Pipamperone

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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[1][2] and as a sleep aid for depression.[3] It is or has been marketed under brand names including Dipiperon, Dipiperal, Piperonil, Piperonyl, and Propitan.[2] Pipamperone was discovered at Janssen Pharmaceutica in 1961, and entered clinical trials in the United States in 1963.[4]

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.[5]

Pharmacology

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Pipamperon Neuraxpharm, 40mg

Pipamperone acts as an antagonist of the 5-HT2A,[6] 5-HT2B,[7] 5-HT2C[8] D2,[6] D3,[9] D4,[6][10] α1-adrenergic,[9] and α2-adrenergic receptors.[9] 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),[6][9][11] being regarded as "highly selective" for the former two sites at low doses.[11][12] Pipamperone has low and likely insignificant affinity for the H1 and mACh receptors, as well as for other serotonin and dopamine receptors.[9]

Pipamperone is considered to have been a forerunner to the atypical antipsychotics, if not an atypical antipsychotic itself, due to its prominent serotonin antagonism.[13][14][15] It is also used to normalise mood and sleep patterns and has antianxiety effects in neurotic patients.[16]

Affinity[17]
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D1 5.61
D2 6.71
D3 6.58
D4 7.95
5 HT1A 5.46
5 HT1B 5.54
5 HT1D 6.14
5 HT1E 5.44
5 HT1F <5
5-HT2A 8.19
5 HT5 5.35
5 HT7 6.26
α1 7.23
α2A 6.15
α2B 7.08
α2C 6.25

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).[11][18]

See also

References

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  17. ↑ Bart A. Ellenbroek, Alexander R. Cools (eds.) (6 December 2012). Atypical Antipsychotics. Basel: Birkhäuser, pp. 62 f. Template:ISBN.
  18. ↑ Script error: No such module "Citation/CS1".

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