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Acetylcysteine

*Acetylcysteinum*

For medical students2 min readUpdated 2026-10-10

Acetylcysteine is an effective mucolytic agent derived from the amino acid cysteine. The drug liquefies sputum by breaking disulfide bonds, exhibits prominent antioxidant properties, and serves as a specific antidote for acetaminophen (paracetamol) overdose.

BioavailabilityLess than 10% following oral administration due to the hepatic first-pass effect.
Onset & DurationThe latent period is 30–90 minutes, with a duration of action of 2–4 hours.
CautionIntravenous administration in patients with bronchial asthma carries a high risk of bronchospasm.
StructureA derivative in which one hydrogen atom of the amino group is replaced by an acetic acid residue.

Chemical Nature and Mechanism of Action

Chemically, the drug is N-acetyl-L-cysteine.

The primary pharmacological property of the drug is its mucolytic effect, which occurs via two pathways:

  1. Direct effect on sputum structure. The molecule contains free sulfhydryl (-SH) groups. These groups are capable of cleaving disulfide bonds in the proteoglycans of bronchial secretions. This leads to the depolymerization of macromolecules, sharply decreasing sputum viscosity and adhesiveness.
  2. Additional effects. The drug stimulates the secretion of mucous cells, increasing the total volume of secretions. Additionally, it causes fibrin lysis, which is particularly important in the presence of purulent or fibrinous sputum.

Systemic Effects: Antioxidant and Antidote

In addition to its effects on the respiratory tract, the drug possesses important systemic properties:

Pharmacokinetics and Administration Routes

The drug is available in various pharmaceutical formulations, determining its route of administration:

Following oral administration, absorption is rapid and complete. However, the final systemic bioavailability remains low (not exceeding 10%). This is due to a pronounced first-pass effect in the liver, where the molecule is deacetylated into regular cysteine.

Indications, Contraindications, and Safety

Main indications for use:

Safety profile and side effects: Therapy may cause dyspeptic symptoms (nausea and vomiting), allergic reactions such as urticaria, and tinnitus.

Absolute contraindications:

Drug Interactions

When prescribing, it is essential to consider pharmaceutical and pharmacological compatibility:

Mnemonic

To easily remember the mechanism of action, picture "SH-scissors": the free sulfhydryl (-SH) groups of acetylcysteine literally "cut" the disulfide bridges in thick mucus, turning it into a fluid.

Frequently asked questions

What is the dosing regimen for acetylcysteine in acute acetaminophen poisoning?

For drug-induced liver injury, including acetaminophen overdose, a stepped intravenous infusion protocol of the antidote is used.

The dosing protocol includes the following stages:

  • Loading dose — 150 mg/kg (infused over 1 hour).
  • Intermediate dose — 12.5 mg/kg/h (infused over 4 hours).
  • Maintenance dose — 6.25 mg/kg/h (infused over 16 hours).

This administration regimen significantly improves patient survival without the need for liver transplantation and shortens overall hospitalization time.

What metabolites are formed during the biotransformation of acetylcysteine in the liver?

When taken orally, acetylcysteine undergoes deacetylation in the liver to form cysteine. The drug's bioavailability is low, remaining at no more than 10% due to the hepatic first-pass effect.

Why is acetylcysteine lifesaving in acetaminophen poisoning?

It acts as a donor for glutathione synthesis. Glutathione is required for the endogenous detoxification of acetaminophen metabolites, preventing severe liver injury (hepatotoxicity).

Can antibiotics be taken with this mucolytic solution?

No, it significantly decreases the absorption of penicillins, cephalosporins, and tetracyclines. An interval of at least two hours must be maintained between administration of these drugs.

Why does the drug solution sometimes develop an unpleasant odor?

Contact of the solution with metals (such as iron or copper) or rubber triggers a chemical reaction resulting in the formation of sulfides, which produce the characteristic odor.

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