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Opipramol – Effects, Uses & Side Effects

Opipramol is a psychotropic medication used to treat anxiety disorders and somatoform disorders. It has calming and anxiolytic effects without the dependency risk associated with benzodiazepines.

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Things worth knowing about "Opipramol"

Opipramol is a psychotropic medication used to treat anxiety disorders and somatoform disorders. It has calming and anxiolytic effects without the dependency risk associated with benzodiazepines.

What is Opipramol?

Opipramol is a tricyclic compound used in psychiatry and general medicine for the treatment of anxiety disorders and somatoform disorders. Somatoform disorders are conditions in which patients experience physical symptoms such as pain, palpitations, or gastrointestinal complaints that lack a clear organic cause and are instead linked to psychological stress. Opipramol has been approved in Germany for several decades and is one of the most commonly prescribed psychotropic medications in that country.

Mechanism of Action

Unlike classical antidepressants, opipramol has little effect on the reuptake of neurotransmitters such as serotonin or noradrenaline. Instead, it acts primarily through the following mechanisms:

Sigma receptor agonism: Opipramol binds to sigma-1 and sigma-2 receptors in the brain, which play an important role in regulating anxiety, mood, and pain processing.
Histamine H1 receptor blockade: This action is responsible for the sedating (calming) properties of the medication.
Blockade of dopamine D2 and serotonin 5-HT2 receptors: This contributes to its mood-stabilizing and mild antipsychotic effects.

Through this combination, opipramol produces anxiolytic (anxiety-reducing), sedating, and mood-stabilizing effects without a significant risk of dependency or addiction.

Indications

Opipramol is approved for the treatment of:

Generalized anxiety disorder: persistent, excessive worry and inner restlessness without a specific trigger
Somatoform disorders: physical complaints such as pain, dizziness, palpitations, or fatigue without an identifiable organic cause

It is also occasionally used as an adjunct therapy for sleep disturbances, irritability, and mild depressive symptoms occurring within these conditions.

Dosage and Administration

Opipramol is usually taken as an oral tablet. The typical daily dose for adults ranges from 50 mg to 150 mg, divided into two to three doses per day. Treatment typically begins with a low dose that is gradually adjusted. Taking part of the dose in the evening can make use of the sedating effect to support sleep. The exact dosage should always be determined by a qualified healthcare professional.

Side Effects

Like all medications, opipramol can cause side effects. Common side effects include:

Drowsiness and sedation, especially at the beginning of treatment
Dry mouth
Dizziness and orthostatic hypotension (a drop in blood pressure upon standing)
Weight gain
Constipation

Less commonly, cardiac arrhythmias, visual disturbances, or allergic reactions may occur. Elderly patients should be monitored particularly carefully for dizziness and the risk of falls.

Contraindications and Interactions

Opipramol should not be used in patients with:

Narrow-angle glaucoma (increased intraocular pressure)
Severe liver or kidney impairment
Urinary retention or enlarged prostate
Concomitant use of MAO inhibitors

Interactions may occur with other centrally depressant substances (e.g., alcohol, sleeping pills), antihypertensive agents, and anticholinergic drugs. A thorough medication review by the treating physician is therefore essential before starting therapy.

Comparison with Other Anxiolytics

Compared to benzodiazepines such as diazepam, opipramol has the advantage of carrying no significant risk of dependency, making it more suitable for longer-term use. Compared to modern antidepressants such as SSRIs (selective serotonin reuptake inhibitors), opipramol acts more rapidly in producing a calming effect, though it has a different side effect profile.

References

Müller WE, Siebert B, Holoubek G, Gentsch C. Neuropharmacology of the anxiolytic drug opipramol, a sigma site and histamine H1 receptor agonist. Pharmacopsychiatry. 2004;37(Suppl 3):S189-S197.
World Health Organization (WHO). Mental health action plan 2013-2030. Geneva: WHO; 2021. Available at: https://www.who.int
Bandelow B, Michaelis S, Wedekind D. Treatment of anxiety disorders. Dialogues in Clinical Neuroscience. 2017;19(2):93-107.

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