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Escitalopram

Escitalopram is a widely prescribed antidepressant medication that belongs to a class of drugs known as Selective Serotonin Reuptake Inhibitors (SSRIs). It is primarily used to treat major depressive disorder (MDD) and generalized anxiety disorder (GAD). Below is a comprehensive overview of the drug:

🔬 Chemical and Pharmacological Details

• Generic Name: Escitalopram

• Brand Names: Lexapro (USA), Cipralex (EU), among others

• Chemical Structure: (S)-(+)-1-[3-(Dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydroisobenzofuran-5-carbonitrile

• Molecular Formula: C20H21FN2O

• Drug Class: SSRI (Selective Serotonin Reuptake Inhibitor)

Escitalopram is the S-enantiomer of citalopram, meaning it is the more pharmacologically active part of the citalopram molecule.

🧠 Mechanism of Action

Escitalopram works by increasing serotonin levels in the brain. It does this by inhibiting the reuptake (reabsorption) of serotonin (5-HT) into the presynaptic neuron, thereby increasing its availability in the synaptic cleft. This improved serotonin signaling is believed to enhance mood and reduce anxiety.

💊 Therapeutic Uses

Major Depressive Disorder (MDD)

Generalized Anxiety Disorder (GAD)

Obsessive-Compulsive Disorder (OCD) – off-label

Panic Disorder – off-label

Social Anxiety Disorder (SAD) – off-label

Post-Traumatic Stress Disorder (PTSD) – off-label

Premenstrual Dysphoric Disorder (PMDD) – off-label

⚖️ Dosage and Administration

• Typical Adult Dose for Depression or Anxiety:

  • Initial: 10 mg once daily

  • Maximum: 20 mg/day

• Elderly or Hepatic Impairment:

  • Recommended: Start at 5 mg daily

• Pediatric Use:

  • Approved for adolescents (≥12 years) in some countries

It is usually taken orally once daily, with or without food.

⏳ Pharmacokinetics

• Bioavailability: ~80%

• Time to peak plasma concentration: 4–5 hours

• Half-life: ~27–32 hours

• Metabolism: Primarily in the liver via CYP2C19, CYP2D6, and CYP3A4

• Excretion: Renal (kidneys)

⚠️ Warnings and Precautions

• Black Box Warning (USA): May increase the risk of suicidal thoughts and behaviors in children, adolescents, and young adults.

• Serotonin Syndrome: Risk increases when combined with other serotonergic agents (e.g., MAOIs, triptans, tramadol).

• QT Prolongation: Can cause abnormal heart rhythms at higher doses.

• Discontinuation Syndrome: Abrupt stopping may lead to symptoms like dizziness, insomnia, irritability, and brain “zaps”.

🤕 Common Side Effects

• Nausea

• Headache

• Drowsiness or insomnia

• Dry mouth

• Increased sweating

• Sexual dysfunction (e.g., decreased libido, delayed ejaculation)

• Fatigue or dizziness

• Appetite or weight changes

🚫 Contraindications

• Concurrent use with monoamine oxidase inhibitors (MAOIs)

• Known hypersensitivity to escitalopram or citalopram

• Use with pimozide (due to QT prolongation risk)

💊 Drug Interactions

• MAOIs: Risk of serotonin syndrome; avoid concurrent use

• NSAIDs, anticoagulants: Increased risk of bleeding

• Other SSRIs/SNRIs: Risk of serotonin syndrome

• CYP enzyme inhibitors/inducers: May affect escitalopram levels

• Alcohol: Escitalopram does not potentiate alcohol effects, but caution is still advised

👶 Use in Pregnancy and Lactation

• Pregnancy Category (varies by country): C

  • Potential risks include persistent pulmonary hypertension of the newborn (PPHN) and neonatal withdrawal syndrome

• Breastfeeding: Present in breast milk; caution advised

🧬 Genetic Considerations

• Individuals with CYP2C19 poor metabolizer status may have increased drug levels and a higher risk of side effects.

• Genetic testing can help guide dosing in some cases.

📊 Comparative Notes

Compared to other SSRIs:

• More selective for serotonin reuptake inhibition

• Generally better tolerated

• Fewer drug-drug interactions

• Commonly preferred in the elderly and those sensitive to side effects