Pipamperon

ATC CodeN05AD05
CAS number1893-33-0
PUB number4830
Drugbank IDDB09286
Empirical formulaC21H30FN3O2
Molar mass (g·mol−1)375,48
Physical statesolid
Melting point (°C)124,5–126

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, BSc

Markus Falkenstätter, BSc

Mag. pharm. Stefanie Lehenauer

Mag. pharm. Stefanie Lehenauer



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