Droperidol

Class	Antipsychotic
Chemistry	Butyrphenone
Routes of administration	Oral, IV, IM, s/c
Absorption	Well absorbed; oral bioavailability ~ 75%
Solubility	pKa 7.46, practically insoluble in water
Distribution	VOD=1.5L/kg; 85-90% protein bound
Metabolism	Extensively metabolised by the liver (CYP3A4) into inactive metabolites
Elimination	Clearance is almost completely hepatic; only soome minimal amount is eliminated by the kidneys
Time course of action	Half life of 2 hours, over which span the antiemetic and sedating effects rapidly wear off
Target receptor	D2 dopamine receptor antagonist (Gi-protein coupled), but also has antimuscarinic and anti-adrenergic effects
Mechanism of action	Multiple mechanisms of action: - Sedation is mainly due to the antidomainergic effect - Antipsychotic effect is due to D2 dopamine receptor effect This is also responsible for the tardive dyskinesia - Undesirable side effects are mainly due to the antimuscarinic and antiadrenergic activity - Antiemetic mechanism is likely due to a combination of all of the receptor effects at the chemoreceptor trigger zone
Clinical effects	#NAME?
Literature reference	NZ PI data sheet
CICM details of understanding	Level 3
Mentioned around Deranged Physiology	Classification of antiemetics
Related SAQs	Question 14 from the first paper of 2022 Question 23 from the first paper of 2016 Question 3 from the first paper of 2013 Question 17 from the second paper of 2012 Question 23 from the first paper of 2012 Question 10(p.2) from the first paper of 2010

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