Source: Medicines Authority (MT) Revision Year: 2017 Publisher: Dompé farmaceutici S.p.A., Via San Martino, 12, 20122 Milano, Italy
Pharmacotherapeutic class: Preparations for cough and cooling diseases; expectorants except for combinations with cough sedatives, mucolytic drugs
ATC code: R05CB03
Carbocysteine lysine salt monohydrate restores the viscosity and elasticity of the mucous secretions at the upper and lower airways in a dose-dependent manner. Its efficacy in normalizing the mucous secretions seems to be due to the capacity of increasing the synthesis of sialomucins thus restoring the equilibrium between sialomucins and fucomucins, it being a basic element that contributing to the fluidity of mucus.
Carbocysteine lysine salt monohydrate moreover stimulates the secretion of chloride ions in the epithelium of the airways: such phenomenon is associated with the transport of water and, thus, with the fluidification of mucus. In the rabbit, the oral administration of carbocysteine lysine salt monohydrate prevents the reduction of the mucociliary transport determined by the intratracheal instillation of exogenous elastase.
Carbocysteine lysine salt monohydrate increases the concentration of lactoferrin, lisozyme and alpha1-antichymotrypsin, in a dose-dependent manner indicating a functional resumption of the serum cells of peribronchial glands and of their mechanisms of proteic synthesis.
Carbocysteine lysine salt monohydrate has demonstrated a positive effect on the production of nasal and tracheobronchial secretory IgA.
Carbocysteine lysine salt monohydrate furthermore improves the mucociliary clearance and the diffusability of the antibiotics.
After oral administration, carbocysteine lysine salt monohydrate is absorbed quite completely and rapidly. The absorption peak occurs in 1.5-2 hours. The plasmatic half-life is about 1.5 hours. The elimination of carbocysteine lysine salt monohydrate and of its metabolites mainly occurs through the kidney. The product is secreted as such in the urines for 30-60% of the given dose, the remaining part is secreted in form of various metabolites.
As all derivatives with blocked thiolytic group, carbocysteine monohydrate lysine salt monohydrate specifically fixes itself to the bronchopulmonary tissue. The drug achieves in the mucus average concentrations of 3.5 µg/ml, with a half-time of about 1.8 hours (2 g/day dose).
The bioavailability of carbocysteine is not affected from the various different pharmaceutical forms.
Acute, subacute and chronic toxicity studies have not evidence any toxicity at dosages remarkably greater than the recommended therapeutical ones (DL50 in mg/kg: mouse and rat i.p. >5760; mouse and rat orally >13500. Non toxic doses in the chronic studies: 3 months dog orally = 300 mg/kg/day; 6 months rat orally = 500 mg/kg/day). Teratogenic studies on two animal species (rat and rabbit) did not evidence organogenetic anomalies. Reproductive toxicity studies in the rat demonstrated that carbocysteine lysine salt monohydrate does not interfere with the fertility, reproduction, embryo-fetal and postnatal development. The product is chemically not correlated with cancerogenic products and has turned out not to be mutagenic in “in vitro” and “in vivo” genotoxicity tests.
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