Antidote
Reactivates cholinesterase that had been inactivated by phosphorylation due to exposure to organophosphate pesticides and cholinesterase-inhibiting nerve agents (eg, terrorism and chemical warfare agents such as sarin) by displacing the enzyme from its receptor sites; removes the phosphoryl group from the active site of the inactivated enzyme
藥動學
Excretion: Urine (as metabolites and unchanged drug)
Elimination Half-life: 74 min to 77 min; (Poisoned patients) 3-4 hours
禁忌症
Hypersensitivity to pralidoxime or any component of the formulation.
懷孕分類
There are no controlled data in human pregnancy. Pralidoxime is only recommended for use during pregnancy when benefit outweighs risk.
哺乳分類
The manufacturer recommends that caution be exercised when administering pralidoxime to nursing women.
Anticholinesterase overdose:
(IV) 1,000 to 2,000 mg, followed by increments of 250 mg every 5 minutes as needed Organophosphate poisoning: IM (preferred), SUBQ:
1. Mild symptoms: 600 mg; repeat as needed every 15 minutes to a maximum total dose of 1,800 mg
2. Severe symptoms: 600 mg; repeat twice in rapid succession to deliver a total dose of 1,800 mg
3. Persistent symptoms: May repeat the entire series (1,800 mg) beginning ~1 hour after administration of the last injection IV (In patients with severe intoxication, maintenance treatment should be administered as a continuous infusion):
1. Loading dose: 30 mg/kg or 2,000 mg
2. Maintenance: (Continuous infusion) 8 to 10 mg/kg/hr (max: 650 mg/hr) or 500 mg/hr; (Intermittent infusion) May repeat loading dose after 1 to 2 hours if muscle weakness has not been relieved, followed by repeated dosing every 4 to 6 hours as needed
小兒調整劑量
Anticholinesterase overdose:
Very limited data available: IV 30 mg/kg/dose for 2 doses Organophosphate poisoning: Infants, Children, and Adolescents ≤16 years:
1. Loading: 20-50 mg/kg (maximum: 2,000 mg/dose)
2. Maintenance: (Continuous IV Infusion) 10-20 mg/kg/hour not to exceed 500 mg/hour; (Intermittent IV) 20-50 mg/kg, maximum 2,000 mg/dose; may be repeated after 1 hour if muscle weakness has not been relieved Adolescents >16 years:
1. Loading: 30 mg/kg or 2,000 mg
2. Maintenance: (Continuous IV Infusion) 8-10 mg/kg/hr or 500 mg/hr, not to exceed 650 mg/hr; (Intermittent IV) 1,000-2,000 mg administered 1 hour after loading dose, repeat every 10 to 12 hours as needed
腎功能調整劑量
Pralidoxime is excreted in the urine, dosage reduction is recommended in patients with renal impairment.
肝功能調整劑量
There are no dosage adjustments provided in the manufacturer's labeling.
安定性
注射給藥指引
給藥途徑
IV
靜脈輸注液
NS
每瓶稀釋液體積
注射濃度
10-20 mg/mL; 50 mg/mL (限水者 )
給藥速率
見注意事項
安定性
注意事項
1. 每次使用時必須新鮮配置
2. Bolus:1-2 gm diluted in 100 ml NS滴注15-30分,之後持續滴注500 mg/hr