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Pronunciation |
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(droe
PER i
dole) |
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U.S. Brand
Names |
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Inapsine® |
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Generic
Available |
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Yes |
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Pharmacological Index |
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Antiemetic |
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Use |
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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 |
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Pregnancy Risk
Factor |
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C |
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Pregnancy/Breast-Feeding
Implications |
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Clinical effects on the fetus: Crosses the placenta
Breast-feeding/lactation: No data available |
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Contraindications |
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Hypersensitivity to droperidol or any component |
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Warnings/Precautions |
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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 |
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Adverse
Reactions |
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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 |
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Overdosage/Toxicology |
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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. |
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Drug
Interactions |
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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 |
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Stability |
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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 |
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Mechanism of
Action |
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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 |
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Pharmacodynamics/Kinetics |
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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%) |
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Usual Dosage |
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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
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Monitoring
Parameters |
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Blood pressure, heart rate, respiratory rate; observe for dystonias,
extrapyramidal side effects, and temperature changes |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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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. |
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Dental Health:
Effects on Dental Treatment |
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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
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Patient
Information |
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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. |
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Nursing
Implications |
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Parenteral: I.V. over 2-5 minutes
Monitor blood pressure, heart rate, respiratory rate |
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Dosage Forms |
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Injection: 2.5 mg/mL (1 mL, 2 mL, 5 mL, 10 mL) |
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References |
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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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