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NERVOUS SYSTEM › PSYCHOANALEPTICS › ANTIDEPRESSANTS › Non-selective monoamine reuptake inhibitors
opipramol
N06AA05
Forms & Strengths
- Film-coated tablets: 50 mg
- Film-coated tablets: 100 mg (extended-release)
Adult Dosing
- Generalized anxiety disorder and somatoform disorders: 50 mg to 100 mg orally once daily (evening) or divided into 2 to 3 doses daily
- Maximum recommended daily dose: 300 mg
Pediatric Dosing
- Safety and efficacy in pediatric patients under 18 years of age have not been established
- Not recommended for use in children and adolescents
Indications
- Generalized anxiety disorder
- Somatoform disorders
- Depressive states associated with anxiety and tension (primarily in European markets)
Mechanism of Action
- Unlike classic tricyclic antidepressants, opipramol does not significantly inhibit the reuptake of noradrenaline or serotonin
- Acts primarily as a high-affinity sigma receptor agonist (sigma-1 and sigma-2 subtypes)
- Exhibits significant antagonistic activity at histamine H1 receptors and serotonin 5-HT2 receptors
- Possesses mild dopamine D2 and alpha-1 adrenergic receptor antagonist properties
Contraindications
- Hypersensitivity to opipramol or any excipients
- Acute alcohol, sleeping pill, analgesic, or psychotropic drug intoxication
- Acute urinary retention
- Untreated narrow-angle glaucoma
- Paralytic ileus
- Concomitant treatment with monoamine oxidase inhibitors (MAOIs)
- Severe heart block or pre-existing severe conduction disorders
Adverse Reactions
- Dry mouth
- Nasal congestion
- Fatigue and somnolence (especially during initial treatment)
- Orthostatic hypotension
- Dizziness
- Weight gain
- Constipation
- Urinary hesitation or retention
- Rare: QT prolongation, arrhythmias, blood dyscrasias (leukopenia)
Drug Interactions
- MAOIs: Risk of severe serotonin syndrome, hypertensive crisis, and hyperpyrexia; contraindicated
- CNS depressants (alcohol, barbiturates, opioids, sedatives): Potentiation of sedative effects and respiratory depression
- Anticholinergic agents: Enhancement of antimuscarinic adverse effects (e.g., paralytic ileus, acute glaucoma)
- CYP2D6 inhibitors: May increase plasma concentrations of opipramol
- QT-prolonging drugs (antiarrhythmics, antipsychotics, macrolides): Increased risk of ventricular arrhythmias
Curated Content: Needs Vetting Before Put to Clinical Use