Ambrobene, 7.5 mg/ml 100 ml

Pharmacotherapeutic group: Extractive mucolytic agent.

ATX code: R05CB06

Pharmacological action

Pharmacodynamics. Ambroxol is a benzylamine, a metabolite of bromhexine. It differs from bromhexin by the absence of a methyl group and the presence of a hydroxyl group in the para-trans position of the cyclohexyl ring. It has secretomotor, secretolytic and expectorant action.

After oral administration the action starts within 30 minutes and lasts for 6-12 hours (depending on the dose taken).

Preclinical studies have shown that ambroxol stimulates serous gland cells of the bronchial mucosa. By activating cells of the ciliated epithelium and reducing the viscosity of sputum, ambroxol improves mucociliary transport.

Ambroxol activates surfactant formation with a direct effect on alveolar type 2 pneumocytes and small airway Clara cells.

Studies on cell cultures and in vivo animal studies have shown that ambroxol stimulates the formation and secretion of a substance (surfactant) active on the surface of the alveoli and bronchi of the embryo and adult.

An antioxidant effect of ambroxol has also been proven in preclinical studies. Ambroxol when used together with antibiotics (amoxicillin, cefuroxime, erythromycin, doxycycline) increases their concentration in sputum and bronchial secretion.

Pharmacokinetics. Ambroxol is almost completely absorbed from the gastrointestinal tract when taken orally. Maximum concentration is reached 1 to 3 hours after oral administration. Due to presystemic metabolism absolute bioavailability of ambroxol after oral administration is reduced by approximately ⅓. The resulting metabolites (such as dibromanthranilic acid, glucuronides) are eliminated in the kidneys. Binding to plasma proteins is about 85% (80-90%). The plasma elimination half-life is 7 to 12 hours. The total half-life of ambroxol and its metabolites is approximately 22 hours.

It is excreted mainly by the kidneys as metabolites – 90%, less than 10% is excreted unchanged.

Given its high plasma protein binding, large volume of distribution and slow redistribution from the tissues into the blood, there is no significant excretion of ambroxol with dialysis or forced diuresis.

In patients with severe liver disease ambroxol clearance is reduced by 20-40%. In patients with severe renal impairment the half-life of ambroxol metabolites is prolonged.

Ambroxol penetrates the cerebrospinal fluid and through the placental barrier, and is excreted in breast milk.

Indications

Colds, Chronic Obstructive Pulmonary Disease, Tracheitis, Bronchitis, Sinusitis, Lung Inflammation (pneumonia), Cough, Bronchial Asthma, Influenza Acute and chronic respiratory diseases accompanied by impaired sputum formation and discharge.

Active ingredient

Ambroxol

Composition

Contents of the preparation: Active substance: ambroxol hydrochloride 0.750 g; Excipients: potassium sorbate 0.100 g, hydrochloric acid (25%) 0.060 g, purified water 99.190 g.

How to take, the dosage

Internal administration

Overly, the drug is taken after meals, added to water, juice or tea using the supplied measuring cup.

Children under 2 years of age should take 1 ml of the drug twice a day (15 mg ambroxol per day).

Children from 2 to 6 years should take 1 ml of the drug 3 times a day (22.5 mg ambroxol per day).

Children from 6 to 12 years should take 2 ml of the drug 2-3 times a day (30-45 mg ambroxol per day).

Adults and children over 12 years in the first 2-3 days of treatment should take 4 ml of the drug 3 times a day (90 mg ambroxol per day). If therapy is ineffective, adults may increase the dose to 8 ml of the drug 2 times a day (120 mg ambroxol per day). On subsequent days, 4 ml of the drug 2 times a day (60 mg ambroxol per day) should be taken.

Application of the drug in the form of inhalation

When using Ambrobene in the form of inhalation any modern equipment (except steam inhalers) may be used. Before inhalation the drug is mixed with 0.9% sodium chloride solution (for optimal air moistening it can be diluted in 1:1 ratio) and heated to body temperature. Since deep inhalation therapy may provoke coughing jolts, inhalation should be carried out in normal breathing mode. Patients with bronchial asthma may be advised to inhale after taking bronchodilators.

The following dosages are used for inhalation (1 ml of solution contains 7.5 mg of ambroxol):

children under 2 years of age: 1 ml of solution 1-2 times a day (7.5-15 mg ambroxol per day);

children from 2 to 6 years: 2 ml of solution 1-2 times daily (15-30 mg ambroxol per day);

children over 6 years of age and adults: 2-3 ml of solution 1-2 times daily (15-45 mg ambroxol per day).

The duration of treatment is chosen individually depending on the course of the disease. It is not recommended to take the drug Ambrobene without a doctor’s prescription for more than 4-5 days.

The mucolytic effect of the drug is manifested when taking a large amount of fluid, so during the treatment it is recommended to drink plenty of fluids.

Interaction

In concomitant use of ambroxol and cough suppressants, cough reflex inhibition may result in secretion stasis. Such combinations should be chosen with caution.

When ambroxol and antibiotics amoxicillin, cefuroxime, erythromycin and doxycycline are taken together, the concentration of the latter in sputum and bronchial secretion increases.

Special Instructions

It should not be combined with anti-cough drugs that make it difficult to expectorate sputum.

In children under 2 years of age the use of the drug is possible only by prescription. Severe skin reactions, such as Stevens-Johnson syndrome and Lyell syndrome, have been extremely rarely observed when using ambroxol. In case of changes in the skin or mucous membranes it is necessary to consult a doctor urgently and stop taking the drug.

Influence on the ability to drive vehicles, machinery

There have been no studies about the effect of the drug Ambrobene on the ability to drive vehicles and operate machinery. In case of side effects, caution should be exercised when performing activities requiring high concentration and quick psychomotor reactions.

Synopsis

Transparent colorless to slightly yellowish-brown solution.

Contraindications

Hypersensitivity to ambroxol or to one of the excipients; pregnancy (I trimester).

With caution

Bronchial motor dysfunction and increased sputum production (in immobile cilia syndrome), gastric and duodenal ulcer during exacerbation, pregnancy (II-III trimester), breast-feeding period.

Patients with impaired renal function or severe liver disease should take Ambrobene with extreme caution, observing long intervals between doses or taking the drug in a smaller dose.