Esmolol Hydrochloride

Approved Indications:

• Major Depressive Disorder (MDD):
• Treatment of acute and maintenance phases in adults and adolescents (≥12 years).
• Generalized Anxiety Disorder (GAD):
• Management of persistent and disabling anxiety symptoms in adults.
• Obsessive-Compulsive Disorder (OCD):
• Indicated in adults and adolescents (off-label in some countries).
• Panic Disorder:
• Treatment of recurrent panic attacks with or without agoraphobia in adults.
• Social Anxiety Disorder (SAD):
• Management of social phobia symptoms in adults.

Off-Label / Clinically Accepted Uses:

• Premenstrual Dysphoric Disorder (PMDD)
• Post-Traumatic Stress Disorder (PTSD)
• Anxiety associated with chronic medical conditions

Administration Route: Oral (tablet or solution)

Adults (MDD, GAD, SAD, Panic Disorder):

• Initial Dose: 10 mg once daily
• Maintenance Dose: 10–20 mg once daily based on clinical response
• Maximum Dose: 20 mg/day

Elderly (≥65 years):

• Start at 5 mg/day; titrate slowly to 10 mg/day
• Maximum: 20 mg/day

Adolescents (12–17 years):

• MDD: Start 10 mg/day; titrate to 20 mg/day if needed
• Monitoring: Close supervision for suicidality

Special Populations:

• Renal Impairment: No dosage adjustment for mild-moderate; caution in severe impairment
• Hepatic Impairment: Start at 5 mg/day; maximum 10 mg/day

Administration Tips:

• Can be taken with or without food
• Administer at the same time each day
• Do not abruptly discontinue to avoid withdrawal symptoms

Escitalopram oxalate is a selective serotonin reuptake inhibitor (SSRI). It binds to the presynaptic serotonin transporter (SERT) in the central nervous system, inhibiting reuptake of serotonin (5-HT) into presynaptic neurons. This increases extracellular serotonin concentration in the synaptic cleft, enhancing serotonergic neurotransmission. The heightened serotonin activity improves mood, reduces anxiety, and alleviates obsessive-compulsive and panic symptoms over time.

• Absorption: Rapid; peak plasma concentration ~4–5 hours post-dose
• Bioavailability: ~80%
• Distribution: Widely distributed; protein binding ~56%
• Metabolism: Hepatic via CYP2C19, CYP3A4, CYP2D6 to inactive metabolites
• Elimination:
• Half-life: 27–32 hours
• Excretion: Primarily renal (≤50% as metabolites), some fecal elimination

• Pregnancy: FDA Category C; animal studies show potential fetal risk; use only if benefits outweigh risks
• Lactation: Excreted in human milk in low amounts; monitor infant for irritability or poor feeding
• Caution: Limited data; use with careful clinical judgment

• Primary Class: Antidepressant
• Subclass: Selective Serotonin Reuptake Inhibitor (SSRI)

• Hypersensitivity to escitalopram, citalopram, or any excipients
• Concomitant use with MAO inhibitors (risk of serotonin syndrome)
• Concurrent use with pimozide
• Recent history of mania or bipolar disorder without mood stabilizer

• Suicidal Thoughts/Behavior: Increased risk in children, adolescents, and young adults (<25 years)
• Serotonin Syndrome: High risk with other serotonergic agents
• QT Prolongation: Risk at doses >20 mg/day, especially in patients with cardiac disease
• Hyponatremia/SIADH: Monitor serum sodium, particularly in elderly
• Seizures: Use cautiously in seizure-prone patients
• Discontinuation Syndrome: Gradual taper recommended

Common:

• CNS: Headache, dizziness, insomnia, somnolence
• GI: Nausea, diarrhea, dry mouth, constipation
• Genitourinary: Erectile dysfunction, delayed ejaculation, anorgasmia
• General: Fatigue, sweating

Serious/Rare:

• Serotonin syndrome
• QT prolongation, Torsades de pointes
• Hyponatremia
• Suicidal ideation, especially in adolescents

Timing & Dose Dependence: Side effects often occur within 1–2 weeks of initiation; severity may decrease over time; dose-dependent effects include QT prolongation and sexual dysfunction.

• MAO Inhibitors: Risk of serotonin syndrome; contraindicated
• Other SSRIs/SNRIs/Triptans: Additive serotonergic effect
• CYP2C19 Inhibitors (Omeprazole, Fluvoxamine): Increased escitalopram levels
• CYP3A4 Inhibitors (Ketoconazole, Itraconazole): Slight increase in levels
• Alcohol: May exacerbate CNS depression

• FDA & EMA: Limit max dose to 20 mg/day due to QT prolongation risk
• Updated Warnings: Enhanced focus on suicidal risk in <25 years
• NICE: Recommends SSRI as first-line in MDD and GAD; monitor response over 4–6 weeks
• Clinical Practice: Emphasis on slow titration in elderly and hepatic impairment

• Temperature: Store at 20°C to 25°C; short excursions 15–30°C allowed
• Humidity: Keep in a dry place
• Light Protection: Store in original container away from light
• Handling: Keep out of reach of children; do not crush or chew tablets unless specified
• Shelf Life: Follow manufacturer instructions; do not use beyond expiry