Composition
Active substance: salbutamol sulfate 120.5 μg in a single dose (equivalent to 100 μg of salbutamol).
Excipients: propellant GR106642X (1,1,1,2-tetrafluoroethane, also known as HFA 134a or norflurane). Does not contain freons of chlorofluorocarbons.
Description
A metal inhaler with a dented bottom, equipped with a metering valve, containing a suspension of white or almost white color. The internal surface of the inhaler should not be damaged.
Pharmachologic effect
Salbutamol is a selective agonist of beta-2-adrenergic receptors. In therapeutic doses, it acts on the beta-2-adrenergic receptors of the bronchial muscles, providing a short-term (4-6 hours) bronchodilation with a rapid onset of action (within 5 minutes) with reversible airway obstruction.
Special patient groups
Children under the age of 4 with bronchospasm associated with reversible airway obstruction, in which the recommended dose of salbutamol was used, show that the safety profile of dosed aerosol Salbutamol in this category of patients is comparable to the safety profile in children over 4 years of age, adolescents and adults.
Pharmacokinetics
Introduced intravenously, salbutamol has a half-life of 4 to 6 hours. It is excreted partially by the kidneys and partly by metabolism to inactive 4′-0-sulfate (phenolic sulfate), which is also excreted mainly in the urine. Only a small part of the administered dose of salbutamol is excreted with feces.
After inhalation, 10-20% of the dose of salbutamol reaches the lower respiratory tract. The rest of the dose remains in the inhaler or is deposited in the oropharynx and then swallowed. The fraction reaching the airways is absorbed into the lung tissue and blood, but not metabolized in the lungs.
After entering the systemic bloodstream, salbutamol undergoes hepatic metabolism and is excreted, mostly with urine, in unchanged form or as phenolic sulfate.
The swallowed portion of the inhalation dose is absorbed from the gastrointestinal tract and is subjected to active metabolism upon first passage through the liver, turning into phenolic sulfate. Unchanged salbutamol and conjugate are excreted mainly in the urine.
The bulk of the dose of salbutamol administered intravenously, orally or by inhalation, is excreted within 72 hours.
The degree of binding of salbutamol with plasma proteins is about 10%.
Indications for use
Salbutamol is shown to adults, adolescents and children aged 4 to 11 years. When using a medicinal product in children under 4 years old, see the section “Method of administration and dose” and “Pharmacokinetic properties”.
With reversible airway obstruction, Salbutamol provides a short-term (4-6 hours) bronchodilating effect with a rapid onset of action (within 5 minutes).
Salbutamol should be used to eliminate the symptoms that arise, and also to prevent them in situations that are considered by the patient as triggering an asthma attack (for example, before physical exertion or unavoidable contact with the allergen).
Salbutamol is of particular value as a means of medical care for asthma of mild, moderate or severe degree, provided that its use does not lead to a delay in the appointment and use of regular inhaled corticosteroid therapy.
Contraindications
Hypersensitivity to any component of the drug.
Despite the fact that salbutamol intravenously and sometimes in the form of tablets is used in the management of premature births not complicated by conditions such as placenta previa, prenatal bleeding or toxemia, salbutamol in the form of a solution for inhalations is not intended for use in the management of preterm labor. Salbutamol should not be used in case of threat of miscarriage
Pregnancy and lactation
Studies in animals have revealed reproductive toxicity.
The safety of salbutamol in pregnant women has not been established, no controlled studies have been conducted. There have been rare reports of various malformations in children (including cleft palate, developmental limbs, heart problems) against intrauterine exposure to salbutamol during pregnancy. In some of these cases, mothers took several medicines during pregnancy. Salbutamol should not be used during pregnancy, except when absolutely necessary.
Salbutamol probably penetrates into breast milk, and therefore its use by nursing mothers requires careful consideration. There is no indication as to whether the salbutamol present in breast milk has a harmful effect on the newborn, so the use of salbutamol by lactating women should be limited.
Dosing and Administration
Salbutamol, aerosol for inhalation dosed, is intended only for inhalation. Patients who are difficult to synchronize the release of aerosol from the inhaler and inhale can use the Volumatic ™ spacer.
Adults (including elderly patients)
For the relief of acute asthma symptoms, including bronchospasm, one inhalation (100 μg) can be used as a single minimal starting dose. If necessary, the dose can be increased to 2 inhalations. To prevent symptoms caused by exposure to an allergen or physical exertion, the recommended dose is 2 inhalations for 10-15 min before exposure to a provoking factor.
With prolonged therapy, 2 inhalations are administered up to 4 times a day.
Children
Elimination of acute bronchospasm
The recommended dose for children under 12 years is 1 inhalation (100 μg). If necessary, the dose can be increased to 2 inhalations.
Children from the age of 12: dosing regimen as adults.
Prevention of bronchospasm caused by exposure to an allergen or physical exertion.
The recommended dose for children under 12 years is 1 inhalation (100 μg) before contact with an allergen or physical exertion. If necessary, the dose can be increased to 2 inhalations.
Children from the age of 12: dosing regimen as adults.
Long-term therapy
The recommended dose for children under 12 years is up to two inhalations 4 times a day.
Children from the age of 12: dosing regimen as adults.
To facilitate the use of the drug in children under five years of age, a Babyhaler ™ spacer can be used.
The maximum daily dose of salbutamol should not exceed 8 inhalations.
The need for frequent use of maximum doses of salbutamol or a sudden increase in dose indicates a poor control or worsening of the course of asthma.
Side effect
Undesired reactions are listed depending on the anatomical and physiological classification and frequency of occurrence, which is defined as follows: very often (> 1/10), often (> 1/100 and <1/10), sometimes (> 1/1000 and <1 / 100), rarely (> 1/10 000 and <1/1000) and very rarely (<1/10 000), including individual cases. Very frequent and frequent adverse reactions were mainly detected during clinical trials. Reports of rare and very rare adverse reactions, as well as reactions with an unknown frequency, have been reported in spontaneous reports.
From the immune system: very rarely: hypersensitivity reactions, including angioedema, hives, bronchospasm, hypotension and collapse. From the side of metabolism: rarely: hypokalemia. Therapy with beta-2 agonists can lead to potentially serious hypokalemia.
From the nervous system: often: tremor, headache; very rarely: hyperactivity.
From the cardiovascular system: often: tachycardia; sometimes: palpitation (pulsation); very rarely: arrhythmias, including atrial fibrillation, supraventricular tachycardia and extrasystole; frequency unknown: myocardial ischemia.
Myocardial ischemia was reported in spontaneous reports obtained during post-marketing surveillance, so the frequency of this adverse reaction is not known.
From the side of the vessels: rarely: the widening of the peripheral vessels.
From the respiratory system, chest and mediastinum: very rarely: a paradoxical bronchospasm.
As with inhalation therapy with other drugs, after the use of salbutamol in the form of a dosed aerosol, a paradoxical bronchospasm can be observed, manifested by an increase in wheezing immediately after inhalation. In such cases, you must immediately use an alternative dosage form or other rapid inhalation bronchodilator. Salbutamol in the form of a dosed aerosol for inhalations should be immediately abolished, an assessment of the patient’s condition should be made and, if necessary, an alternative therapy should be prescribed.
From the gastrointestinal tract: sometimes: irritation of the mucous membrane of the oral cavity and pharynx.
From the musculoskeletal system: sometimes: muscle cramps.
If these side effects occur, and reactions not mentioned in the instructions for medical use, you should contact your doctor.
Overdose
The most common symptoms and signs of overdose are reversible and are related to the pharmacological properties of beta-agonists. Symptoms include tachycardia, tremors, hyperactivity, changes in the metabolism, including hypokalemia.
An overdose of salbutamol can cause hypokalemia, so you should monitor the potassium level in the blood serum.
In case of an overdose, consideration should be given to withdrawing treatment and prescribing appropriate symptomatic therapy, such as cardioselective beta-blockers in patients with symptoms of heart failure (eg, tachycardia, palpitations). Beta-blockers should be used with caution in patients with bouts of bronchospasm in the anamnesis.
Precautionary measures
For optimum drug delivery to the lungs, you should make sure that the patient correctly uses the inhaler and synchronizes the inhalation with the release of the drug. Patients should be warned that the taste after inhalation of Salbutamol may differ from the taste that patients felt after using other inhalers.
Bronchodilators are not false or the main component of the therapy of asthma of unstable or severe course. Treatment of patients with severe asthma requires regular medical evaluation of the patient’s condition with the performance of functional pulmonary tests, since there is a possibility of severe attacks with a life threatening patient. Physicians should consider setting the maximum recommended dose of inhaled corticosteroids and / or oral corticosteroids in this category of patients.
The dose or frequency of use of the drug may be increased only on the advice of a physician. If the effect of a normal dose of Salbutamol becomes less effective or less prolonged (the drug should last at least 3 hours), the patient should consult a doctor. The increased need for the use of inhaled beta-2-adrenergic receptor agonists with a short duration of action to control the symptoms of bronchial asthma indicates an exacerbation of the disease. The patient should be informed of the need to consult a doctor in this situation. The doctor should evaluate the patient’s condition and consider the need for strengthening anti-inflammatory therapy (increasing the dose of inhaled corticosteroids or the appointment of a course of oral corticosteroids).
Severe exacerbation of asthma should be treated with standard methods. The use of sympathomimetics, including salbutamol, may have an effect on the cardiovascular system. According to the post-marketing application and published literature, rare cases of myocardial ischemia associated with salbutamol administration have been documented. Patients with existing heart disease (eg, coronary heart disease, arrhythmia or severe heart failure) who use salbutamol should be warned about the need to see a doctor if chest pain or other symptoms that indicate an exacerbation of heart disease. Attention should be paid to the assessment of such symptoms as dyspnea and chest pain, since they can be a consequence of both heart disease and respiratory system diseases.
Salbutamol should be used with caution in patients with thyrotoxicosis.
Therapy with beta-2-adrenergic agonists, mainly with their parenteral administration or with the help of a nebulizer, can lead to hypokalemia. It is recommended to exercise extreme caution in the treatment of severe attacks of bronchial asthma, because in these cases, hypokalemia may be exacerbated by the simultaneous use of xanthine derivatives, steroids, diuretics, and also due to hypoxia. In such situations, it is necessary to monitor the potassium level in the blood serum.
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Form of issue
For 200 doses in an aluminum inhaler equipped with a plastic dosing device with a protective cap. The inhaler and the metering device are assembled together with the instructions for use in a cardboard box.
Storage conditions
At temperatures not exceeding 30 ° C, do not freeze, do not allow exposure to sunlight. Keep out of the reach of children.
Like most other inhalers in aerosol packages, Salbutamol may be less effective at low temperatures. When cooling the can, it is recommended to remove it from the plastic case and warm it with your hands for several minutes. A balloon can not be disassembled, pierced and thrown into the fire, even if it is empty.
Shelf life
2 years. Do not use after the expiration date indicated on the package.
Conditions of leave from pharmacies
On prescription.