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Acetylcysteine information from DrugsUpdate  

See Available Brands of Acetylcysteine in India

P - Caution when used during pregnancy
L - Caution when used during lactation

Acetylcysteine is an antioxidant drug used to reduce the thickness of mucus and ease its removal. It is also used to reverse the toxicity of high doses of acetaminophen. Acetylcysteine with hydration significantly reduces the risk of contrast nephropathy in patients with chronic renal insufficiency. Also called N-acetyl-L-cysteine.

Pharmacodynamics

Decreases thickness of mucous secretions in lung.

Pharmacokinetics

Acetylcysteine may decrease the viscosity of secretions by splitting of disulphide bonds in mucoproteins. It also promotes the detoxification of an intermediate paracetamol metabolite which is used in the management of paracetamol overdosage.

Absorption
Rapidly absorbed from the GI tract (oral); peak plasma concentrations after 0.5-1 hour.

Distribution
Protein-binding: 50%

Metabolism
Extensively hepatic

Excretion
Urine; elimination half-life: 6.25 hours (oral); 5.58 (IV)

Acetylcysteine Indications / Acetylcysteine Uses

The viscosity of pulmonary mucous secretions depends on the concentrations of mucoprotein and, to a lesser extent, deoxyribonucleic acid (DNA). The latter increases with increasing purulence owing to the presence of cellular debris. The mucolytic action of Acetylcysteine is related to the sulfhydryl group in the molecule. This group probably ``opens′′ disulfide linkages in mucus thereby lowering the viscosity. The mucolytic activity of Acetylcysteine is unaltered by the presence of DNA, and increases with increasing pH. Significant mucolysis occurs between pH 7 and 9. Acetylcysteine undergoes rapid deacetylation in vivo to yield cysteine or oxidation to yield diacetylcystine. Occasionally, patients exposed to the inhalation of an Acetylcysteine aerosol respond with the development of increased airways obstruction of varying and unpredictable severity. Those patients who are reactors cannot be identified a priori from a random patient population. Even when patients are known to have reacted previously to the inhalation of an Acetylcysteine aerosol, they may not react during a subsequent treatment. The converse is also true; patients who have had inhalation treatments of Acetylcysteine without incident may still react to subsequent inhalation with increased airways obstruction. Most patients with bronchospasm are quickly relieved by the use of a bronchodilator given by nebulization. If bronchospasm progresses, the medication should be discontinued immediately

Acetylcysteine Adverse Reactions / Acetylcysteine Side Effects

Flushing, fever, stomatitis, nausea, vomiting, rhinorrhoea, bronchospasm, anaphylactoid reactions, rashes. Rarely, blurred vision, bradycardia, syncope, thrombocytopenia, convulsions. Potentially Fatal: Rarely, respiratory or cardiac arrest.

Precautions

Information Not Available

Special Precautions

Asthmatic patients, history of bronchospasm, peptic ulceration. Pregnancy, lactation.

Other Drug Interactions

Information Not Available

Other Interactions

Information Not Available

Dosage

Oral
Mucolytic
Adult: As lozenges/ effervescent granules or tablets: 200 mg tid.
Child: As lozenges/ effervescent granules or tablets: 2-7 years: 200 mg bid; <2 years: 200 mg daily.

Oral
Paracetamol Poisoning
Adult: After gastric lavage or induction of emesis with ipecac syrup, admin loading dose of 140 mg/kg, followed by maintenance doses of 70 mg/kg every 4 hours for a total of 17 doses. 1st maintenance dose to be given 4 hours after the loading dose. Repeat dose if the patient vomits within 1 hour of admin. Continue therapy until paracetamol levels are not detectable and there is no evidence of hepatotoxicity.
Child: After gastric lavage or induction of emesis with ipecac syrup, admin loading dose of 140 mg/kg, followed by maintenance doses of 70 mg/kg every 4 hours for a total of 17 doses. 1st maintenance dose to be given 4 hours after the loading dose. Repeat dose if the patient vomits within 1 hour of admin. Continue therapy until paracetamol levels are not detectable and there is no evidence of hepatotoxicity.

Intravenous
Paracetamol Poisoning
Adult: Initially, 150 mg/kg in 200 ml of infusion fluid given over 15 minutes, followed by 50 mg/kg in 500 ml of infusion given over the next 4 hr, then 100 mg/kg in 1 L of infusion fluid over the next 16 hours.
Child: Child ≥20 kg: Initially, 150 mg/kg in 100 ml of infusion fluid given over 15 min, followed by 50 mg/kg in 250 ml of infusion given over the next 4 hours, then 100 mg/kg in 500 mL of infusion fluid over the next 16 hours.
Child <20 kg: Doses as per adult dose but adjust volume of based on child age and wt to avoid fluid overload.


Opthalmic
Dry eye associated with abnormal mucus production
Adult: Instill 1-2 drops of a 5% solution into the affected eye 3-4 times daily.

Inhalation
Mucolytic
Adult: 3-5 ml of a 20% solution or 6-10 ml of a 10% solution 3-4 times daily by nebulising through a face mask, mouth piece or tracheostomy. May increase to 1-10 ml of a 20% solution or 2-20 ml of a 10% solution every 2-6 hours if needed.
Child: 3-5 ml of a 20% solution or 6-10 ml of a 10% solution 3-4 times daily by nebulising through a face mask, mouth piece or tracheostomy. May increase to 1-10 ml of a 20% solution or 2-20 ml of a 10% solution every 2-6 hours if needed.

Endotracheal
Mucolytic
Adult: Instill 1-2 ml of a 10-20% solution as often as every hourly.
Child: Instill 1-2 ml of a 10-20% solution as often as every hourly.

Reconstitution
To be diluted for IV infusion with 5% dextrose, 0.9% sodium chloride, 0.3% potassium chloride with 5% glucose, 0.3% potassium chloride with 0.9% sodium chloride.

Incompatibility
Incompatible with metals (e.g. iron, copper, nickel), rubber, oxygen, oxidising substances (e.g. hydrogen peroxide), and some antibiotics (e.g. tetracycline HCl, oxytetracycline HCl, erythromycin lactobionate, ampicillin sodium, amphotericin B). A change in colour of solution to light purple may be observed and does not indicate significant change in safety or efficacy.

Food(before/after)

Information Not Available

List of Contraindications

Acetylcysteine and Pregnancy

Caution when used during pregnancy


Category B: Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies in women in the 1st trimester (and there is no evidence of a risk in later trimesters).

Acetylcysteine and Lactation

Caution when used during lactation

Acetylcysteine and Children

Although there is no specific information comparing use of acetylcysteine in children with use in other age groups, this medicine is not expected to cause different side effects or problems in children than it does in adults.

Acetylcysteine and Geriatic

Information Not Available

Acetylcysteine and Other Contraindications

Information Not Available

Storage

Endotracheal
Store between 59-86°F (15-30°C).
Undiluted solution may be kept refrigerated for 96 hours.

Inhalation
Store between 59-86°F (15-30°C).
Undiluted solution may be kept refrigerated for 96 hours.
Diluted solution to be used within 1 hour.

Intravenous

Store below 25°C.

Ophthalmic
Store below 25°C.

Oral
Store below 25°C.

Lab interference

Endotracheal
Store between 59-86°F (15-30°C).
Undiluted solution may be kept refrigerated for 96 hours.

Inhalation
Store between 59-86°F (15-30°C).
Undiluted solution may be kept refrigerated for 96 hours.
Diluted solution to be used within 1 hour.

Intravenous

Store below 25°C.

Ophthalmic
Store below 25°C.

Oral
Store below 25°C.

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