Acetadote - General Information
The N-acetyl derivative of cysteine. It is used as a mucolytic agent to reduce the viscosity of mucous secretions. It has also been shown to have antiviral effects in patients with HIV due to inhibition of viral stimulation by reactive oxygen intermediates.
Pharmacology of Acetadote
Acetadote has been shown to reduce the extent of liver injury following acetaminophen overdose. It is most effective when given early, with benefit seen principally in patients treated within 8-10 hours of the overdose. Acetadote likely protects the liver by maintaining or restoring the glutathione levels, or by acting as an alternate substrate for conjugation with, and thus detoxification of, the reactive metabolite.
Additional information about Acetadote
Acetadote Indication: Used mainly as a mucolytic and in the management of paracetamol (acetaminophen) overdose.
Mechanism Of Action: Acetadote may protect against acetaminophen overdose-induced hepatotoxicity by maintaining or restoring hepatic concentrations of glutathione. Glutathione is required to inactivate an intermediate metabolite of acetaminophen that is thought to be hepatotoxic. In acetaminophen overdose, excessive quantities of this metabolite are formed because the primary metabolic (glucuronide and sulfate conjugation) pathways become saturated. Acetadote may act by reducing the metabolite to the parent compound and/or by providing sulfhydryl for conjugation of the metabolite. Experimental evidence also suggests that a sulfhydryl-containing compound such as acetylcysteine may also directly inactivate the metabolite. Inhalation - Acetadote exerts its mucolytic action through its free sulfhydryl group, which opens the disulfide bonds and lowers mucus viscosity. This action increases with increasing pH and is most significant at pH 7 to 9. The mucolytic action of acetylcysteine is not affected by the presence of DNA.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Acetylcysteine
Synonyms: N-acetylcysteine; NAC
Drug Category: Antiviral Agents; Expectorants; Free Radical Scavengers
Drug Type: Small Molecule; Approved
Other Brand Names containing Acetylcysteine: ACC; Mucomyst; Acetadote; Fluimucil; Parvolex; Lysox; Mucolysin;
Absorption: Bioavailability is 6–10% following oral administration and less than 3% following topical administration.
Toxicity (Overdose): Single intravenous doses of acetylcysteine at 1000 mg/kg in mice, 2445 mg/kg in rats, 1500 mg/kg in guinea pigs, 1200 mg/kg in rabbits and 500 mg/kg in dogs were lethal. Symptoms of acute toxicity were ataxia, hypoactivity, labored respiration, cyanosis, loss of righting reflex and convulsions.
Protein Binding: 83%
Biotransformation: Hepatic. Deacetylated by the liver to cysteine and subsequently metabolized.
Half Life: 5.6 hours (adults), 11 hours (neonates)
Dosage Forms of Acetadote: Liquid Respiratory (inhalation)
Solution Respiratory (inhalation)
Chemical IUPAC Name: (2R)-2-acetamido-3-sulfanylpropanoic acid
Chemical Formula: C5H9NO3S
Acetylcysteine on Wikipedia: http://en.wikipedia.org/wiki/Acetylcysteine
Organisms Affected: Humans and other mammals