Pharmacotherapeutic group: Mucolytic. ATC code: R05CB03.
Pharmacology: Pharmacodynamics: Carbocisteine (S-carboxymethyl L-cysteine) is a mucolytic agent. It has been shown in normal and bronchitic animal models to affect the nature and amount of mucus glycoprotein which is secreted by the respiratory tract. An increase in the acid:neutral glycoprotein ratio of the mucus and a transformation of serous cells to mucus cells is known to be the initial response to irritation and will normally be followed by hypersecretion. Carbocisteine serves to restore equilibrium between sialomucins and fucomucins, likely by intracellular stimulation of sialyl transferase enzyme, thus reducing mucus viscosity.
Several studies have demonstrated that carbocisteine reduces goblet cell hyperplasia. Carbocisteine can therefore be demonstrated to have a role in the management of disorders characterised by abnormal mucus.
Pharmacokinetics: Absorption: Carbocisteine is rapidly absorbed in the gastrointestinal tract when taken orally with peak serum concentrations achieved within 1 to 1.7 hours (plasma half-life 1.33 hour).
Distribution: Vd: ~60 to 105 L; distributed to lungs and respiratory mucous.
Metabolism: Multiple metabolic pathways leading to multiple metabolites may be involved, including glucuronidation, N-acetylation, and sulfoxidation. Metabolism may vary due to circadian rhythm and genetic polymorphisms
Excretion: Excrete via urine as a primary route; about 30% to 60% of an orally administered dose is detected unchanged.
Bioavailability: Up to 17.5% of administered dose can be found in the bronchial secretions.
Toxicology: Preclinical safety data: Not applicable.
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