Salbutamol-MCFP, aerosol 100 µg/dose 200 doses

Salbutamol is a selective agonist of ß₂-adrenoreceptors. In therapeutic doses, it acts on ß₂-adrenoceptors of bronchial smooth muscle, having little effect on ß₁-adrenoceptors of the myocardium. It has a pronounced bronchodilator effect, preventing or arresting bronchial spasm, reduces resistance in the airways. It increases the vital capacity of the lungs.

In the recommended therapeutic doses it does not have adverse effects on the cardiovascular system, 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. It causes dilation of the coronary arteries.

It has a number of metabolic effects: it decreases the concentration of potassium in the plasma, affects glycogenolysis and insulin secretion, has hyperglycemic (especially in patients with bronchial asthma) and lipolytic effect, increasing the risk of acidosis.

After application of inhaled forms the effect is quick, the beginning of the effect – within 5 minutes, the maximum effect – within 30-90 minutes (75% of the maximum effect is reached within 5 minutes), the duration – 4-6 hours.

Pharmacokinetics

After inhalation, 10-20% of the salbutamol dose reaches the lower airways. The remainder of the dose remains in the inhaler or is deposited on the oropharyngeal mucosa and then swallowed. The fraction deposited on the respiratory mucosa is absorbed into lung tissue and blood, but is not metabolized in the lungs.

The degree of binding of salbutamol to plasma proteins is about 10%.

Salbutamol is metabolized in the liver and is excreted mainly in the urine unchanged and in the form of phenolic sulfate. The ingested portion of the inhaled dose is absorbed from the gastrointestinal tract and undergoes active metabolism on “first passage” through the liver, converting to phenolic sulfate. The unchanged salbutamol and the conjugate are excreted mainly in the urine.

The elimination half-life of salbutamol is 4-6 hours. It is excreted by the kidneys partially unchanged and partially as the inactive metabolite 4′-O-sulfate (phenol sulfate). A small part is excreted with bile (4%), with feces. Most of the dose of salbutamol is excreted within 72 hours.

Indications

1. 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.

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

Pharmacological effect

Salbutamol is a selective ß2-adrenergic receptor agonist. In therapeutic doses, it acts on ß2-adrenergic receptors of bronchial smooth muscle, having a slight effect on ß1-adrenergic receptors of the myocardium. It has a pronounced bronchodilator effect, preventing or relieving bronchospasm, and reduces resistance in the respiratory tract. Increases vital capacity of the lungs.

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 number of metabolic effects: it reduces the concentration of potassium in plasma, affects glycogenolysis and insulin secretion, has a hyperglycemic (especially in patients with bronchial asthma) and lipolytic effect, increasing the risk of developing acidosis.

After using inhalation forms, the action develops quickly, the onset of the effect is after 5 minutes, the maximum is after 30-90 minutes (75% of the maximum effect is achieved within 5 minutes), duration is 4-6 hours.

Pharmacokinetics

After inhalation administration, 10-20% of the dose of salbutamol reaches the lower respiratory tract. The rest of the dose remains in the inhaler or settles on the mucous membrane of the oropharynx and is then swallowed. The fraction deposited on the mucous membrane of the respiratory tract is absorbed into the lung tissue and blood, but is not metabolized in the lungs.

The degree of binding of salbutamol to plasma proteins is about 10%.

Salbutamol is metabolized in the liver and excreted primarily in the urine unchanged and in the form of phenolic sulfate. The ingested portion of the inhalation dose is absorbed from the gastrointestinal tract and undergoes active first-pass metabolism through the liver, turning into phenolic sulfate. Unchanged salbutamol and the conjugate are excreted primarily in the urine.

The half-life of salbutamol is 4-6 hours. It is excreted by the kidneys partly unchanged and partly in the form of an inactive metabolite 4′-O-sulfate (phenolic sulfate). A small part is excreted in bile (4%) and in feces. Most of the dose of salbutamol is excreted within 72 hours.

Special instructions

Patients should be instructed on the correct use of Salbutamol. Correct use of the drug and strict adherence to the instructions are necessary to ensure that salbutamol enters the bronchi. At the beginning of treatment, the drug should be used under the supervision of medical personnel and after training in front of a mirror.

As with other inhaled medications, the therapeutic effect may decrease as the balloon cools. Therefore, before use, the container with the drug must be warmed to room temperature (warm the container with your hands for several minutes, other methods cannot be used!).

The contents of the cylinders are under pressure and therefore the cylinders must not be heated, broken, punctured or burned, even when empty.

If you experience discomfort in the mouth or a sore throat after inhalation, rinse your mouth with water.

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 the drug becomes less effective or shorter lasting (the effect of the drug should last at least 3 hours), the patient should consult a doctor.

Increasing the dose or frequency of taking salbutamol should only be done under the supervision of a physician. Reducing the interval between taking subsequent doses is possible only in exceptional cases and must be strictly justified. An increased need for the use of inhaled ß2-adrenergic receptor agonists with a short duration of action for the treatment of bronchial asthma indicates an exacerbation of the disease.

In such cases, the patient’s treatment plan should be reconsidered. Taking high doses of salbutamol during exacerbation of bronchial asthma can cause “rebound” syndrome (each subsequent attack becomes more intense). In case of a severe attack of suffocation, the break between inhalations should be at least 20 minutes.

The risk of complications increases both with a significant duration of treatment and with abrupt discontinuation of the drug. Long-term use of salbutamol should be accompanied by the use of anti-inflammatory drugs for basic therapy.

A sudden and progressive deterioration of bronchial asthma can pose a threat to the patient’s life, so in such cases it is necessary to urgently decide on prescribing or increasing the dose of glucocorticosteroids. In such patients, daily monitoring of peak expiratory flow is recommended.

Salbutamol should be used with caution in patients with thyrotoxicosis.
Therapy with ß2-adrenergic agonists, especially when administered parenterally or when administered 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 cases, it is necessary to monitor the concentration of potassium in the blood serum.

Impact on the ability to drive a car and/or other mechanisms.

Since Salbutamol can cause side effects such as convulsions and dizziness, it is recommended to exercise extreme caution when taking the drug for the first time or avoid driving or engaging in other potentially hazardous activities.

Active ingredient

Salbutamol

Composition

Composition for 1 bottle/1 dose:

Contraindications

hypersensitivity to any component of the drug;
rhythm disturbances (paroxysmal tachycardia, polytopic ventricular extrasystole);
myocarditis;
heart defects;
aortic stenosis;
coronary heart disease;
tachyarrhythmia;
thyrotoxicosis;
decompensated diabetes mellitus;
glaucoma;
epileptic seizures;
pyloroduodenal narrowing;
renal or liver failure;
simultaneous use of non-selective beta-blockers;
pregnancy;
children under 2 years of age.

With caution – chronic heart failure, hyperthyroidism, arterial hypertension, pheochromocytoma.

Side Effects

By frequency, side effects can be divided into the following categories: very often (>1/10), often (>1/100 and 1/1000 and 1/10,000 and From the immune system: rarely – dermatitis; very rarely – hypersensitivity reactions, including angioedema, skin rash;

From the side of metabolic processes: rarely – hypokalemia.

From the nervous system: often – tremor, headache, anxiety; rarely – dizziness, drowsiness, fatigue; very rarely – hyperactivity.

From the cardiovascular system: often – tachycardia, palpitations; rarely – dilatation of peripheral vessels with skin hyperemia, discomfort or chest pain; very rarely – arrhythmia, including atrial fibrillation, supraventricular tachycardia, extrasystole, decreased blood pressure and collapse.

From the respiratory system: rarely – cough, irritation of the respiratory tract; very rarely – bronchospasm (paradoxical or caused by hypersensitivity to the drug).

From the gastrointestinal tract: rarely – dryness and irritation of the mucous membrane of the mouth and pharynx, changes in taste, nausea, vomiting.

From the musculoskeletal system: rarely – muscle cramps.

Interaction

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).

Enhances the effect of central nervous system stimulants.

Theophylline and other xanthines, when used simultaneously, increase the likelihood of developing tachyarrhythmias; agents for inhalation anesthesia, levodopa – severe ventricular arrhythmias.
Simultaneous use with m-anticholinergic blockers (including inhaled ones) may increase intraocular pressure.

Diuretics and glucocorticosteroids enhance the hypokalemic effect of salbutamol.

Overdose

Symptoms of overdose: more frequent – hypokalemia, decreased blood pressure, tachycardia, muscle tremors, nausea, vomiting; less frequent – ​​agitation, hyperglycemia, respiratory alkalosis, hypoxemia, headache; rare – hallucinations, convulsions, tachyarrhythmia, ventricular flutter, dilatation of peripheral vessels.

In case of overdose of salbutamol, the best antidotes are cardioselective b-blockers. However, b-adrenergic receptor blockers must be used with caution (risk of developing bronchospasm).
The use of large doses of salbutamol can cause hypokalemia, therefore, if an overdose is suspected, the concentration of potassium in the blood serum should be monitored.

Storage conditions

Store at a temperature not exceeding 25 °C. Do not freeze.

Shelf life

2 years

Manufacturer

Moskhimfarmpreparat, Russia