Salbutamol-neo

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT SALBUTAMOL-NEO (SALBUTAMOL-NEO)

Composition:

Active substance: salbutamol sulfate;

1 dose of aerosol contains 100 mcg of salbutamol sulfate (calculated as salbutamol);

Excipients: oleic alcohol, ethanol 96%, tetrafluoroethane.

Pharmaceutical form. Pressurized inhalation, 100 mcg/dose.

Main physicochemical properties: white or almost white suspension under pressure in a container (aluminum canister with a metering valve), equipped with an inhaler adapter and a protective cap; the preparation is released from the canister as a spray jet.

Pharmacotherapeutic group. Drugs used in obstructive respiratory diseases. Anti-asthmatic agents. Adrenergic agents for inhalation use. Selective beta-2-adrenergic agonists. Salbutamol.

ATC Code R03AC02.

Pharmacological properties.

Pharmacodynamics.

Salbutamol-NEO is a selective beta2-adrenoreceptor agonist. In therapeutic doses, it acts on beta2-adrenoreceptors of bronchial smooth muscle, providing rapid (within 5 minutes) and short-term (4–6 hours) bronchodilation in patients with reversible airway obstruction.

Pharmacokinetics.

When the drug is inhaled, 10–20% of the administered dose reaches the lower airways. The remainder of the dose remains in the "delivery" system or in the oropharynx, from where it is absorbed. Part of the dose that reaches the airways is absorbed into lung tissue and enters the bloodstream, but is not metabolized in the lungs. After entering systemic circulation, the drug is metabolized in the liver and excreted primarily by the kidneys, both unchanged and as an inactive phenolsulfate metabolite. Part of the dose that enters the gastrointestinal tract 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.

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 caused by allergens or triggered by physical exertion.

As part of combination therapy in patients with bronchial asthma.

Contraindications.

Hypersensitivity to any component of the medicinal product. Although salbutamol in the form of a solution for intravenous injection and sometimes in tablet form is used in preterm labor, salbutamol in the form of an inhalation aerosol is not indicated for these conditions. Salbutamol should not be used in cases of threatened abortion.

Interaction with other medicinal products and other forms of interaction.

Salbutamol should not be co-administered with non-selective beta-adrenergic blockers such as propranolol.

Salbutamol is not contraindicated for use in patients receiving monoamine oxidase inhibitors (MAOIs).

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 informed that they may experience a different taste compared to that when using their previous inhaler.

Sudden and progressive worsening of bronchial asthma is a life-threatening condition requiring initiation of treatment or an increase in the dose of corticosteroids. Patients at risk should be advised to perform daily monitoring of peak expiratory flow.

Bronchodilators should not be the sole or primary treatment for patients with severe or unstable bronchial asthma. These patients require regular monitoring, including pulmonary function tests, as severe bronchial asthma is a life-threatening condition and may require administration of inhaled and/or oral glucocorticosteroids.

If the effect of the usual dose of salbutamol becomes less effective or the duration of action decreases (less than 3 hours), the patient should consult a physician. Any increase in dose or frequency of administration must be prescribed only by a doctor.

Patients who are on regular anti-inflammatory therapy should be advised to continue taking anti-inflammatory medications even when symptoms subside and they do not require Salbutamol-NEO.

An increased need for bronchodilators, particularly short-acting inhaled beta-2 agonists, to control symptoms of bronchial asthma indicates an exacerbation 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 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, 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 undergo reassessment (e.g., daytime symptoms, nocturnal awakenings, and activity limitations due to asthma) to allow appropriate adjustment of therapy, as these patients belong to a high-risk group for excessive salbutamol use.

Severe exacerbations of bronchial asthma should be treated according to standard protocols.

Sympathomimetics, including salbutamol, affect the cardiovascular system. According to post-marketing surveillance data and scientific literature, rare cases of myocardial ischemia associated with salbutamol use have been reported. Patients with heart conditions (e.g., ischemic heart disease, arrhythmia, or severe heart failure) being treated with salbutamol should seek medical help if they experience chest pain or other symptoms suggestive of worsening cardiac disease. 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 formulations or nebulizer use. Particular attention should be paid to patients with acute severe bronchial 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 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 increase in dyspnea after administration may occur. In such cases, alternative formulations or other fast-acting inhaled bronchodilators should be prescribed immediately. Salbutamol should be discontinued promptly, the patient's condition reassessed, and if necessary, another fast-acting bronchodilator prescribed for ongoing use.

Use during pregnancy or breastfeeding

Animal studies have shown that salbutamol has reproductive toxicity. Safety in human 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 intrauterine development, including cleft palate, limb defects, and cardiac abnormalities (some women used multiple other medications during pregnancy). Salbutamol should not be used during pregnancy—use is possible only if clearly needed.

Salbutamol is likely excreted in breast milk; therefore, it should be administered to breastfeeding women with caution. It is unknown whether the presence of salbutamol in breast milk causes 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 child.

Ability to influence reaction speed when driving or operating machinery

No data are available on this effect. If nervous system side effects (e.g., tremor) occur, driving or operating machinery should be avoided.

Method of Administration and Dosage

Salbutamol is an aerosol intended for oral inhalation only. For patients who have difficulty coordinating breathing with inhaler use, it is recommended to additionally use a spacer device to facilitate inhalation of inhaled medications.

Adults (including elderly patients)

To relieve acute symptoms of bronchial asthma, 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, 200 mcg (2 inhalations) should be administered.

For long-term maintenance therapy, 200 mcg (2 inhalations) 4 times daily is recommended.

Children aged 4 to 12 years

For relief of acute bronchospasm, 1 inhalation (100 mcg) is administered. If necessary, the dose may be increased to 200 mcg (2 inhalations).

Children aged 12 years and older should receive doses as recommended for adults.

For prophylaxis 10–15 minutes before physical exertion or anticipated exposure to allergens, 200 mcg (2 inhalations) should be administered.

For long-term maintenance therapy, 200 mcg (2 inhalations) 4 times daily is recommended.

The total daily dose of salbutamol must not exceed 800 mcg (8 inhalations). Increased need for beta-2 agonists may indicate worsening of bronchial asthma. In such cases, the patient’s treatment regimen should be reviewed and the need for initiating glucocorticosteroid therapy should be considered.

Preparation before First Use

Before first use, remove the protective cap from the inhaler nozzle. Then shake the container well vertically, turn the container upside down with the inhaler nozzle facing downward, and release two sprays into the air to ensure proper functioning. If the inhaler has not been used for several days, one spray into the air should be released after shaking the container thoroughly.

Instructions for Use:

1. Remove the protective cap from the inhaler nozzle. Ensure that both the inner and outer surfaces of the inhaler nozzle are clean.

1. Shake the container well using vertical movements.

1. Turn the container upside down with the inhaler nozzle facing downward. Hold the container vertically between the thumb and the middle and index fingers, with the thumb positioned under the inhaler nozzle.
2. Breathe out as deeply as possible, then place the inhaler nozzle in the mouth between the teeth and close the lips around it without biting.
3. While starting to inhale slowly through the mouth, press down on the top of the container to release a spray, continuing to inhale slowly and deeply.
4. Hold the breath, remove the inhaler nozzle from the mouth, and remove the finger from the top of the container. Continue holding the breath as long as possible.

1. If another inhalation is required, wait approximately 30 seconds while holding the inhaler vertically, then repeat steps 2–6.

Replace the protective cap on the inhaler nozzle.

IMPORTANT:

Perform steps 4, 5, and 6 without rushing. It is essential to begin inhaling as slowly as possible just before actuating the spray. For the first few times, practice in front of a mirror. If a "mist" appears around the mouth, restart from step 2.

Cleaning:

The inhaler nozzle should be cleaned at least once a week.

1. Remove the protective cap from the inhaler nozzle, then detach the inhaler nozzle from the container.
2. Wash the inhaler nozzle and protective cap thoroughly under warm running water.
3. Dry the inhaler nozzle and protective cap thoroughly, both inside and outside.
4. Reattach the inhaler nozzle to the container and valve stem, and cover the open end of the inhaler nozzle with the protective cap.

Do not immerse the container in water!

Children

For use in children aged 4 years and older.

Overdose

The most common signs and symptoms of salbutamol overdose are transient, pharmacologically mediated effects induced by beta-agonists, such as tachycardia, tremor, hyperactivity, and metabolic disturbances, including hypokalemia (see sections "Special Warnings and Precautions for Use" and "Adverse Reactions").

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 monitored, especially in cases of persistent or increasing tachypnea despite improvement in bronchospasm symptoms such as stridorous breathing.

Side effects.

The adverse reactions listed below are classified by system organ class and 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, arterial hypotension, and collapse.

Metabolism and nutritional disorders

Rare: hypokalaemia. Beta-2 agonists have the potential to 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 for use").

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.

Shelf life. 2 years.

Do not use after the expiry date stated on the packaging.

Storage conditions.

Store at a temperature not exceeding 25°C. Do not freeze. Protect from falls, impacts, and direct sunlight. Keep out of reach of children.

Packaging. 12 ml/200 doses in a container; 1 container in a cardboard box.

Prescription category.

Prescription only.

Manufacturer. LLC "Micropharm".

Manufacturer's address and place of business.

20 Shevchenka Street, Kharkiv, 61013, Ukraine.