Exopram
Generic composition: Escitalopram oxalate
General Description
Escitalopram is a selective serotonin re-uptake inhibitor (SSRI) and the S-enantiomer of racemic citalopram.
Therapeutic category
- Selective serotonin reuptake inhibitors Antidepressant
Mechanism of action
It increases concentration of serotonin at neuronal synapse by inhibiting pre-synaptic SERT with minimal effects on NE (Nor-epinephrine) or DA (Dopamine) reuptake.
Pharmacokinetics
Absorption: Readily absorbed from GU tract, oral bioavailability is 80%, plasma protein binding is approximately 56%, peak plasma concentration in 5 hours.
Distribution: Volume of distribution is approximately 107 ± 42L
Metabolism: Metabolised in liver by hepatic Cytochrome. P450 (Isoenzymes CYP2C19 and CYP3A4) to active metabolite S-demthylescitalopram (major) and S-didemethylescitalopram (minor)
Elimination: Elimination mainly via liver and minorly from urine
Half-life: 27-32 hours, elimination half-life of escitalopram’s primary metabolite, S-desmethylcitalopram, is approximately 54 hours at steady state
Dosage forms available
- EXOPRAM 5mg Tablets
- EXOPRAM 10mg Tablets
- EXOPRAM 20mg Tablets
Uses
- Major depressive disorder
- Generalized anxiety disorder
- Panic disorder
- Social anxiety disorder
- Obsessive compulsive disorder
Dose
- 10 mg once daily, increased after at least a week, maximum dose 20 mg daily for depression, Generalized anxiety disorder, social anxiety disorder, obsessive compulsive disorder.
- Initial dose 5 mg, increased to 10 mg at least after a week, maximum dose 20 mg daily for panic disorder
- *Dose reduction in hepatic impairment, renal impairment and in elderly
Side effect
Insomnia, ejaculation disorder (primarily ejaculatory delay), nausea, constipation, sweating increased, fatigue and somnolence
Contraindications
Contraindicated in bipolar depression due to risk of serotonin syndrome.
Drug interaction
- MAOIs or other serotonergic medications.
- Medications that have ability to prolong QT interval such as antimicrobials (Erythromycin, Clarithromycin, Fluconazole, Ketoconazole), antipsychotics, anti-arrhythmics (Dronedarone, Sotalol, Quinidine, Amiodarone, Flecainide) etc.
- Weak inhibitor of CYP2D6 thus increases the plasma level of aripiprazole, risperidone, tramadol, codeine etc.
- Caution when taken with cough medicine containing Dextromethorphan; may lead to serotonin syndrome, liver damage and other side effects.
Precaution
- Hepatic and Renal impairement
- High caution when taken with Saint John’s Wort; May lead to serotonin syndrome.
