Opipramol

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Opipramol
File:Opipramol2.svg
Systematic (IUPAC) name
4-[3-(5H-dibenz[b,f]azepin- 5-yl)propyl]- 1-piperazinethanol
Clinical data
Routes of
administration
Oral
Legal status
Legal status
  • ℞ (Prescription only)
Identifiers
CAS Number 315-72-0
ATC code N06AA05 (WHO)
PubChem CID 9417
Chemical data
Formula C23H29N3O
Molar mass 363.496 g/mol[[Script error: No such module "String".]]
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Opipramol (Insidon, Pramolan, Ensidon, Oprimol) is an antidepressant and anxiolytic used in Germany and other European countries.[1][2] Although it is a member of the tricyclic antidepressants, opipramol's primary mechanism of action is much different in comparison.[2] Most TCAs act as reuptake inhibitors, but opipramol does not, and instead acts as a sigma receptor agonist, among other properties.[2]

Indications

Opipramol is typically used in the treatment of generalized anxiety disorder (GAD).[1] Its anxiolysis becomes prominent after only 1-2 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.

Pharmacology

Opipramol acts as a high affinity sigma receptor agonist, primarily at the σ1 subtype, but also at the σ2 subtype with somewhat lower affinity.[1] It is this property which is responsible for its therapeutic benefits against anxiety and depression.[2] Opipramol also acts as a low to moderate affinity antagonist for the D2, 5-HT2, H1, H2, and muscarinic acetylcholine receptors. H1 and H2 receptor antagonism account for its antihistamine effects, and muscarinic acetylcholine receptor antagonism is responsible for its anticholinergic properties.[1]

Contraindications

Opipramol should not be taken with alcohol, or in patients with benign prostatic hyperplasia (BPH) or glaucoma.

See also

References

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