Description

Simple

A medication used to thin the mucus in certain lung conditions, and also as an antidote for acetaminophen overdose.

Clinical

A medication that can be used as a mucolytic in patients with certain lung conditions and as an antidote for acetaminophen overdose.

Overview

Acetylcysteine (also known as N-acetylcysteine or N-acetyl-L-cysteine or NAC) is primarily used as a mucolytic agent and in the management of acetaminophen poisoning. It is a derivative of cysteine with an acetyl group attached to the amino group of cysteine. NAC is essentially a prodrug that is converted to cysteine (in the intestine by the enzyme aminoacylase 1) and absorbed in the intestine into the blood stream. Cysteine is a key constituent to glutathione and hence administration of acetylcysteine replenishes glutathione stores. Acetylcysteine can also be used as a general antioxidant which can help mitigate symptoms for a variety of diseases exacerbated by reactive oxygen species (ROS). For instance, acetylcysteine is commonly used in individuals with renal impairment to prevent the precipitation of acute renal failure. Acetylcysteine has been shown to have efficacy in treating mild to moderate traumatic brain injury including ischemic brain injury, particularly in reducing neuronal losses, and also reducing cognitive and neurological symptoms when administered promptly after injury. N-acetylcysteine is now widely used in the treatment of HIV, and it has reported efficacy in chronic obstructive pulmonary disease and contrast-induced nephropathy. Acetylcysteine is also being successfully used to treat a variety of neuropsychiatric and neurodegenerative disorders including cocaine, cannabis, and smoking addictions, Alzheimer's and Parkinson's diseases, autism, compulsi... Read more

Pharmacology

Indication

Acetylcysteine is used mainly as a mucolytic and in the management of paracetamol (acetaminophen) overdose.

Pharmacodynamic

Acetylcysteine 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. Acetylcysteine likely protects the liver by maintaining or restoring the gl... Read more

Mechanism of action

Acetylcysteine protects against acetaminophen overdose-induced hepatotoxicity by maintaining or restoring hepatic concentrations of glutathione. It does this by producing the glutathione precursor L-cysteine. Glutathione is required to inactivate an intermediate metabolite (N-acetyl-p-benzoquinoneim... Read more

Absorption

Bioavailability is 6–10% following oral administration and less than 3% following topical administration.

Protein binding

83%

Volume of distribution

Information currently not available.

Clearance

Information currently not available.

Half life

5.6 hours (adults), 11 hours (neonates)

Route of elimination

Information currently not available.

Toxicity

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.

Adverse Effects

Contraindications

Information currently not available.

Food Interactions

    Information currently not available.

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
Ambrisentan
The excretion of Ambrisentan can be decreased when combined with Acetylcysteine.
Asunaprevir
The excretion of Asunaprevir can be decreased when combined with Acetylcysteine.
Atorvastatin
The excretion of Atorvastatin can be decreased when combined with Acetylcysteine.
Atrasentan
The excretion of Atrasentan can be decreased when combined with Acetylcysteine.
Axitinib
The excretion of Axitinib can be decreased when combined with Acetylcysteine.
Benzylpenicillin
The excretion of Benzylpenicillin can be decreased when combined with Acetylcysteine.
Bosentan
The excretion of Bosentan can be decreased when combined with Acetylcysteine.
Caspofungin
The excretion of Caspofungin can be decreased when combined with Acetylcysteine.
Cerivastatin
The excretion of Cerivastatin can be decreased when combined with Acetylcysteine.
Cholecystokinin
The excretion of Cholecystokinin can be decreased when combined with Acetylcysteine.
Cholic Acid
The excretion of Cholic Acid can be decreased when combined with Acetylcysteine.
Cobimetinib
The excretion of Cobimetinib can be decreased when combined with Acetylcysteine.
Conjugated estrogens
The excretion of Conjugated estrogens can be decreased when combined with Acetylcysteine.
Digoxin
The excretion of Digoxin can be decreased when combined with Acetylcysteine.
Dinoprostone
The excretion of Dinoprostone can be decreased when combined with Acetylcysteine.
Elagolix
The excretion of Elagolix can be decreased when combined with Acetylcysteine.
Eluxadoline
The serum concentration of Eluxadoline can be increased when it is combined with Acetylcysteine.
Enalapril
The excretion of Enalapril can be decreased when combined with Acetylcysteine.
Erythromycin
The excretion of Erythromycin can be decreased when combined with Acetylcysteine.
Ezetimibe
The excretion of Ezetimibe can be decreased when combined with Acetylcysteine.
6 References
  1. 1 . Bachert C, Hormann K, Mosges R, Rasp G, Riechelmann H, Muller R, Luckhaupt H, Stuck BA, Rudack C: An update on the diagnosis and treatment of sinusitis and nasal polyposis. Allergy. 2003 Mar;58(3):176-91.PubMed: 12653791
  2. 2 . Bailey B, McGuigan MA: Management of anaphylactoid reactions to intravenous N-acetylcysteine. Ann Emerg Med. 1998 Jun;31(6):710-5.PubMed: 9624310
  3. 3 . Breitkreutz R, Pittack N, Nebe CT, Schuster D, Brust J, Beichert M, Hack V, Daniel V, Edler L, Droge W: Improvement of immune functions in HIV infection by sulfur supplementation: two randomized trials. J Mol Med (Berl). 2000;78(1):55-62.PubMed: 10759030
  4. 4 . Dawson AH, Henry DA, McEwen J: Adverse reactions to N-acetylcysteine during treatment for paracetamol poisoning. Med J Aust. 1989 Mar 20;150(6):329-31.PubMed: 2716644
  5. 5 . Fulghesu AM, Ciampelli M, Muzj G, Belosi C, Selvaggi L, Ayala GF, Lanzone A: N-acetyl-cysteine treatment improves insulin sensitivity in women with polycystic ovary syndrome. Fertil Steril. 2002 Jun;77(6):1128-35.PubMed: 12057717
  6. 6 . Jones AL: Mechanism of action and value of N-acetylcysteine in the treatment of early and late acetaminophen poisoning: a critical review. J Toxicol Clin Toxicol. 1998;36(4):277-85.PubMed: 9711192