acetylcysteine (Antidote) (Rx)

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

AdultPediatric

Dosage Forms and Strengths

injectable solution

  • 20% (200mg/mL)

effervescent tablets for oral solution (Cetylev)

  • 500mg (DSC)
  • 2.5g (DSC)

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)

Acute Hepatic Failure (Orphan)

Orphan sponsor

  • Cumberland Pharmaceuticals, Inc, 2525 West End Ave, Suite 950, Nashville, TN 37203

Other Indications and Uses

Delayed presentation of acetaminophen-induced hepatic failure

Dosage Forms and Strengths

injectable solution

  • 200mg/mL

effervescent tablets for oral solution (Cetylev)

  • 500mg (DSC)
  • 2.5g (DSC)

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)
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Interactions

Interaction Checker

and acetylcysteine (Antidote)

No Results

     activity indicator 
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    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

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             activity indicator 

            Contraindicated (0)

              Serious - Use Alternative (0)

                Monitor Closely (1)

                • activated charcoal

                  activated charcoal decreases effects of acetylcysteine (Antidote) by Other (see comment). Use Caution/Monitor. Comment: Conflicting reports exist; however, charcoal administration does not preclude acetylcysteine administration for acetaminophen overdose .

                Minor (9)

                • isosorbide dinitrate

                  acetylcysteine (Antidote) increases effects of isosorbide dinitrate by Other (see comment). Minor/Significance Unknown. Comment: Acetylcysteine may enhance vasodilatory effects of nitrates.

                • isosorbide mononitrate

                  acetylcysteine (Antidote) increases effects of isosorbide mononitrate by Other (see comment). Minor/Significance Unknown. Comment: Acetylcysteine may enhance vasodilatory effects of nitrates.

                • nitroglycerin IV

                  acetylcysteine (Antidote) increases effects of nitroglycerin IV by Other (see comment). Minor/Significance Unknown. Comment: Acetylcysteine may enhance vasodilatory effects of nitroglycerin.

                • nitroglycerin PO

                  acetylcysteine (Antidote) increases effects of nitroglycerin PO by Other (see comment). Minor/Significance Unknown. Comment: Acetylcysteine may enhance vasodilatory effects of nitroglycerin.

                • nitroglycerin rectal

                  acetylcysteine (Antidote) increases effects of nitroglycerin rectal by Other (see comment). Minor/Significance Unknown. Comment: Acetylcysteine may enhance vasodilatory effects of nitroglycerin.

                • nitroglycerin sublingual

                  acetylcysteine (Antidote) increases effects of nitroglycerin sublingual by Other (see comment). Minor/Significance Unknown. Comment: Acetylcysteine may enhance vasodilatory effects of nitroglycerin.

                • nitroglycerin topical

                  acetylcysteine (Antidote) increases effects of nitroglycerin topical by Other (see comment). Minor/Significance Unknown. Comment: Acetylcysteine may enhance vasodilatory effects of nitroglycerin.

                • nitroglycerin transdermal

                  acetylcysteine (Antidote) increases effects of nitroglycerin transdermal by Other (see comment). Minor/Significance Unknown. Comment: Acetylcysteine may enhance vasodilatory effects of nitroglycerin.

                • nitroglycerin translingual

                  acetylcysteine (Antidote) increases effects of nitroglycerin translingual by Other (see comment). Minor/Significance Unknown. Comment: Acetylcysteine may enhance vasodilatory effects of nitroglycerin.

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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

                Asthma patient reported to develop bronchospasm and die after intravenous administration of drug; should be used with caution in patients with asthma, or where there is a history of bronchospasm; patients with asthma should be closely monitored during initiation of therapy and throughout therapy

                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

                Hypersensitivity reactions

                • 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
                • Acute flushing and erythema of skin may occur in patients receiving drug intravenously; these reactions usually occur 30 to 60 minutes after initiating the infusion and often resolve spontaneously despite continued infusion of the drug; If a reaction to acetylcysteine involves more than simply flushing and erythema of the skin, it should be treated as a hypersensitivity reaction
                • IV may cause severe anaphylactic reactions, however, new 2011 IV formulation (replaces original 2004 IV formulation) does not contain ethylene diamine tetracetic acid or any other stabilization and chelating agents and is free of preservatives
                • Management of less severe hypersensitivity reactions should be based upon the severity of the reaction and include temporary interruption of the infusion and/or administration of antihistaminic drugs; infusion may be carefully restarted after treatment of hypersensitivity symptoms initiated; however, if hypersensitivity reaction returns upon re-initiation of treatment or increases in severity, the drug should be discontinued and alternative patient management considered
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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.

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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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                Images

                BRAND FORM. UNIT PRICE PILL IMAGE
                N-A-C Sustain oral
                -
                600 mg tablet
                acetylcysteine
                -
                100 mg/mL (10 %) vial
                acetylcysteine
                -
                100 mg/mL (10 %) vial
                acetylcysteine
                -
                200 mg/mL (20 %) vial
                acetylcysteine
                -
                100 mg/mL (10 %) vial
                acetylcysteine
                -
                200 mg/mL (20 %) vial
                acetylcysteine
                -
                200 mg/mL (20 %) vial
                acetylcysteine
                -
                200 mg/mL (20 %) vial
                acetylcysteine
                -
                100 mg/mL (10 %) vial
                acetylcysteine
                -
                100 mg/mL (10 %) vial
                acetylcysteine
                -
                200 mg/mL (20 %) vial
                acetylcysteine
                -
                200 mg/mL (20 %) vial
                acetylcysteine
                -
                100 mg/mL (10 %) vial
                acetylcysteine
                -
                200 mg/mL (20 %) vial
                acetylcysteine intravenous
                -
                200 mg/mL (20 %) vial
                acetylcysteine intravenous
                -
                200 mg/mL (20 %) vial
                acetylcysteine intravenous
                -
                200 mg/mL (20 %) vial
                acetylcysteine intravenous
                -
                200 mg/mL (20 %) vial
                acetylcysteine intravenous
                -
                200 mg/mL (20 %) vial
                Acetadote intravenous
                -
                200 mg/mL (20 %) vial
                acetylcysteine oral
                -
                600 mg capsule
                NAC oral
                -
                600 mg capsule

                Copyright © 2010 First DataBank, Inc.

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                Patient Handout

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                Patient Education
                acetylcysteine

                ACETYLCYSTEINE - ORAL INHALATION/ORAL

                (a-SEET-il-SIS-teen)

                COMMON BRAND NAME(S): Mucomyst

                USES: When inhaled by mouth, acetylcysteine is used to help thin and loosen mucus in the airways due to certain lung diseases (such as emphysema, bronchitis, cystic fibrosis, pneumonia). This effect helps you to clear the mucus from your lungs so that you can breathe easier.When taken by mouth, acetylcysteine is used to prevent liver damage from acetaminophen overdose.

                HOW TO USE: If you are using this medication to treat lung disease, inhale this medication by mouth as directed by your doctor. A health care professional will show you the proper way to use this medication. Learn all preparation and usage instructions.You may notice a slight odor when you first breathe in the medication. This odor will quickly go away. If you are using a face mask to breathe in the medication, there may be some stickiness on your face after use. Wash your face with water to remove the stickiness.Do not mix acetylcysteine with other inhaled medications unless directed by the doctor or pharmacist.If you are taking this medication by mouth, take it as directed by your doctor. The solution is usually mixed with another liquid (such as cola) to decrease nausea and vomiting. Drink the medication within 1 hour of mixing.Tell your doctor if you vomit within 1 hour after taking your medication. You may need to take another dose.The dosage is based on your medical condition and response to treatment. For acetaminophen overdose, the dosage is also be based on your weight.Tell your doctor if your condition does not improve or if it worsens.

                SIDE EFFECTS: Nausea and vomiting may occur. Mouth sores and runny nose may also occur if you are inhaling this medication by mouth. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.If you are taking this medication by mouth, tell your doctor right away if any of these unlikely but serious side effects occur: severe stomach/abdominal pain, black stools, vomit that looks like coffee grounds.If you are inhaling this medication by mouth, seek immediate medical attention if any of these rare but very serious side effects occur: chest pain/tightness, trouble breathing.A very serious allergic reaction to this drug is rare. However, seek immediate medical attention if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

                PRECAUTIONS: Before using acetylcysteine, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: asthma, stomach/intestinal ulcer.During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.It is unknown if this drug passes into breast milk. Consult your doctor before breast-feeding.

                DRUG INTERACTIONS: See also How to Use section.Your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor or pharmacist first.Before using this medication, tell your doctor or pharmacist of all prescription and nonprescription/herbal products you may use.This medication may interfere with certain laboratory tests (including urine ketone test), possibly causing false test results. Make sure laboratory personnel and all your doctors know you use this drug.Keep a list of all your medications with you, and share the list with your doctor and pharmacist.

                OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.

                NOTES: Do not share this medication with others.For acetaminophen overdose, laboratory and/or medical tests (such as liver/kidney function test, acetaminophen drug levels, blood mineral levels) should be performed periodically to monitor your progress or check for side effects. Consult your doctor for more details.

                MISSED DOSE: If you are using this medication to treat lung disease and miss a dose, use it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Use your next dose at the regular time. Do not double the dose to catch up.If you are using this medication to treat acetaminophen overdose, it is important to take each dose as scheduled. If you miss a dose, ask your doctor or pharmacist right away for a new dosing schedule.

                STORAGE: Store at room temperature between 59-86 degrees F (15-30 degrees C) away from light. After opening the vial, store in the refrigerator between 35-46 degrees F (2-8 degrees C) and use within 96 hours (4 days). The solution may change to a light purple color. This is normal and will not affect how the drug works. Do not store in the bathroom. Keep all medicines away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company for more details about how to safely discard your product.

                Information last revised August 2021. Copyright(c) 2021 First Databank, Inc.

                IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

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                Tier Description
                1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
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                Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.