Pipamperone Explained

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. Pipamperone was discovered at Janssen Pharmaceutica in 1961, and entered clinical trials in the United States in 1963.[4]

Pharmacology

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

Pipamperone is considered to have been a forerunner to the atypical antipsychotics, if not an atypical antipsychotic itself, due to its prominent serotonin antagonism.[12] [13] [14] It is also used to normalise mood and sleep patterns and has antianxiety effects in neurotic patients.[15]

Affinity[16]
Site pKi
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).[17]

See also

Notes and References

  1. Book: Morton IK, Hall JM . Concise Dictionary of Pharmacological Agents: Properties and Synonyms. 31 October 1999. Springer Science & Business Media. 978-0-7514-0499-9. 222–.
  2. Book: Elks J . The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. 14 November 2014. Springer. 978-1-4757-2085-3. 985–.
  3. Ansoms C, Backer-Dierick GD, Vereecken JL . Sleep disorders in patients with severe mental depression: double-blind placebo-controlled evaluation of the value of pipamperone (Dipiperon) . Acta Psychiatrica Scandinavica . 55 . 2 . 116–122 . February 1977 . 320830 . 10.1111/j.1600-0447.1977.tb00147.x . 40758854 .
  4. Book: Healy D . The Creation of Psychopharmacology. 1 July 2009. Harvard University Press. 978-0-674-03845-5. 251–.
  5. Schotte A, Janssen PF, Gommeren W, Luyten WH, Van Gompel P, Lesage AS, De Loore K, Leysen JE . 6 . Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding . Psychopharmacology . 124 . 1–2 . 57–73 . March 1996 . 8935801 . 10.1007/bf02245606 . 12028979 .
  6. Wainscott DB, Lucaites VL, Kursar JD, Baez M, Nelson DL . Pharmacologic characterization of the human 5-hydroxytryptamine2B receptor: evidence for species differences . The Journal of Pharmacology and Experimental Therapeutics . 276 . 2 . 720–727 . February 1996 . 8632342 .
  7. Prinssen EP, Koek W, Kleven MS . The effects of antipsychotics with 5-HT(2C) receptor affinity in behavioral assays selective for 5-HT(2C) receptor antagonist properties of compounds . European Journal of Pharmacology . 388 . 1 . 57–67 . January 2000 . 10657547 . 10.1016/s0014-2999(99)00859-6 .
  8. Book: Leyson JE . Receptor profile of antipsychotics . Ellenbroek BA, Cools AR . Atypical Antipsychotics. https://books.google.com/books?id=08kGCAAAQBAJ&pg=PA62 . 6 December 2012. Birkhäuser. 978-3-0348-8448-8. 62–.
  9. Van Craenenbroeck K, Gellynck E, Lintermans B, Leysen JE, Van Tol HH, Haegeman G, Vanhoenacker P . Influence of the antipsychotic drug pipamperone on the expression of the dopamine D4 receptor . Life Sciences . 80 . 1 . 74–81 . December 2006 . 16978659 . 10.1016/j.lfs.2006.08.024 .
  10. Wade AG, Crawford GM, Nemeroff CB, Schatzberg AF, Schlaepfer T, McConnachie A, Haazen L, Buntinx E . 6 . Citalopram plus low-dose pipamperone versus citalopram plus placebo in patients with major depressive disorder: an 8-week, double-blind, randomized study on magnitude and timing of clinical response . Psychological Medicine . 41 . 10 . 2089–2097 . October 2011 . 21349239 . 10.1017/S0033291711000158 . 19189492 .
  11. Book: Abi-Dargham A, Krystal J . Serotonin Receptors as Targets of Antipsychotic Medications . Lidow MS . Neurotransmitter Receptors in Actions of Antipsychotic Medications. https://books.google.com/books?id=HIHLBQAAQBAJ&pg=PA88. 22 June 2000. CRC Press. 978-1-4200-4177-4. 88–.
  12. Awouters FH, Lewi PJ . Forty years of antipsychotic Drug research--from haloperidol to paliperidone--with Dr. Paul Janssen . Arzneimittel-Forschung . 57 . 10 . 625–632 . 2007 . 18074755 . 10.1055/s-0031-1296660 . 5713281 .
  13. Vanden Bussche G, Gelders YG, Heylen SL . [Development of new antipsychotic drugs] . es . Acta Psiquiatrica y Psicologica de America Latina . 36 . 1–2 . 13–25 . 1990 . 2127339 .
  14. Niemegeers CJ, Awouters F, Janssen PA . [Serotonin antagonism involved in the antipsychotic effect. Confirmation with ritanserine and risperidone] . fr . L'Encéphale . 16 . 2 . 147–151 . 1990 . 1693560 .
  15. Book: Psychotropic Agents: Part I: Antipsychotics and Antidepressants. 2012-12-06. Springer Science & Business Media. 9783642675386. en.
  16. Bart A. Ellenbroek, Alexander R. Cools (eds.) (6 December 2012). Atypical Antipsychotics. Basel: Birkhäuser, pp. 62 f. .
  17. Kirk R . Clinical trials in CNS--SMi's eighth annual conference . IDrugs . 13 . 2 . 66–69 . February 2010 . 20127552 .

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