Opipramol

Products

Opipramol is commercially available in the form of dragées (Insidon). It has been approved in many countries since 1961, originally by Geigy, later by Novartis.

Structure and properties

Opipramol (C23H29N3O, Mr = 363.5 g/mol) structurally belongs to the tricyclic antidepressants and is a dibenzazepine derivative. It is present in the drug as opipramol dihydrochloride.

Effects

Opipramol (ATC N06AA05) has antianxiety, sedative, depressant, antihistamine, weak antidepressant, weak anticholinergic, and weak alpha-adrenolytic properties. Unlike other tricyclic antidepressants, its effects are not based on inhibition of neurotransmitter reuptake. Opipramol is a nonselective MAO inhibitor, a mild antagonist at dopamine receptors, an agonist at sigma receptors, and an antagonist at serotonin receptors, among others. The half-life is in the range of 7 to 11 hours.

Indications

  • Mood states accompanied by anxiety, restlessness, tension, sleep disturbances and depressiveness.
  • Psychosomatic disorders and secondary moods associated with cardiovascular, gastrointestinal, dermal disease patterns, menopausal symptoms and headaches.

Dosage

According to the SmPC. The drugs are usually administered one to a maximum of three times daily with or after meals. Discontinuation should be gradual.

Contraindications

  • Hypersensitivity, including to related agents.
  • Fresh myocardial infarction
  • AV block
  • Diffuse supraventricular or ventricular conduction disorders.
  • Acute intoxication with central depressant drugs or alcohol
  • Acute delirium
  • Acute urinary retention
  • Untreated narrow-angle glaucoma
  • Prostate enlargement with residual urine formation
  • Paralytic ileus
  • Combination with an MAO inhibitor

For complete precautions, see the drug label.

Interactions

Opipramol is metabolized by CYP2D6. It has a high potential for drug-drug interactions, for example with MAO inhibitors, anticoagulants, central depressant drugs, SSRIs, anticholinergics, and sympathomimetics.

Adverse effects

The most common possible adverse effects include:

  • Drowsiness, drowsiness, fatigue.
  • Dizziness
  • Visual disturbances