Opipramol
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| Trade names | Insidon, Opipram |
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| Routes of administration |
Oral |
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| Pharmacokinetic data | |
| Bioavailability | 94% |
| Protein binding | 91% |
| Metabolism | CYP2D6-mediated metabolism |
| Biological half-life | 6-11 hours |
| Excretion | Urine (70%), faeces (10%) |
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| ECHA InfoCard | 100.005.687 |
| Chemical and physical data | |
| Formula | C23H29N3O |
| Molar mass | 363.496 g/mol |
| 3D model (Jmol) | |
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Opipramol (Insidon, Pramolan, Ensidon, Oprimol) is an antidepressant and anxiolytic used in Germany and other European countries. Although it is a member of the tricyclic antidepressants, opipramol's primary mechanism of action is much different in comparison. Most TCAs act as reuptake inhibitors, but opipramol does not, and instead acts as a sigma receptor agonist, among other properties. It is an iminostilbene derivative, belonging to dibenzazepine group. Opipramol was developed by Schindler and Blattner in 1961.
Opipramol is typically used in the treatment of generalized anxiety disorder (GAD) and somatoform disorders. Its anxiolysis becomes prominent after only one to two weeks of chronic administration. Upon first commencing treatment, opipramol is rather sedating in nature due to its antihistamine properties, but this effect becomes less prominent with time.
Opipramol's sigma-1 agonistic effects likely impart potent antitussive effects, many other sigma-1 agonists (ex. codeine, hydrocodone, and dextromethorphan) are used for this purpose.
Experimental animal studies did not indicate injurious effects of opipramol on the embryonic development or the fertility. Opipramol should be prescribed during pregnancy, particularly in the first trimester, only for compelling indication. Opipramol should not be used during lactation period, since the active ingredient passes into the milk in small quantities.
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