Pipamperon

Pipamperon
ATC Code N05AD05
Formula C21H30FN3O2
Molar Mass (g·mol−1) 375,48
Physical State solid
Melting Point (°C) 124,5–126
CAS Number 1893-33-0
PUB Number 4830
Drugbank ID DB09286
Solubility soluble in methanol

Basics

Pipamperone is a typical antipsychotic of the butyrophenone family and is used to treat schizophrenia and as a sleep aid for depression.

Pharmacology

Pharmacodynamics

Pipamperone binds primarily to 5-HT2A receptors, with nearly equal affinity to D4 receptors and moderate affinity to 5-HT2C, D2-3, and alpha-adrenoceptors. Pipamperone has a 15-fold higher affinity for D4 than for D2 receptors. Binding to the above receptors results in the antipsychotic and antidepressant effects.

Pharmacokinetics

Pipamperone is taken orally and metabolized in the liver. Excretion is mainly by the kidneys. The half-life is about 16-27 hours.

Toxicity

Side effects

  • Dyskinesia
  • Loss of appetite
  • Nausea
  • Vomiting
  • Hyperprolactinemia
  • Menstrual irregularities
  • Increased pulse
  • QT prolongation (ECG)
  • Depression
  • Fatigue
  • Drowsiness
  • Insomnia
  • Headache

Toxicological data

LD50 (rat, oral): 160 mg-kg-1

Sources

  • Drugbank
  • PubChem
  • Aktories, Förstermann, Hofmann, Starke: Allgemeine und spezielle Pharmakologie und Toxikologie, Elsvier, 2017
Markus Falkenstätter

Markus Falkenstätter
Author

Markus Falkenstätter ist Autor zu pharmazeutischen Themen in der Medizin-Redaktion von Medikamio. Er befindet sich im letzten Semester seines Pharmaziestudiums an der Universität Wien und liebt das wissenschaftliche Arbeiten im Bereich der Naturwissenschaften.

Mag. pharm Stefanie Lehenauer

Mag. pharm Stefanie Lehenauer
Lector

Stefanie Lehenauer ist seit 2020 freie Autorin bei Medikamio und studierte Pharmazie an der Universität Wien. Sie arbeitet als Apothekerin in Wien und ihre Leidenschaft sind pflanzliche Arzneimittel und deren Wirkung.

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