Drug reference

Sertraline

SSRI · Antidepressant

Also known as Sertraline hydrochloride, Zoloft, Lustral, Seralin

START

25-50 mg PO once daily; titrate weekly

TYPICAL MAX

200 mg/day

STOP IF

MAOI within 14 days · linezolid · pimozide · serotonin syndrome

WATCH

Mood (esp. <25y suicidality black-box) · bleeding risk (NSAIDs) · QTc at high dose · GI symptoms

CDSCO approvedSchedule HJan AushadhiNPPA price-controlledATC N06AB06

Dose laddermg/d

Renal dose adjustmenteGFR mL/min/1.73m²

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours

ONSET: 2w · clinical response at 2-4 weeks
PEAK: 6h · Cmax
t½: 1.1d · plasma t½ (active metabolite 62-104h)
DURATION: 1d · once-daily dosing window

EXCRETION

Hepatic CYP2B6/3A4 → active metabolite · biliary/renal

route + CYP

INTERACTIONS

12 major

incl. contraindicated

PREGNANCY

Category C — most reproductive safety data; preferred SSRI in pregnancy

FDA category + note

Top interactionssee all 12 →

LinezolidContraindicatedDatabaseDDInter
Monoamine Oxidase Inhibitors (maois) (e.g., Phenelzine, Tranylcypromine, Selegiline, Linezolid, Methylene Blue)ContraindicatedDatabase
PhenelzineContraindicatedDatabaseDDInter
PimozideContraindicatedDatabaseDDInter

Available in India

327 branded formulations and 60 fixed-dose combinations. Look up specific brands in the Drugs workspace.

Jan Aushadhi — generic available at GoI pharmacies

Mechanism

Sertraline selectively inhibits the reuptake of serotonin (5-hydroxytryptamine, 5-HT) into presynaptic neurons in the central nervous system. This action leads to an increased concentration of serotonin in the synaptic cleft, enhancing serotonergic neurotransmission. Chronic administration results in downstream adaptive changes, including desensitization of postsynaptic serotonin receptors, contributing to its therapeutic effects.

Indications

Major Depressive Disorder (MDD)Obsessive-Compulsive Disorder (OCD)Panic DisorderPost-traumatic Stress Disorder (PTSD)Social Anxiety Disorder (SAD)Premenstrual Dysphoric Disorder (PMDD)Generalized Anxiety Disorder (GAD) (off-label)Major depressive disorderObsessive-compulsive disorderGeneralized anxiety disorderFibromyalgiaNeuropathic painAnxietymajor depressiongeneralized anxietysocial anxietyPTSDpremenstrual dysphoric syndromepreventing vasovagal symptoms in postmenopausal womenDepression in cancer patients

Dosing

Adult: Oral: For Major Depressive Disorder or OCD, initiate at 50 mg once daily. For Panic Disorder, PTSD, or Social Anxiety Disorder, initiate at 25 mg once daily for one week, then increase to 50 mg once daily. Doses may be increased in 25-50 mg increments at weekly intervals, based on clinical response and tolerability, up to a maximum of 200 mg once daily.…
Pediatric: Oral: For OCD in children 6-12 years, initiate at 25 mg once daily, titrate to 50 mg after one week, then up to 200 mg once daily as tolerated. For OCD in adolescents 13-17 years, initiate at 50 mg once daily, titrate up to 200 mg once daily as tolerated.
Renal adjustment: No dose adjustment is required for renal impairment, including severe impairment or end-stage renal disease. Clinical monitoring for adverse effects is advised for patients with severe renal impairment (eGFR <30 mL/min). Sertraline is not removed by dialysis.
Max dose: 200 mg/day

Pharmacokinetics

Onset

Initial anxiolytic effects may be seen within 1 week. Antidepressant effects typically begin within 2-4 weeks, with full effect potentially taking up to 8-12 weeks for some conditions like OCD.

Peak effect

Plasma concentration (Cmax): 4.5-8.4 hours (single dose). Steady-state plasma concentrations are achieved within approximately 7 days with once-daily dosing.

Duration

Duration of antidepressant effects is sustained with daily dosing, related to half-life and steady-state concentrations.

Half-life

Parent drug: Approximately 26 hours. Active metabolite (N-desmethylsertraline): 62-104 hours.

Bioavailability

Approximately 44% (due to extensive first-pass metabolism)

Protein binding

Approximately 98%

Metabolism

Extensive hepatic metabolism, primarily via multiple cytochrome P450 (CYP) isoenzymes, including CYP2D6, CYP2C19, CYP3A4, CYP2B6, and CYP2C9, to the weakly active N-desmethylsertraline and then to inactive metabolites.

Excretion

Primarily renal and fecal excretion, mainly as metabolites (40-45% in urine, 40-45% in feces). Less than 0.2% excreted unchanged in urine.

Contraindications

Concomitant use with Monoamine Oxidase Inhibitors (MAOIs) or within 14 days of discontinuing an MAOI (risk of serotonin syndrome)
Concomitant use with pimozide
Known hypersensitivity to sertraline or any excipients
Uncontrolled narrow-angle glaucoma

Side effects

Common

NauseaDiarrheaInsomniaSomnolenceHeadacheDizzinessDry mouthFatigueTremorIncreased sweatingSexual dysfunction (e.g., ejaculatory delay, anorgasmia)Anorexia/Weight lossSexual dysfunctionincreased anxietyirritabilitydecreased libidoerectile dysfunctionanorgasmiaejaculatory delayemesisdullness of intellectual abilitiesconcentration issues

Serious

Serotonin syndrome (agitation, hallucinations, tachycardia, hyperthermia, incoordination)
Suicidal ideation and behavior (especially in children, adolescents, and young adults)
Hyponatremia (Syndrome of Inappropriate Antidiuretic Hormone secretion - SIADH)
Seizures
Abnormal bleeding (e.g., gastrointestinal hemorrhage)
QTc prolongation and Torsade de Pointes (rare)
Activation of mania/hypomania
Angle-closure glaucoma
Serotonin syndrome
serotonin syndrome (with MAOIs)
suicidal ideation or behavior (black-box warning in children and adolescents)
discontinuation syndrome
persistent pulmonary hypertension in newborns

Pregnancy & lactation

Pregnancy

Category C — most reproductive safety data; preferred SSRI in pregnancy

Lactation

Sertraline is excreted into breast milk in small amounts. It is generally considered compatible with breastfeeding, especially at lower doses, but caution is advised. Monitor breastfed infants for potential adverse effects such as sedation, irritability, poor feeding, or changes in weight gain. Consult a physician before use during lactation.

Drug interactions

Linezolid

Contraindicated

Database

Serotonin syndrome: hyperthermia, rigidity, myoclonus, mental status changes.

Do not combine. Stop SSRI 2 weeks before linezolid or use alternative antibiotic.

Source: DDInter

Monoamine Oxidase Inhibitors (maois) (e.g., Phenelzine, Tranylcypromine, Selegiline, Linezolid, Methylene Blue)

Contraindicated

Database

Serotonin syndrome (hyperthermia, rigidity, myoclonus, autonomic instability, mental status changes)

Sertraline is contraindicated with MAOIs. A washout period of at least 14 days is required between discontinuing an MAOI and starting sertraline, and at least 14 days between discontinuing sertraline and starting an MAOI.

Phenelzine

Contraindicated

Database

Serotonin syndrome: agitation, hyperthermia, rigidity, seizures, potentially fatal

Contraindicated. Allow 14-day washout between SSRI and MAOI

Source: DDInter

Pimozide

Contraindicated

Database

Increased risk of QT prolongation and cardiac arrhythmias (e.g., Torsades de Pointes)

Concomitant use is contraindicated. Sertraline significantly increases pimozide exposure.

Source: DDInter