Fluifort Mechanism of Action

Pharmacology: Mechanism of Action: Carbocysteine monohydrate lysine salt restores in a dose-dependent manner the viscosity and elasticity of the mucous secretions at the level of the upper and lower airways. The drug efficacy in normalizing the mucous secretions seems to be due to the capacity of increasing the synthesis of sialomucins, thus restoring the equilibrium between sialo- and fuco-mucins, a fundamental element that contributes to the fluidity of mucus.
Moreover, carbocysteine monohydrate lysine salt stimulates the secretion of chloride ions in the epithelium of the airways, a phenomenon which is associated with the transport of water and, thus, with the fluidification of mucus. In the rabbit, oral administration of carbocysteine monohydrate lysine salt prevents the reduction of mucociliary transport determined by the intratracheal instillation of exogenous elastase.
Carbocysteine monohydrate lysine salt increases in a dose-dependent manner the concentration of lactoferrin, lysosome and alpha1-antichymotrypsin, indicating a functional resumption of the serum cells of peribronchial glands and of their mechanisms of proteic synthesis.
Carbocysteine monohydrate lysine salt has demonstrated a positive effect on the production of nasal secretory and tracheobronchial IgA.
Furthermore, carbocysteine monohydrate lysine salt improves the mucociliary clearance and the diffusibility of the antibiotic.
Pharmacokinetics: After oral administration, carbocysteine monohydrate lysine salt is quite completely and rapidly absorbed. The absorption peak occurs in 1.5-2 hours. The plasma half-life is about 1.5 hours. The elimination of carbocysteine monohydrate lysine salt and of its metabolites mainly occurs through the kidneys. The product is excreted unchanged in the urine for 30-60% of the administered dose; the remainder is excreted in the form of various metabolites.
As for all derivatives with a blocked thiolytic group, carbocysteine monohydrate lysine salt specifically fixes to the bronchopulmonary tissue. The drug achieves median concentrations of 3.5 µg/ml in the mucus, with a half-time of about 1.8 hours (2 g/day dose).
The bioavailability of carbocysteine is not affected by the different pharmaceutical forms.