Lazolvan solution for infusions 15 mg/2 ml. ampoules №10

Description

Lazolvan solution Storage
active substance: ambroxol hydrochloride (ambroxol hydrochloride);

1 ampoule contains ambroxol hydrochloride 15 mg;

excipients: citric acid, monohydrate (E 330); sodium hydrogen phosphate, dihydrate; sodium chloride; water for injections.

Lazolvan solution Dosage form
Solution for infusion.

Basic physical and chemical properties: transparent, colorless solution, practically free of particles.

Lazolvan solution Pharmacotherapeutic group
Remedies used for coughs and colds. Mucolytics. ATX code R05C B06.

Lazolvan solution Pharmacological properties
Pharmacodynamics.

Ambroxol hydrochloride, substituted by benzylamine, is a metabolite of bromhexine. It differs from bromhexine by the absence of a methyl group and the presence of a hydroxyl group in the para-trans position of the cyclohexyl ring.

Ambroxol has a secretolytic and secretomotor effect in the bronchial tract.

In preclinical studies, it increased the proportion of the serous component of bronchial secretion. Ambroxol helps to remove mucus by reducing the viscosity and activating the ciliary epithelium.

Ambroxol activates the surfactant system by directly affecting type II pneumocytes in the alveoli and Clara cells in the small airway. It enhances the formation and excretion of surfactant material in the alveoli and bronchial tree of the fetus and adult body. These effects have been demonstrated in various species on cell cultures and in vivo.

In addition, the antioxidant effects of ambroxol have been demonstrated in various preclinical studies.

Pharmacokinetics.

When administered intravenously, the bioavailability of the drug by definition is 100%. After intravenous administration, the kinetics of ambroxol in the therapeutic range of application is 15 – 90 mg with a linear dose dependence, and even with intravenous administration of 1.0 g there are no significant deviations from the linearity of the dose.

Distribution

Approximately 85% (80-90%) of the drug is bound to plasma proteins. In lung tissue, ambroxol reaches a higher concentration than in blood plasma when administered parenterally. Ambroxol can enter the cerebrospinal fluid through the placental barrier and is excreted in breast milk.

Biotransformation

The formation of metabolites capable of penetrating the kidneys (eg, dibromanthranilic acid, glucuronide) occurs in the liver.

Breeding

Almost 90% of the drug is excreted by the kidneys in the form of metabolites formed in the liver. Less than 10% of ambroxol is excreted unchanged by the kidneys. Due to the high degree of protein binding, large volume of distribution and slow redistribution of the drug from tissues into the blood during dialysis or forced diuresis, significant excretion of ambroxol is unlikely.

The terminal half-life from plasma is 7-12 hours. The plasma half-life of ambroxol and its metabolites is approximately 22 hours.

Patients with impaired liver and kidney function

In patients with severe hepatic impairment, the clearance of ambroxol is reduced by 20-40%. Accumulation of ambroxol metabolites should be considered in patients with severe renal impairment.

Children

In neonates re-administered intravenously with ambroxol, the half-life was approximately doubled, indicating reduced clearance.

Indication
To enhance the production of pulmonary surfactant in premature infants and newborns with respiratory failure syndrome.

Contraindication
Known hypersensitivity to ambroxol hydrochloride or other components of the drug.