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Droperidol
Pronunciation
U.S. Brand Names
Generic Available
Pharmacological Index
Use
Pregnancy Risk Factor
Pregnancy/Breast-Feeding Implications
Contraindications
Warnings/Precautions
Adverse Reactions
Overdosage/Toxicology
Drug Interactions
Stability
Mechanism of Action
Pharmacodynamics/Kinetics
Usual Dosage
Monitoring Parameters
Dental Health: Local Anesthetic/Vasoconstrictor Precautions
Dental Health: Effects on Dental Treatment
Patient Information
Nursing Implications
Dosage Forms
References

Pronunciation
(droe PER i dole)

U.S. Brand Names
Inapsine®

Generic Available

Yes


Pharmacological Index

Antiemetic


Use

Tranquilizer and antiemetic in surgical and diagnostic procedures; preoperative medication; induction and adjunct in the maintenance of general and regional anesthesia; neuroleptanalgesia, in which droperidol is given concurrently with a narcotic analgesic (fentanyl) to aid in producing tranquility and decreasing anxiety and pain


Pregnancy Risk Factor

C


Pregnancy/Breast-Feeding Implications

Clinical effects on the fetus: Crosses the placenta

Breast-feeding/lactation: No data available


Contraindications

Hypersensitivity to droperidol or any component


Warnings/Precautions

Safety in children <6 months of age has not been established; use with caution in patients with seizures, bone marrow suppression, or severe liver disease

Tardive dyskinesia (TD): TD is a chronic, potentially irreversible abnormal movement disorder associated with long-term use of antipsychotic medication. Movements may be choreiform, tonic, or athetotic and most commonly involve the face and mouth. Those at greater risk for developing TD are on prolonged antipsychotic therapy, older than 50 years of age, and with diabetes or primary affective disorder. TD prevalence estimates for neuroleptic-treated patients range from 10% to 15% in young patients, 12% to 25% in chronic patients, and 25% to 45% of state hospital patients.

Extrapyramidal syndromes: Extrapyramidal reactions are more common in elderly.

Acute dystonias are uncomfortable, involuntary muscle spasms of the face, neck, trunk, or extremities associated with antipsychotic treatment. Dystonias occur in 10% to 15% of patients on conventional antipsychotic medications, usually in the first several weeks of treatment.

Akathisia is a subjective feeling of restlessness seen in 10% to 40% of patients on typical antipsychotic medications. Patients may appear agitated, with frequent pacing and inability to keep their legs still.

Antipsychotic medication-associated parkinsonism is characterized by rigidity, bradykinesia, masked facies, drooling, and tremor. While not strictly an emergency the disabling symptoms occur subacutely within the first month of therapy on 10% to 15% of patients on typical antipsychotics.

Increased confusion, memory loss, psychotic behavior, and agitation frequently occur as a consequence of anticholinergic effects

Orthostatic hypotension is due to alpha-receptor blockade, the elderly are at greater risk for orthostatic hypotension

Antipsychotic associated sedation in nonpsychotic patients is extremely unpleasant due to feelings of depersonalization, derealization, and dysphoria

Life-threatening arrhythmias have occurred at therapeutic doses of antipsychotics


Adverse Reactions

Cardiovascular: Mild to moderate hypotension, tachycardia, hypertension, dizziness, chills, postoperative hallucinations

Central nervous system: Postoperative drowsiness, extrapyramidal reactions, shivering

Respiratory: Respiratory depression, apnea, muscular rigidity, laryngospasm, bronchospasm


Overdosage/Toxicology

Symptoms of overdose include hypotension, tachycardia, hallucinations, extrapyramidal symptoms

Following initiation of essential overdose management, toxic symptom treatment and supportive treatment should be initiated. Hypotension usually responds to I.V. fluids or Trendelenburg positioning. If unresponsive to these measures, the use of a parenteral inotrope may be required (eg, norepinephrine 0.1-0.2 mcg/kg/minute titrated to response). Seizures commonly respond to diazepam (I.V. 5-10 mg bolus in adults every 15 minutes if needed up to a total of 30 mg; I.V. 0.25-0.4 mg/kg/dose up to a total of 10 mg in children) or to phenytoin or phenobarbital. Critical cardiac arrhythmias often respond to I.V. phenytoin (15 mg/kg up to 1 g), while other antiarrhythmics can be used. Neuroleptics often cause extrapyramidal symptoms (eg, dystonic reactions) requiring management with diphenhydramine 1-2 mg/kg (adults) up to a maximum of 50 mg I.M. or I.V. slow push followed by a maintenance dose for 48-72 hours. When these reactions are unresponsive to diphenhydramine, benztropine mesylate I.V. 1-2 mg (adults) may be effective. These agents are generally effective within 2-5 minutes.


Drug Interactions

Droperidol in combination with certain forms of conduction anesthesia may produce peripheral vasodilitation and hypotension

Droperidol and CNS depressants will likely have additive CNS effects

Droperidol and cyclobenzaprine may have an additive effect on prolonging the QT interval


Stability

Droperidol ampuls/vials should be stored at room temperature and protected from light

Stability of parenteral admixture at room temperature (25°C): 7 days

Standard diluent: 2.5 mg/50 mL D5W

Incompatible with barbiturates


Mechanism of Action

Butyrophenone derivative that produces tranquilization, sedation, and an antiemetic effect; other effects include alpha-adrenergic blockade, peripheral vascular dilation, and reduction of the pressor effect of epinephrine resulting in hypotension and decreased peripheral vascular resistance; may also reduce pulmonary artery pressure


Pharmacodynamics/Kinetics

Following parenteral administration:

Peak effect: Within 30 minutes

Duration: 2-4 hours, may extend to 12 hours

Metabolism: In the liver

Half-life: Adults: 2.3 hours

Elimination: In urine (75%) and feces (22%)


Usual Dosage

Titrate carefully to desired effect

Premedication: I.M.: 0.1-0.15 mg/kg; smaller doses may be sufficient for control of nausea or vomiting

Adjunct to general anesthesia: I.V. induction: 0.088-0.165 mg/kg

Nausea and vomiting: I.M., I.V.: 0.05-0.06 mg/kg/dose every 4-6 hours as needed

Adults:

Premedication: I.M.: 2.5-10 mg 30 minutes to 1 hour preoperatively

Adjunct to general anesthesia: I.V. induction: 0.22-0.275 mg/kg; maintenance: 1.25-2.5 mg/dose

Alone in diagnostic procedures: I.M.: Initial: 2.5-10 mg 30 minutes to 1 hour before; then 1.25-2.5 mg if needed

Nausea and vomiting: I.M., I.V.: 2.5-5 mg/dose every 3-4 hours as needed

Rapid tranquilization of agitated patient (administered every 30-60 minutes): I.M.: 2.5-5 mg; average total dose for tranquilization: 5-20 mg


Monitoring Parameters

Blood pressure, heart rate, respiratory rate; observe for dystonias, extrapyramidal side effects, and temperature changes


Dental Health: Local Anesthetic/Vasoconstrictor Precautions

Manufacturer's information states that droperidol may block vasopressor activity of epinephrine. This has not been observed during use of epinephrine as a vasoconstrictor in local anesthesia.


Dental Health: Effects on Dental Treatment

Significant hypotension may occur, especially when the drug is administered parenterally; orthostatic hypotension is due to alpha-receptor blockade, the elderly are at greater risk for orthostatic hypotension

Extrapyramidal reactions are more common in elderly with up to 50% developing these reactions after 60 years of age; drug-induced Parkinson's syndrome occurs often; akathisia is the most common extrapyramidal reaction in elderly

Increased confusion, memory loss, psychotic behavior, and agitation frequently occur as a consequence of anticholinergic effects

Antipsychotic associated sedation in nonpsychotic patients is extremely unpleasant due to feelings of depersonalization, derealization, and dysphoria


Patient Information

This drug may cause you to feel very sleepy; do not attempt to get up without assistance. Immediately report any difficulty breathing, confusion, loss of thought processes, or palpitations. Pregnancy/breast-feeding precautions: Inform prescriber if you are pregnant. Consult prescriber if breast-feeding.


Nursing Implications

Parenteral: I.V. over 2-5 minutes

Monitor blood pressure, heart rate, respiratory rate


Dosage Forms

Injection: 2.5 mg/mL (1 mL, 2 mL, 5 mL, 10 mL)


References

Cersosimo RJ, Bromer R, Hoffer S, et al, "The Antiemetic Activity of Droperidol Administered by Intramuscular Injection During Cisplatin Chemotherapy: A Pilot Study," Drug Intell Clin Pharm, 1985, 19(2):118-21.

Ghoneim MM and Korttila K, "Pharmacokinetics of Intravenous Anaesthetics: Implications for Clinical Use," Clin Pharmacokinet, 1977, 2(5):344-72.

Grunberg SM and Hesketh PJ, "Control of Chemotherapy-Induced Emesis," N Engl J Med, 1993, 329(24):1790-6.

Peabody CA, Warner MD, Whiteford HA, et al, "Neuroleptics and the Elderly," J Am Geriatr Soc, 1987, 35(3):233-8.

Risse SC and Barnes R, "Pharmacologic Treatment of Agitation Associated With Dementia," J Am Geriatr Soc, 1986, 34(5):368-76.

Saltz BL, Woerner MG, Kane JM, et al, "Prospective Study of Tardive Dyskinesia Incidence in the Elderly," JAMA, 1991, 266(17):2402-6.

Seifert RD, "Therapeutic Drug Monitoring: Psychotropic Drugs," J Pharm Pract, 1984, 6:403-16.

Sridhar KS and Donnelly E, "Combination Antiemetics for Cisplatin Chemotherapy," Cancer, 1988, 61(8):1508-17.

Tortorice PV and O'Connell MB, "Management of Chemotherapy-Induced Nausea and Vomiting," Pharmacotherapy, 1990, 10(2):129-45.

Yaster M, Sola JE, Pegoli W Jr, et al, "The Night After Surgery: Postoperative Management of the Pediatric Outpatient - Surgical and Anesthetic Aspects," Pediatr Clin North Am, 1994, 41(1):199-220.


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