Pharmacology

Sertraline is a selective serotonin reuptake inhibitor (SSRI). It enhances serotonergic activity by selectively inhibiting the reuptake of serotonin (5-HT) at the presynaptic neuronal membrane, increasing serotonin levels in the central nervous system. It has minimal effect on norepinephrine and dopamine reuptake.

Indication

Sertraline is indicated for:

  • Major Depressive Disorder (MDD)

  • Obsessive-Compulsive Disorder (OCD)

  • Panic Disorder

  • Post-Traumatic Stress Disorder (PTSD)

  • Social Anxiety Disorder (SAD)

  • Premenstrual Dysphoric Disorder (PMDD)

Dosage & Administration

Adults:

  • Depression & OCD: Start with 50 mg once daily; max 200 mg/day

  • Panic Disorder, PTSD, SAD: Start with 25 mg once daily; after 1 week increase to 50 mg once daily

  • PMDD: 50 mg/day continuously or during luteal phase only

Children & Adolescents (OCD only):

  • Aged 6–12: Start with 25 mg/day; max 200 mg/day

  • Aged 13–17: Start with 50 mg/day; max 200 mg/day

Administration:

  • Can be taken with or without food.

  • Dose adjustments should occur at intervals of no less than 1 week.

Interaction

  • MAO Inhibitors: Serious or fatal reactions (e.g., serotonin syndrome)

  • Pimozide: Risk of QT prolongation (contraindicated)

  • Warfarin: Increased bleeding risk

  • NSAIDs/Antiplatelets: Increased bleeding risk

  • Other serotonergic drugs (e.g., triptans, tramadol): Serotonin syndrome risk

  • CYP450 Interactions: Sertraline is a weak inhibitor of CYP2D6 and CYP3A4

Contraindications

  • Concomitant use with MAO inhibitors or pimozide

  • Hypersensitivity to sertraline or its components

Side Effects

Common:

  • Nausea, diarrhea, insomnia, dry mouth, dizziness, fatigue, sexual dysfunction, tremor, sweating

Serious:

  • Suicidal ideation (especially in young adults), serotonin syndrome, hyponatremia, seizures, QT prolongation

Pregnancy & Lactation

  • Pregnancy (Category C): Use only if potential benefit justifies potential risk. May be associated with Persistent Pulmonary Hypertension of the Newborn (PPHN) if used in late pregnancy.

  • Lactation: Excreted in breast milk. Monitor infants for irritability, poor feeding, or sleep disturbances.

Precautions & Warnings

  • Monitor for suicidal thoughts, especially in young adults

  • Caution in patients with hepatic or renal impairment

  • Risk of serotonin syndrome, especially when combined with other serotonergic drugs

  • Can cause hyponatremia, particularly in the elderly

  • Abrupt discontinuation may lead to withdrawal symptoms; taper gradually

Overdose Effects

Symptoms may include:

  • Nausea, vomiting, dizziness, sedation, tachycardia, tremor, agitation, seizures, coma

  • No specific antidote; treatment is symptomatic and supportive

Therapeutic Class

  • Antidepressants

  • Subclass: Selective Serotonin Reuptake Inhibitors (SSRIs)

Storage Conditions

  • Store at 20–25°C (68–77°F)

  • Protect from light and moisture

  • Keep out of reach of children

Chemical Structure

  • IUPAC Name: (1S)-cis-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-naphthalenamine hydrochloride

  • Molecular Formula: C₁₇H₁₇Cl₂N·HCl

  • Molecular Weight: ~342.7 g/mol (hydrochloride salt)

Structure:

     Cl          HCl
      \         /
       C6H3–CH–C10H6CH(CH3)NH
      /
     Cl

Scroll to Top