droperidol INAPSINE

Class: First Generation Antipsychotic/​Butyrophenone
FDA Indications: Postoperative Nausea/vomiting
Off-Label Use: Agitation/aggression
Prescribing
Forms: mg single-dose vial; 5 mg/2 mL (2.5 mg/mL) IM
Dose Range: 0.625-10 mg/day
Starting: Off label agitation: Start 2.5 mg (IV) or 5 mg (IM), wait at least 10-30 min before providing additional Postoperative nausea/vomiting: 0.625 to 1.25 mg IV administered at the end of surgery

NAMI drug fact sheet

Precautions
Contraindications: Droperidol is contraindicated in patients with known or suspected QT prolongation (i.e., QTc interval greater than 440 msec for males or 450 msec for females). This would include patients with congenital long QT syndrome.
Serious Side Effects: BLACK BOX: Cases of QT prolongation and/or torsade de pointes have been reported in patients receiving droperidol at doses at or below recommended doses. Some cases have occurred in patients with no known risk factors for QT prolongation and some cases have been fatal. , ,
Known Risk of TdP
Side Effects: EPS, akathisia, Neuroleptic-Induced Deficit Syndrome, decreased sweating, sedation/somnolence, dizziness, orthostatic hypotension
Pharmacodynamics
1° MOA: Dopamine 2 (D2) receptor antagonism in mesolimbic area
Target: D1 (high), D2 (very high), 5HT2 (high), α1 (low), H1 (low), M1 (low)
Pharmacokinetics
t½: 2.2° TMAX: 0.5°
Substrate of: 3A4
Inhibits: ∅ ; Induces:
Active Metabolites:
DDIs
Misc
  • - Short-acting, sedating butyrophenone, used in anesthesia for its sedating and antiemetic effects and, sometimes, in psychiatric emergencies as a sedative-neuroleptic
  • - Often is administered in combination with fentanyl for preanesthetic sedation and anesthesia Prolongs QT interval via its blockade of IKr (Inward-rectifier potassium) channel that's responsible for repolarization of cardiac cells in the later phase of the cardiac action potential
  • - Propofol, which is often coadminsitered for postoperative N/V, can counteract droperidol-induced prolonged QTc
  • - In an observational study set in hospital ERs, of the 1009 patients administered parenteral droperidol only 13 patients (1.28%) had an abnormal QT. In 7 of these cases another contributory factor was identified. There were no cases of TdP.
Special Populations

Category C—The limited animal and human data suggest that droperidol does not represent a significant risk to the fetus for major anomalies. The drug is a potent antiemetic that is effective for the treatment of severe nausea and vomiting of pregnancy, however ACOG does not recommend its use for the treatment of persistent symptoms of nausea and vomiting in pregnancy.

No reports describing the use of droperidol during lactation have been located. The molecular weight (about 379) is low enough that excretion into human milk should be expected. Because the drug is only available as an injectable formulation, the opportunity for exposure of a nursing infant appears to be limited. The effect of exposure on a nursing infant is unknown.

Use reduced initial dose



2019 BEE℞S Recommendation: Avoid, except in schizophrenia or bipolar disorder. Increased risk of CVA and greater rate of cognitive decline and mortality in persons with dementia. Avoid antipsychotics for behavioral problems of dementia or delirium unless nonpharmacological options have failed or are not possible and the older adult is threatening substantial harm to self or others.

No dosage adjustment necessary.


No dosage adjustment necessary.

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Last updated February 03 2021 21:57:17. Disclaimer: This website does not provide medical advice, nor is it a substitute for clinical judgment.