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Pharmacology: Pharmacodynamics: Escitalopram oxalate, a selective serotonin reuptake inhibitor (SSRI) and S-enantiomer of racemic citalopram, enhances serotonergic activity in the central nervous system (CNS) as a result of its inhibition of serotonin (5-HT) reuptake in CNS neurons. It possesses no or very low affinity for serotonergic (5-HT1-7), alpha- and beta-adrenergic, dopamine (D1-5), histamine (H1-3), muscarinic (M1-5), and benzodiazepine receptors as well as various ion channels including Na+, K+, Cl-, and Ca2+ channels.
Pharmacokinetics: Absorption: Time to peak concentration: about 5 hours in adults, 2.9 hours in adolescents.
Effect of food: no effect.
Bioavailability: 80%.
Distribution: Protein binding: approximately 56% to plasma protein.
Vd: approximately 20 L/kg.
Metabolism: Hepatic via CYP3A4 and CYP2C19; N-demethylation.
Excretion: Renal: urine (8% as unchanged drug, 10% as S-DCT).
Hepatic impairment: decreased by 37%.
Mild to moderate renal impairment: decreased by 17%.
Severe renal impairment (CrCl <20 mL/minute): No information available.
Elimination Half Life:
Adolescents: 19 hours.
Adults: 27 to 32 hours.
Elderly: increased by approximately 50% and doubled in patients with hepatic impairment.
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