Generic Name: Droperidol
Class: Anxiolytics, Sedatives, and Hypnotics; Miscellaneous
VA Class: CN205
CAS Number: 548-73-2
- QT Interval Prolongation
QT interval prolongation and/or torsades de pointes (including fatalities) have occurred at doses at or below those recommended, in some cases when no known risk factors were present.114
Because of potential for serious proarrhythmic effects and death, use only when response to other treatment is unacceptable (due to lack of efficacy or intolerable adverse effects).114
Prior to administration, obtain 12-lead ECG to exclude the presence of prolonged QT interval (QTc interval >440 msec in males, >450 msec in females).114
Do notadminister droperidol if QT interval is prolonged.114
If potential benefit outweighs risk of serious arrhythmia, monitor for arrhythmia with ECG prior to administration and for 2–3 hours after completion of therapy.114
Contraindicated in patients with known or suspected QT prolongation, including congenital long QT syndrome.114
Use with extreme caution in patients at risk for prolonged QT syndrome (e.g., CHF, bradycardia, diuretic use, cardiac hypertrophy, hypokalemia, hypomagnesemia, use of other drugs known to prolong QT interval).114 Other risk factors may include age >65 years, alcohol abuse, and concomitant use of benzodiazepines, volatile anesthetics, or IV opiates.114 (See Prolonged QT Syndrome under Cautions.)
Initiate droperidol at low dose and increase with caution as needed to achieve desired effect.114
Introduction
Butyrophenone derivative; structurally similar to haloperidol; pharmacologically similar to haloperidol and phenothiazines.a
Uses for Inapsine
Nausea and Vomiting Associated with Surgical and Diagnostic Procedures
Reduction of the incidence of nausea and vomiting associated with surgical and diagnostic procedures.114 a Because of the risk of serious, sometimes fatal proarrhythmic effects, use only in patients who fail to respond adequately (because of insufficient efficacy or intolerable adverse effects) to other antiemetic therapy.114 (See Boxed Warning.)
Adjunct to Anesthesia and Neuroleptanalgesia
Has been used preoperatively† and as an adjunct during induction and maintenance of general anesthesia† and as an adjunct to regional anesthesia†; also has been used in combination with an opiate analgesic (e.g., fentanyl) for neuroleptanalgesia† as an anxiolytic and to potentially increase the opiate analgesic effect.a No longer recommended for these uses because of the risk of serious adverse effects.112 113
Nausea and Vomiting Associated with Cancer Chemotherapy
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.100 101 102 103 104 105 106 107
Delirium
Occasionally used in the management of delirium†;108 has been effective in the management of agitation (not necessarily delirium) and may be preferred to haloperidol in some delirious patients due to shorter half-life, more rapid onset of effect, and increased sedative effects.108 109 110 111
Inapsine Dosage and Administration
General
Routinely monitor vital signs and ECG.114
Administration
For solution and drug compatibility information, see Compatibility under Stability.
Administer IM or by slow IV injection.114 a
Dosage
Individualize dosage according to the patient’s age, weight, physical status, and underlying pathologic condition.114 Also consider other drugs, type of anesthesia used, and surgical procedure.114
Pediatric Patients
Nausea and Vomiting Associated with Surgical and Diagnostic Procedures
IV or IM
Children 2–12 years of age: Initially, up to 0.1 mg/kg (maximum of 2.5 mg), based on the patient’s age and clinical condition.114 116 Administer additional doses with caution and only if potential benefit outweighs potential risk.114
Adults
Nausea and Vomiting Associated with Surgical and Diagnostic Procedures
IV or IM
Initially, up to 2.5 mg.114 Administer additional doses of 1.25 mg with caution to achieve the desired effect, if potential benefit outweighs the potential risk.114
Delirium†
IM
Usually, 5 mg.108 110 111
Prescribing Limits
Pediatric Patients
Nausea and Vomiting Associated with Surgical and Diagnostic Procedures
IV of IM
Children 2–12 years of age: Maximum initial dose of 0.1 mg/kg (up to 2.5 mg) based on age and clinical condition.114 116
Adults
Nausea and Vomiting Associated with Surgical and Diagnostic Procedures
IV or IM
Maximum initial dose: 2.5 mg.114
Special Populations
Geriatric, Debilitated, and High-Risk Patients
Reduce initial dose in geriatric, debilitated, or high-risk patients.114 Carefully adjust subsequent dosage (if needed) according to response and tolerance following the initial dose.114
Cautions for Inapsine
Contraindications
Known or suspected QT interval prolongation (i.e., QTc interval >440 msec in males, >450 msec in females), including congenital long QT syndrome.114
Known hypersensitivity to droperidol or any ingredient in the formulation.114
Warnings/Precautions
Warnings
Prolonged QT Syndrome
QT interval prolongation and serious, sometimes fatal arrhythmias (torsades de pointes, ventricular arrhythmias, cardiac arrest) have occurred.114 (See Boxed Warning.)
ECG monitoring is recommended; do not use if QT interval prolongation is present.114
Use with extreme caution in patients with risk factors for prolonged QT syndrome, including clinically important bradycardia (<50 bpm) or heart disease (e.g., CHF , cardiac hypertrophy); treatment with class I or III antiarrhythmic agents, MAO inhibitors, or other drugs known to prolong the QT interval; electrolyte imbalance (particularly hypomagnesemia or hypokalemia); or treatment with drugs (e.g., diuretics) that may cause electrolyte imbalance.114
Promptly evaluate any signs or symptoms suggestive of irregular cardiac rhythm (e.g., palpitations, syncope).114
Hypotension
Possibility of severe hypotension; parenteral fluids and other supportive measures should be readily available.114
If hypotension occurs, consider possibility of hypovolemia and institute appropriate therapy with IV fluids.114
Consider repositioning patient to improve venous return to the heart when operative conditions permit; however, during spinal and peridural anesthesia, placing the patient into a head-down position may result in a higher level of anesthesia than is desirable and may impair venous return to the heart.114 Because of the possibility of orthostatic hypotension, use care when moving and positioning patients during anesthesia.114
If hypotension is not corrected with fluids or repositioning, consider use of pressor agents, but not epinephrine (may paradoxically decrease BP due to droperidol’s α-adrenergic blockade).114
CNS Depression
CNS depressant effects; monitor vital signs routinely.114
Concurrent Use With Opiate Agonists
When concurrent use of opiates and droperidol is required, administer opiates in reduced dosage.114 Be familiar with each drug, particularly widely differing durations of action.a
Respiratory depression induced by opiates persists longer than analgesic effects.a Before ordering opiate analgesics during anesthesia recovery, consider total dosage of administered opiates; if opiates are required during the recovery period, use initially in reduced dosages (as low as one-fourth to one-third of those usually recommended).a Keep resuscitative equipment and an opiate antagonist readily available to manage apnea.a
Neuroleptic Malignant Syndrome (NMS)
NMS (altered consciousness, muscular rigidity, autonomic instability) has occurred.114
May be difficult to distinguish NMS from malignant hyperthermia perioperatively; consider prompt dantrolene treatment if increases in temperature, heart rate, and/or carbon dioxide production occur following administration of droperidol.114
General Precautions
Anesthesia
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 also has cardiovascular effects.114
When droperidol is used to supplement these forms of anesthesia, be prepared to manage physiologic alterations involved.114
Hemodynamic Assessments
Droperidol may decrease pulmonary arterial pressure and interfere with interpretation of hemodynamic measurements made during diagnostic or surgical procedures.112
Monitoring
Monitor ECG and vital signs regularly.114
Effects on EEG
When EEG is used for postoperative monitoring, consider that the EEG pattern returns to normal slowly following droperidol use.114
Pheochromocytoma
Severe hypertension and tachycardia have occurred following droperidol administration in patients with diagnosed or suspected pheochromocytoma.114
Specific Populations
Pregnancy
Category C.114
Use in labor and delivery not recommended.114
Lactation
Not known whether droperidol is distributed into milk.114 Use with caution.114
Pediatric Use
Safety and efficacy not established in children <2 years of age.114
Geriatric Use
Use with caution; reduce initial dose and carefully adjust subsequent dosage.a
Hepatic Impairment
Use with caution.114
Renal Impairment
Use with caution.114
Common Adverse Effects
Hypotension, tachycardia, dysphoria, postoperative drowsiness, restlessness, hyperactivity, anxiety, extrapyramidal reactions (dystonia, akathisia, oculogyric crisis).114 a
Interactions for Inapsine
Drugs That Prolong QT Interval
Risk of prolonged QT interval and potentially serious or life-threatening arrhythmias.114 Avoid concomitant use of droperidol with drugs known to prolong the QT interval.114
Specific Drugs
Drug | Interaction | Comments |
|---|---|---|
Anesthetics, regional or conduction (e.g., spinal or peridural anesthesia) | Possible altered respiration, peripheral vasodilation, and hypotension.114 (See Anesthesia under Cautions.) | Use with caution114 |
Antiarrhythmics, class I or III | Possible prolongation of the QT interval; potentially arrhythmogenic114 | Avoid concomitant use of droperidol with drugs known to prolong the QT interval114 |
Antidepressants (e.g., tricyclics) | Potentially arrhythmogenic; some antidepressants known to prolong the QT interval114 | Avoid concomitant use of droperidol with drugs known to prolong the QT interval114 |
Antihistamines known to prolong the QT interval (terfenadine, astemizole [no longer commercially available in US]) | Potentially arrhythmogenic114 | Avoid concomitant use of droperidol with drugs known to prolong the QT interval114 |
Antimalarials | Potentially arrhythmogenic; some antimalarials known to prolong the QT interval114 | Avoid concomitant use of droperidol with drugs known to prolong the QT interval114 |
Calcium-channel blocking agents | Potentially arrhythmogenic; some calcium-channel blockers known to prolong the QT interval114 | Avoid concomitant use of droperidol with drugs known to prolong the QT interval114 |
CNS depressants (alcohol, barbiturates, benzodiazepines, general or volatile anesthetics, opiates and other analgesics, sedatives, tranquilizers) | Possible additive or potentiated CNS depression114 a | Reduce initial droperidol dose in patients who have received other CNS depressants, or vice versa114 |
Cyclobenzaprine | Torsades de pointes, with progression to ventricular fibrillation, reported with concomitant use of droperidol, cyclobenzaprine, and fluoxetine.115 (Possible mechanism: inhibition of cyclobenzaprine metabolism by fluoxetine; droperidol may have contributed to QT interval prolongation and development of torsades de pointes.115 ) | |
Diuretics | Potential for diuretic-induced hypokalemia or hypomagnesemia resulting in prolongation of the QT interval114 | Use with caution114 |
Epinephrine | Possible paradoxical decrease in BP due to droperidol’s α-adrenergic blockade114 | Use pressor agents other than epinephrine to treat hypotension that is unresponsive to IV fluids or repositioning of the patient114 |
Fentanyl | Increased BP reported (with or without preexisting hypertension) when droperidol administered with fentanyl or other parenteral analgesics (increased BP possibly resulted from unexplained changes in sympathetic activity after large doses or due to anesthetic/surgical stimulation during light anesthesia)114 | |
Laxatives | Potential for laxative-induced hypokalemia or hypomagnesemia resulting in prolongation of the QT interval114 | Use with caution114 |
MAO inhibitors | Risk factor for prolonged QT syndrome114 | Use concomitantly with extreme caution or do not use114 |
Mineralocorticoids | Supraphysiologic doses of steroid hormones with mineralocorticoid activity may induce hypokalemia or hypomagnesemia, prolonging the QT interval114 | Use with caution114 |
Neuroleptic agents known to prolong the QT interval (e.g., phenothiazines) | Potentially arrhythmogenic114 | Avoid concomitant use of droperidol with drugs known to prolong the QT interval114 |
Inapsine Pharmacokinetics
Absorption
Onset
Onset occurs within 3–10 minutes following IM or IV administration, but peak effects may not be apparent until 30 minutes.114
Duration
Following IM or IV administration, sedative and tranquilizing effects generally persist for 2–4 hours; alteration of consciousness may persist for up to 12 hours.114
Distribution
Extent
Reportedly crosses the blood-brain barrier and is distributed into the CSF.a
Reportedly crosses the placenta; not known whether droperidol is distributed into milk.a
Elimination
Metabolism
Metabolized in the liver.a
Elimination Route
Droperidol and its metabolites are excreted in urine (10% as unchanged drug) and feces.a
Stability
Storage
Parenteral
Injection
15–25°C; protect from light.114
Compatibility
For information on systemic interactions resulting from concomitant use, see Interactions.
Parenteral
Solution CompatibilityHID
Compatible |
|---|
Dextrose 5% in water |
Ringer’s injection, lactated |
Sodium chloride 0.9% |
Drug Compatibility
Compatible |
|---|
Amifostine |
Azithromycin |
Aztreonam |
Bivalirudin |
Bleomycin sulfate |
Cladribine |
Cisplatin |
Cyclophosphamide |
Cytarabine |
Dexmedetomidine HCl |
Docetaxel |
Doxorubicin HCl |
Doxorubicin HCl liposome injection |
Etoposide phosphate |
Famotidine |
Fenoldopam mesylate |
Filgrastim |
Fluconazole |
Fludarabine phosphate |
Gatifloxacin |
Gemcitabine HCl |
Granisetron HCl |
Hetastarch in lactated electrolyte injection (Hextend) |
Hydrocortisone sodium succinate |
Idarubicin HCl |
Linezolid |
Melphalan HCl |
Meperidine HCl |
Metoclopramide HCl |
Mitomycin |
Ondansetron HCl |
Paclitaxel |
Potassium chloride |
Propofol |
Remifentanil HCl |
Sargramostim |
Teniposide |
Thiotepa |
Vinblastine sulfate |
Vincristine sulfate |
Vinorelbine tartrate |
Vitamin B complex with C |
Incompatible |
Allopurinol sodium |
Amphotericin B cholesteryl sulfate complex |
Cefepime HCl |
Fluorouracil |
Foscarnet sodium |
Furosemide |
Leucovorin calcium |
Nafcillin sodium |
Piperacillin sodium–tazobactam sodium |
Variable |
Heparin sodium |
Methotrexate sodium |
ActionsActions
Exhibits strong sedative and tranquilizing effects.a Potentiates the actions of other CNS depressants but apparently has no analgesic activity.114 a
Has antiemetic activity.114 a
Acts principally at CNS subcortical levels;a may cause extrapyramidal reactions.114 a
Exhibits some α-adrenergic blocking activity; attenuates the cardiovascular response to sympathomimetic amines (e.g., reduces pressor effect of epinephrine).114 a
Direct peripheral vasodilatory effects, alone or in conjunction with α-adrenergic blockade, may cause hypotension and decreased peripheral vascular resistance.114 a
May decrease pulmonary arterial pressure (particularly if abnormally high).114 a
May reduce the incidence of epinephrine-induced arrhythmias but does not appear to prevent other arrhythmias.114 a
Advice to Patients
Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses or alcohol use.114
Importance of avoiding alcohol during therapy due to risk of additive effects.114
Importance of women informing clinicians if they are or plan to become pregnant or to breast-feed.114
Importance of informing patients of other important precautionary information.114 (See Cautions.)
Preparations
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name
Routes | Dosage Forms | Strengths | Brand Names | Manufacturer |
|---|---|---|---|---|
Parenteral | Injection | 2.5 mg/mL* | Droperidol Injection (preservative-free) | American Regent, Hospira |
Inapsine (preservative-free in ampuls or with parabens in multiple-dose vials) | Akorn |
Disclaimer
This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.
The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.
AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions July 2006. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.
† Use is not currently included in the labeling approved by the US Food and Drug Administration.
References
100. Grossman B, Lessin LS, Cohen P. Droperidol prevents nausea and vomiting from cis-platinum. N Engl J Med. 1979; 301:47. [PubMed 449910]
101. Jacobs AJ, Deppe G, Cohen CJ. A comparison of the antiemetic effects of droperidol and prochlorperazine in chemotherapy with cis-platinum. Gynecol Oncol. 1980; 10:55-7. [PubMed 7190532]
102. Wilson J, Weltz M, Solimando D et al. Continuous infusion droperidol: anti-emetic therapy for cis-platinum (DDP) toxicity. Proc Am Soc Clin Oncol. 1981; 22:421.
103. Mason BA, Dambra J, Grossman B et al. Effective control of cisplatin-induced nausea using high-dose steroids and droperidol. Cancer Treat Rep. 1982; 66:243-5. [IDIS 145462] [PubMed 7198937]
104. Brown RE, Gregg RE, Hood JC. Droperidol treatment in streptozocin-induced nausea and vomiting. Drug Intell Clin Pharm. 1982; 16:775-6. [IDIS 157659] [PubMed 6216088]
105. Owens NJ, Schauer AR, Nightingale CH et al. Antiemetic efficacy of prochlorperazine, haloperidol, and droperidol in cisplatin-induced emesis. Clin Pharm. 1984; 3:167-70. [IDIS 182892] [PubMed 6373102]
106. Lewis GO, Bernath AM, Ellison NM et al. Double-blind crossover trial of droperidol, metoclopramide, and prochlorperazine as antiemetics in cisplatin therapy. Clin Pharm. 1984; 3:618-21. [IDIS 193407] [PubMed 6391784]
107. 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; 19:118-21. [IDIS 195459] [PubMed 4038643]
108. Trzepacz P, Breitbart W, Levenson J et al for the American Psychiatric Association Working Group on Delirium. Practice guideline for the treatment of patients with delirium. Am J Psychiatry. 1999; 156(Supp 5):1-20.
109. Van Leeuwen A, Molders J, Sterkmans P et al. Droperidol in acutely agitated patients. J Nerv Ment Dis. 1977; 164:280-3. [PubMed 321727]
110. Resnick M, Burton B. Droperidol vs haloperidol in the initial management of acutely agitated patients. J Clin Psychiatry. 1984; 45:298-9. [IDIS 188732] [PubMed 6376480]
111. Thomas H, Schwartz E, Petrilli R et al. Droperidol versus haloperidol for chemical restraint of agutated and combative patients. Ann Emerg Med. 1992; 21:407-13. [PubMed 1554179]
112. Ahmed S. Dear healthcare professional letter regarding QT prolongation and torsades de pointes. Emeryville, CA: Akorn Inc.; 2001 Dec 4.
113. FDA strengthens warnings for droperidol. FDA Talk Paper. Rockville, MD: Food and Drug Administration; 2001 Dec 5.
114. Taylor Pharmaceuticals. Inapsine (droperidol) injection for intravenous or intramuscular use prescribing information. Decatur, IL; 2001 Nov.
115. Michalets EL, Smith LK, Van Tassel ED. Torsade de pointes resulting from the addition of droperidol to an existing cytochrome P450 drug interaction. Ann Pharmacother. 1998; 32:761-5. [IDIS 408347] [PubMed 9681092]
116. Gunn VL, Nechyba C, eds. The Harriett Lane handbook: a manual for pediatric house officers. 16th ed. Philadelphia, PA: Mosby; 2002:672-3.
a. AHFS drug information 2004. McEvoy GK, ed. Droperidol. Bethesda, MD: American Society of Health-System Pharmacists; 2004:2412-14
HID. Trissel LA. Handbook on injectable drugs. 13th ed. Bethesda, MD: American Society of Health-System Pharmacists; 2005:546-552.
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