Ambrobene
Ambrobene (ambroxol hydrochloride) is a drug that facilitates expectoration of sputum and has mucolytic activity. It is used in otorhinolaryngological practice for acute and chronic respiratory tract diseases, accompanied by impaired production and evacuation of sputum. Impaired removal of mucus from the respiratory tract is one of the key factors underlying the pathogenesis of inflammatory diseases of various parts of the respiratory tract. Stagnation of bronchial contents causes a deterioration in the ventilation and respiratory abilities of the lungs and an increased risk of infection. The production of secretions by the bronchi is an essential condition for the proper functioning of the respiratory system. The composition of sputum produced by the bronchi is complex and depends on the coordinated work and proper condition of a number of physiological links. Inflammation of any part of the respiratory tract (trachea, bronchi) through a compensatory mechanism increases mucus production, with which, in turn, the consistency of sputum changes in the direction of increasing viscosity. Accordingly, the more viscous the sputum, the lower the rate of its evacuation from the respiratory tract. The insufficiency of the drainage function of the ciliated epithelium of the bronchi and trachea contributes to the retention of sputum in the respiratory tract, resulting in the development of cough. In this case, taking antitussive medications will not only not improve the situation, but will also worsen it. And here drugs that facilitate sputum discharge come to the fore and, in particular, Ambrobene as one of the most effective and safe representatives of this pharmacological group.
In most clinical situations, this mucolytic agent is the best choice in the treatment of infectious and inflammatory diseases of the respiratory tract, incl. in patients of the younger age group. Ambrobene is a new generation secretolytic, which is a derivative of bromhexine and has a powerful expectorant effect. Ambrobene does not affect the production of bronchial secretions produced by mucosal cells. It thins mucus by destroying acidic mucopolysaccharides and DNA, while facilitating the passage of secretions. In addition, the drug increases the concentration of pulmonary surfactant, which improves lung compliance, which indirectly improves mucociliary transport and gives a pronounced expectorant effect. At the same time, Ambrobene does not cause bronchial obstruction. The effect of taking the drug is noticeable within half an hour. It is dose-dependent and is maintained at a clinically significant level for another 6-12 hours. Ambroxol is also an antioxidant that protects the cells of the respiratory tract from the aggressive effects of free radicals. Simultaneous use of antitussive drugs with Ambrobene is contraindicated, because in this case, the cough reflex will be suppressed, which will lead to stagnation of sputum in the respiratory tract.
Ambrobene syrup
Release form
Syrup: a clear, colorless to slightly yellow solution with a raspberry odor.
Compound
Active ingredients : ambroxol hydrochloride (0.30 g/100 ml).
Excipients : liquid sorbitol 70%; propylene glycol; raspberry flavor; saccharin; purified water .
Pharmacological group
Mucolytic and expectorant drug. Secretolytics and stimulants of motor function of the respiratory tract.
Action
Mucolytic agent with expectorant action. Ambroxol increases the secretion of the glands of the respiratory tract, stimulates the activity of the villi of the respiratory tract, and enhances the formation of surfactant in the lungs. Ambroxol is a metabolite of bromhexine.
Ambroxol - description of the substance
The effect occurs 30 minutes after administration and lasts 6-12 hours.
Indications
Acute and chronic diseases of the respiratory tract, accompanied by impaired formation and discharge of sputum.
Contraindications and restrictions
- Hypersensitivity to ambroxol or one of the excipients;
- Pregnancy (first trimester);
- Sucrase/isomaltase deficiency, fructose intolerance, glucose-galactose malabsorption.
Carefully:
- impaired bronchial motor function and increased sputum production (with immotile cilia syndrome);
- pregnancy (II–III trimester), lactation period;
- peptic ulcer of the stomach and duodenum during an exacerbation;
- impaired renal function or severe liver disease.
Application and dosage
Inside , after meals, using the included measuring cup.
Children: up to 2 years old - 1/2 measuring cup (2.5 ml syrup) 2 times a day (15 mg ambroxol per day); from 2 to 6 years - 1/2 measuring cup (2.5 ml syrup) 3 times a day (22.5 mg 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 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).
It is not recommended to take Ambrobene for more than 4-5 days without a doctor's prescription.
The mucolytic effect of the drug occurs when taking large amounts of fluid, so drinking plenty of fluids is recommended during treatment.
Side effect
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, incl. anaphylactic shock. Rarely - nausea, abdominal pain, vomiting, diarrhea, constipation, dry mucous membrane of the oral cavity and respiratory tract, exanthema, rhinorrhea, dysuria.
special instructions
It should not be combined with antitussive drugs that impede the removal of sputum.
Severe skin reactions, such as Stevens-Johnson syndrome and Lyell's syndrome, have been observed extremely rarely when using Ambrobene. If there is a change in the skin or mucous membranes, you must immediately consult a doctor and stop taking the drug.
In children under 2 years of age, the drug can only be used as prescribed by a doctor.
Caloric content is 2.6 kcal/g sorbitol. Sorbitol may have a mild laxative effect. One measuring cup (5 ml of syrup) contains 2.1 g of sorbitol, which corresponds to 0.18 XE.
Storage
At a temperature not exceeding 25 °C. Keep out of the reach of children. Shelf life - 5 years, after opening - 1 year.
Production
- Teva Pharmaceutical Enterprises Ltd (Israel);
- Merkle GmbH (Germany).
Package
100 ml with a measuring cup (cup) in a cardboard pack or in a dark glass bottle.
Recipe
Available without a prescription.
Ambrobene syrup 15mg/5ml 100ml
Compound
Active substance: ambroxol hydrochloride 15 mg. Excipients: liquid sorbitol 70% - 60 g, propylene glycol - 5 g, raspberry flavor - 0.1 g, saccharin - 0.01 g, purified water - 49.44 g.
Pharmacokinetics
Absorption, distribution, metabolism
When taken orally, ambroxol is almost completely absorbed from the gastrointestinal tract. Cmax is achieved 1-3 hours after oral administration. Due to first-pass metabolism, the absolute bioavailability of ambroxol after oral administration is reduced by approximately 1/3. The resulting metabolites (such as dibromoanthranilic acid, glucuronides) are eliminated by the kidneys.
Plasma protein binding is about 85% (80-90%).
Ambroxol penetrates into the cerebrospinal fluid and through the placental barrier, and is also excreted in breast milk.
Removal
T1/2 from plasma ranges from 7 to 12 hours. The total T1/2 of ambroxol and its metabolites is approximately 22 hours. It is excreted mainly by the kidneys in the form of metabolites - 90%, less than 10% is excreted unchanged.
Given the high binding to plasma proteins, large Vd and slow redistribution from tissues to the blood, significant elimination of ambroxol does not occur during dialysis or forced diuresis.
Pharmacokinetics in special clinical situations
In patients with severe liver disease, the clearance of ambroxol is reduced by 20-40%.
In patients with severe renal impairment, T1/2 of ambroxol metabolites increases
Indications for use
Acute and chronic diseases of the respiratory tract, accompanied by impaired formation and discharge of sputum.
Contraindications
- fructose intolerance, sucrase/isomaltase deficiency, glucose-galactose malabsorption;
- I trimester of pregnancy;
- hypersensitivity to the components of the drug.
The drug should be used with caution in patients with impaired bronchial motor function and increased sputum production (with immobile cilia syndrome), with gastric and duodenal ulcers in the acute phase, in the second and third trimesters of pregnancy, and during lactation.
In patients with impaired renal function or severe liver disease, Ambrobene should be prescribed with extreme caution, and patients should observe longer intervals between doses or take the drug in a lower dose.
Directions for use and doses
The duration of treatment is selected individually depending on the course of the disease. It is not recommended to take Ambrobene for more than 4-5 days without a doctor's prescription. The mucolytic effect of the drug occurs when taking large amounts of liquid. Therefore, drinking plenty of fluids is recommended during treatment.
The syrup should be taken after meals using the supplied measuring cup.
Children under 2 years of age should take 1/2 measuring cup (2.5 ml syrup) 2 times a day (15 mg ambroxol/day).
Children aged 2 to 6 years should take 1/2 measuring cup (2.5 ml syrup) 3 times / day (22.5 mg ambroxol / day).
Children aged 6 to 12 years should take 1 measuring cup (5 ml of syrup) 2-3 times / day (30-45 mg ambroxol / day).
Adults and children over 12 years of age should take 2 measuring cups (10 ml of syrup) 3 times a day (90 mg ambroxol/day) in the first 2-3 days of treatment. If therapy is ineffective for adults, you can increase the dose to 4 measuring cups (20 ml of syrup) 2 times / day (120 mg ambroxol / day). In the following days, you should take 2 measuring cups (10 ml of syrup) 2 times a day (60 mg ambroxol/day).
Storage conditions
The drug should be stored out of the reach of children at a temperature not exceeding 25°C.
Best before date
5 years. After opening the bottle, the drug is suitable for use for 1 year.
special instructions
It should not be combined with antitussive drugs that impede the removal of sputum.
Severe skin reactions, such as Stevens-Johnson syndrome and Lyell's syndrome, have been observed extremely rarely with the use of ambroxol. If there is a change in the skin or mucous membranes, the patient should immediately consult a doctor and stop taking the drug.
When using Ambrobene in syrup form, it should be taken into account that the calorie content is 2.6 kcal/g of sorbitol. Sorbitol may have a mild laxative effect. 1 measuring cup (5 ml of syrup) contains 2.1 g of sorbitol, which corresponds to 0.18 XE.
Use in pediatrics
In children under 2 years of age, the use of Ambrobene in syrup form is possible only as prescribed by a doctor.
Description
Mucolytic and expectorant drug.
Dosage form
The syrup is clear, colorless to slightly yellow, with a raspberry scent.
Use in children
The drug in the form of tablets and injection solution is contraindicated for use in children under 6 years of age.
The drug in the form of retard capsules is contraindicated for use in children under 12 years of age.
Treatment of children under 2 years of age should be carried out only under the supervision of a physician.
Action
Mucolytic and expectorant drug.
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 within 30 minutes and lasts for 6-12 hours (depending on the dose taken). 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 type 2 alveolar pneumocytes and Clara cells of the small airways.
Studies on cell cultures and in vivo studies on animals 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.
Also, preclinical studies have proven the antioxidant effect of ambroxol. Ambroxol, when used together with antibiotics (amoxicillin, cefuroxime, erythromycin and doxycycline), increases their concentration in sputum and bronchial secretions.
Side effects
Allergic reactions: rarely (from ≥0.1% to <1%) - urticaria, skin rash, angioedema of the face, shortness of breath, itching); very rarely (<0.01%) - anaphylactic reactions, incl. anaphylactic shock.
From the digestive system: rarely (from ≥0.1% to <1%) - nausea, abdominal pain, vomiting, diarrhea, constipation.
General disorders: rarely (from ≥0.1% to <1%) - fever, weakness, headache.
Other: rarely (from ≥0.1% to <1%) - dryness of the mucous membrane of the oral cavity and respiratory tract, exanthema, rhinorrhea, dysuria.
Use during pregnancy and breastfeeding
There is insufficient data regarding the use of ambroxol during pregnancy, especially in the first 28 weeks. The use of Ambrobene in the second and third trimesters of pregnancy is possible only as prescribed by a doctor, after a careful assessment of the expected benefits of therapy for the mother and the potential risk for the fetus.
The use of the drug in women during lactation has not been studied enough, so taking Ambrobene is possible only as prescribed by a doctor, after a careful assessment of the ratio of the expected benefits of therapy for the mother and the potential risk for the infant.
Experimental studies on animals did not reveal a teratogenic effect; Ambroxol has been shown to be excreted in breast milk.
Interaction
With the simultaneous use of ambroxol and antitussives, stagnation of secretions may occur due to suppression of the cough reflex. Therefore, such combinations should be selected with caution.
When ambroxol is taken together with the antibiotics amoxicillin, cefuroxime, erythromycin and doxycycline, the concentration of the latter in sputum and bronchial secretions increases.
Overdose
Symptoms: no symptoms of intoxication with an overdose of ambroxol have been identified. 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 case of severe overdose, increased salivation, nausea, vomiting, and decreased blood pressure are possible.
Treatment: intensive therapy 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.
Impact on the ability to drive vehicles and operate machinery
The effect on the ability to drive vehicles and operate machines and mechanisms is still unknown.
