Opipramol
Atypical tricyclic and sigma receptor ligand: a prescription anxiolytic without dependence.
Pharmacology
Contents
WHAT IS OPIPRAMOL?
Detailed overview
Opipramol is an atypical tricyclic compound that, unlike classical tricyclic antidepressants, does not inhibit monoamine reuptake; instead it acts primarily as a ligand at sigma-1 and sigma-2 receptors and as an antagonist of histamine H1 receptors. In Europe (e.g. Germany, Poland) it is an approved prescription medicine for generalized anxiety disorder (GAD) and somatoform disorders. In placebo-controlled trials its anxiolytic effect was comparable to alprazolam but without the dependence and tolerance typical of benzodiazepines. It is not FDA-approved and is not marketed in the United States.
Mechanism
Sigma-1/2 ligand + H1 antagonist
Half-life
About 11 hours (once-daily dosing)
Legal status
Prescription medicine (EU), not in US
Receptor profile
- Sigma-1 / sigma-2 receptorsStrong
- Histamine H1 receptorStrong
- D2 / 5-HT2 receptors (weak)Weak
Safety
Side effects, stop signs, contraindications
Side effects · 5
- Tiredness and drowsiness, especially in the first days of treatment (H1 blockade)
- Dry mouth and other mild anticholinergic-type effects
- Orthostatic hypotension: dizziness or lightheadedness on standing
- Weight gain and increased appetite with longer use
- Rare liver function and blood count changes, so periodic monitoring is advised
Contraindications · 5
- Acute intoxication with alcohol, hypnotics, analgesics or psychotropic drugs
- Urinary retention, narrow-angle glaucoma, severe prostate enlargement (anticholinergic effect)
- Should not be combined with MAO inhibitors or given immediately after stopping them
- Severe liver or kidney impairment and known QT prolongation require increased caution
- Pregnancy and breastfeeding: only under a clear medical indication after risk-benefit assessment
Related Nootropics
Same therapeutic category
Studies
Related research and clinical findings
Opipramol for the treatment of generalized anxiety disorder: a placebo-controlled trial including an alprazolam-treated group
Moller HJ, Volz HP, Reimann IW, Stoll KD
Opipramol for the treatment of somatoform disorders results from a placebo-controlled trial
Volz HP, Moller HJ, Reimann I, Stoll KD
Kava-Kava extract LI 150 is as effective as Opipramol and Buspirone in Generalised Anxiety Disorder: an 8-week randomized, double-blind multi-centre clinical trial in 129 out-patients
Boerner RJ, Sommer H, Berger W, Kuhn U, Schmidt U
Neuropharmacology of the anxiolytic drug opipramol, a sigma site ligand
Muller WE, Siebert B, Holoubek G, Gentsch C
Clinical trials with sigma ligands
Volz HP, Stoll KD
FAQ
FAQ
Atypical tricyclic and sigma receptor ligand: a prescription anxiolytic without dependence.
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Structure & chemistry
The information here is strictly for educational and scientific purposes. It does not replace medical advice or clinical consultation, and it does not encourage illegal substance or pharmaceutical use. Data is sourced. When in doubt, consult your doctor.