Dosing and uses of Inapsine (droperidol)
Adult dosage forms and strengths
injectable solution
- 2.5mg/mL
Antiemetic
Initial: No more than 2.5 mg IV/IM; additional doses of 1.25 mg may be given if benefit outweighs potential risk
Delirium (Off-label)
5 mg Im
Renal Impairment
Use caution; safety and efficacy not established
Hepatic Impairment
Use caution; safety and efficacy not established
Other Information
Monitor: EKG, cardiac function
Other Indications & Uses
Prevention of nausea/vomiting during surgery
Off-label: Adjunct to general anesthesia, prevention of CINV, sedation
Pediatric dosage forms and strengths
injectable solution
- 2.5mg/mL
Antiemetic
2-12 years: 0.03-0.07 mg/kg IV/IM over 2-5 minutes q4-6hr PRn
Not to exceed 0.1 mg/kg IV/IM, additional dose (no more than 2.5 mg) may be given ONLY IF benefit outweighs potential risk
Other Information
Monitor: EKG, cardiac function
Geriatric dosage forms and strengths
Antiemetic
Initial: No more than 2.5 mg IV/IM; additional doses of 1.25 mg may be given if benefit outweighs potential risk
Inapsine (droperidol) adverse (side) effects
>10%
Restlessness
Anxiety
Extrapyramidal Symptoms
Dystonic reactions
Pseudoparkinsonian signs and symptoms
Tardive dyskinesia
Seizure
Altered central temperature regulation
Sedation
Drowsiness
Prolonged QT interval (dose dependent)
Swelling of breasts
Weight gain
Constipation
1-10%
Hallucinations
Persistent tardive dyskinesia
Akathisia
Orthostatic hypotension
Tachycardia
ECG: abnormal T waves
Hypertension
Nausea
Vomiting
Dysuria
Frequency not defined
Serious, potentially fatal cardiac effects: prolonged QT interval, torsades de pointes, cardiac arrest, ventricular tachycardia
Warnings
Black box warnings
Patients with dementia-related psychosis who are treated with antipsychotic drugs are at an increased risk of death as shown in short-term controlled trials. The deaths appeared to be either cardiovascular (eg, heart failure, sudden death) or infectious (eg, pneumonia) in nature
This drug is not approved for the treatment of patients with dementia-related psychosis
Contraindications
Hypersensitivity
Known or suspected prolonged QT interval; QTc interval >450 msec in females or 400 msec in males
Cautions
May cause potentially fatal QT interval prolongation/torsades de pointes at or below recommended doses; should be used only in patients who have failed to respond to other drugs
Use as sedative or anesthesia adjunct no longer recommended
Shares the toxic potentials of phenothiazines
Risk factors for prolonged QT intervaL
- Use with extreme cautions in patients at risk for development of prolonged QT syndrome
- CHF, bradycardia, diuretic use, hypokalemia, hypomagnesemia, cardiac hypertrophy
- Use of drug known to cause prolonged QT interval: class I or III antiarrhythmias, some antihistamines, antimalarials, calcium channel blockers, neuroleptics, antidepressants or drugs which may induce hypokalemia or hypomagnesemia
- >65 years, alcohol abuse, concomitant use of benzodiazepines or IV opiates, impaired hepatic/renal function
Pregnancy and lactation
Pregnancy category: C
Lactation: distributed into breast milk; avoid
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Inapsine (droperidol)
Mechanism of action
Antiemesis: dopamine receptor blockade in brain, predominantly dopamine-2 receptor & when reuptake is prevented, a strong antidopaminergic, antiserotonic response occurs
Droperidol reduced motor activity, anxiety, and causes sedation; also possesses adrenergic-blocking, antifibrillatory, antihistaminic, & anticonvulsive properties
Pharmacotherapy
Half-Life elimination: 2 hr (parent drug), 8-12 hr (metabolites)
Onset: 3-10 min
Duration: 2-4 hr, may persist up to12 hr
Peak Response Time: 10-30 min
Peak Plasma Time: 60 min (IM)
Protein Bound: extensive
Metabolism: extensively in the liver
Metabolites: [Benzimidazolone, p-Fluorophenylacetic acid, p-Hydroxypiperidine] (inactive)
Vd: 2 L/kg (Adults); 0.58 L/kg (Children)
Excretion: Urine (75%); feces (22%)
Administration
IV Incompatibilities
Syringe: fluorouracil, furosemide, heparin, leucovorin, methotrexate, ondansetron, pentobarbitaL
Y-site: allopurinol, amphotericin B cholesteryl SO4, cefepime, fluorouracil, fascarnet, furosemide, heparin(?), leucovorin, methotrexate(?), nafcillin, piperacillin/tazobactam
IV Compatibilities
Solution: D5W, LR, Ns
Syringe: atropine, bleomycin, butorphanol, chlorpromazine, cimetidine, cisplatin, cyclophosphamide, dimenhydrinate, diphenhydramine, doxorubicin, fentanyl, glycopyrrolate, hydroxyzine, meperidine, metoclopramide, midazolam, mitomycin, morphine sulfate, nalbuphine, papaveretum, pentazocine, perphenzine, prochlorperazine, promazine, promethazine, scopolamine, vinblastine, vincristine
Y-site: alatrofloxacin, amifostine, azithromycin, aztreonam, bivalirudin, bleomycin, cisatracurium, cladribine, cisplatin, cyclophosphamide, cytarabine, dexmedetomidine, docetaxel, doxorubicin, doxorubicin liposomal, etoposide phosphate, famotidine, fenoldopam, filgrastim, fluconazole, fludarabine, gatifloxacin, gemcitabine, granisetron, Hextend, hydrocortisone sodium succinate, idarubicin, linezolid, melphalan, meperidine, metoclopramide, mitomycin, ondansetron, paclitaxel, potassium chloride, propofol, remifentanil, sargramostim, teniposide, thiotepa, vinblastine, vincristine, vinorelbine, vitamin B/C
IV/IM Administration
Administered IM or slow IV (2-5 min)
IV infusion has been used in high-risk pts
Storage
Controlled room temperature
Protect from light
