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


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

Pharmacotherapeutic group:

selective bronchodilator beta2-adrenergic agonist.

ATX code: R03AC02.

pharmachologic effect

Bronchodilator. Salbutamol is a beta2-adrenergic receptor stimulant. The bronchodilator effect appears already 1-3 minutes after inhalation of the drug and significantly increases by 10 minutes, the maximum effect is achieved by 15-20 minutes, the duration of action is 4-5 hours. In therapeutic doses, it also has a pronounced stimulating effect on beta2-adrenergic receptors of blood vessels and myometrium. It has virtually no effect on beta1-adrenergic receptors of the heart. Inhibits the release of inflammatory mediators and basophils from mast cells, in particular, anti-IgE-induced release of histamine, leukotrienes and prostaglandin D2, eliminates antigen-dependent suppression of mucociliary transport and the release of neutrophil chemotaxis factor. Suppresses the early and late phases of the allergic reaction. It has a pronounced bronchodilator effect, preventing or stopping bronchospasms, reduces resistance in the respiratory tract, and increases the vital capacity of the lungs. It has a positive effect on mucociliary clearance, stimulates mucus secretion, and activates the functions of the ciliated epithelium. Prevents the development of allergen-induced bronchospasm. May cause desensitization and a decrease in the number of beta-adrenergic receptors, incl. on lymphocytes. It has a number of metabolic effects: it reduces the potassium content in plasma, affects glycogenolysis and insulin secretion, has a hyperglycemic and lipolytic effect, and increases the risk of developing acidosis. In recommended therapeutic doses, it does not have a negative effect on the cardiovascular system and does not cause an increase in blood pressure. To a lesser extent, compared with drugs of this group, it has a positive chrono- and inotropic effect. Causes dilation of the coronary arteries. It has a tocolytic effect: it reduces the 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. Subjected to first-pass metabolism in the liver and intestinal wall. The half-life is about 4 hours. It is excreted in urine and bile, mainly unchanged (90%) or in the form of a glucuronide.

Salbutamol-solopharm 1 mg/ml 2.5 ml 10 pcs. solution for inhalation

pharmachologic effect

Beta-adrenergic agonist with a predominant effect on β2-adrenergic receptors (localized, in particular, in the bronchi, myometrium, blood vessels). Prevents and relieves bronchospasm; reduces resistance in the respiratory tract, increases the vital capacity of the lungs. Prevents the release of histamine, a slow-reacting substance from mast cells and neutrophil chemotaxis factors. Compared to other drugs in this group, it has a less pronounced positive chrono- and inotropic effect on the myocardium. Causes expansion of the coronary arteries, practically does not reduce blood pressure. It has a tocolytic effect, reducing the tone and contractile activity of the myometrium.

Composition and release form Salbutamol-solopharm 1 mg/ml 2.5 ml 10 pcs. solution for inhalation

Solution for inhalation - 1 ml:

  • Active ingredients: salbutamol (in the form of sulfate) 1.2 mg, which corresponds to the content of salbutamol 1 mg;
  • Excipients: sodium chloride - 9 mg, sulfuric acid solution 0.05M - up to pH 3.0-5.0, water for injection - up to 1 ml.

2.5 ml - ampoules (10) - bags (1) - cardboard packs.

Description of the dosage form

Solution for inhalation in the form of a clear, colorless to slightly brownish or yellowish-brown liquid.

Directions for use and doses

Orally as a bronchodilator for adults and children over 12 years of age - 2-4 mg 3-4 times a day, if necessary, the dose can be increased to 8 mg 4 times a day. Children aged 6-12 years - 2 mg 3-4 times a day; children 2-6 years old - 1-2 mg 3 times a day.

When administered by inhalation, the dose depends on the dosage form used, the frequency of use depends on the indications and the clinical situation.

As a tocolytic agent, it is administered intravenously in a dose of 1-2 mg.

Pharmacokinetics

When using an aerosol, rapid absorption of salbutamol into the blood is observed; however, its plasma concentrations when used at recommended doses are very low or do not reach the detection limit.

After oral administration, salbutamol is well absorbed from the gastrointestinal tract. Plasma protein binding is 10%. Metabolized on first pass through the liver and possibly in the intestinal wall; the main metabolite is an inactive sulfate conjugate. Salbutamol is not metabolized in the lungs, so its ultimate metabolism and elimination after inhalation depends on the route of administration, which determines the ratio between inhaled and inadvertently ingested salbutamol.

T1/2 from blood plasma is 2-7 hours. Salbutamol is quickly excreted in the urine in the form of metabolites and unchanged substance; excreted in small quantities in feces.

Indications for use Salbutamol-solopharm 1 mg/ml 2.5 ml 10 pcs. solution for inhalation

Prevention and relief of bronchospasm in all forms of bronchial asthma. Reversible airway obstruction in chronic bronchitis and emphysema, broncho-obstructive syndrome in children.

Threatened premature birth with contractile activity of the uterus; childbirth before 37-38 weeks of pregnancy; isthmic-cervical insufficiency, a decrease in fetal heart rate depending on uterine contractions during periods of cervical dilatation and expulsion. For preventive purposes during operations on the pregnant uterus (application of a circular suture in case of insufficiency of the internal os of the uterus).

Contraindications

Threat of miscarriage in the first and second trimesters of pregnancy, premature placental abruption, bleeding or toxicosis in the third trimester of pregnancy; children under 2 years of age; hypersensitivity to salbutamol.

Application Salbutamol-solopharm 1 mg/ml 2.5 ml 10 pcs. solution for inhalation during pregnancy and lactation

Salbutamol is contraindicated in cases of threatened miscarriage in the first and second trimesters of pregnancy, premature placental abruption, bleeding or toxicosis in the third trimester of pregnancy.

If it is necessary to use salbutamol during pregnancy, the expected benefits of treatment for the mother should be weighed against the potential risk to the fetus. Currently, there is insufficient data on the safety of the use of salbutamol in early pregnancy. Salbutamol is excreted in breast milk, so if it is necessary to use it during lactation, the expected benefit of treatment for the mother and the possible risk for the child should also be assessed.

Use in children

Contraindicated in children under 2 years of age.

special instructions

Use with caution for tachyarrhythmias and other heart rhythm disorders, arterial hypertension, myocarditis, heart defects, aortic stenosis, diabetes mellitus, thyrotoxicosis, glaucoma, acute heart failure (subject to careful medical supervision).

Increasing the dose or frequency of taking salbutamol should be done under the supervision of a physician. Reducing the interval is possible only in exceptional cases and must be strictly justified.

When using salbutamol, there is a risk of developing hypokalemia, therefore, during treatment in patients with severe bronchial asthma, the level of potassium in the blood should be monitored. The risk of hypokalemia increases with hypoxia.

Side effects Salbutamol-solopharm 1 mg/ml 2.5 ml 10 pcs. solution for inhalation

From the cardiovascular system: transient dilatation of peripheral vessels, moderate tachycardia.

From the central nervous system: headache, dizziness, nausea, vomiting.

Metabolism: hypokalemia.

Allergic reactions: in isolated cases - angioedema, allergic reactions in the form of skin rash, urticaria, arterial hypotension, collapse.

Other: tremor of the hands, internal trembling, tension; rarely - paradoxical bronchospasm, muscle cramps.

Drug interactions

With simultaneous use of salbutamol with non-cardioselective beta-blockers, mutual suppression of therapeutic effects is possible; with theophylline - the risk of developing tachycardia and arrhythmia, in particular supraventricular extrasystole, increases.

With the simultaneous use of salbutamol and xanthine derivatives, corticosteroids or diuretics, the risk of developing hypokalemia increases.

Ventolin nebula 1 mg/ml n20 solution for inhalation

Latin name

Ventolin

Release form

Solution for inhalation.

Package

Ampoules 20 doses.

pharmachologic effect

Salbutamol is a selective b2-adrenergic receptor agonist. In therapeutic doses, it acts on b2-adrenergic receptors of bronchial smooth muscle, having little or no effect on b1-adrenergic receptors of the myocardium.

Indications

Bronchial asthma

— relief of attacks of bronchial asthma, including exacerbation of severe bronchial asthma;

- prevention of bronchospasm attacks associated with exposure to an allergen or caused by physical activity;

— use as one of the components in long-term maintenance therapy of bronchial asthma.

Chronic obstructive pulmonary disease (COPD), accompanied by reversible airway obstruction, including chronic bronchitis and emphysema.

Contraindications

— Hypersensitivity to any component of the drug.

— Management of premature birth.

- Threatened abortion.

— Children up to 2 years old.

Use during pregnancy and breastfeeding

During pregnancy and lactation, the drug is prescribed only in cases where the expected benefit to the mother exceeds any possible risk to the fetus.

Salbutamol is likely to pass into breast milk, so it is not recommended for nursing women to take it unless the expected benefit to the mother outweighs any potential risk to the baby. It is not known whether salbutamol present in breast milk has any negative effects on a newborn baby.

special instructions

Patients should be instructed on the correct use of the Ventolin inhaler.

Bronchodilators should not be the only or main component of the treatment of unstable or severe bronchial asthma.

If the effect of the usual dose of Ventolin becomes less effective or less durable (the effect of the drug should last at least 3 hours), the patient should consult a doctor.

An increased need for the use of inhaled β2-adrenergic agonists with a short duration of action to control the symptoms of bronchial asthma indicates an exacerbation of the disease. In such cases, the patient's treatment plan should be reconsidered. A sudden and progressive deterioration of bronchial asthma can pose a threat to the patient's life, so in such situations it is necessary to urgently decide on the issue of prescribing or increasing the dose of glucocorticosteroids. In such patients, daily monitoring of peak expiratory flow is recommended.

Very high doses of salbutamol can lead to the development of adverse reactions, so only a doctor can decide on increasing the dose or frequency of use of the drug. Patients using Ventolin Nebula at home should be warned that if the effect of the usual dose becomes less effective or less durable, they should not independently increase the dose or frequency of administration of the drug, but should immediately consult a doctor.

Ventolin Nebula should be used with caution in patients who have already taken high doses of other sympathomimetics.

Salbutamol should be used with caution in patients with thyrotoxicosis.

Therapy with β2-adrenergic agonists, especially when administered parenterally or via nebulizer, can lead to hypokalemia. Particular caution is recommended when treating severe attacks of bronchial asthma, since in these cases hypokalemia may increase as a result of the simultaneous use of xanthine derivatives, glucocorticosteroids, diuretics, as well as due to hypoxia. In such situations, it is necessary to monitor the level of potassium in the blood serum.

Compound

1 dose contains 100 mcg of salbutamol (in the form of salbutamol sulfate).

Directions for use and doses

Ventolin dosed aerosol is intended for inhalation administration only.

Only a doctor can decide whether to increase the dose or frequency of use of the drug.

It is not recommended to use the Ventolin inhaler more than 4 times a day. The need for frequent use of maximum doses of Ventolin or a sudden increase in dose indicates a worsening of the disease.

Adults (including elderly patients)

Relieving an attack of bronchospasm: the recommended dose is 100-200 mcg (1-2 inhalations).

Prevention of bronchospasm attacks associated with exposure to an allergen or caused by physical activity: the recommended dose is 200 mcg (2 inhalations) 10-15 minutes before exposure to the provoking factor.

Long-term maintenance therapy: the recommended dose is up to 200 mcg (2 inhalations) 4 times a day.

Ventolin can be administered through the Volumatic spacer.

Children

Relieving an attack of bronchospasm: the recommended dose is 100-200 mcg (1-2 inhalations).

Prevention of bronchospasm attacks associated with exposure to an allergen or caused by physical activity: the recommended dose is 100-200 mcg (1-2 inhalations) 10-15 minutes before exposure to the provoking factor.

Long-term maintenance therapy: the recommended dose is up to 200 mcg (2 inhalations) 4 times a day.

Ventolin can be administered through the Babyhaler or Volumatic spacer.

Side effects

Salbutamol may cause mild tremor of skeletal muscles, which is usually most pronounced in the arms and is a characteristic side effect of all β2-adrenergic agonists. Occasionally, patients experience headache, peripheral vasodilatation, and a slight compensatory increase in heart rate. Very rarely, hypersensitivity reactions develop (including angioedema, urticaria, bronchospasm, hypotension and collapse), muscle cramps, and tachycardia.

Inhaled drugs can cause paradoxical bronchospasm. Paradoxical bronchospasm must be immediately relieved with another dosage form of salbutamol or another fast-acting inhaled bronchodilator. You should immediately stop using the Ventolin inhaler, assess the patient's condition, conduct the necessary examination and prescribe appropriate therapy.

Inhaled medications may cause irritation to the mucous membranes of the mouth and throat.

Therapy with beta2-adrenergic agonists sometimes causes hypokalemia, which can pose a serious danger to the patient.

Like other beta2-adrenergic agonists, salbutamol may occasionally cause mental agitation and increased motor activity in children.

In patients with a predisposition to the development of arrhythmias, salbutamol can cause cardiac arrhythmias, including atrial fibrillation, supraventricular tachycardia and extrasystole.

Drug interactions

It is not recommended to use salbutamol and non-selective beta-adrenergic receptor blockers simultaneously, such as propranolol.

Salbutamol is not contraindicated in patients receiving monoamine oxidase inhibitors (MAOIs).

Overdose

In case of overdose of salbutamol, the best antidotes are cardioselective b-blockers. However, beta-adrenergic blockers should be used with caution in patients with a history of bronchospasm attacks. The use of large doses of salbutamol can cause hypokalemia, therefore, if overdose is suspected, serum potassium levels should be monitored.

Storage conditions

Store at temperatures below 30°C.

Best before date

2 years.

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