayed or absent ejaculation, erectile dysfunction, and delayed or absent orgasm. (medlineplus.gov)
U.S. labeling carries a boxed warning about increased suicidal thoughts and behaviors in pediatric and young adult patients in short-term antidepressant studies. Other important risks include serotonin syndrome, abnormal bleeding, low blood sodium, activation of mania or hypomania, seizures, angle-closure glaucoma, and QTc prolongation. Mania-related warnings are particularly relevant to bipolar disorder. (dailymed.nlm.nih.gov)
Abrupt discontinuation can produce symptoms such as dizziness, nausea, sweating, anxiety, irritability, sleep disturbance, and sensory disturbances. (medlineplus.gov)
Interactions and special populations
Concurrent use with monoamine oxidase inhibitors or pimozide is contraindicated. Other serotonergic substances can increase serotonin-syndrome risk. Aspirin, nonsteroidal anti-inflammatory drugs, antiplatelet medicines, and anticoagulants can increase bleeding risk. Sertraline also inhibits CYP2D6, potentially increasing exposure to medicines metabolized by this enzyme. (dailymed.nlm.nih.gov)
Hepatic impairment can increase exposure to sertraline. U.S. labeling specifies reduced dosages for mild hepatic impairment and does not recommend use in moderate or severe impairment. Exposure during late pregnancy has been associated with neonatal complications, including persistent pulmonary hypertension and discontinuation-related symptoms. (dailymed.nlm.nih.gov)
Regulatory history
The U.S. Food and Drug Administration first approved Zoloft for depression on December 30, 1991. Subsequent U.S. approvals included OCD on October 25, 1996, panic disorder on July 8, 1997, and post-traumatic stress disorder on December 7, 1999. (accessdata.fda.gov)
References
- Sertraline: MedlinePlus Drug Informationmedlineplus.gov
- DailyMed — Zoloft prescribing informationdailymed.nlm.nih.gov
- DailyMed — Sertraline hydrochloride tablets prescribing informationdailymed.nlm.nih.gov
- Zoloft Medical Review: NDA 19-839/S-035accessdata.fda.gov