Droperidol – Uses, Side Effects, Contraindications, Drug Interactions, Mechanism of Action

Droperidol Brand Name– Inapsine

What is Droperidol

Droperidol is a butyrophenone derivative structurally similar to haloperidol. Droperidol has more potent antiemetic properties, while haloperidol is the more potent antipsychotic.

Droperidol carries an approved indication for reducing the incidence of nausea and vomiting associated with surgical and diagnostic procedures.

Due to the serious risk of proarrhythmic events, the use of droperidol is not recommended for any indication other than for the treatment of perioperative nausea and vomiting in patients for whom other treatments are ineffective or inappropriate.

Nevertheless, it has also been used for nausea and vomiting induced by anesthetics or emetogenic antineoplastic medications such as cisplatin.

Along with other off-label uses, droperidol has also been used as an inducing agent and as an adjuvant to general anesthesia.

Droperidol received FDA approval in June 1970. In December 2001, the FDA changed the labeling of droperidol to include a black box warning describing the risk of QT prolongation and torsade de pointes.

Indications and Uses of Droperidol

  1. anxiety
  2. general anesthesia induction
  3. general anesthesia maintenance
  4. migraine
  5. nausea/vomiting prophylaxis
  6. post-operative nausea/vomiting (PONV)
  7. post-operative nausea/vomiting (PONV) prophylaxis
  8. preanesthesia
  9. sedation induction

NOTE: Due to a risk of QT prolongation and torsade de pointes, the approved indication of droperidol is limited to the prevention of surgical nausea and vomiting. Usage outside of the labeled indication is not recommended

Mechanism of Action

Droperidol is a butyrophenone neuroleptic. Similar to haloperidol, droperidol antagonizes multiple receptor sites in the CNS including serotonin, GABA, norepinephrine, and especially, dopamine.

There is evidence that butyrophenones antagonize dopamine-mediated neurotransmission at the synapse as well as block postsynaptic dopamine receptor sites. The antiemetic activity of droperidol is most likely due to blockade of dopamine receptors in the chemoreceptor trigger zone of the brain.

In addition, droperidol has peripheral alpha-adrenergic antagonistic activity leading to vasodilation and reduction of the pressor effect of epinephrine.

It can produce hypotension, decreased peripheral vascular resistance, and may decrease pulmonary arterial pressure, particularly if it is abnormally high.

Droperidol may reduce the incidence of epinephrine-induced arrhythmias, but it has been associated with prolongation of the QTc interval and serious arrhythmias including torsade de pointes.

Droperidol delays the recharging of potassium channels, thereby blocking the rapid component of the delayed rectifier potassium current, within minutes of a dose at the upper limit of the dosage range.

Side Effects of Droperidol

  1. akathisia
  2. anaphylactoid reactions
  3. anxiety
  4. bronchospasm
  5. cardiac arrest
  6. chills
  7. depression
  8. dizziness
  9. drowsiness
  10. dysphoria
  11. dystonic reaction
  12. hallucinations
  13. hyperactivity
  14. hypertension
  15. hypotension
  16. laryngospasm
  17. neuroleptic malignant syndrome
  18. QT prolongation
  19. restlessness
  20. shivering
  21. sinus tachycardia
  22. torsade de pointes
  23. ventricular tachycardia

Monitoring Parameters

  • ECG
  • serum magnesium
  • serum potassium

Contraindications

  • apheresis
  • AV block
  • bradycardia
  • breast-feeding
  • cardiomyopathy
  • celiac disease
  • children
  • epidural anesthesia
  • females
  • fever
  • geriatric
  • heart failure
  • hepatic disease
  • human immunodeficiency virus (HIV) infection
  • hyperparathyroidism
  • hypocalcemia
  • hypokalemia
  • hypomagnesemia
  • hypotension
  • hypothermia
  • hypothyroidism
  • infants
  • labor
  • long QT syndrome
  • MAOI therapy
  • myocardial infarction
  • neonates
  • obstetric delivery
  • orthostatic hypotension
  • Parkinson’s disease
  • phenothiazine hypersensitivity
  • pheochromocytoma
  • pregnancy
  • QT prolongation
  • renal failure
  • renal impairment
  • rheumatoid arthritis
  • seizure disorder
  • seizures
  • sickle cell disease
  • sleep deprivation
  • spinal anesthesia
  • stroke
  • systemic lupus erythematosus (SLE)
  • torsade de pointes

Interactions

  • Abarelix
  • Acetaminophen; Butalbital
  • Acetaminophen; Butalbital; Caffeine
  • Acetaminophen; Butalbital; Caffeine; Codeine
  • Acetaminophen; Caffeine; Dihydrocodeine
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  • Acetaminophen; Chlorpheniramine; Dextromethorphan; Pseudoephedrine
  • Acetaminophen; Chlorpheniramine; Phenylephrine; Phenyltoloxamine
  • Acetaminophen; Codeine
  • Acetaminophen; Dextromethorphan; Doxylamine
  • Acetaminophen; Dichloralphenazone; Isometheptene
  • Acetaminophen; Diphenhydramine
  • Acetaminophen; Hydrocodone
  • Acetaminophen; Oxycodone
  • Acetaminophen; Tramadol
  • Acetazolamide
  • Aldesleukin, IL-2
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  • Alfuzosin
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  • Amitriptyline; Chlordiazepoxide
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  • Amphotericin B
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  • Asenapine
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  • Aspirin, ASA; Butalbital; Caffeine; Codeine
  • Aspirin, ASA; Caffeine; Dihydrocodeine
  • Aspirin, ASA; Caffeine; Orphenadrine
  • Aspirin, ASA; Carisoprodol
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  • Aspirin, ASA; Oxycodone
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