VitalsCentral

Sertraline

Zoloft

FDA ApprovedPsychotherapeuticsSSRI Antidepressants
FDA: 1991Half-life: 26 hours (sertraline), 62-104 hours (desmethylsertraline)Pregnancy: Category C

Overview

Sertraline is a selective serotonin reuptake inhibitor (SSRI) antidepressant used to treat major depressive disorder, panic disorder, OCD, PTSD, social anxiety disorder, and premenstrual dysphoric disorder.

Indications

  • Major Depressive Disorder
  • Panic Disorder
  • OCD
  • PTSD
  • Social Anxiety Disorder
  • Premenstrual Dysphoric Disorder

Contraindications

  • MAO inhibitor use within 14 days
  • Pimozide use
  • Disulfiram use (oral concentrate)

Mechanism of Action

Selectively inhibits serotonin reuptake at the presynaptic neuronal membrane, enhancing serotonergic neurotransmission in the CNS.

Pharmacodynamics

Increases serotonin availability in synaptic cleft. Antidepressant effects typically seen after 2-4 weeks of treatment.

Pharmacokinetics

Absorption
Well absorbed. Food increases bioavailability slightly.
Distribution
Extensively distributed. Highly protein bound.
Metabolism
Hepatic via CYP2C19, CYP2D6, CYP3A4. Active metabolite: desmethylsertraline.
Excretion
Feces (40-45%) and urine (40-45%) as metabolites.
Half-life
26 hours (sertraline), 62-104 hours (desmethylsertraline)
Bioavailability
44%
Protein Binding
98%

Dosage

Typical dosage: 50-200 mg once daily

Available Forms

  • Tablet
  • Oral concentrate

Side Effects

Common

  • Nausea
  • Diarrhea
  • Insomnia
  • Sexual dysfunction
  • Headache

Serious

  • Serotonin syndrome
  • Suicidal ideation in youth
  • Bleeding

Rare

  • Hyponatremia
  • Angle-closure glaucoma

Drug Interactions

MAO Inhibitorsmajor

Risk of serotonin syndrome. Contraindicated.

Warfarinmoderate

Increased bleeding risk. Monitor INR.

Warnings

⚠️BLACK BOX WARNING

Antidepressants increased the risk of suicidal thinking and behavior in children, adolescents, and young adults. Monitor closely for clinical worsening and suicidal ideation.

Pregnancy

Category C

Toxicity

Serotonin syndrome in overdose. Supportive care, cyproheptadine for serotonin syndrome.

Overdose

Symptoms include somnolence, vomiting, tachycardia, ECG changes. Activated charcoal and supportive care.

References

Looking for patient-friendly information? Visit RemedyDoor for easy-to-read guides about this medication.