Acetaminophen overdose: Only the 72-hour oral and 21-hour IV regimens are FDA approved. Treatment should begin within 8 hours of ingestion or as soon as possible after ingestion.
藥理
Antidote; Mucolytic Agent
藥動學
Distribution: Vdss: 0.47 L/kg Protein binding: 66% to 87% Metabolism: Undergoes extensive first pass metabolism to form cysteine and disulfides (N,N-diacetylcysteine and N-acetylcysteine); cysteine is further metabolized to form glutathione and other metabolites Half-life elimination: Reduced acetylcysteine: 2 hours Total acetylcysteine: Adults: 5.6 hours; Newborns: 11 hours Excretion: Urine (13% to 38%)
禁忌症
Hypersensitivity to acetylcysteine or any component of the formulation.
懷孕分類
Acetylcysteine crosses the placenta. Delaying treatment to pregnant women with acetaminophen toxicity may increase the risk of adverse maternal and fetal outcomes.
哺乳分類
It is not known if acetylcysteine is excreted in breast milk. According to the manufacturer, the decision to continue or discontinue breast-feeding during therapy should take into account the risk of infant exposure, the benefits of breast-feeding to the infant, and benefits of treatment to the mother. Based on pharmacokinetics, acetylcysteine should be nearly completely cleared 30 hours after administration; breast-feeding women may consider pumping and discarding breast milk for 30 hours after administration.
副作用
>10%:
Immunologic: Autoimmune disease (14% to 18%)
Miscellaneous: Anaphylactoid reaction (1% to 18%) 1% to 10%:
Cardiovascular: Flushing (1% to 3%), tachycardia (1% to 4%), edema (1% to 2%)
Dermatologic: Urticaria (?21%), rash (2% to ?21%), pruritus (1% to ?21%)
Gastrointestinal: Vomiting (2% to 10%), nausea (1% to 6%)
Second dose: 50 mg/kg (maximum: 5 g) infused over 4 hours.
Third dose: 100 mg/kg (maximum: 10 g) infused over 16 hours. Note: The fluid volume should be reduced in patients weighing ?40 kg.
Alternative recommendations :
"""Two bag method""" (off-label dosing): Consists of 2 doses; total dose delivered: 300 mg/kg (Wong 2016b): First dose: 200 mg/kg infused over 4 hours. Second dose: 100 mg/kg infused over 16 hours. Note: The """two bag method""" has been associated with fewer and milder nonallergic anaphylactic reactions as compared to the manufacturer's labeled dosing (Wong 2016b).
"""Single bag method""" (off-label dosing): Total dose delivered 430 mg/kg: Initiate therapy with 150 mg/kg infused over 1 hour; then decrease the rate to 14 mg/kg/hour and infuse for an additional 20 hours (Johnson 2011). Note: Patients weighing >69 kg will require a second bag to complete the dosing regimen.
Obesity: In patients who weigh >100 kg, the following dosing regimen is recommended: IV (Acetadote):
21-hour regimen: Consists of 3 doses; total dose delivered: 30 g.
Loading dose: 15 g infused over 1 hour.
Second dose: 5 g infused over 4 hours.
Third dose: 10 g infused over 16 hours.
小兒調整劑量
Acetaminophen poisoning: IV: Acetadote: Three-bag method: Infants, Children, and Adolescents: 21-hour regimen: Consists of 3 doses; total dose delivered: 300 mg/kg.
Loading dose: IV: 150 mg/kg infused over 60 minutes; maximum dose: 15 g/dose.
Second dose: IV: 50 mg/kg infused over 4 hours; maximum dose: 5 g/dose.
Third dose: IV: 100 mg/kg infused over 16 hours; maximum dose: 10 g/dose. Two-bag method: Limited data available: Note: The """two-bag method""" has been associated with fewer and milder nonallergic anaphylactic reactions as compared to the manufacturer's labeled dosing (Wong 2016b).
Children ?12 years and Adolescents: 20-hour regimen: Consists of 2 doses; total dose delivered: 300 mg/kg; maximum total dose: 30 g (Wong 2016b):