Salbutamol-nativ for inhalation 1 mg/ml 2.5 ml, 10 pcs.

Pharmacotherapeutic group:

Bronchodilator beta2-adrenomimetic selective.

The ATX code: R03AC02.

Pharmacological action

The bronchodilator. Salbutamol is a stimulator of beta2-adrenergic receptors. Bronchodilator effect appears within 1-3 minutes after inhalation of the drug and significantly increases by 10 minutes, the maximum effect is reached by 15-20 minutes, the duration of action is 4-5 hours.

In therapeutic doses it also has a marked stimulating effect on beta2-adrenoreceptors of blood vessels and myometrium. It has practically no effect on the beta1-adrenoreceptors of the heart. It inhibits release of inflammatory mediators from mast cells and basophils, in particular anti-lgE-induced release of histamine, leukotrienes and prostaglandin D2, eliminates antigen-dependent suppression of mucociliary transport and release of neutrophil chemotaxis factor.

Suppresses early and late phase of allergic reaction. It has a pronounced bronchodilator effect, preventing or arresting bronchial spasms, reduces resistance in the airways, increases lung vital capacity. It has a positive effect on mucociliary clearance, stimulates mucus secretion and activates the functions of the atrial fibrillation epithelium.

Prevent development of bronchospasm induced by allergen. It can cause desensitization and decrease in the number of beta-adrenoceptors, including on lymphocytes. It has a number of metabolic effects: it reduces plasma potassium content, affects glycogenolysis and insulin release, has hyperglycemic and lipolytic effects, increases the risk of acidosis.

In the recommended therapeutic doses it does not have adverse effects on the cardiovascular system and does not cause increase in blood pressure. To a lesser extent compared to the drugs of this group, it has positive chrono- and inotropic effects. Causes dilation of the coronary arteries. It has a tocolytic effect: it reduces tone and contractile activity of the myometrium.

Pharmacokinetics

When inhaled, 10-20% reaches the small bronchi and is gradually absorbed, part of the dose after swallowing is absorbed from the gastrointestinal tract. It is subjected to presystemic metabolism in the liver and intestinal wall. The elimination half-life is about 4 hours. It is excreted with urine and bile, mainly unchanged (90%) or as glucuronide.

Indications

Bronchial asthma (for relief of choking attacks), reversible bronchial obstruction (prevention and treatment), including chronic obstructive pulmonary disease.

Active ingredient

Composition

Inhalation solution.

Active ingredient:

salbutamol hemisuccinate 1.0 mg.

Associates:

Acetic acid 0.2 mg,

Purified water 1.0 ml.

How to take, the dosage

The drug “Salbutamol-nativ” shall be used by inhalation only with a nebulizer of any design. 1 ml of the drug contains 1 mg of salbutamol hemisuccinate (in terms of salbutamol 0.8 mg/ml).

The nebulizer turns the solution into an aerosol for inhalation. When using the solution should be at room temperature (cold solution may cause coughing effect). Before using the product, carefully read the instructions for use for the nebulizer:

Prepare the nebulizer for use. Place the drug solution in the nebulizer. Do not mix the solution with other medicines. The solution may be diluted with distilled water or 0.9% sodium chloride.” When you have finished inhaling, remove any residual solution and wash the nebulizer. When using Salbutamol-nativ solution through a nebulizer, the initial dose of the drug is 2.5 mg for adults and children over 12 years of age, but may be increased to 5 mg. Inhalations are carried out every 4-6 hours during the first 24-48 hours of therapy or until the clinical picture stabilizes. Improvement of condition is observed after inhalation usually in 10-15 minutes. In severe exacerbations of chronic obstructive pulmonary disease, the frequency of drug administration may be increased significantly – it is possible to prescribe the drug every 30-60 minutes until clinical effect is achieved (in adults, up to 40 mg per day).

Application in children from 18 months to 12 years.

To relieve an attack of bronchospasm: single dose of 2 mg per inhalation up to 4 times daily under the supervision of specialists. For prophylaxis, 2 mg/day.

Interaction

Salbutamol-nativ combines well with anti-asthmatic drugs of other pharmacological groups (glucocorticosteroids, membrane stabilizers, antihistamines, expectorants, mucolytics, cholinolytics, xanthines).

Theophylline and other xanthines when used concomitantly increase the likelihood of tachyarrhythmias; agents for inhalation anesthesia, levodopa – severe ventricular arrhythmias.

Monoamine oxidase inhibitors and tricyclic antidepressants increase the effect of salbutamol, may lead to a sharp decrease in blood pressure.
Simultaneous administration of salbutamol and non-selective beta-adrenoblockers (such as propranolol) in patients with bronchial asthma is not recommended because of the risk of severe bronchospasm.

Anticholinergic agents in inhaled form may cause increased intraocular pressure when used concomitantly.

Diuretics and glucocorticosteroids increase the hypokalemic effect of salbutamol. Increases the effect of central nervous system stimulants, the side effects on the heart of thyroid hormones. Increases the need for nitrates and hypotensive drugs in the case of increased heart rate and, consequently, blood pressure during treatment with salbutamol. Increases the likelihood of extrasystole against the background of taking cardiac glycosides.

Special Instructions

There are no data on the negative effect on the ability to drive motor transport and other activities requiring special attention and quick reactions. Nevertheless, the question about the possibility of driving a vehicle should be decided after assessing the individual tolerability of the drug.

If the effects of the usual dose of the drug become less effective, the patient should consult a physician.

If paradoxical bronchospasm occurs, it should be immediately managed with another form of salbutamol or a rapid-acting inhaled bronchodilator, treatment should be discontinued and therapy with other drugs should be prescribed.

Contraindications

Hypersensitivity to the components of the drug, coronary heart disease, severe heart failure, rhythm disorders (paroxysmal tachycardia, polytopic ventricular extrasystole), myocarditis, heart defects, aortic stenosis, decompensated diabetes mellitus, glaucoma, epilepsy, pyloroduodenal constriction, renal and hepatic diseases with dysfunction, pregnancy, concomitant use of non-selective beta-adrenoblockers, children under 18 months.

With caution:

Chronic heart failure, arterial hypertension, hyperthyroidism, pheochromocytoma, thyrotoxicosis.

Side effects

Sense of inner restlessness and mild skeletal muscle tremor, seizures, palpitations, sleep disturbance, paradoxical bronchospasm, cough, facial hyperemia, nervous tension, anxiety, headache, dizziness, tachycardia (in pregnancy – in the mother and in the fetus), agitation, dyspepsia, nasal congestion, pharyngitis, Urinary retention, sweating, hyperglycemia, increased content of free fatty acids in blood, hypokalemia, angioedema, allergic reactions (urticaria, erythema, facial edema), decreased blood pressure, arrhythmia, irritation of airways, dry mucous membranes of the mouth and throat, changes in taste sensation, dermatitis.

Overdose

Symptoms: tachycardia, impaired heart rate, peripheral vasodilation, decreased blood pressure, hypoxemia, hypokalemia, hyperglycemia, muscle tremor, headache, agitation.

Treatment.

Cancellation of the drug and symptomatic therapy (administration of selective beta-adrenoblockers requires caution in patients with bronchial asthma because of the risk of severe bronchospasm).

Similarities