Ambroxol, Salbutamol

Pharmacological properties

Combined drug, the therapeutic effect of which is due to the pharmacological properties of the active components that make up its composition.

Pharmacodynamics Ambroxol is a secretolytic and secretory of the benzylamine group. It normalizes the pathologically altered formation of bronchial secretions due to the stimulation of serous cells of the glands of the bronchial mucosa, as a result of which the content of the mucous secretion increases and the ratio of the mucous and serous components of sputum changes. Ambroxol activates hydrolyzing enzymes and enhances the release of lysosomes from Clark cells, changes the structure of bronchial secretion by reducing and fragmenting mucopolysaccharide fibers, selectively inhibits sodium absorption by the epithelium of the respiratory tract, which leads to a decrease in sputum viscosity. It enhances the movement of the cilia of the ciliated epithelium of the bronchi, increasing the mucociliary transport of sputum, which facilitates its discharge. In addition, ambroxol stimulates the synthesis of surfactant phospholipids by alveolar pneumocytes, and has an antioxidant effect. Ambroxol penetrates well through the placental barrier and improves the synthesis of surfactant during fetal development.

Salbutamol is a selective β agonist₂-adrenoreceptors. It has a bronchodilator effect, prevents and relieves bronchospasm, reduces resistance in the airways, and increases the vital capacity of the lungs. Increases the resistance of mast cells and basophils to degranulation upon contact with an allergen and thereby prevents the release of histamine, a slow-reacting substance of anaphylaxis and neutrophil chemotaxis factor. Compared to other β₂-adrenomimetics, salbutamol has a less pronounced positive chrono- and inotropic effect on the myocardium, practically does not change blood pressure and heart rate.

Pharmacokinetics Ambroxol after oral administration is rapidly and completely absorbed in the digestive tract. The pharmacological effect occurs 30 minutes after taking the drug, C_max in the blood plasma, it is detected after 1-3 hours and is retained for 6-12 hours. The bioavailability of ambroxol is 30%. This is due to the effect of the primary passage through the liver. Plasma protein binding is about 85%. About 90% of ambroxol is excreted in the form of metabolites in the urine, less than 10% is unchanged.

Salbutamol slightly binds to plasma proteins, its bioavailability when administered orally is 40-50%. T_½ for salbutamol and its active metabolite, it is 6 hours. The main metabolites of salbutamol are conjugated sulfates (42%), the main of which is salbutamol ether sulfate, which has β₂-adrenostimulatory effect. Conjugated sulfates are excreted mainly in the urine and, to a small extent, in the bile.

Salbutamol and ambroxol cross the placental barrier and are secreted with breast milk.

Indications

Ba; chronic obstructive bronchitis; emphysema.

Application

Apply inside. adults and children over the age of 12 are prescribed 1 tablet 3-4 times a day.

The drug must be taken between meals. The intervals between doses should be at least 6 hours.

For adults, if necessary, the dose can be increased to 2 tablets 4 times a day.

In case of side effects, it is recommended to reduce the dose to¹/₂ tablets 4 times a day.

The duration of treatment is determined by the doctor depending on the clinical picture of the disease.

Contraindications

Hypersensitivity to the components of the drug; tachyarrhythmia; ag; myocarditis; heart defects; acute heart failure; peptic ulcer of the stomach and duodenum; diabetes; hyperthyroidism; thyrotoxicosis; glaucoma; the use of β-adreceptor blockers, especially non-selective; i trimester of pregnancy; lactation period; children under 12 years old.

Side effects

Hand tremor, tension; less commonly, short-term peripheral vasodilation, headache, dizziness, moderate tachycardia, nausea, vomiting, sensation of fullness of the stomach, epigastric pain, diarrhea, anorexia, difficulty urinating, sweating, increased blood glucose.

In isolated cases - angioedema, allergic reactions in the form of skin rashes, arterial hypotension, collapse, paradoxical bronchospasm, muscle cramps.

special instructions

Increasing the dose or reducing the intervals between doses of the drug should be carried out under the supervision of a doctor. reducing the interval is possible only in exceptional cases and should be strictly justified.

When using salbroxol, the development of hypokalemia is possible, therefore, during the treatment period, the level of potassium in the blood should be monitored.

With caution, the drug should be used for diseases of the liver and / or kidneys.

Use during pregnancy and lactation. The use of the drug in the first trimester of pregnancy is contraindicated. When appointing in the II and III trimester of pregnancy, the benefit / risk ratio should be taken into account.

If it is necessary to use the drug by women during lactation, it is recommended to stop feeding.

Children. There is no experience with the use of the drug for the treatment of children under the age of 12 years.

The ability to influence the reaction rate when driving vehicles and working with other mechanisms. The use of the drug can worsen the reaction when driving vehicles and working with mechanisms. This effect is enhanced with the simultaneous use of alcohol and the use of tranquilizers.

Interactions

The antagonistic effect (in relation to salbutamol) of β-adreceptor blockers not only weakens the bronchodilator effect of the drug, but can also increase bronchospasm.

The combination with M-cholinergic receptor blockers and theophylline increases the severity and duration of bronchodilation, however, the risk of developing tachycardia and arrhythmia, in particular supraventricular extrasystole, increases.

GCS increase the sensitivity of receptors to β-adrenoreceptor agonists, including salbutamol.

Ambroxol, which is part of the drug, improves the penetration of antibiotics into bronchial secretion.

The simultaneous use of antitussive agents (codeine, Glaucine, etc.) can worsen sputum discharge.

With the simultaneous administration of xanthine derivatives, corticosteroids, cardiac glycosides, diuretics, there is a risk of hypokalemia.

When combined with antidepressants and MAO inhibitors, an increase in the effect of salbutamol and a sharp decrease in blood pressure are possible.

Overdose

It is manifested by tachycardia, arrhythmia, sleep disturbance, chest pain, tremor of the hands and the whole body. when taking the drug in high doses, serious complications are possible: arterial hypotension, collapse, angioedema.

Symptomatic treatment - gastric lavage is carried out, cardioselective β blockers are prescribed₁-adreceptors.

Storage conditions

In a dry, dark place at a temperature of no higher than 25 ° C.