Proventil (Salbutamol) Inhaler

Composition

1 dose of the drug contains Active ingredient Salbutamol sulfate (recalculated to 100 % substance) 0.1208 mg (equivalent to 0.1 mg of salbutamol).

Pharmacological action

Salbutamol is a selective β2-adrenoreceptor agonist. In therapeutic doses, it acts on β2-adrenoreceptors of bronchial smooth muscle, with a minor effect on β1-receptors of the myocardium. It has a pronounced bronchodilator effect, preventing or arresting bronchial spasm, reduces airway resistance. Increases the vital capacity of the lungs.

In recommended therapeutic doses, it does not adversely affect the cardiovascular system and does not cause an increase in arterial pressure.
To a lesser extent, compared to the drugs of this group, it has positive chrono- and inotropic effects. Causes dilatation 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 hyperglycemic (especially in patients with bronchial asthma) and lipolytic effects, increasing the risk of acidosis.

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

Indications

• Bronchial asthma:

– relief of bronchial asthma attacks, including exacerbations 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.

• Сhronic obstructive pulmonary disease (COPD), accompanied by reversible airway obstruction, chronic bronchitis.

Contraindications

Hypersensitivity to any component of the drug.

Childhood under 2 years of age.

With caution:

• If there is a history of tachyarrhythmia, myocarditis, heart defects, aortic stenosis, coronary heart disease, severe chronic heart failure, arterial hypertension, thyrotoxicosis, pheochromocytoma, decompensated diabetes, glaucoma, epilepsy, renal or liver failure.
• Simultaneous use of non-selective β2-adrenoblockers, pregnancy, lactation.

Side effects

According to the frequency of side effects can be divided into the following categories: very common (1/10), common (1/100 and < 1/10), infrequent (1/1000 and < 1/100), rare (1/10 000 and < 1/100), very rare (< 1/10 000).

• Immune system: rare – dermatitis, very rare – hypersensitivity reactions, including angioedema, skin rash.
• Metabolism: rare – hypokalemia.
• The nervous system: often – tremor, headache, anxiety, rarely – dizziness, drowsiness, fatigue, very rare – hyperactivity.
• Cardiovascular system: frequent – tachycardia, palpitations, rarely – peripheral vasodilation with skin hyperemia, discomfort or pain in the chest, very rare – arrhythmia, including atrial fibrillation, supraventricular tachycardia, extrasystole, decreased blood pressure and collapse.
• Respiratory system: rarely – cough, irritation of the airways; very rare – bronchospasm (paradoxical or caused by hypersensitivity to the drug).
• Gastrointestinal tract: rare – dryness and irritation of the mucous membrane of the mouth and throat, changes in taste, nausea, vomiting.
• Musculoskeletal system: rarely – muscle cramps.

Interaction

It is not recommended to use salbutamol and non-selective β2-adrenoreceptor blockers such as propranolol simultaneously.

Salbutamol is not contraindicated in patients receiving monoamine oxidase inhibitors.

It enhances the effects of central nervous system stimulants.

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

Concomitant use with m-cholinoblockers (including inhaled) may increase intraocular pressure.

Diuretics and glucocorticosteroids increase the hypokalemic effect of salbutamol.

How to take Salbutamol, course of treatment and dosage

Salbutamol aerosol for inhalation dosed 100 mcg/dose is intended for inhalation administration only.

Only a physician may decide on increasing the dose or frequency of administration of the drug.

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

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

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

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

Children. Long-term maintenance therapy in bronchial asthma and COPD as a part of complex therapy: the recommended dose is up to 200 micrograms (2 inhalations) 4 times a day.

Cure of bronchospasm attack: 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 provocative factor.

Preparation for the first use:

• Before using the drug for the first time, remove the protective cap from the inhaler nozzle. Then shake the bottle vigorously with a vertical motion, turn the bottle with the inhaler nozzle down and spray two times in the air to make sure that the valve works properly.
• If the product has not been used for several days, one spray should be made into the air after shaking the can thoroughly.

Overdose

Symptoms:

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, peripheral vasodilation.

Treatment:

For salbutamol overdose, the best antidotes are cardioselective β2-adrenoblockers. However, β2-adrenoreceptor blockers should be used with caution (risk of bronchospasm).

High doses of salbutamol may cause hypokalemia; therefore, serum potassium concentration should be monitored in case of suspected overdose.

Special instructions

Patients should be instructed on the correct use of Salbutamol. Correct use of the drug and clear fulfillment of the instructions are necessary in order to ensure that salbutamol reaches 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 drugs, the therapeutic effect may decrease when the balloon is cooled. Therefore, the drug cylinder must be warmed up to room temperature before use.

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, you should rinse your mouth with water after inhalation.

Bronchodilators should not be the sole or main component of therapy for unstable or severe bronchial asthma.

If the effect of the usual dose of the drug becomes less effective or less prolonged (the action of the drug should last at least 3 hours), the patient should consult a physician. Increasing the dose or frequency of administration of salbutamol should be done only under the supervision of a physician. 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 β2-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). At a severe attack 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.

Sudden and progressive worsening of bronchial asthma may be life threatening for the patient, so in such cases it is necessary to urgently address the issue of prescribing or increasing the dose of glucocorticosteroids. Daily monitoring of peak expiratory velocity is recommended in such patients.

Salbutamol should be used with caution in patients with thyrotoxicosis.

Therapy with β2-adrenoreceptor agonists, especially when administered parenterally or with nebulizer, may lead to hypokalemia. Particular caution is recommended during treatment of severe attacks of bronchial asthma, because in these cases hypokalemia may be increased as a result of simultaneous use of xanthine derivatives, glucocorticosteroids, diuretics, as well as due to hypoxia. In such cases, serum potassium levels should be monitored.