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acetylcysteine (Antidote) (Rx)Brand and Other Names:Acetadote, Cetylev, more...N-acetylcysteine (Antidote)

 
 
 

Dosing & Uses

AdultPediatric

Dosing Forms and Strengths

injectable solution

  • 20% (200mg/mL)

effervescent tablets for oral solution (Cetylev)

  • 500mg
  • 2.5g

Acetaminophen Overdose

May administer injectable orally

Continuous IV infusion recommended for acute ingestion (ideally within 8-10 hr following ingestion, but may administer if >10 hr)

Intermittent IV infusion may be considered for late presenting or chronic ingestion (more than 10 hr after ingestion)

Oral administration

  • May administer injectable orally
  • Loading dose: 140 mg/kg PO 
  • Maintenance dose: 4 hr after loading dose, start 70 mg/kg PO q4hr for a total 17 doses; repeat dose if emesis occurs within 1 hr of administration

IV continuous infusion

  • Acute ingestion (within 8-10 hr after ingestion)
  • Administer as 3 doses
  • Loading dose: 150 mg/kg IV; mix in 200 mL of D5W and infuse over 1 hr 
  • Dose 2: 50 mg/kg IV in 500 mL D5W over 4 hr, THEN
  • Dose 3: 100 mg/kg IV in 1000 mL D5W over 16 hr
  • >100 kg: No specific studies have conducted; limited data suggest a loading dose of 15,000 mg infused IV over 1 hr, then a first maintenance dose of 5,000 mg IV over 4 hr and a second maintenance dose of 10,000 mg over 16 hr

Intermittent IV administration (Off-label)

  • Total treatment time 48 hr
  • Late presenting or chronic ingestion (>10 hr after ingestion) in patients >40 kg
  • Loading dose: 140 mg/kg IV infused over 1 hr (dilute in 500 mL D5W), THEN
  • Maintenance dose: 70 mg/kg IV q4h for at least 12 doses (dilute each dose in 250 mL of D5W and infuse over minimum 1 hr)
  • Heard K, et al. Clinical Toxicology. 2014 Jun;52(5):512-8. Rocky Mountain Poison and Drug Center

Acetaminophen Overdose (Orphan)

Effervescent tablets for oral solution

Orphan designation to prevent hepatic injury from acetaminophen overdose

Sponsor

  • Arbor Pharmaceuticals, LLC; 980 Hammond Drive, Bldg Two, suite 1250; Atlanta, GA 30328

Other Indications and Uses

Delayed presentation of acetaminophen-induced hepatic failure

Dosing Forms and Strengths

injectable solution

  • 200mg/mL

effervescent tablets for oral solution (Cetylev)

  • 500mg
  • 2.5g

Acetaminophen Overdose

May administer injectable orally

Continuous IV infusion recommended for acute ingestion (ideally within 8-10 hr following ingestion, but may administer if >10 hr)

Intermittent IV infusion may be considered for late presenting or chronic ingestion (>10 hr after ingestion)

Oral administration (Cetylev)

  • Loading dose: 140 mg/kg PO
  • Maintenance dose: 4 hr after loading dose, give 70 mg/kg PO q4hr for a total of 17 doses; repeat dose if emesis occurs within 1 hr of administration

IV continuous infusion (Acetadote) weight ≤20 kg

  • Loading Dose: 150 mg/kg  IV in 3 mL diluent/kg body-weight over 1 hr
  • Dose 2: 50 mg/kg IV in 7 mL diluent/kg body-weight over 4 hr
  • Dose 3: 100 mg/kg in 14 mL diluent/kg body-weight over 16 hr

IV continuous infusion (Acetadote) >20 kg to <40 kg

  • Loading Dose: 150 mg/kg IV in 100 mL of diluent administered over 1hr
  • Dose 2: 50 mg/kg IV in 250 mL of diluent administered over 4 hr
  • Dose 3: 100 mg/kg IV in 500 mL of diluent administered over 16 hr

IV continuous infusion (Acetadote) weight ≥40 kg

  • As adults
  • Loading dose: 150 mg/kg IV; mix in 200 mL of D5W and infuse over 1 hr
  • Dose 2: 50 mg/kg IV in 500 mL D5W over 4 hr, THEN
  • Dose 3: 100 mg/kg IV in 1000 mL D5W over 16 hr

Intermittent infusion (Off-label)

  • Total treatment time 48 hr
  • Late presenting or chronic (more than 10 hr after ingestion) in patients >40 kg
  • Loading dose: 140 mg/kg IV infused over 1 hr (dilute in 200 mL D5W), THEN
  • Maintenance dose: 70 mg/kg IV q4h for at least 12 doses (dilute each dose in 250 mL of D5W and infuse over minimum 1 hr)
  • Heard K, et al. Clinical Toxicology. 2014 Jun;52(5):512-8. Rocky Mountain Poison and Drug Center
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Interactions

Interaction Checker

acetylcysteine (Antidote) and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            Frequency Not Defined

            Oral Administration

            • Nausea
            • Vomiting
            • Drowsiness
            • Chills
            • Fever

            IV Administration

            • Anaphylactoid reaction due to pyrogens
            • Flushing
            • Edema
            • Urticaria
            • Pruritus
            • Nausea
            • Pharyngitis
            • Rhinorrhea
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            Warnings

            Contraindications

            Hypersensitivity

            Cautions

            Obtain serum acetaminophen concentration at least 4 hr postingestion to determine if toxic levels present before treatment or whether full course necessary

            IV used if persistent vomiting precludes PO administration in 1st 8 hr

            Consult local regional PCC or medical toxicologist for assistance

            IV may cause severe anaphylactic reactions, however, new 2011 IV formulation (replaces the original 2004 IV formulation) does not contain ethylene diamine tetracetic acid or any other stabilization and chelating agents and is free of preservatives

            Serious acute hypersensitivity reactions during acetylcysteine administration including rash, hypotension, wheezing, and/or shortness of breath reported in patients receiving intravenous acetylcysteine for acetaminophen overdose; occurred soon after initiation

            Total volume administered should be adjusted for patients <40 kg and for those requiring fluid restriction; to avoid fluid overload, volume of diluent should be reduced as needed; if volume not adjusted fluid overload can occur, potentially resulting in hyponatremia, seizure and death

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            Pregnancy & Lactation

            Pregnancy Category: B

            Delaying treatment in pregnant women with acetaminophen overdose and potentially toxic acetaminophen plasma levels may increase risk of maternal and fetal morbidity and mortality

            Lactation: Developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for therapy and potential adverse effects on the breastfed child from therapy or from underlying maternal condition

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

            more...
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            Pharmacology

            Mechanism of Action

            Acts as sulfhydryl group donor to restore liver glutathione; may also scavenge free radicals to prevent delayed hepatotoxicity as antioxidant; encourages sulfation pathway of metabolism for acetaminophen

            Might be useful against free radicals or reactive metabolites formed by chloroform, carbon tetrachloride, 1,2-dichloropropane, acrylonitrite, doxyrubicin and cyclophosphamide

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            Administration

            Instructions

            May pretreat with diphenhydramine, hydrocortisone, cimetidine

            Should be given within 8 hr of acetaminophen ingestion for maximum benefit; however effective even after 24 hr of ingestion

            Acetadote is hyperosmolar (2600 mOsm/L) and is compatible with 5% dextrose (D5W), 0.45% NaCl injection, and sterile water for injection

            Decrease total IV volume for patients who weigh <40 kg or if fluid restriction is required

            See adult and pediatric dosing for detailed information on oral, intermittent IV infusion, or continuous IV infusion

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            Formulary

            FormularyPatient Discounts

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            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
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