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Drug overview for ACETADOTE (acetylcysteine):
Generic name: ACETYLCYSTEINE
Drug class: Acetaminophen Poisoning Antidotes
Therapeutic class: Antidotes and other Reversal Agents
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.
No enhanced Uses information available for this drug.
Generic name: ACETYLCYSTEINE
Drug class: Acetaminophen Poisoning Antidotes
Therapeutic class: Antidotes and other Reversal Agents
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.
No enhanced Uses information available for this drug.
DRUG IMAGES
ACETADOTE 200 MG/ML VIAL
The following indications for ACETADOTE (acetylcysteine) have been approved by the FDA:
Indications:
Acetaminophen overdose
Professional Synonyms:
Acetaminophen toxicity
Paracetamol overdose
Indications:
Acetaminophen overdose
Professional Synonyms:
Acetaminophen toxicity
Paracetamol overdose
The following dosing information is available for ACETADOTE (acetylcysteine):
Acetylcysteine is used orally or by IV infusion as an antidote to prevent or lessen hepatic injury, which may occur following the ingestion of a potentially hepatotoxic quantity of acetaminophen. Acetylcysteine injection is designated an orphan drug by FDA for the treatment of moderate to severe acetaminophen overdosage.
When administered within 8 hours of acetaminophen ingestion, oral or IV acetylcysteine can effectively prevent or minimize hepatotoxicity associated with acute overdosage of acetaminophen. The effectiveness of oralacetylcysteine depends on early administration, with benefits seen principally in patients treated within 16 hours of overdose. The manufacturer of oral acetylcysteinestates that itis essential to initiate treatment as soon as possible after the overdose, with treatment beginning within 24 hours of ingestion.
According to the manufacturer of acetylcysteine injection, the critical ingestion-treatment interval for maximal protection against severe hepatic injury is between 0 and 8 hours. Efficacy diminishes progressively after 8 hours and treatment initiation between 15 and 24 hours after ingestion of acetaminophen yields limited efficacy. However, acetylcysteine does not appear to worsen the patient's condition and should not be withheld, particularly since the reported time of ingestion may be incorrect.
Clinical studies have clearly demonstrated efficacy of orally administered acetylcysteine, and oral administration may result in higher intrahepatic concentrations of the drug than IV administration. However, oral administration often produces nausea and vomiting, and administration of antiemetic agents may be needed to complete therapy; IV administration obviates potential difficulties associated with administration of an antiemetic. Intravenous administration achieves higher plasma concentrations compared with oral administration; it has been suggested that higher plasma concentrations may exert useful extrahepatic effects.
However, anaphylactoid reactions have been reported following IV administration.
In all cases of suspected acetaminophen overdosage, a regional poison control center (800-222-1222) may be contacted immediately for assistance in diagnosis and for directions in the use of acetylcysteine as an antidote. Consult the manufacturer's labeling for information on appropriate acetaminophen assay methodology and supportive treatment for acetaminophen overdosage.
When indicated, initiate acetylcysteine therapy as soon as possible with an IV or oral loading dose in adults and pediatric patients.
When administered within 8 hours of acetaminophen ingestion, oral or IV acetylcysteine can effectively prevent or minimize hepatotoxicity associated with acute overdosage of acetaminophen. The effectiveness of oralacetylcysteine depends on early administration, with benefits seen principally in patients treated within 16 hours of overdose. The manufacturer of oral acetylcysteinestates that itis essential to initiate treatment as soon as possible after the overdose, with treatment beginning within 24 hours of ingestion.
According to the manufacturer of acetylcysteine injection, the critical ingestion-treatment interval for maximal protection against severe hepatic injury is between 0 and 8 hours. Efficacy diminishes progressively after 8 hours and treatment initiation between 15 and 24 hours after ingestion of acetaminophen yields limited efficacy. However, acetylcysteine does not appear to worsen the patient's condition and should not be withheld, particularly since the reported time of ingestion may be incorrect.
Clinical studies have clearly demonstrated efficacy of orally administered acetylcysteine, and oral administration may result in higher intrahepatic concentrations of the drug than IV administration. However, oral administration often produces nausea and vomiting, and administration of antiemetic agents may be needed to complete therapy; IV administration obviates potential difficulties associated with administration of an antiemetic. Intravenous administration achieves higher plasma concentrations compared with oral administration; it has been suggested that higher plasma concentrations may exert useful extrahepatic effects.
However, anaphylactoid reactions have been reported following IV administration.
In all cases of suspected acetaminophen overdosage, a regional poison control center (800-222-1222) may be contacted immediately for assistance in diagnosis and for directions in the use of acetylcysteine as an antidote. Consult the manufacturer's labeling for information on appropriate acetaminophen assay methodology and supportive treatment for acetaminophen overdosage.
When indicated, initiate acetylcysteine therapy as soon as possible with an IV or oral loading dose in adults and pediatric patients.
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 available.
No generic dosing information available.
The following drug interaction information is available for ACETADOTE (acetylcysteine):
There are 0 contraindications.
There are 0 severe interactions.
There are 0 moderate interactions.
The following contraindication information is available for ACETADOTE (acetylcysteine):
Drug contraindication overview.
*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.
*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 0 contraindications.
There are 1 severe contraindications.
Adequate patient monitoring is recommended for safer drug use.
| Severe List |
|---|
| Acute asthma attack |
There are 2 moderate contraindications.
Clinically significant contraindication, where the condition can be managed or treated before the drug may be given safely.
| Moderate List |
|---|
| Bronchospastic pulmonary disease |
| Hypotension |
The following adverse reaction information is available for ACETADOTE (acetylcysteine):
Adverse reaction overview.
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.
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.
There are 10 severe adverse reactions.
| More Frequent | Less Frequent |
|---|---|
|
Skin rash Urticaria |
Angioedema Bronchospastic pulmonary disease Hypersensitivity drug reaction Hypotension Syncope Throat constriction |
| Rare/Very Rare |
|---|
|
Anaphylaxis Erythema |
There are 14 less severe adverse reactions.
| More Frequent | Less Frequent |
|---|---|
|
Flushing Nausea Pruritus of skin |
Cough Dyspnea Pharyngitis Rhinorrhea Tachycardia Vomiting |
| Rare/Very Rare |
|---|
|
Dyspepsia Gait abnormality Hyperhidrosis Ocular pain Wheezing |
The following precautions are available for ACETADOTE (acetylcysteine):
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.
Contraindicated
Severe Precaution
Management or Monitoring Precaution
Contraindicated
| None |
Severe Precaution
| None |
Management or Monitoring Precaution
| None |
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.
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.
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.
The following prioritized warning is available for ACETADOTE (acetylcysteine):
No warning message for this drug.
No warning message for this drug.
The following icd codes are available for ACETADOTE (acetylcysteine)'s list of indications:
| Acetaminophen overdose | |
| T39.1x1A | Poisoning by 4-aminophenol derivatives, accidental (unintentional), initial encounter |
| T39.1x2A | Poisoning by 4-aminophenol derivatives, intentional self-harm, initial encounter |
| T39.1x3A | Poisoning by 4-aminophenol derivatives, assault, initial encounter |
| T39.1x4A | Poisoning by 4-aminophenol derivatives, undetermined, initial encounter |
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