Flavamed (ambroxol hydrochloride) tablets against cough 30 mg. №50

Description

Flavamed №50 Storage
active substance: ambroxol hydrochloride;

1 tablet contains ambroxol hydrochloride 30 mg;

Excipients: lactose monohydrate, corn starch, povidone K 30, powdered cellulose, croscarmellose sodium, magnesium stearate.

Flavamed №50 Dosage form
Tablets.

Main physical and chemical properties: round flat-parallel tablets of white color, with beveled edges and a notch for separation on one side. The tablet can be divided into two dose levels.

Flavamed №50 Pharmacotherapeutic group
Remedies used for coughs and colds. Mucolytics. ATX code R05C B06.

Pharmacological properties
Pharmacodynamics.

It has been preclinically proven that the active substance of the drug FLAVAMEDA COUGH TABLETS – ambroxol hydrochloride – increases the secretion of the respiratory glands. Ambroxol enhances pulmonary surfactant secretion by directly affecting type II pneumocytes in alveoli and Clara cells in bronchioles, and stimulates ciliary activity, thereby facilitating mucus secretion and excretion (mucociliary clearance). Improvement in mucociliary clearance has been demonstrated in clinical pharmacology studies.

Increased serous secretion and improved mucociliary clearance facilitate mucus excretion and relieve cough.

The local anesthetic effect of ambroxol hydrochloride was observed in a rabbit eye model, which may be due to the blocking properties of sodium channels. In vitro studies have shown that ambroxol hydrochloride blocks neural sodium channels; binding was reversible and concentration-dependent.

Ambroxol hydrochloride has been shown to have anti-inflammatory effects in vitro. Thus, ambroxol hydrochloride significantly reduces the release of cytokines from mononuclear and polymorphonuclear cells in the blood and tissues.

After administration of ambroxol hydrochloride, the concentration of antibiotics (amoxicillin, cefuroxime, erythromycin and doxycycline) in bronchopulmonary secretions and sputum increases. To date, no clinical significance of this fact has been identified.

Pharmacokinetics.

Absorption. Absorption of ambroxol hydrochloride from all oral immediate release forms is rapid and complete, with a linear dose-response in the therapeutic range. The peak level in blood plasma is reached in 1-2,5 hours at oral administration of dosage forms of fast release and on the average in 6,5 hours after application of forms of slow release.

Distribution. When taken orally, the distribution of ambroxol hydrochloride from blood to tissues is rapid and pronounced, with the maximum concentration of the active substance in the lungs. The expected volume of distribution when taken orally is 552 liters. In plasma in the therapeutic dose range, approximately 90% of the drug is protein bound.

Metabolism and excretion. Approximately 30% of the dose after oral administration is excreted by presystemic metabolism. Ambroxol hydrochloride is metabolized mainly in the liver by glucuronidation and cleavage to dibromanthranilic acid (approximately 10% of the dose). Studies on human liver microsomes have shown that CYP3A4 is responsible for the metabolism of ambroxol hydrochloride to dibromanthranilic acid.

After 3 days of oral administration, about 6% of the dose is excreted in the urine in free form, about 26% of the dose – in conjugated form.

The half-life from blood plasma is about 10 hours. The total clearance is approximately 660 ml / min with a renal clearance of approximately 8% of the total. After 5 days, approximately 83% of the total dose is excreted in the urine.

Pharmacokinetics in special groups of patients. In patients with impaired liver function, the excretion of ambroxol hydrochloride is reduced, which leads to 1.3-2 times higher levels in blood plasma. Because the therapeutic range of ambroxol hydrochloride is quite wide, no dosage adjustment is required.

Age and sex do not have a clinically relevant effect on the pharmacokinetics of ambroxol hydrochloride, therefore no dose adjustment is required.

Food intake does not affect the bioavailability of ambroxol hydrochloride.

Indication
Secretolytic therapy for acute and chronic bronchopulmonary diseases, accompanied by impaired bronchial secretion and impaired mucus.

Contraindication
Hypersensitivity to ambroxol hydrochloride or to any component of the drug. Due to the high content of the active substance, the drug FLAVAMED Cough Pills is contraindicated for use in children under 6 years of age. Flavamed® oral solution, 15 mg / 5 ml or Flavamed® forte, oral solution 30 mg / 5 ml is recommended for children under 6 years of age.