Ambroxol retard

• Secretolytics and stimulants of motor function of the respiratory tract

R05CB06 Ambroxol

Ambroxol retard

Ambroxol

Long-acting capsules

Acute and chronic diseases of the respiratory tract, accompanied by a violation of the formation and discharge of sputum.

Inside, inhaled, in/in.

The duration of treatment is selected individually, depending on the course of the disease. It is not recommended to take Ambroxol retard 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 liquid. Therefore, during treatment, it is recommended to drink plenty of water.

Pills

Inside, after eating, swallowing whole, without chewing, with plenty of liquid.

Children from 6 to 12 years old: 1/2 table 2-3 times a day (15 mg of ambroxol 2-3 times a day).

Adults and children over 12 years of age: in the first 2-3 days of treatment — 1 table. 3 times a day (30 mg of ambroxol 3 times a day). If the therapy is ineffective, adults can increase the dose to 2 tablets. 2 times a day (120 mg of ambroxol per day). In the following days, you should take 1 tablet. 2 times a day (30 mg ambroxol 2 times a day).

Long-acting capsules

Inside, after eating, swallowing whole, without chewing, with plenty of liquid.

Adults and children over 12 years of age: 1 capsule per day (75 mg ambroxol per day).

Syrup

Inside, after eating, using the supplied measuring cup.

For children: up to 2 years — 1/2 measuring cup (2.5 ml of syrup) 2 times a day (15 mg of ambroxol per day), from 2 to 6 years — 1/2 measuring cup (2.5 ml of syrup) 3 times a day (22.5 mg of ambroxol per day), from 6 to 12 years — 1 measuring cup (5 ml of syrup) 2-3 times a day (30-45 mg of ambroxol per day).

Adults and children over 12 years of age: in the first 2-3 days of treatment — 2 measuring cups (10 ml of syrup) 3 times a day (90 mg of ambroxol per day). If the therapy is ineffective, adults can increase the dose to 4 measuring cups (20 ml of syrup) 2 times a day (120 mg of ambroxol per day). In the following days, you should take 2 measuring cups (10 ml of syrup) 2 times a day (60 mg of ambroxol per day).

Solution for oral administration and inhalation

Inside, after eating, adding to water, juice, or tea using the supplied measuring cup.

For children: up to 2 years — 1 ml, 2 times a day (15 mg Ambroxol per day), from 2 to 6 years — 1 ml 3 times a day (22.5 mg Ambroxol per day), from 6 to 12 years: 2 ml of the drug 2-3 times a day (30-45 mg of Ambroxol per day).

Adults and children over 12 years of age: in the first 2-3 days of treatment — 4 ml of the drug 3 times a day (90 mg of ambroxol per day). If the therapy is ineffective, adults can increase the dose to 8 ml of the drug 2 times a day (120 mg of ambroxol per day). In the following days, you should take 4 ml of the drug 2 times a day (60 mg of ambroxol per day).

Inhaled. When using Ambroxol retard in the form of inhalations, you can use any modern equipment (except steam inhalers). Before inhalation, the drug is mixed with 0.9% sodium chloride solution (for optimal humidification of the air, it can be diluted in a ratio of 1:1) and is heated to body temperature. Since inhaling deep breaths can trigger coughing, inhalation should be performed in the normal breathing mode. Patients with bronchial asthma can be recommended to inhale after taking bronchodilators.

1 ml of the solution contains 7.5 mg of ambroxol.

For children: up to 2 years — 1 ml of the solution 1-2 times a day (7.5-15 mg of ambroxol per day), from 2 to 6 years — 2 ml of the solution 1-2 times a day (15-30 mg of ambroxol per day).

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

Solution for intravenous administration

V/v, slow, jet, or drip. As a solvent, use 0.9% sodium chloride solution, 5% glucose solution, Ringer-Locke solution or other basic solution with a pH not higher than 6.3.

The daily dose is 30 mg / kg, evenly distributed over 4 injections per day.

The solution should be administered in / in, slowly, for at least 5 minutes.

Injections are discontinued after the disappearance of acute manifestations of the disease and switch to oral administration of other dosage forms of the drug.

hypersensitivity to ambroxol or one of the excipients,

pregnancy (I trimester).

Optional for tablets

children under 6 years of age,

lactose intolerance, lactase deficiency, glucose-galactose malabsorption.

Optional for long-acting capsules

children under 12 years of age.

In addition to syrup

sucrose/isomaltase deficiency, fructose intolerance, glucose-galactose malabsorption.

With caution: violation of the motor function of the bronchi and increased sputum formation (with the syndrome of fixed cilia), pregnancy (II-III trimester), lactation - for all dosage forms, gastric ulcer and duodenal ulcer during exacerbation - for oral dosage forms.

Patients with impaired renal function or severe liver disease should take Ambroxol retard with extreme caution, observing long intervals between doses or taking the drug at a lower dose.

Tablets, long-acting capsules, syrup

General violations: rarely (from ≥0.1% to <1%) — allergic reactions (urticaria, skin rash, angioedema of the face, shortness of breath, itching), fever, weakness, headache, very rarely (<0.01%) — anaphylactic reactions, including anaphylactic shock.

From the gastrointestinal tract: rarely — nausea, abdominal pain, vomiting, diarrhea, constipation.

Other: rarely — dry mucous membranes of the oral cavity and respiratory tract, exanthema, runny nose, dysuria.

Solution for oral administration and inhalation

The frequency of side effects is classified according to WHO recommendations: very common (≥10%), common (≥1%, but <10%), infrequent (≥0.1%, but <1%), rare (≥0.01%, but <0.1%), very rare (<0.01%).

On the part of the immune system: infrequently-hypersensitivity reaction, the frequency is not established-anaphylactic reactions, including rash, itching, urticaria, angioedema, anaphylactic shock.

From the nervous system: often-a violation of taste perception.

From the gastrointestinal tract: often-nausea, infrequently-dryness of the mucous membrane of the mouth and throat, vomiting, dyspepsia, abdominal pain, diarrhea.

Solution for intravenous administration

General violations: rarely (from ≥0.1% to <1%) — allergic reactions (skin rash, facial edema, shortness of breath, itching), fever, very rarely (<0.01%) — anaphylactic reactions, including anaphylactic shock.

In rare cases, with rapid administration of the drug, severe headaches, fatigue, weakness, and venous edema were observed.

From the gastrointestinal tract: rarely — nausea, abdominal pain, vomiting.

Symptoms: there were no signs of intoxication in an overdose of ambroxol. There are reports of nervous agitation and diarrhea.

Ambroxol is well tolerated when taken orally at a dose of up to 25 mg / kg / day.

In the case of a severe overdose, increased salivation, nausea, vomiting, and a decrease in blood pressure are possible.

Treatment: intensive care methods, such as inducing vomiting, gastric lavage, should be used only in cases of severe overdose, in the first 1-2 hours after taking the drug. Symptomatic treatment is indicated.

Ambroxol is a benzylamine metabolite of bromhexine. It differs from bromhexine in 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 effects.

After oral administration, the effect occurs after 30 minutes and continues for 6-12 hours (depending on the dose taken) - for tablets, syrup and solution for oral administration and inhalation, for 24 hours - for long-acting capsules.

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

Ambroxol activates the formation of surfactant, having a direct effect on alveolar pneumocytes of type 2 and Klara cells of the small respiratory tract.

Cell culture studies and research in vivo In animals, ambroxol has been shown to stimulate the formation and secretion of a substance (surfactant) active on the surface of the alveoli and bronchi of the embryo and adult.

Also, in preclinical studies, the antioxidant effect of ambroxol was proven. Ambroxol in combination with antibiotics (amoxicillin, cefuroxime, erythromycin and doxycycline) increases their concentration in sputum and bronchial secretions.

When administered parenterally, ambroxol quickly penetrates into the tissues. The highest concentration is found in the lungs.

When ingested, ambroxol is almost completely absorbed from the gastrointestinal tract.

C_max it is reached after 1-3 hours — for tablets, syrup, solution for oral administration and inhalation and solution for intravenous administration, C_maxit is approximately 140±54 ng / ml and is reached 4 hours after oral administration-for long-acting capsules.

Due to the presystemic metabolism, the absolute bioavailability of ambroxol after oral administration is reduced by approximately 1/3. Formed in this regard metabolites (such as dibromoanisole acid, glucuronide) are eliminated in the kidneys.

Binding to plasma proteins is about 85% (80-90%). T_1/2 from the plasma is from 7 to 12 hours, the total T_1/2 ambroxol and its metabolites is approximately 22 h - for tablets, syrup, solution for oral administration and inhalation and solution for intravenous administration, T_1/2 about 18 hours — for long-acting capsules.

It is mainly excreted by the kidneys in the form of metabolites-90%, less than 10% is excreted unchanged.

Given the high binding to plasma proteins, a large V_d and slow redistribution from the tissues to the blood, significant removal of ambroxol during dialysis or forced diuresis does not occur.

In patients with severe liver diseases, ambroxol clearance decreases by 20-40%. In patients with severe renal impairment T_1/2 the metabolites of ambroxol are increased.

Ambroxol penetrates into the cerebrospinal fluid and through the placental barrier, and is also released into breast milk.

With the simultaneous use of ambroxol and antitussive agents, due to the suppression of the cough reflex, stagnation of the secretion may occur. Therefore, such combinations should be selected with caution.

With the combined administration of ambroxol and the antibiotics amoxicillin, cefuroxime, erythromycin and doxycycline, the concentration of the latter in sputum and bronchial secretions increases.

The introduction of ambroxol (pH 5) should not be combined with the introduction of other solutions with a pH greater than 6.3, since the difference between the pH values of the solutions can lead to precipitation of the ambroxol base.