Droperidol uses, brand name injection and its dose

Description of Droperidol and its uses

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.

Mechanism of Action of Droperidol

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.

Pharmacokinetics of Droperidol

Droperidol is administered via the intramuscular or intravenous route. The extent of distribution has not been determined, but droperidol crosses the blood-brain barrier, appears in the CSF, and readily crosses the placenta. Droperidol is metabolized in the liver to 4-fluorophenylacetic acid, which conjugates with glycine. The other metabolites are benzimidazolone and 4-hydroxypiperidine. The drug and its metabolites are excreted in urine and feces, and about 10% of administered droperidol is excreted unchanged in the urine.

Route-Specific Pharmacokinetics Intravenous Route
The effects are seen within 3—10 minutes of an intravenous droperidol injection, but peak response may not occur for up to 30 minutes. The sedative and tranquilizing effects of a single dose usually last for 2—4 hours, while alteration of consciousness can persist for up to 12 hours.

Intramuscular Route

Following intramuscular administration of droperidol, effects are seen within 3—10 minutes with peak response occurring up to 30 minutes after injection. The sedative and tranquilizing effects of a single dose usually last for 2—4 hours, while alteration of consciousness can persist for up to 12 hours.

Brand names of Drug

Generic Name- Droperidol

Brand Names –Inapsine

• Antiemetic
• Butyrophenone
• Dopamine Antagonist

• Nausea and vomiting, Associated with surgical or diagnostic procedures; Prophylaxis: Adult
• Nausea and vomiting, Associated with surgical or diagnostic procedures; Prophylaxis: Pediatric: yes (2 years or older)

• Cardiovascular: Hypotension, Tachycardia
• Neurologic: Somnolence, Postoperative
• Psychiatric: Anxiety, Dysphoric mood, Hyperactive behavior, Restlessness

• Cardiovascular: Cardiac arrest, Prolonged QT interval, Torsades de pointes, Ventricular tachycardia
• Immunologic: Anaphylaxis
• Neurologic: Neuroleptic malignant syndrome (very rare )

• Intravenous: Administer slowly

• Intravenous Solution: 0.625 MG/1 ML
• Injection Solution: 2.5 MG/1 ML

• Agitation – Psychotic disorder: 5 mg IM as a single dose (off-label dosage)
• Agitation – Psychotic disorder: 5 or 10 mg IV as a single dose (off-label dosage)
• General anesthesia; Adjunct: 5 mg IV prior to meperidine and diazepam (off-label dosage)
• Headache, Benign: 5 mg IM (off-label dosage)
• Headache, Benign: 2.5 mg IV (off-label dosage)
• Migraine: 2.5 mg IM (off-label dosage)
• Nausea and vomiting, Associated with surgical or diagnostic procedures; Prophylaxis: Maximum initial dose, 2.5 mg IM or slow IV; additional 1.25 mg-doses may be administered with caution and if potential benefit outweighs potential risk (FDA dosage)
• Nausea and vomiting, Associated with surgical or diagnostic procedures; Prophylaxis: 0.625 to 1.25 mg IV 5 minutes before termination of anesthesia (guideline dosage)

• General anesthesia; Adjunct: 0.15 mg/kg orally given with trimeprazine and methadone 2.5 hours prior to surgery (off-label dosage)
• Nausea and vomiting, Associated with surgical or diagnostic procedures; Prophylaxis: (2 to 12 years) Maximum initial dose, 0.1 mg/kg IM or slow IV; additional doses should be administered with caution and if potential benefit outweighs potential risk (FDA dosage)
• Nausea and vomiting, Associated with surgical or diagnostic procedures; Prophylaxis: (Greater than 2 years) 0.015 to 0.075 mg/kg/dose IV (guideline dosage)