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:

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

Active ingredient

Composition

How to take, the dosage

Interaction

The simultaneous use of salbutamol and non-selective b-adrenoceptor blockers, such as propranolol, is not recommended.

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

It potentiates the effects of central nervous system stimulants.

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

Diuretics and glucocorticosteroids increase the hypokalemic effect of salbutamol.

Special Instructions

Patients should be instructed on the correct use of Salbutamol. Correct use of the drug and clear 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 when the balloon is cooled. Therefore, before use, the cylinder with the drug must be warmed to room temperature (warm the cylinder by hand for a few minutes, no other methods should be used!).

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

If your mouth feels uncomfortable and your throat feels clammy after inhalation, rinse your mouth with water.

Bronchodilators should not be the sole or main component of therapy for unstable or severe bronchial asthma. If the effects of a regular dose of medication become less effective or less prolonged (the medication must last at least 3 hours), the patient should see his or her physician.

Increasing the dose or frequency of salbutamol should only be done under medical supervision. Reducing the interval between subsequent doses is possible only in exceptional cases and should be strictly justified. An increased need for the use of inhaled ß2 adrenoreceptor 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 an exacerbation of bronchial asthma may cause “ricochet” syndrome (each subsequent attack becomes more intense). In severe attacks of suffocation, a break between inhalations should be at least 20 minutes.

The risk of complications increases with both significant duration of treatment and abrupt withdrawal of the drug. Prolonged use of salbutamol should be accompanied by the use of anti-inflammatory drugs for basal therapy.

The sudden and progressive worsening of bronchial asthma may be life-threatening for the patient, so in such cases the issue of prescribing or increasing the dose of glucocorticosteroids should be urgently addressed. Daily monitoring of peak expiratory velocity is recommended in such patients.

Salbutamol should be used with caution in patients with thyrotoxicosis.
Therapy with ß2 adrenoreceptor agonists, especially when administered parenterally or when used with a nebulizer, may lead to hypokalemia.

Particular caution is recommended during treatment of severe attacks of bronchial asthma since in these cases hypokalemia may increase as a result of simultaneous use of xanthine derivatives, glucocorticosteroids, diuretics as well as due to hypoxia. In such cases it is necessary to monitor serum potassium concentration.

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

Because Salbutamol may cause side effects such as seizures and dizziness, it is recommended to be extra cautious or to refrain from driving and engaging in other potentially dangerous activities during the first doses.

Contraindications

Side effects

According to the frequency of side effects can be divided into the following categories: very often (>1/10), often (>1/100 and 1/1000 and 1/10 000 and Immune system disorders: rare – dermatitis; very rare – hypersensitivity reactions, including angioneurotic edema, skin rash;

Metabolic disorders: rare – hypokalemia.

Nervous system disorders: often – tremor, headache, anxiety; rarely – dizziness, somnolence, fatigue; very rarely – hyperactivity.

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

Respiratory system disorders: rarely – cough, irritation of airways; very rarely – bronchospasm (paradoxical or caused by hypersensitivity to the drug).

Gastro-intestinal tract: rarely – dryness and irritation of the mucous membrane of the mouth and throat, altered sense of taste, nausea, vomiting.

Muscular system disorders: rare – muscle cramps.

Overdose

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

In overdose of salbutamol, the best antidotes are cardioselective b-adrenoblockers. However, b-adrenoreceptor blockers should be used with caution (risk of bronchospasm).
Use of large doses of salbutamol may cause hypokalemia; therefore, serum potassium concentration should be monitored if overdose is suspected.

Similarities