Citalopram

Class

    • Furancarbonitrile SSRI

Indications

Administration/Absorption

    • Oral

    • Single daily dose

    • Bioavailability is 80% following oral administration

Dosage

Distribution

    • Volume of distribution 12 L/kg

Mechanism

    • The antidepressant, antiobsessive-compulsive, and antibulimic actions of Citalopram are presumed to be linked to its inhibition of CNS neuronal uptake of serotonin

    • Citalopram blocks the reuptake of serotonin at the serotonin reuptake pump of the neuronal membrane, enhancing the actions of serotonin on 5HT1A autoreceptors

    • Has only very weak effects on norepinephrine and dopamine neuronal reuptake

    • Has no significant affinity for adrenergic (alpha1, alpha2, beta), cholinergic, GABA, dopaminergic, histaminergic, serotonergic (5HT1A, 5HT1B, 5HT2), or benzodiazepine receptors

      • Antagonism of such receptors has been hypothesized to be associated with various anticholinergic, sedative, and cardiovascular effects for other psychotropic drugs

    • Citalopram does not inhibit monoamine oxidase.

Excretion

    • Half-life 35 hrs

    • The systemic clearance of citalopram was 330 mL/min, with approximately 20% of that due to renal clearance

    • Citalopram is metabolized to demethylcitalopram (DCT), didemethylcitalopram (DDCT), citalopram-N-oxide, and a deaminated propionic acid derivative

Side effects

Interactions

Contraindications