DROPERIDOL

Clinical safety rating: safe

Animal studies have demonstrated safety

How it works

Droperidol is a butyrophenone antipsychotic that acts primarily as a dopamine D2 receptor antagonist. It also exhibits antiemetic effects via blockade of dopamine D2 receptors in the chemoreceptor trigger zone. Additionally, it has alpha-adrenergic blocking properties and can prolong the QT interval by blocking cardiac potassium channels (hERG).

What the body does with it

Metabolism	Primarily metabolized by CYP3A4 and to a lesser extent by CYP2D6; also undergoes N-dealkylation and hydroxylation. Metabolites include p-fluorobenzoylpropionic acid and droperidol N-oxide.
Excretion	Renal (75% as metabolites, <1% unchanged); fecal (22%); biliary excretion contributes to enterohepatic circulation.
Half-life	Terminal elimination half-life: 2.3 hours (range 1.5–4.7 hours). Clinical context: Short half-life allows rapid titration but requires repeated dosing or continuous infusion for sustained effect; accumulation with hepatic impairment.
Protein binding	~90% bound to albumin and α1-acid glycoprotein.
Volume of Distribution	2–3 L/kg (mean 2.5 L/kg). Clinical meaning: Extensive tissue distribution, with high affinity for CNS and peripheral tissues.
Bioavailability	IM: 60–80% (due to first-pass metabolism); oral: approximately 60% (significant first-pass effect; oral use not common in clinical practice).
Onset of Action	IV: 3–10 minutes; IM: 10–30 minutes. Peak effect: IV within 10 minutes; IM within 30–60 minutes.
Duration of Action	Duration: 2–4 hours for sedative and antipsychotic effects; antiemetic effect may persist up to 6–12 hours. Clinical notes: Prolonged duration in elderly, hepatic impairment, or with higher doses.

Classification & Brands

Dosing & administration

2.5-10 mg IV/IM every 3-4 hours as needed for nausea and vomiting; for agitation or psychosis in perioperative settings: 0.625-1.25 mg IV/IM, may repeat every 6 hours.

Dosage form	INJECTABLE
Renal impairment	No dose adjustment required for renal impairment per FDA labeling; use caution in severe renal disease due to potential accumulation of metabolite.
Liver impairment	Child-Pugh A: no adjustment; Child-Pugh B: use 50% of normal dose; Child-Pugh C: avoid use due to risk of QT prolongation and hepatic metabolism.
Pediatric use	For postoperative nausea/vomiting: 0.05-0.06 mg/kg IV/IM (maximum 1 mg) for children >2 years; for agitation: 0.01-0.03 mg/kg IV/IM every 4-6 hours as needed (max 2.5 mg).
Geriatric use	Start at 50% of adult dose (e.g., 0.625-1.25 mg IV/IM); titrate slowly due to increased sensitivity to QT prolongation, extrapyramidal symptoms, and hypotension.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Other QT-prolonging agents increase risk of torsades de pointes Can cause QT prolongation and severe hypotension.

Breastfeeding	Limited data; excreted into breast milk, M/P ratio unknown. Use with caution, monitor infant for sedation and extrapyramidal effects.
Teratogenic Risk	FDA Pregnancy Category C. First trimester: Limited human data; animal studies show embryotoxicity but not teratogenicity at high doses. Second and third trimesters: Avoid near term due to risk of neonatal extrapyramidal symptoms, sedation, and respiratory depression.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

WARNING: QT PROLONGATION AND TORSADES DE POINTES. Droperidol can cause QT interval prolongation and torsades de pointes, which can be fatal. Use is contraindicated in patients with known QT prolongation or concurrent use of QT-prolonging drugs. ECG monitoring is recommended before and during administration.

Side Effect Profile

Common Effects	sedation
Serious Effects

Absolute Contraindications

["Known hypersensitivity to droperidol or any component","Prolonged QT interval (QTc >450 ms in males or >470 ms in females)","Concurrent use of other QT-prolonging drugs","Hypokalemia, hypomagnesemia, or other electrolyte disturbances","Bradycardia (<50 bpm) or untreated severe cardiac disease","Parkinson's disease (relative contraindication due to dopamine blockade)"]

Clinical Precautions

Precautions

["Risk of QT prolongation and torsades de pointes; monitor ECG and electrolytes","Extrapyramidal symptoms (dystonia, akathisia, parkinsonism)","Neuroleptic malignant syndrome (NMS)","Hypotension and tachycardia","Central nervous system depression and respiratory depression when combined with opioids","Increased risk of falls in elderly patients","Potential for paradoxical excitement or agitation"]

Drug interactions

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DROPERIDOL

Clinical safety rating: safe

Animal studies have demonstrated safety

How it works

What the body does with it

Metabolism	Primarily metabolized by CYP3A4 and to a lesser extent by CYP2D6; also undergoes N-dealkylation and hydroxylation. Metabolites include p-fluorobenzoylpropionic acid and droperidol N-oxide.
Excretion	Renal (75% as metabolites, <1% unchanged); fecal (22%); biliary excretion contributes to enterohepatic circulation.
Half-life	Terminal elimination half-life: 2.3 hours (range 1.5–4.7 hours). Clinical context: Short half-life allows rapid titration but requires repeated dosing or continuous infusion for sustained effect; accumulation with hepatic impairment.
Protein binding	~90% bound to albumin and α1-acid glycoprotein.
Volume of Distribution	2–3 L/kg (mean 2.5 L/kg). Clinical meaning: Extensive tissue distribution, with high affinity for CNS and peripheral tissues.
Bioavailability	IM: 60–80% (due to first-pass metabolism); oral: approximately 60% (significant first-pass effect; oral use not common in clinical practice).
Onset of Action	IV: 3–10 minutes; IM: 10–30 minutes. Peak effect: IV within 10 minutes; IM within 30–60 minutes.
Duration of Action	Duration: 2–4 hours for sedative and antipsychotic effects; antiemetic effect may persist up to 6–12 hours. Clinical notes: Prolonged duration in elderly, hepatic impairment, or with higher doses.

Classification & Brands

Dosing & administration

2.5-10 mg IV/IM every 3-4 hours as needed for nausea and vomiting; for agitation or psychosis in perioperative settings: 0.625-1.25 mg IV/IM, may repeat every 6 hours.

Dosage form	INJECTABLE
Renal impairment	No dose adjustment required for renal impairment per FDA labeling; use caution in severe renal disease due to potential accumulation of metabolite.
Liver impairment	Child-Pugh A: no adjustment; Child-Pugh B: use 50% of normal dose; Child-Pugh C: avoid use due to risk of QT prolongation and hepatic metabolism.
Pediatric use	For postoperative nausea/vomiting: 0.05-0.06 mg/kg IV/IM (maximum 1 mg) for children >2 years; for agitation: 0.01-0.03 mg/kg IV/IM every 4-6 hours as needed (max 2.5 mg).
Geriatric use	Start at 50% of adult dose (e.g., 0.625-1.25 mg IV/IM); titrate slowly due to increased sensitivity to QT prolongation, extrapyramidal symptoms, and hypotension.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Other QT-prolonging agents increase risk of torsades de pointes Can cause QT prolongation and severe hypotension.

Breastfeeding	Limited data; excreted into breast milk, M/P ratio unknown. Use with caution, monitor infant for sedation and extrapyramidal effects.
Teratogenic Risk	FDA Pregnancy Category C. First trimester: Limited human data; animal studies show embryotoxicity but not teratogenicity at high doses. Second and third trimesters: Avoid near term due to risk of neonatal extrapyramidal symptoms, sedation, and respiratory depression.
Fetal Monitoring

Warnings & precautions

■ FDA Black Box Warning

Side Effect Profile

Common Effects	sedation
Serious Effects

DROPERIDOL

How it works

What the body does with it

Classification & Brands

Dosing & administration

Use during pregnancy

Warnings & precautions

Side Effect Profile

Absolute Contraindications

Clinical Precautions

Drug interactions

DROPERIDOL

How it works

What the body does with it

Classification & Brands

Dosing & administration

Use during pregnancy

Warnings & precautions

Side Effect Profile

Absolute Contraindications

Clinical Precautions

Drug interactions

Clinical Tips & Counseling