Acetadote (acetylcysteine)
Acetaminophen Poisoning Antidotes Intravenous Vial (ML)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Acetylcysteine, the N-acetyl derivative of the naturally occurring amino acid, l-cysteine, is an antidote for acetaminophen overdosage as well as a mucolytic agent and sulfhydryl donor.
The exact mechanism(s) by which acetylcysteine prevents or minimizes acetaminophen-induced hepatotoxicity has not been fully determined. Acetylcysteine may protect the liver following acetaminophen overdosage by maintaining or restoring glutathione levels or by acting as an alternate substrate for conjugation with (and detoxification of) a toxic intermediate metabolite of acetaminophen.
Acetylcysteine reduces the viscosity of purulent and nonpurulent pulmonary secretions and facilitates their removal by coughing, postural drainage, or mechanical means. The mucolytic effect of the drug has been shown to depend on the free sulfhydryl group, which is thought to reduce disulfide linkages of mucoproteins.
The exact mechanism(s) by which acetylcysteine might prevent radiographic contrast media-associated nephrotoxicity is unclear. It has been suggested that since radiographic contrast media-induced renal toxicity may be related to formation of reactive oxygen species or to reduced antioxidant activity; acetylcysteine, a thiol-containing antioxidant, may reduce the ability of the generated oxygen free radicals to damage cells by acting as an oxygen free-radical scavenger. In addition, the drug also may increase the biologic effects of nitric oxide by combining with the oxide to formS-nitrosothiol, a potent vasodilator.
The interaction of acetylcysteine and nitric oxide may limit the production of the damaging peroxinitrate radical, because acetylcysteine would compete with the superoxide radical for nitric oxide. Acetylcysteine also increases the expression of nitric oxide synthase and therefore may improve blood flow. Evidence suggesting the possibility that decreases in serum creatinine associated with acetylcystine may occur in the absence of any actual effect on kidney function has been observed.
Following oral administration (e.g., when used as an antidote for acetaminophen overdosage), acetylcysteine is absorbed from the GI tract, with peak plasma concentrations achieved within 1-2 hours. The drug is 50-87% bound to plasma proteins. Acetylcysteine is deacetylated to cysteine and oxidized to yield diacetylcysteine; cysteine is further metabolized to form glutathione and other metabolites.
Following oral administration of acetylcysteine, a mean elimination half-life of 6.25 hours has been reported. Following IV administration of acetylcysteine, a mean elimination half-life of 5.6 hours has been reported in adults. Elimination of acetylcysteine is principally (70%) nonrenal.
Following IV administration of acetylcysteine in subjects with mild (Child-Pugh class A), moderate (Child-Pugh class B), or severe (Child-Pugh class C) hepatic impairment, mean elimination half-life is increased by 80% compared with normal subjects. Mean clearance is decreased by 30% and systemic exposure increased 1.6-fold in subjects with hepatic impairment compared to subjects with normal hepatic function. These changes are not considered clinically meaningful.
Hemodialysis may remove some of total acetylcysteine.
Generic name: acetylcysteine
Drug class: Acetaminophen Poisoning Antidotes
Therapeutic class: Antidotes and other Reversal Agents
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Acetadote
Indications
The following indications are listed for Acetadote:
- Acetaminophen Overdose
Also known as: Acetaminophen Toxicity, Paracetamol Overdose.
Dosing
No dosing information is available for this tab.
As an antidote for acetaminophen overdosage, acetylcysteine is administered as an oral solution or by IV infusion. As a mucolytic agent, acetylcysteine, usually in a 10-20% solution, may be administered by nebulization, direct instillation, or intratracheal instillation.
Acetylcysteine has been administered orally or by IV infusion for prevention ofradiographic contrast media-induced nephropathy+.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
There is no enhanced messaging for this drug.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*Acetylcysteine injection is contraindicated in patients with known hypersensitivity or previous anaphylactoid reaction to acetylcysteine or any ingredient in the formulation.
*Acetylcysteine solution for oral inhalation or intratracheal instillation is contraindicated in patients with known hypersensitivity to the drug.
*When administered orally as an antidote, no contraindications.
There are no contraindication contraindications for this drug.
- Acute asthma attack
- Bronchospastic pulmonary disease
- Hypotension
Adverse reactions
Common adverse effects following oral administration of acetylcysteine include nausea, vomiting, and other GI symptoms.
Common adverse effects following IV administration of acetylcysteine reported in >2% of patients include rash, urticaria/facial flushing, and pruritus.
Common adverse effects following oral inhalation or intratracheal instillation of acetylcysteine include stomatitis, nausea, vomiting, fever, rhinorrhea, drowsiness, clamminess, chest tightness, and bronchoconstriction.
More Frequent
- Skin rash
- Urticaria
Less Frequent
- Angioedema
- Bronchospastic pulmonary disease
- Hypersensitivity drug reaction
- Hypotension
- Syncope
- Throat constriction
Rare or Very Rare
- Anaphylaxis
- Erythema
More Frequent
- Flushing
- Nausea
- Pruritus of skin
Less Frequent
- Cough
- Dyspnea
- Pharyngitis
- Rhinorrhea
- Tachycardia
- Vomiting
Rare or Very Rare
- Dyspepsia
- Gait abnormality
- Hyperhidrosis
- Ocular pain
- Wheezing
Precautions
No enhanced messaging available.
Efficacy of IV acetylcysteine as an antidote for acetaminophen overdosage in pediatric patients appears to be similar to that in adults. Safety and efficacy of IV acetylcysteine in pediatric patients have not been established by adequate and well-controlled studies; use of IV acetylcysteine as an antidote for acetaminophen overdosage in pediatric patients >=5 kg is based on clinical practice.
Reproductive studies in rabbits using oral acetylcysteine dosages of 500 mg/kg daily (2.6 times the human mucolytic dose) on days 6 through 16 of gestation revealed no teratogenicity. Studies in rabbits exposed for 30-35 minutes twice daily to a nebulized solution containing acetylcysteine and isoproterenol hydrochloride on days 6 through 18 of pregnancy revealed no teratogenicity. Perinatal and postnatal studies in rats exposed to a nebulized solution containing acetylcysteine and isoproterenol did not reveal harm to the fetus or newborns. Acetylcysteine has been reported to cross the placenta in humans following oral or IV administration. However, there are no adequate and controlled studies to date using acetylcysteine in pregnant women, and the drug should be used during pregnancy only when clearly needed.
Limited published case reports and case series of pregnant women exposed to acetylcysteine during various trimesters are not sufficient to inform any drug-associated risk. Delaying treatment of acetaminophen overdose may increase the risk of maternal or fetal morbidity and mortality. Reproduction studies in rats and rabbits following oral administration of acetylcysteine during the period of organogenesis at doses similar to the total IV dose (based on body surface area) did not result in any adverse effects to the fetus.
It is not known whether acetylcysteine is distributed into human milk; the drug's effects on the breast-fed infant or on milk production also are not known. Consider the developmental and health benefits of breast-feeding along with the mother's need for acetylcysteine and any potential adverse effects on the breast-fed child from acetylcysteine or from the underlying maternal condition. Use acetylcysteine with caution in nursing women.
Based on pharmacokinetic data, acetylcysteine should be nearly completely cleared 30 hours after IV administration of the drug. Breast-feeding women may consider pumping and discarding their milk for 30 hours after administration.
Insufficent experience with IV acetylcysteine in patients 65 years of age or older in order to determine whether these patients respond differently than younger adults.
ICD codes
| Code | Type | Description |
|---|---|---|
| Acetaminophen overdose | ||
| T39.1x1A | ICD10CM | Poisoning by 4-aminophenol derivatives, accidental (unintentional), initial encounter |
| T39.1x2A | ICD10CM | Poisoning by 4-aminophenol derivatives, intentional self-harm, initial encounter |
| T39.1x3A | ICD10CM | Poisoning by 4-aminophenol derivatives, assault, initial encounter |
| T39.1x4A | ICD10CM | Poisoning by 4-aminophenol derivatives, undetermined, initial encounter |
ICD code information from First Databank (FDB).
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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