Salbutamol
Ukraine
Table of Contents
INSTRUCTION FOR MEDICAL USE OF THE MEDICINAL PRODUCT SALTERBUTAMOL (SALBUTAMOLUM)
Composition:
Active substance: salbutamol;
1 dose contains 100 mcg of salbutamol (as salbutamol sulfate);
Excipients: ethanol 96%, propellant HFC-134a.
Pharmaceutical form. Pressurized inhalation, suspension.
Main physicochemical characteristics: white or almost white pressurized suspension contained in a monoblock aluminium canister equipped with a metering valve and an inhalation nozzle, protected by a cap; the preparation is released from the canister as a spray aerosol jet.
Pharmacotherapeutic group.
Medicinal products for treatment of obstructive airway diseases. Selective beta-2-adrenergic agonists. ATC code R03AC02.
Pharmacological properties.
Pharmacodynamics.
Salbutamol is a selective beta-2 adrenergic receptor agonist. At therapeutic doses, it acts on beta-2 adrenergic receptors of bronchial smooth muscle, providing rapid (within 5 minutes) and short-acting (4–6 hours) bronchodilation in patients with reversible airway obstruction.
Pharmacokinetics.
After inhaled administration, 10 to 20% of the dose reaches the lower respiratory tract. The remainder remains in the inhalation device or is deposited 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.
Once in the systemic circulation, the drug is metabolized in the liver and is primarily excreted by the kidneys, both unchanged and as a phenolsulfate metabolite.
The portion of the dose that is swallowed from the oropharynx is absorbed from the gastrointestinal tract, undergoes first-pass metabolism in the liver to the 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 10%.
Clinical characteristics.
Indications.
Relief of bronchospasm attacks in bronchial asthma and other conditions associated with reversible airway obstruction.
Prevention of bronchospasm attacks caused by allergens or physical exertion.
As part of combination therapy in patients with bronchial asthma.
Contraindications.
Hypersensitivity to any component of the medicinal product. Do not use salbutamol formulations not intended for intravenous administration to suppress uncomplicated preterm labor or threatened abortion.
Interaction with other medicinal products and other forms of interaction.
Salbutamol must not be used concomitantly with non-selective beta-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. Sudden and progressive worsening of bronchial asthma is a life-threatening condition requiring initiation or increase in the use of corticosteroids. Patients belonging to high-risk groups should perform daily monitoring of peak expiratory flow.
Bronchodilator agents should not be the sole or primary treatment for patients with severe or unstable bronchial asthma. The condition of such patients must be monitored regularly, including pulmonary function tests, as severe asthma is a life-threatening disease, and treatment of such patients may require consideration of prescribing maximum recommended doses of inhaled and/or oral glucocorticosteroids.
Patients receiving regular anti-inflammatory therapy (e.g., inhaled corticosteroids) should be advised to continue taking anti-inflammatory medications even when symptoms subside and they do not require salbutamol.
If the usual dose of salbutamol becomes less effective or its duration of action decreases (less than 3 hours), the patient should consult a physician. Dose adjustment or increased frequency of administration should be performed only by a physician.
An increased need for bronchodilators, particularly short-acting inhaled beta-2 agonists, to control symptoms of bronchial asthma indicates worsening of the disease, and patients should be warned to seek medical help as soon as possible. In such cases, the treatment plan should be reviewed, and consideration should be given to increasing the dose of inhaled corticosteroids or initiating a course of oral corticosteroids.
Excessive use of short-acting beta-agonists may mask the progression of the underlying disease and contribute to worsening asthma control, thereby increasing the risk of severe asthma exacerbations and mortality.
Patients who use salbutamol more than twice a week on an as-needed basis (excluding prophylactic use before physical exertion) should undergo reassessment (e.g., daytime symptoms, nocturnal awakenings, and activity limitations due to asthma) for appropriate adjustment of therapy, as these patients belong to the high-risk group for excessive salbutamol use.
Severe asthma exacerbations should be treated according to standard protocols.
Sympathomimetics, including salbutamol, affect the cardiovascular system. Post-marketing surveillance and published data have reported rare cases of myocardial ischemia associated with salbutamol use. Patients with heart disease (e.g., ischemic heart disease, arrhythmia, or severe heart failure) receiving salbutamol should seek medical help if chest pain or other symptoms suggestive of worsening cardiac disease occur. Symptoms such as dyspnea and chest pain should be carefully evaluated, as they may result from either cardiac or respiratory disorders.
Salbutamol should be prescribed with caution to patients with thyrotoxicosis.
Treatment with beta-2 agonists may result in severe hypokalemia; this is mainly observed with parenteral administration or nebulizer use. 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 cautiously in patients receiving high doses of other sympathomimetic agents. Like other beta-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 administration may occur. In such cases, alternative formulations of the drug or other rapid-acting inhaled bronchodilators should be prescribed immediately. Salbutamol should be discontinued promptly, the patient's condition assessed, and if necessary, another rapid-acting bronchodilator prescribed for regular use.
Use during pregnancy or breastfeeding.
Animal studies have shown that salbutamol has reproductive toxicity. Safety of 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 of fetal development, including cleft palate, limb defects, and cardiac abnormalities. Salbutamol may be used in the treatment of women during pregnancy or breastfeeding only if the expected benefit to the mother outweighs the potential risk to the fetus or newborn.
Salbutamol is likely to pass into breast milk; therefore, it should be administered to breastfeeding women with caution. It is unknown whether the presence of salbutamol in breast milk has harmful effects on the infant; therefore, its use in breastfeeding women should be restricted to cases where the benefit to the woman outweighs the potential risk to the infant.
Ability to affect reaction speed when driving or operating machinery.
There are no data on the effect of salbutamol on driving or operating machinery. If adverse reactions affecting the nervous system (e.g., tremor) occur, driving or operating machinery should be avoided.
Method of Administration and Dosage
Salbutamol is a medication intended solely for inhalation via the mouth. For patients who have difficulty coordinating breathing with the use of an inhaler, 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 initial minimum dose is 1 inhalation (100 mcg). If necessary, the dose may be increased to 200 mcg (2 inhalations).
For prophylaxis, 200 mcg (2 inhalations) should be administered 10–15 minutes before physical exertion or anticipated exposure to allergens.
For long-term maintenance therapy, 200 mcg (2 inhalations) four times daily is recommended. The total daily dose of salbutamol should not exceed 800 mcg (8 inhalations).
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).
Children aged 12 years and older should receive the adult dosage.
For prophylaxis, 200 mcg (2 inhalations) should be administered 10–15 minutes before physical exertion or anticipated exposure to allergens.
For long-term maintenance therapy, 200 mcg (2 inhalations) four times daily is recommended.
An increased need for beta-2 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 Using the Inhaler
Checking the Inhaler
Before first use or after a period of non-use exceeding 1 week, remove the mouthpiece cap, shake the inhaler well, and release one spray into the air to ensure proper functioning.
Using the Inhaler
- Remove the mouthpiece cap (Fig. 1).
- Ensure that the inside and outside of the inhaler, including the mouthpiece, are free from foreign objects.
- Shake the inhaler thoroughly to dislodge any foreign particles and to evenly mix its contents.
- Turn the inhaler container upside down and hold it vertically between the thumb and the index and middle fingers, with the thumb positioned beneath the inhaler (Fig. 2).
- Breathe out as deeply as possible, then place the mouthpiece in the mouth between the teeth and seal lips around it without biting (Fig. 3).
- While inhaling slowly and deeply through the mouth, press down on the top of the inhaler to release a dose of salbutamol. One press equals one dose.
Fig.1 Fig.2 Fig.3
- Hold your breath, remove the inhaler from the mouth, and remove your finger from the top of the inhaler. Continue holding your breath for as long as possible.
- If additional inhalations are required, wait approximately 30 seconds while keeping the inhaler upright. Then repeat steps 3–7.
- Replace the mouthpiece cap.
IMPORTANT:
Perform steps 5, 6, and 7 without rushing. Inhalation immediately before actuation should be as slow as possible. For the first few times, practice in front of a mirror. 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 using the inhaler, follow those. Seek advice if you experience any difficulties.
Children: Children may require assistance, and it may be necessary for an adult to administer the inhalation. Ask the child to breathe out, and administer the spray immediately after inhalation begins. 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 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 plastic inhaler holder and remove the mouthpiece cap.
- Wash the plastic holder and mouthpiece cap with warm water.
- Dry them thoroughly inside and out.
- Reinsert the canister and replace the mouthpiece cap.
DO NOT PUT THE METAL CANISTER IN WATER.
Children
The medication is indicated for the treatment of children aged 4 years and older.
Overdose
The most common symptoms of salbutamol overdose are transient pharmacologically induced beta-agonist effects, such as tachycardia, tremor, hyperactivity, and metabolic disturbances, including hypokalemia (see sections "Special Warnings and Precautions for Use" and "Undesirable Effects").
Salbutamol overdose may lead to hypokalemia; therefore, serum potassium levels should be monitored. Cases of lactic acidosis have been reported following administration of high therapeutic doses or overdose of short-acting beta-agonists. Serum lactate levels should therefore be checked, and metabolic acidosis should be appropriately managed, particularly in cases of persistent or worsening tachypnea despite improvement in bronchospasm symptoms such as stridor.
Side effects
The adverse reactions listed below are classified by organ systems and by frequency of occurrence: very common (≥1/10), common (≥1/100 to <1/10), uncommon (≥1/1000 to <1/100), rare (≥1/10,000 to <1/1000), very rare (<1/10,000), including isolated cases, frequency not known.
Immune system disorders
Very rare: hypersensitivity reactions including angioedema, urticaria, bronchospasm, hypotension, and collapse.
Metabolism and nutritional disorders
Rare: hypokalaemia. Beta-2 agonists may potentially cause pronounced hypokalaemia.
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 ischaemia (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 pharynx.
Musculoskeletal and connective tissue disorders
Uncommon: muscle cramps.
Shelf life.
2 years.
Storage conditions.
Store at a temperature not exceeding 25 °C. Do not freeze. Keep out of reach of children. Avoid exposure to direct sunlight. Do not disassemble, puncture, or incinerate the container, even after complete use.
Packaging.
An aluminium container containing 200 doses of the medicinal product, hermetically sealed with a metering valve and equipped with an inhalation nozzle and a protective cap. The container is placed in a cardboard box.
Prescription status. Prescription only.
Manufacturer.
LLC "Multispray".
Manufacturer's address and place of business.
24, Valeriy Petrosov St., lit. A-2, Kharkiv, Kharkiv region, 61052, Ukraine.