Droperidol

Table of contents

  • Brand Names
  • Drug Combinations
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Toxicological Effects
  • Genes that may be involved
  • Substrate of
  • Drug Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Xomolix; Belgium: Dehydrobenzperidol; Cyprus: Dehydrobenzperidol; Czech Republic: Xomolix; Denmark: Dehydrobenzperidol; Finland: Dehydrobenzperidol; France: Droleptan; Germany: Xomolix; Ireland: Xomolix; Italy: Xomolix; Luxembourg: Dehydrobenzperidol; Netherlands: Dehydrobenzperidol; Poland: Droperidol, Xomolix; Portugal: Dehidrobenzoperidol, Xomolix; Slovakia: Xomolix; Slovenia: Xomolix; Spain: Xomolix; Sweden: Dridol; UK: Xomolix.

North America

Canada: Droperidol; USA: Droperidol, Inapsine.

Latin America

Brazil: Droperdal.

Asia

Japan: Droleptan.

Drug combinations

Droperidol and Fentanyl

Chemistry

Droperidol: C~22~H~22~FN~3~O~2~. Mw: 379.43. (1) 2H-Benzimidazol-2-one, 1-[1-[4-(4-fluorophenyl)-4-oxobutyl]-1,2,3,6-tetrahydro-4-pyridinyl]-1,3-dihydro-; (2) 1-[1-[3-(p-Fluorobenzoyl)propyl]-1,2,3,6-tetrahydro-4-pyridyl]-2-benzimidazolinone. CAS-548-73-2 (1963).

Pharmacologic Category

Anxiolytics, Sedatives, and Hypnotics; Miscellaneous. Antiemetic. Typical Antipsychotic Agent. (ATC-Code: N01AX01; N05AD08).

Mechanism of action

Droperidol, a butyrophenone derivative that is structurally similar to haloperidol, has pharmacologic actions similar to those of haloperidol and phenothiazines. Its antiemetic effect is a result of blockade of dopamine stimulation of the chemoreceptor trigger zone. Other effects include α-adrenergic blockade, peripheral vascular dilation, and reduction of the pressor effect of epinephrine, resulting in hypotension and decreased peripheral vascular resistance. May reduce pulmonary artery pressure. Does not possess analgesic effects. Has few or no amnesic properties.

Therapeutic use

Treatment of perioperative nausea and vomiting. However, use should be reserved only for those patients who have failed to respond adequately to other drugs.

Pregnancy and lactiation implications

Should be used during pregnancy only when potential benefits justify possible risks to fetus. It is not known if droperidol is distributed into milk (use caution during lactation).

Unlabeled use

The drug has been used preoperatively and as an adjunct during induction and maintenance of general anesthesia and as an adjunct to regional anesthesia. Droperidol has been used effectively alone or in combination antiemetic regimens to prevent and/or reduce cancer chemotherapy-induced nausea and vomiting, principally that induced by cisplatin. Antipsychotic agents, principally haloperidol but occasionally droperidol, are used in the management of delirium.

Contraindications

Hypersensitivity to droperidol or any component of the formulation. QT prolongation, congenital long QT syndrome.

Warnings and precautions

May cause anticholinergic effects (use with caution in decreased GI motility, urinary retention, BPH, xerostomia, or visual problems). Esophageal dysmotility/aspiration may occur (use with caution in patients at risk of pneumonia (e.g. Alzheimer’s disease)). May cause extrapyramidal symptoms, including pseudoparkinsonism, acute dystonic reactions, akathisia, and tardive dyskinesia. Risk of dystonia (with increased doses, use of conventional antipsychotics, in males and younger patients). May cause orthostatic hypotension (use with caution in patients at risk of this effect or in those who would not tolerate transient hypotensive episodes (cerebrovascular disease, cardiovascular disease, hypovolemia, or concurrent medication use which may predispose to hypotension/bradycardia)). May be associated with pigmentary retinopathy. May be sedating. Impaired core body temperature regulation may occur (caution with strenuous exercise, heat exposure, dehydration, and concomitant medication possessing anticholinergic effects). Use with caution in narrow-angle glaucoma, myasthenia gravis (these conditions may be exacerbated by cholinergic blockade). Use with caution in breast cancer or other prolactin-dependent tumors (may elevate prolactin levels). Use with caution in patients at risk of seizures, including those with history of seizures, head trauma, brain damage, alcoholism, or concurrent therapy with medications which may lower seizure threshold. May mask toxicity of other drugs or conditions (e.g. intestinal obstruction, Reye’s syndrome, brain tumor) due to antiemetic effects. QT interval prolongation and serious, sometimes fatal arrhythmias (torsades de pointes, ventricular arrhythmias, cardiac arrest) have occurred (use with extreme caution in patients with risk factors for prolonged QT syndrome). Hypotension may occur. May cause CNS depression. Neuroleptic malignant syndrome (altered consciousness, muscular rigidity, autonomic instability) has occurred. Certain forms of conduction anesthesia (e.g. spinal anesthesia, peridural anesthesia) can alter respiration by blocking intercostal nerves and can cause peripheral vasodilation and hypotension. Droperidol may decrease pulmonary arterial pressure and interfere with interpretation of hemodynamic measurements. Use with caution in diagnosed or suspected pheochromocytoma (severe hypertension and tachycardia may occur). Use with caution in the elderly. Use with caution in hepatic or renal impairment.

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