sertraline

Brand: Zoloft

⚠ BBW Prototype: fluoxetine
Drug Class: antidepressant
Drug Family: antidepressant
Subclass: SSRI
Organ Systems: cns

Mechanism of Action

Selective SERT inhibitor with mild dopamine transporter inhibition; fewer CYP interactions than fluoxetine; also has modest sigma receptor activity.

serotonin reuptake transporter (SERT)

Indications

  • major depressive disorder
  • PTSD
  • OCD
  • panic disorder
  • social anxiety disorder
  • premenstrual dysphoric disorder

Contraindications

  • concurrent MAOIs
  • concurrent pimozide
  • disulfiram (oral concentrate contains alcohol)

Adverse Effects

Common

  • nausea (especially initially)
  • diarrhea
  • insomnia
  • sexual dysfunction
  • dry mouth
  • dizziness

Serious

  • serotonin syndrome
  • suicidal ideation
  • hyponatremia
  • QTc prolongation
  • abnormal bleeding

Pharmacokinetics (ADME)

Absorption Bioavailability ~44%; food increases absorption of oral concentrate
Distribution Highly protein-bound (98%); Vd ~20 L/kg
Metabolism CYP2C19, CYP2C9, CYP2D6, CYP3A4 to inactive N-desmethylsertraline
Excretion Fecal (~44%) and renal (~40%)
Half-life 22–36 hours
Onset 1–2 weeks (partial); 4–6 weeks (full antidepressant effect)
Peak 4.5–8.4 hours
Duration 24 hours
Protein Binding 98%
Vd ~20 L/kg

Drug Interactions

Drug / Agent Mechanism Severity
MAOIs serotonin syndrome major
NSAIDs/anticoagulants additive bleeding risk via platelet serotonin depletion moderate
pimozide QTc prolongation via CYP2D6 inhibition at higher sertraline doses major

Nursing Considerations

  1. Monitor suicidal ideation in first 4 weeks; schedule follow-up within 1 week of initiation
  2. Take with food to reduce GI side effects, especially nausea in the first 1–2 weeks
  3. Monitor serum sodium (particularly in elderly patients on diuretics) — hyponatremia/SIADH can occur
  4. Advise patients that full antidepressant effect takes 4–6 weeks; do not discontinue prematurely if initial response seems limited

Clinical Pearls

  • Sertraline has the most extensive safety data in pregnancy of all SSRIs and is often the preferred SSRI during pregnancy — though all SSRIs carry neonatal adaptation syndrome risk
  • Among SSRIs, sertraline is considered to have the fewest drug interactions because it has the least potent CYP inhibitory profile at standard doses

Safety Profile

Pregnancy safe
Lactation use-with-caution
Renal Adjustment Not required
Hepatic Adjustment Required
TDM Not required

Concordance Terms

Cross-referenced clinical concepts — click any term to see all content where it appears.