Source: Υπουργείο Υγείας (CY) Revision Year: 2021 Publisher: Chiesi Hellas A.E.B.E., Geroulanou sq & 1, Renou Poggi str., 17455 Alimos, Greece
Pharmaceutical group: Mucolytic
ATC code: R05CB06
Ambroxol acts by regularizing mucus secretion transportation throughout the respiratory tree. Moreover, it owns a marked mucolytic and mucoregulating activity. Its pharmacological effect is exerted on mucus quality, ciliary functionality and production of alveolar surfactant.
Mucus quality: ambroxol stimulates the activity of serous gland cells, discharges the formed granules of mucus, normalizes mucus viscosity and finally regulates the activity of the respiratory tree tubuloalveolar glands.
Ciliary functionality: ambroxol increases both the number of the microvilli in the vibratile epithelium, and the ciliary movements rate, with a consequent enhancement of transportation speed of the produced mucus, and finally leads to normalization of respiratory parameters, thus improving expectoration.
Increase of surfactant production: ambroxol stimulates type II pneumocytes to a higher production of alveolar surfactant, thus ensuring pulmonary tissue stability, allowing a correct bronchiolar and alveolar purification and, finally, improving the respiratory mechanics and favouring gas-exchanges.
Ambroxol bioavailability was assessed in humans after oral administration of the drug in healthy volunteers. Ambroxol was deduced to be rapidly absorbed through the intestinal tract. Its half life is 10 hours approximately, and the maximum serum levels are reached around the 2nd hour. The drug is almost completely eliminated by renal route either in the form of metabolites or as unchanged.
For the sustained release capsules the active ingredient is gradually absorbed, with peak levels obtained around the 4th hour (139 ng/ml). At the 24th hour the plasma level is still higher than 25 ng/ml.
Suppositories have a 60% bioavailability compared to the oral route.
Acute toxicity: Fluibron acute toxicity, evaluated on small animals, showed to be very low (LD50/os in mice = 2842 mg/kg; LD50/os in rats >4000 mg/kg).
Chronic toxicity: the evaluation of the considered parameters shows that Fluibron is endowed with a good systemic and local tolerability. Particularly, no impairements of main biochemical and hematic parameters were observed; no lesions on the main organs taken into consideration and no modifications of their functionality occurred.
Teratogenic activity: Fluibron has no teratogenic activity, as confirmed by tests in pregnant rats and rabbits.
Mutagenic activity: the usual mutagenic tests did not show any mutagenic activity of Fluibron.
Influence on the various organs and apparatuses: Fluibron was proven not to cause any significant variations of left ventricular pressure, blood femural pressure, ECG and heart rate in awake dogs. Similarly, at the doses of 160 mg/kg/os and 40 mg/kg/s.c., Fluibron did not show any action on the peristaltic activity in dogs.
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