Opipramol is a tricyclic antidepressant (TCA) and anxiolytic (anti-anxiety agent) with a delayed onset of action. Mood-improving effects have also been demonstrated. Its multidirectional action is achieved through effects on various receptors: agonistic activity at sigma σ1 and σ2 receptors (through which it modulates the NMDA system), weak to moderate inhibitory effects on dopamine D2, serotonin 5-HT2, histamine H1 and H2 receptors, as well as muscarinic cholinergic receptors.
After oral administration, opipramol is rapidly and completely absorbed from the gastrointestinal tract.
Opipramol is predominantly bound to plasma proteins. The volume of distribution is approximately 10 L/kg.
The elimination half-life is approximately 11 hours. Opipramol is primarily metabolised by the CYP2D6 isoenzyme in the liver.
Approximately 70% of the drug is excreted renally in urine, of which approximately 5–9% is in unchanged form. The remainder is excreted in faeces.
⚠️ Warnings
Treatment must always be conducted under medical supervision.
Opipramol should not be used in the following conditions:
Prostatic hyperplasia without urinary retention
Hepatic and renal disease
Increased susceptibility to seizures (e.g. brain damage of various aetiology, epilepsy, alcoholism)
Cerebrovascular insufficiency and pre-existing cardiac damage, particularly with conduction disorders
In patients with pre-existing first-degree atrioventricular block or other conduction disorders, opipramol should not be used unless frequent ECG monitoring is possible.
Very rarely, changes in blood count (neutropenia, agranulocytosis) may occur; therefore, blood count should be monitored during treatment.
The medicinal product may cause allergic reactions, including delayed-type reactions.
During long-term treatment, monitoring of hepatic function is recommended.
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