Zoloft
sertraline
Boxed Warning
Suicidality risk in children, adolescents, and young adults under 25 during initial treatment.
Overview
Sertraline is an SSRI antidepressant approved for major depressive disorder, OCD, panic disorder, PTSD, social anxiety disorder, and premenstrual dysphoric disorder. It is one of the most widely prescribed antidepressants worldwide.
25mg, 50mg, 100mg, 200mg
Tablets: 25mg, 50mg, 100mg; Oral concentrate: 20mg/mL
Category C (risk cannot be ruled out)
Mechanism of Action
Potent and selective inhibitor of serotonin reuptake at the presynaptic membrane (SERT), with minimal effects on norepinephrine and dopamine reuptake. Also has mild affinity for the dopamine transporter.
Taper Notes
Liquid formulation available for precise dosing. Hyperbolic taper recommended.
Maudsley Deprescribing Guidance
Follow hyperbolic reduction schedule. Liquid concentrate (20mg/mL) useful for fine adjustments.
Common Withdrawal Symptoms
Interactions & Safety
Drug Interactions
- MAOIs — contraindicated (serotonin syndrome risk)
- Pimozide — contraindicated
- Disulfiram — oral concentrate contains alcohol
Food Interactions
- Food increases peak plasma levels by ~25%
- Oral concentrate must be diluted before use; avoid mixing with grapefruit juice
- Avoid alcohol during treatment
Contraindications
- MAOIs within 14 days
- Pimozide
- Disulfiram (oral concentrate contains alcohol)
Toxicity
Serotonin syndrome in overdose or with serotonergic combinations. QT prolongation reported rarely. GI bleeding risk increased with NSAIDs.
Pharmacokinetics
ADME Profile
Slowly absorbed after oral administration, Tmax 4.5–8.4 hours. Bioavailability subject to extensive first-pass metabolism. Food increases Tmax slightly.
~20 L/kg
Extensive hepatic metabolism primarily via CYP2B6, CYP2C9, CYP2C19, CYP2D6, and CYP3A4 to N-desmethylsertraline (substantially less active).
Renal (~40–45% as metabolites) and fecal (~40–45%). Less than 0.2% excreted unchanged in urine.
~98%
~1.5 L/min (oral clearance)
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