Droperidol


Thông tin thuốc gốc
Chỉ định và Liều dùng
Intravenous
Treatment and prophylaxis of postoperative nausea and vomiting
Adult: 0.625-1.25 mg 30 min prior to anticipated end of surgery, repeat 6 hrly, as necessary.
Child: 2-18 yr 10-50 mcg/kg (Max: 1.25 mg) 30 min prior to anticipated end of surgery, repeat 6 hrly, as necessary.
Elderly: 0.625 mg 30 min prior to anticipated end of surgery, repeat 6 hrly, as necessary.

Intravenous
Prophylaxis of nausea and vomiting associated with postoperative patient controlled analgesia (PCA)
Adult: 15-50 mcg per mg of morphine. Max: 5 mg daily.
Renal Impairment
Treatment and prophylaxis of postoperative nausea and vomiting: 0.625 mg 30 min prior to anticipated end of surgery, repeat 6 hrly, as necessary.
Hepatic Impairment
Treatment and prophylaxis of postoperative nausea and vomiting: 0.625 mg 30 min prior to anticipated end of surgery, repeat 6 hrly, as necessary.
Tương kỵ
Y-site: Allopurinol, amphotericin B cholesteryl sulfate complex, cefepime, cefotetan, fluorouracil, foscarnet, furosemide, leucovorin Ca, nafcillin, pemetrexed, piperacillin/tazobactam. Syringe: Fluorouracil, furosemide, heparin, leucovorin Ca, methotrexate, pentobarbital.
Chống chỉ định
Severe depression, Parkinson’s disease, coma, phaeochromocytoma, hypokalaemia, hypomagnesaemia, bradycardia (<55 heartbeats/min), known or suspected QT prolongation (QTc >440 millisecond in male and >450 millisecond in female). Concomitant use w/ class IA/III antiarrhythmics, macrolides, fluoroquinolones, antihistamines, certain antipsychotics, antimalarials, cisapride, domperidone, methadone, pentamidine, metoclopramide and other neuroleptics.
Thận trọng
Patient w/ epilepsy, risk factors for cardiac arrhythmia (e.g. history of serious ventricular arrhythmia, 2nd- or 3rd-degree AV block, sinus node dysfunction, CHF, ischaemic heart disease and left ventricular hypertrophy), glaucoma, COPD, resp failure, prolactin-dependent tumours (e.g. breast cancer), risk factors for electrolyte imbalance, history of alcohol abuse. Renal and hepatic impairment. Elderly, childn. Pregnancy and lactation.
Phản ứng phụ
Mild to moderate hypotension and tachycardia, hypovolaemia, drowsiness, restlessness, hyperactivity, anxiety, dystonia, akathisia, oculogyric crisis, dizziness, chills, laryngospasm, bronchospasm, constipation, xerostomia, blurred vision, urinary retention. Rarely, blood dyscrasias, dysphoria, convulsion, tremor.
Potentially Fatal: QT interval prolongation, torsades de pointes, cardiac arrest, ventricular tachycardia.
IM/IV/Parenteral: C
Thông tin tư vấn bệnh nhân
This drug may cause drowsiness, if affected, do not drive or operate machinery. Avoid exposure to direct sunlight.
MonitoringParameters
Perform ECG monitoring at baseline and continue for 2-3 hr after admin. Monitor vital signs, serum Mg and K, mental status, abnormal involuntary movement scale (AIMS). Observe for dystonia, extrapyramidal side effects and temp changes.
Quá liều
Symptoms: Extrapyramidal effects (e.g. salivation, abnormal movements, muscle rigidity), QT prolongation, serious arrhythmias (e.g. torsades de pointes), convulsions. Management: Supportive and symptomatic treatment. Maintain clear airway and adequate oxygenation; an oropharyngeal airway or endotracheal tube may be indicated. Maintain adequate fluid intake and body warmth. An anticholinergic drug may be given if extrapyramidal reactions occur.
Tương tác
May induce electrolyte imbalance when used w/ K-wasting diuretics, laxatives and glucocorticoids. May potentiate the sedative effect of barbiturates, benzodiazepines, morphine derivatives. May cause orthostatic hypotension w/ antihypertensive agents. May inhibit the action of dopamine agonists (e.g. bromocriptine, lisuride, levodopa). Prolonged effects w/ CYP1A2 (e.g. ciprofloxacin) and CYP3A4 (e.g. ketoconazole) inhibitors.
Potentially Fatal: Increased risk of extrapyramidal symptoms when used w/ metoclopramide and other neuroleptics. May cause torsades de pointes through QT prolongation w/ class IA/III antiarrhythmics (e.g. quinidine, disopyramide, procainamide, amiodarone, sotalol), macrolides (e.g. erythromycin), fluoroquinolones (e.g. sparfloxacin), antihistamine (e.g. astemizole, terfenadine), antimalarial agents (e.g. chloroquine), cisapride, domperidone, methadone, pentamidine, antipsychotics (e.g. chlorpromazine).
Food Interaction
Avoid alcohol.
Tác dụng
Description: Droperidol blocks dopamine in the chemoreceptor trigger zone in the area postrema. It produces mild α-adrenergic blockade, peripheral vasodilation and reduction of the pressor effect of epinephrine resulting in hypotension and decreased peripheral resistance. It may also reduce pulmonary artery pressure.
Onset: 3-10 min.
Duration: 2-4 hr, may extend up to 12 hr.
Pharmacokinetics:
Distribution: Crosses placenta and blood-brain barrier. Volume of distribution: Approx 1.5 L/kg. Plasma protein binding: 85-90%.
Metabolism: Metabolised hepatically to p-fluorophenylacetic acid, benzimidazolone, p-hydroxypiperidine by CYP1A2 and CYP3A4 isoenzymes, and to a lesser extent by CYP2C19.
Excretion: Via urine (approx 75%, >1% as unchanged drug); faeces (22%, 11% as unchanged drug). Elimination half-life: Approx 2-3 hr.
Đặc tính

Chemical Structure Image

Source: National Center for Biotechnology Information. PubChem Database. Droperidol, CID=3168, https://pubchem.ncbi.nlm.nih.gov/compound/Droperidol (accessed on Jan. 21, 2020)

Bảo quản
Store between 15-25°C. Protect from light.
Phân loại MIMS
Phân loại ATC
N05AD08 - droperidol ; Belongs to the class of butyrophenone derivatives antipsychotics.
References
Anon. Droperidol. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 17/10/2016.

Buckingham R (ed). Droperidol. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 17/10/2016.

Droperidol Injection, Solution (American Regent, Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 17/10/2016.

Joint Formulary Committee. Droperidol. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 17/10/2016.

McEvoy GK, Snow EK, Miller J et al (eds). Droperidol. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 17/10/2016.

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