Drug intelligence / Profile preview

droperidol

Development stage
Approved
Lead developer
Janssen Pharmaceutica
Modality
Small Molecules
Administration
Intravenous, Intramuscular
01

Overview

Droperidol is a butyrophenone derivative and potent dopamine D2 receptor antagonist used primarily as an antiemetic to prevent and treat postoperative nausea and vomiting, as well as for sedation in cases of severe agitation or psychosis. It produces marked tranquilization, sedation, and mental detachment while maintaining reflex alertness. Droperidol also exhibits mild alpha-adrenergic blockade, leading to peripheral vascular dilation and potential hypotension. Its mechanism of action is mainly through antagonism of dopamine D2 receptors in the central nervous system, with additional minor antagonistic effects on alpha-1 adrenergic receptors; it may also have weak anticholinergic activity[1][5][6][8]. Discovered by Janssen Pharmaceutica in 1961, droperidol has been widely used for its antiemetic properties during surgical procedures[5]. The drug was reintroduced to the US market by American Regent after a period of limited availability due to safety concerns regarding QT prolongation at higher doses[6].

Brand names
Inapsine
Other names
droperidoldehidrobenzperidoldehydrobenzperidol
02

Targets

CHRM5 (M5)HRH1 (Histamine H1 Receptor)ADRA1A (α1A)HTR2A (Serotonin receptor 5-HT2A)DRD2 (Dopamine D2 Receptor)KCNH2 (Voltage-gated potassium channel subfamily H member 2)HTR1A (Serotonin receptor 1A (5-hydroxytryptamine receptor 1A))

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