Sertraline is a selective serotonin reuptake inhibitor (SSRI) antidepressant. It is a first-line agent for the treatment of major depressive disorder (MDD), obsessive-compulsive disorder (OCD), panic disorder, social anxiety disorder, post-traumatic stress disorder (PTSD), and premenstrual dysphoric disorder (PMDD). It works by increasing serotonin levels in the synaptic cleft, which is thought to improve mood, reduce anxiety, and decrease obsessive thoughts and compulsive behaviors. In the Indian context, it is widely prescribed due to its efficacy, tolerability, and availability across multiple price points.
Adult: MDD, PTSD, SAD, PD, PMDD: Initial: 50 mg once daily. May be increased in increments of 50 mg at intervals of at least one week. Usual range: 50-200 mg/day. OCD: Initial: 50 mg once daily. Usual range: 50-200 mg/day.
Note: Administer once daily, either in the morning or evening, with or without food (food enhances absorption). Tablet should be swallowed whole with water. For PMDD, it may be administered either daily throughout the menstrual cycle or during the luteal phase only (starting 14 days before menses).
Sertraline is a potent and selective inhibitor of neuronal serotonin (5-HT) reuptake into presynaptic neurons. It binds with high affinity to the serotonin transporter (SERT), blocking the reuptake of serotonin from the synaptic cleft back into the presynaptic neuron. This leads to increased concentrations of serotonin in the synaptic cleft, enhancing serotonergic neurotransmission. This action is believed to be responsible for its therapeutic effects in depression and anxiety disorders. It has very weak effects on norepinephrine and dopamine reuptake and has negligible affinity for muscarinic, cholinergic, serotonergic (5-HT1A, 5-HT1B, 5-HT2), dopaminergic, adrenergic, histaminergic, GABA, or benzodiazepine receptors.
Pregnancy: Pregnancy Category C (US FDA). Epidemiological data suggest a possible increased risk of cardiovascular malformations (particularly septal defects) with first-trimester exposure. Also associated with persistent pulmonary hypertension of the newborn (PPHN) when used in late pregnancy. Risk vs. benefit must be carefully evaluated. Should not be stopped abruptly if patient is stable. Neonates exposed late in third trimester may have complications (respiratory distress, feeding difficulty, seizures, irritability).
Driving: May cause dizziness, drowsiness, or blurred vision. Patients should not drive or operate machinery until they know how the medication affects them.
| Monoamine Oxidase Inhibitors (MAOIs) - e.g., Phenelzine, Selegiline, Linezolid | Risk of serotonin syndrome (hyperthermia, rigidity, myoclonus, autonomic instability). | Contraindicated |
| Pimozide | Increased pimozide levels due to CYP2D6 inhibition; risk of QT prolongation and cardiac arrhythmias. | Contraindicated |
| Warfarin, NSAIDs, Aspirin | Increased risk of bleeding due to sertraline's effect on platelet serotonin. | Major |
| CYP2D6 Substrates - e.g., Tricyclic Antidepressants (Amitriptyline), Antipsychotics (Risperidone), Codeine, Tamoxifen | Increased plasma levels of the substrate drug due to sertraline's inhibition of CYP2D6. | Moderate to Major |
| Serotonergic Drugs - e.g., Tramadol, Triptans, Other SSRIs/SNRIs, Fentanyl, Lithium, St. John's Wort | Additive serotonergic effects; increased risk of serotonin syndrome. | Moderate to Major |
| CYP3A4 Inducers - e.g., Rifampicin, Carbamazepine, Phenytoin | May decrease sertraline plasma levels, reducing efficacy. | Moderate |
| CYP3A4 Inhibitors - e.g., Ketoconazole, Itraconazole | May increase sertraline plasma levels. | Moderate |
| Digoxin | Sertraline may slightly decrease digoxin levels; monitor. | Minor |