Ascoril®

Ascoril - bronchodilator, mucolytic, expectorant.

Pharmacodynamics

The combined drug has a bronchodilator, expectorant and mucolytic action.

Salbutamol - bronchodilator, stimulates beta₂-adrenoreceptors of the bronchi, blood vessels and myometrium. Prevents or eliminates bronchospasm, reduces resistance in the airways, increases lung capacity. It causes the expansion of the coronary arteries, does not reduce blood pressure.

Bromhexine is a mucolytic agent, it has expectorant and antitussive action. Increases the serous component of bronchial secretions; activates the cilia of the ciliated epithelium, reduces the viscosity of sputum, increases its volume and improves the discharge.

Guaifenesin - mucolytic agent, reduces the surface tension of the structures of the bronchopulmonary apparatus; stimulates the secretory cells of the bronchial mucosa, producing neutral polysaccharides, depolymerizes the acid mucopolysaccharides, reduces the viscosity of sputum, activates the ciliary apparatus of the bronchi, facilitates the removal of sputum and promotes the transition of non-productive cough into productive.

Pharmacokinetics

Salbutamol

When ingestion absorption is high. Eating reduces the rate of absorption, but does not affect bioavailability. Communication with plasma proteins - 10%. Penetrates through the placenta. Subjected to presystemic metabolism in the liver and intestinal wall, is inactivated by phenol sulfotransferase to 4-o-sulfate ester. T_1/2 - 3.8–6 hours. Excreted by the kidneys (69–90%), mainly as an inactive phenolsulfate metabolite (60%) for 72 hours and with bile (4%). The bioavailability of orally administered salbutamol is about 50%.

Bromhexine

When administered almost completely (99%) absorbed in the digestive tract within 30 minutes. Bioavailability is low (the effect of the primary passage through the liver). It penetrates the placental barrier and the BBB. In the liver it undergoes demethylation and oxidation, it is metabolized to pharmacologically active ambroxol. T_1/2 - 15 hours (due to slow reverse diffusion from tissues). Excreted by the kidneys. When CRF is impaired excretion of metabolites. With repeated use may accumulate.

Guaifenesin

Absorption from the gastrointestinal tract is fast (25–30 minutes after ingestion). T_1/2 - 1 h. Penetrates into tissues containing acid mucopolysaccharides. Approximately 60% of the administered drug is metabolized in the liver. It is excreted by the lungs (with sputum) and kidneys, both unchanged and in the form of inactive metabolites.