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Medically reviewed by Kovalenko Svetlana Olegovna, PharmD. Last updated on 26.06.2023
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Studies have shown that ambroxol is the active ingredient of A-Phyl® - increases the secretion in the respiratory tract. It enhances the production of pulmonary surfactant and stimulates ciliary activity. These effects lead to increased mucus flow and transport (mucociliary clearance). Increased mucociliary clearance improves sputum discharge and relieves cough. In patients with COPD, long-term therapy with A-Phyl® (for at least 2 months) resulted in a significant reduction in the number of exacerbations. There was a significant decrease in the duration of exacerbations and the number of days of antibiotic therapy.
The effect occurs 30 minutes after administration and lasts 6-12 hours.
Increasing the content of mucosal secretions, changes the disturbed ratio of serous and mucosal components of sputum, increases the release of lysosomes (from Clark cells), leading to a decrease in the viscosity of sputum
All immediate-release ambroxol dosage forms are characterized by rapid and almost complete absorption with a linear dose dependence in the therapeutic concentration range. Cmax when taken orally is reached after 1-2. 5 hours.
Vd-552 l. In the therapeutic range of concentrations, binding to plasma proteins is approximately 90%.
The transition of ambroxol from the blood to the tissues with oral administration is rapid. The highest concentrations of the active component of the drug are observed in the lungs.
Approximately 30% of the oral dose is exposed to the effect of primary passage through the liver. Studies on human liver microsomes have shown that the CYP3A4 isoenzyme is the predominant isoform responsible for the metabolism of ambroxol to dibromantranilic acid. The remaining part of ambroxol is metabolized in the liver, mainly by glucuronidation and partial cleavage to dibromantranilic acid (approximately 10% of the administered dose), as well as a small amount of additional metabolites.
Terminal T1/2 of ambroxol is 10 h. The total clearance is in the range of 660 ml / min, the renal clearance accounts for approximately 8% of the total clearance. Using a radioactive label, it was estimated that after taking a single dose of the drug for the next 5 days, about 83% of the dose is excreted in the urine. There was no clinically significant effect of age and gender on the pharmacokinetics of ambroxol, so there is no reason to select a dosage based on these signs.
- Secretolytics and stimulants of motor function of the respiratory tract
Increases the penetration of amoxicillin, cefuroxime, erythromycin and doxycycline into the bronchial secretions. Simultaneous use with antitussive agents leads to difficulty in the discharge of sputum. It is compatible with drugs that inhibit labor activity.
