Mechanism of Action of Droperidol

Primary Mechanisms

• Droperidol acts as a potent dopamine D2 receptor antagonist in the central nervous system, occupying GABA receptors on postsynaptic membranes and producing mild alpha-adrenergic blockade peripherally, contributing to its antiemetic, sedative, and antipsychotic effects 1
• The American Gastroenterological Association notes that droperidol blocks postsynaptic dopaminergic D2 receptors in the brain, which is the primary mechanism responsible for its antiemetic, sedative, and antipsychotic effects 1

Clinical Pharmacokinetics

• The onset of action of droperidol occurs within 3-10 minutes following intravenous or intramuscular administration, with a duration of tranquilizing and sedative effects typically lasting 2-4 hours 1