Salbutamol-zdorovya
Ukraine
Table of Contents
INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT SALBUTAMOL-ZDOROVYE (SALBUTAMOL-ZDOROVYE)
Composition:
Active ingredient: salbutamol;
One dose of the preparation contains salbutamol 100 mcg (in the form of micronized salbutamol sulfate – 120 mcg);
Excipient: propellant 134a.
Pharmaceutical form. Pressurized metered dose inhalation aerosol.
Main physicochemical properties: white or almost white suspension.
Pharmacotherapeutic group. Medicinal products for the treatment of obstructive respiratory diseases. Adrenergic agents for inhalation use. Selective β2-adrenoreceptor agonists. Salbutamol. ATC code R03AC02.
Pharmacological properties.
Pharmacodynamics. Salbutamol is a selective β2-adrenergic receptor agonist. In therapeutic doses, it acts on β2-adrenergic receptors of bronchial smooth muscle, providing rapid (within 5 minutes) and short-term (4–6 hours) bronchodilation in patients with reversible airway obstruction.
Pharmacokinetics. After inhaled administration, 10 to 20% of the administered dose reaches the lower airways. The remainder remains in the inhalation device or in the oropharynx, from where it is swallowed. Part of the dose that reaches the airways is absorbed into lung tissue and enters the systemic circulation but is not metabolized in the lungs.
After entering the systemic circulation, the drug is metabolized in the liver and is excreted mainly by the kidneys, primarily in unchanged form and as a phenolsulfate metabolite.
The portion of the dose that reaches the gastrointestinal tract from the oropharynx is absorbed from the gastrointestinal tract, undergoes first-pass metabolism in the liver to form a phenolsulfate compound, and is then excreted by the kidneys. Most of the drug is eliminated from the body within 72 hours. Plasma protein binding is approximately 10%.
Clinical characteristics.
Indications. Short-term (4 to 6 hours) bronchodilation with rapid onset (approximately within 5 minutes) in airway obstruction.
Relief of asthma attacks in diseases associated with airway obstruction, such as bronchial asthma.
Prevention of bronchospasm attacks related to allergen exposure or induced by physical exertion.
As part of combination therapy in patients with bronchial asthma.
Contraindications. Hypersensitivity to any component of the drug. Do not use for suppression of uncomplicated premature labor or threatened abortion medicinal forms of salbutamol not intended for intravenous administration.
Interaction with other medicinal products and other types of interactions. Salbutamol must not be used concomitantly with non-selective β-adrenergic blockers (e.g., propranolol).
Concomitant use of salbutamol with monoamine oxidase inhibitors (MAO inhibitors) is not contraindicated.
Special precautions for use.
To ensure optimal delivery of the medicinal product to the patient's lungs, the patient's inhalation technique should be checked. Patients should be warned about the possibility of experiencing a different taste compared to that with their previous inhaler.
Patients receiving regular anti-inflammatory therapy (e.g., inhaled corticosteroids) should be advised to continue taking anti-inflammatory medications even when symptoms subside and salbutamol is not required.
An increased need for bronchodilators, particularly short-acting inhaled β2-agonists, to control symptoms of bronchial asthma indicates disease exacerbation; therefore, patients should be advised to seek medical help as soon as possible. In such cases, the treatment plan should be reassessed, and consideration should be given to increasing the dose of inhaled corticosteroids or initiating a course of oral corticosteroids.
Excessive use of short-acting β-agonists may mask the progression of the underlying disease and lead to worsening asthma control, increasing the risk of severe asthma exacerbations and mortality.
Patients using salbutamol more than twice a week on an as-needed basis (excluding prophylactic use before physical exertion) should be evaluated for daytime symptoms, nocturnal awakenings, and activity limitations due to asthma to allow appropriate treatment adjustment, as these patients belong to the risk group for excessive salbutamol use.
Sudden and progressive worsening of bronchial asthma is a life-threatening condition requiring initiation or intensification of corticosteroid therapy. Patients at risk are recommended to perform daily peak expiratory flow monitoring.
Bronchodilators should not be the sole or primary treatment for patients with severe or unstable bronchial asthma. The condition of such patients should be monitored regularly, including pulmonary function testing, as severe asthma is a life-threatening condition, and treatment should include consideration of maximum recommended doses of inhaled and/or oral glucocorticosteroids.
If the usual dose of the drug becomes less effective or its duration of action decreases (less than 3 hours), the patient should consult a physician. Dose or frequency increases should only be made by a physician.
Severe asthma exacerbations should be treated according to standard protocols.
Sympathomimetics, including salbutamol, affect the cardiovascular system. Post-marketing and published data provide evidence of rare cases of myocardial ischemia associated with salbutamol use. Patients with heart disease (e.g., ischemic heart disease, arrhythmia, or severe heart failure) treated with salbutamol should seek medical help if they develop chest pain or other symptoms indicating worsening cardiac disease. Particular attention should be paid to evaluating symptoms such as dyspnea and chest pain, which may result from either cardiac or respiratory disease.
Salbutamol should be prescribed with caution to patients with thyrotoxicosis.
Treatment with β2-agonists may result in severe hypokalemia, particularly with parenteral formulations or nebulizers. Particular attention should be paid to patients with acute severe asthma, as hypokalemia may be potentiated by concomitant use of xanthine derivatives, steroids, diuretics, and hypoxia. In such cases, serum potassium levels should be monitored.
Salbutamol should be used with caution in patients receiving high doses of other sympathomimetics. Like other β-adrenergic agonists, salbutamol may cause reversible metabolic changes, such as increased blood glucose levels. Compensation for these changes in diabetic patients is not always possible, and there have been isolated reports of ketoacidosis in such patients. Concomitant use of corticosteroids may exacerbate this condition.
As with other inhaled medications, paradoxical bronchospasm with immediate worsening of dyspnea after drug administration may occur. In such cases, alternative formulations or other fast-acting inhaled bronchodilators should be administered immediately. Salbutamol should be discontinued immediately, the patient's condition assessed, and if necessary, another fast-acting bronchodilator should be prescribed for ongoing use.
Use during pregnancy or breastfeeding. Animal studies indicate that salbutamol has reproductive toxicity. The safety of salbutamol use during pregnancy has not been established. Controlled clinical studies on the use of salbutamol in pregnant women have not been conducted. There have been isolated reports of various congenital malformations during fetal development, including cleft palate, limb defects, and cardiac abnormalities. Some women received multiple other medications during pregnancy. Salbutamol may be used during pregnancy only if clearly needed.
Salbutamol is likely excreted in breast milk; therefore, it should be prescribed to breastfeeding women with caution. It is unknown whether salbutamol in breast milk has harmful effects on the newborn/infant; therefore, its use in breastfeeding women should be limited to cases where the benefit to the mother outweighs the potential risk to the infant.
Ability to affect reaction speed when driving or operating machinery. No data are available. If adverse reactions affecting the nervous system (e.g., tremor) occur, driving or operating machinery should be avoided.
Dosage and Administration
The medicinal product is an aerosol intended for oral inhalation only. For patients who have difficulty synchronizing breathing with inhaler use, it is recommended to use a spacer device to facilitate inhalation of the medication.
Adults (including elderly patients)
To relieve acute asthma symptoms, including acute bronchospasm, the minimum starting dose is 1 inhalation (100 mcg). If necessary, the dose may be increased to 200 mcg (2 inhalations).
For prophylaxis, 10–15 minutes before physical exertion or anticipated exposure to allergens, administer 200 mcg (2 inhalations).
For long-term maintenance therapy, the recommended dose is 200 mcg (2 inhalations) four times daily. The total daily dose of salbutamol should not exceed 800 mcg (8 inhalations).
For children over 12 years of age, use the same doses as for adults.
Children aged 4 to 12 years
To relieve acute bronchospasm, administer 1 inhalation (100 mcg). If necessary, the dose may be increased to 200 mcg (2 inhalations).
For prophylaxis, 10–15 minutes before physical exertion or anticipated allergen exposure, administer 100 mcg (1 inhalation); if necessary, the dose may be increased to 200 mcg (2 inhalations).
For long-term maintenance therapy, the recommended dose is 200 mcg (2 inhalations) four times daily. The total daily dose of salbutamol should not exceed 800 mcg (8 inhalations).
An increased need for β2-agonists may indicate worsening asthma control. In such cases, the patient's treatment regimen should be reviewed, and the need for initiating glucocorticosteroid therapy should be considered.
Instructions for Inhaler Use
Inhaler Check
Before first use or after not using the inhaler for 5 days or more, remove the protective cap from the actuator mouthpiece by gently pressing the sides, shake the inhaler well, and release two sprays into the air to ensure proper functioning.
Using the Inhaler
- Remove the cap from the actuator mouthpiece by gently pressing the sides.
- Ensure that there are no foreign objects inside or outside the inhaler, including in the mouthpiece.
- Shake the inhaler thoroughly to remove any foreign particles and to evenly mix the contents.
- Hold the inhaler vertically between the thumb and other fingers, with the thumb positioned below the mouthpiece on the inhaler body.
- Breathe out fully, then place the mouthpiece between the teeth and close the lips around it without biting.
- While inhaling slowly and deeply through the mouth, press down on the top of the inhaler to release the salbutamol spray, continuing to inhale slowly and deeply. One press delivers one dose.
- Hold your breath, remove the mouthpiece from the mouth, and release pressure from the top of the inhaler. Continue holding your breath as long as possible.
- If additional sprays are needed, wait approximately 30 seconds, keeping the inhaler upright. Then repeat steps 3–7.
- Replace the cap securely.
IMPORTANT:
Perform steps 5, 6, and 7 without rushing. Inhale as slowly as possible just before actuating the spray. Practice the procedure in front of a mirror for the first few times. If a "mist" appears around the top of the inhaler or at the corners of the mouth, restart the procedure from step 2.
If your doctor has provided different instructions for inhaler use, follow them, and seek advice if you experience any difficulties.
Children. Young children may require assistance; it may be necessary for an adult to administer the inhalation. Ask the child to exhale, and actuate the spray immediately after they begin to inhale. It is recommended to practice the technique together. Older children or weakened adults may hold the inhaler with both hands. Place both index fingers on the top of the inhaler and both thumbs on the base below the mouthpiece.
Cleaning
The inhaler should be cleaned at least once a week.
- Remove the canister from the actuator and remove the cap from the actuator.
- Wash the actuator and cap with warm water.
- Dry them thoroughly inside and out.
- Reinsert the canister and replace the cap.
Do not immerse the canister in water.
Children. This medication is indicated for the treatment of children aged 4 years and older.
Overdose. The most common symptoms of salbutamol overdose are transient, pharmacologically mediated β-agonist effects, such as tachycardia, tremor, hyperactivity, and metabolic disturbances, including hypokalemia (see sections "Special Warnings and Precautions" and "Adverse Reactions").
Salbutamol overdose may cause hypokalemia; therefore, serum potassium levels should be monitored. Cases of lactic acidosis have been reported following high therapeutic doses or overdose of short-acting β2-agonists. Serum lactate levels should be checked, and metabolic acidosis should be monitored accordingly, especially in the presence of persistent or worsening tachypnea, despite improvement in bronchospasm symptoms such as stridorous breathing.
Adverse Reactions
The adverse reactions listed below are classified by organs and systems, as well as by frequency of occurrence: very common (≥ 1/10), common (≥ 1/100 and < 1/10), uncommon (≥ 1/1,000 and < 1/100), rare (≥ 1/10,000 and < 1/1,000), very rare (< 1/10,000), including isolated cases, frequency not known. Overall, very common and common adverse effects are determined from clinical trial data, whereas rare, very rare, and those with unknown frequency are derived from spontaneous reports.
Immune system disorders
Very rare: hypersensitivity reactions, including angioedema, urticaria, bronchospasm, arterial hypotension, and collapse.
Metabolism and nutritional disorders
Rare: hypokalemia. Potentially, the use of β2-agonists may lead to pronounced hypokalemia.
Nervous system disorders
Common: tremor, headache.
Very rare: hyperactivity.
Cardiac disorders
Common: tachycardia.
Uncommon: palpitations.
Very rare: cardiac arrhythmias, including atrial fibrillation, supraventricular tachycardia, and extrasystoles.
Frequency not known: myocardial ischemia (see section "Special precautions").
Vascular disorders
Rare: peripheral vasodilation.
Respiratory, thoracic and mediastinal disorders
Very rare: paradoxical bronchospasm.
Gastrointestinal disorders
Uncommon: irritation of the mucous membranes of the mouth and throat.
Musculoskeletal and connective tissue disorders
Uncommon: muscle cramps.
Reporting of suspected adverse reactions
Reporting of suspected adverse reactions after drug registration is important. It allows continued monitoring of the benefit-risk balance of the medicinal product. Healthcare professionals and patients, as well as their legal representatives, should report all suspected adverse reactions and lack of efficacy via the Automated Pharmacovigilance Information System at the following link: https://aisf.dec.gov.ua.
Shelf life. 2 years.
Storage conditions. Store in the original packaging at a temperature not exceeding 25 °C.
Do not freeze.
Avoid exposure to direct sunlight. Do not disassemble, puncture, or incinerate the canister, even after complete use. The canister is under pressure. Do not heat above 50 °C.
Keep out of reach of children.
Packaging. 200 doses in a pressurized canister with metering valve, with a pharmaceutical inhalation actuator and dust cap, in a cardboard box.
Prescription category. Prescription only.
Manufacturer. Limited liability company "Pharmaceutical Company "Zdorovya".
Manufacturer's address and place of business. 22, Shevchenka Street, Kharkiv, Kharkiv region, 61013, Ukraine.