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Pipamperone
Antipsychotic drug From Wikipedia, the free encyclopedia
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Pipamperone (INN, USAN, BAN), sold under the brand name Dipiperon, is a typical antipsychotic of the butyrophenone family used in the treatment of schizophrenia[2][3] and as a sleep aid for depression.[4] It is or has been marketed under brand names including Dipiperon, Dipiperal, Piperonil, Piperonyl, and Propitan.[3] Pipamperone was discovered at Janssen Pharmaceutica in 1961, and entered clinical trials in the United States in 1963.[5]
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Medical uses
Pipamperone was developed for use as an antipsychotic in the treatment of schizophrenia.
Pipamperone might be useful as a hallucinogen antidote or "trip killer" in blocking the effects of serotonergic psychedelics like psilocybin.[6]
Pharmacology
Pipamperone acts as an antagonist of the 5-HT2A,[7] 5-HT2B,[8] 5-HT2C[9] D2,[7] D3,[10] D4,[7][11] α1-adrenergic,[10] and α2-adrenergic receptors.[10] It shows much higher affinity for the 5-HT2A and D4 receptors over the D2 receptor (15-fold in the case of the D4 receptor, and even higher in the case of the 5-HT2A receptor),[7][10][12] being regarded as "highly selective" for the former two sites at low doses.[12][13] Pipamperone has low and likely insignificant affinity for the H1 and mACh receptors, as well as for other serotonin and dopamine receptors.[10]
Pipamperone is considered to have been a forerunner to the atypical antipsychotics, if not an atypical antipsychotic itself, due to its prominent serotonin antagonism.[14][15][16] It is also used to normalise mood and sleep patterns and has antianxiety effects in neurotic patients.[17]
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Antidepressant effects
Low-dose pipamperone (5 mg twice daily) has been found to accelerate and enhance the antidepressant effect of citalopram (40 mg once daily), in a combination (citalopram/pipamperone) referred to as PipCit (code name PNB-01).[12][19]
See also
References
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