Pharmacological properties of the drug Salbutamol
Salbutamol is a selective β2-adrenergic receptor agonist. Stimulates mainly β2-adrenergic receptors localized in the bronchi, myometrium, and blood vessels. When administered by inhalation, it acts mainly on β2-adrenergic receptors of the bronchi, with little effect on β2-adrenergic receptors of other localizations. Has a pronounced bronchodilator effect. By causing dilation of the bronchi, it relieves and prevents bronchospasm. Has virtually no effect on β1-adrenergic receptors of the heart. Prevents the release of allergy and inflammatory mediators (histamine, SRSA) from mast cells. Improves mucociliary clearance. The effect of the drug develops quickly and lasts 3–4 hours. After inhalation, approximately 10–20% of the active substance reaches the small bronchi, the rest settles in the upper respiratory tract. Plasma protein binding is 10%. Salbutamol is metabolized in the liver. It is excreted mainly in the urine unchanged and as an inactive metabolite. Most of the dose of salbutamol administered by inhalation or taken orally is eliminated within 72 hours.
Indications for use of the drug Salbutamol
BA (prevention and relief of attacks), chronic obstructive bronchitis, emphysema and other diseases that occur with bronchospasm. As a tocolytic agent, it is indicated for the threat of premature birth, isthmic-cervical insufficiency, a decrease in the fetal pulse depending on uterine contractions during periods of cervical dilatation and expulsion, for prophylactic purposes - during operations on the pregnant uterus (application of a circular suture for insufficiency of the internal uterine pharynx) .
Salbutamol-Pharmstandard HF 100 mcg/dose dosed aerosol for inhalation, 200 doses
Registration Certificate Holder
PHARMSTANDARD-LEKSREDSTVA (Russia)
Dosage form
Medicine - Salbutamol-Pharmstandart
Description
Aerosol for inhalation dosed
in the form of a white or almost white suspension; upon exiting the container, it is sprayed in the form of an aerosol cloud.
1 dose
salbutamol sulfate 120 mcg, which corresponds to the content of salbutamol 100 mcg
Excipients
: ethanol (absolute ethyl alcohol) - 5.905 mg, oleic acid - 0.009 mg, propellant R134a (1,1,1,2-tetrafluoroethane) - 67.966 mg.
200 doses - aluminum cylinders (1) with a dosing valve and a spray nozzle - cardboard packs.
Indications
Prevention and relief of bronchospasm in all forms of bronchial asthma. Reversible airway obstruction in chronic bronchitis and emphysema, broncho-obstructive syndrome in children.
Threatened premature birth with contractile activity of the uterus; childbirth before 37-38 weeks of pregnancy; isthmic-cervical insufficiency, a decrease in fetal heart rate depending on uterine contractions during periods of cervical dilatation and expulsion. For preventive purposes during operations on the pregnant uterus (application of a circular suture in case of insufficiency of the internal os of the uterus).
Contraindications for use
Threat of miscarriage in the first and second trimesters of pregnancy, premature placental abruption, bleeding or toxicosis in the third trimester of pregnancy; children under 2 years of age; hypersensitivity to salbutamol.
pharmachologic effect
Beta-adrenergic agonist with a predominant effect on β2-adrenergic receptors (localized, in particular, in the bronchi, myometrium, blood vessels). Prevents and relieves bronchospasm; reduces resistance in the respiratory tract, increases the vital capacity of the lungs. Prevents the release of histamine, a slow-reacting substance from mast cells and neutrophil chemotaxis factors. Compared to other drugs in this group, it has a less pronounced positive chrono- and inotropic effect on the myocardium. Causes expansion of the coronary arteries, practically does not reduce blood pressure. It has a tocolytic effect, reducing the tone and contractile activity of the myometrium.
Drug interactions
With simultaneous use of salbutamol with non-cardioselective beta-blockers, mutual suppression of therapeutic effects is possible; with theophylline - the risk of developing tachycardia and arrhythmia, in particular supraventricular extrasystole, increases.
With the simultaneous use of salbutamol and xanthine derivatives, corticosteroids or diuretics, the risk of developing hypokalemia increases.
Dosage regimen
Orally as a bronchodilator for adults and children over 12 years of age - 2-4 mg 3-4 times a day, if necessary, the dose can be increased to 8 mg 4 times a day. Children aged 6-12 years - 2 mg 3-4 times a day; children 2-6 years old - 1-2 mg 3 times a day.
When administered by inhalation, the dose depends on the dosage form used, the frequency of use depends on the indications and the clinical situation.
As a tocolytic agent, it is administered intravenously in a dose of 1-2 mg.
Side effect
From the cardiovascular system:
transient dilatation of peripheral vessels, moderate tachycardia.
From the side of the central nervous system:
headache, dizziness, nausea, vomiting.
From the side of metabolism:
hypokalemia.
Allergic reactions:
in isolated cases - angioedema, allergic reactions in the form of skin rash, urticaria, arterial hypotension, collapse.
Other:
tremor of the hands, internal trembling, tension; rarely - paradoxical bronchospasm, muscle cramps.
special instructions
Use with caution for tachyarrhythmias and other heart rhythm disorders, arterial hypertension, myocarditis, heart defects, aortic stenosis, diabetes mellitus, thyrotoxicosis, glaucoma, acute heart failure (subject to careful medical supervision).
Increasing the dose or frequency of taking salbutamol should be done under the supervision of a physician. Reducing the interval is possible only in exceptional cases and must be strictly justified.
When using salbutamol, there is a risk of developing hypokalemia, therefore, during treatment in patients with severe bronchial asthma, the level of potassium in the blood should be monitored. The risk of hypokalemia increases with hypoxia.
Use during pregnancy and breastfeeding
Restrictions during pregnancy - Contraindicated. Restrictions when breastfeeding - With caution.
Salbutamol is contraindicated in cases of threatened miscarriage in the first and second trimesters of pregnancy, premature placental abruption, bleeding or toxicosis in the third trimester of pregnancy.
If it is necessary to use salbutamol during pregnancy, the expected benefits of treatment for the mother should be weighed against the potential risk to the fetus. Currently, there is insufficient data on the safety of the use of salbutamol in early pregnancy. Salbutamol is excreted in breast milk, so if it is necessary to use it during lactation, the expected benefit of treatment for the mother and the possible risk for the child should also be assessed.
Use in children
Restrictions for children - Contraindicated.
Contraindicated in children under 2 years of age.
Use of the drug Salbutamol
Inhalation - adults and children over 4 years of age are prescribed 0.1 mg of salbutamol for inhalation to eliminate bronchial obstruction. If the attack does not stop within 5–10 minutes after the first inhalation, inhalation can be repeated. For preventive purposes, 0.1 mg of salbutamol is also recommended to be administered by inhalation 10–15 minutes before possible contact with the suspected allergen. With long-term use of salbutamol, use 1-2 inhalations (0.1 mg) 3-4 times a day with an interval of at least 3 hours. Long-term use of salbutamol for COPD or asthma is carried out only against the background of basic therapy. Do not use more than 10 doses (1 mg of salbutamol) per day. Orally, adults are usually prescribed 0.002 g 3-4 times a day. As a tocolytic agent to eliminate the threat of premature birth, as well as after operations on the pregnant uterus, it is administered intravenously in a dose of 5 mg in 400–500 ml of isotonic solution or 5% glucose solution at a rate of 15–20 drops (starting from 5 drops) per minute. The infusion rate is adjusted taking into account the intensity of uterine contractions and tolerance (heart rate and other hemodynamic indicators are monitored). Duration of administration: 6–12 hours.
Special instructions for the use of the drug Salbutamol
Use with extreme caution in case of hypersensitivity to sympathomimetics, severe heart disease (chronic ischemic heart disease, acute myocardial infarction, hypertrophic obstructive cardiomyopathy, rhythm disturbances), hyperthyroidism, unstable diabetes mellitus, pheochromocytoma. During pregnancy, it can be used only for health reasons. Since salbutamol passes into breast milk, its use during breastfeeding is possible only if the expected therapeutic effect for the mother outweighs the potential risk for the child. The use of salbutamol in high doses may worsen the reaction when driving a car or operating machinery. This effect is enhanced by simultaneous use of alcohol and tranquilizers.
Salbutamol aerosol for inhalation dosed 100 mcg/dose 200 doses No. 1
Name
Salbutamol aer. ding.dosage.100mcgdose in ing.200dose in pack No.1
Description
A metal inhaler with a depressed bottom, equipped with a metering valve, containing a white or almost white suspension. There should be no damage to the inner surface of the inhaler.
Main active ingredient
Salbutamol
Release form
200 doses in an aluminum inhaler equipped with a plastic dosing device with a protective cap. The assembled inhaler and dosing device, together with instructions for use, are placed in a cardboard box.
Dosage
100 mcg / 1 dose 200 doses
special instructions
No data.
pharmachologic effect
Drugs for the treatment of obstructive respiratory diseases. Adrenergic agents for inhalation use. Selective beta-2 adrenergic receptor agonists. ATX code: R03AC02.
Pharmacodynamics
Salbutamol is a selective beta-2 adrenergic receptor agonist. After inhalation, salbutamol has a stimulating effect on beta-2 adrenergic receptors of bronchial smooth muscle, thus providing rapid bronchodilation, which manifests itself within a few minutes and lasts for 4–6 hours.
Pharmacokinetics
Salbutamol After inhalation administration of the drug, its concentration in the blood plasma when taking usual doses is insignificant (10–50 times less than when taking the drug orally or by injection). There is no relationship between blood concentration levels and efficacy. After pulmonary resorption, the drug is excreted mainly by the kidneys, partly unchanged (less than 2%), partly in the form of inactive metabolites (phenolic sulfates). 1,1,1,2-tetrafluoroethane: propellant gas Following inhalation administration of the drug, adsorption of 1,1,1,2-tetrafluoroethane is slight and rapid, with maximum concentrations achieved in less than 6 minutes. In animals (mice and rats), negligible hepatic metabolism of the drug was observed with the formation of trifluoroacetic acid and trifluoroacetic aldehyde. However, according to the results of kinetic studies conducted among patients taking 1,1,1,2-tetrafluoroethane in the presence of pathologies, cases of trifluoroacetic acid formation were not identified.
Indications for use
Symptomatic treatment of bronchial asthma attacks. Symptomatic treatment of exacerbations of bronchial asthma or chronic obstructive bronchitis. Preventing exercise-induced asthma attacks. Test for reversibility of bronchial obstruction during functional studies of the respiratory tract.
Directions for use and doses
Dosage Regardless of age: Treatment of attacks and exacerbations of bronchial asthma: when the first symptoms appear, take 1-2 inhalations. Prevention of exercise-induced asthma attacks: 1-2 inhalations 15-30 minutes before the start of physical activity. In general, a dose of 1–2 inhalations is sufficient to treat breathing difficulties. If symptoms persist, the dose can be repeated after a few minutes. The duration of the bronchodilating effect of salbutamol when administered by inhalation is from 4 to 6 hours. If symptoms recur, the drug can be repeated. Typically, the daily dose of the drug should not exceed 8 inhalations within 24 hours. If this dose is exceeded, the patient should be informed of the need for medical consultation in order to review the indications for use (see section "Precautions"). In the case of a severe acute attack of asthma or severe exacerbation of chronic obstructive bronchopneumopathy, the dose of the drug is from 2 to 6 inhalations, which should be repeated every 5-10 minutes until emergency medical professionals arrive. In such situations, it is recommended that the patient use an inhalation chamber, as it helps to accelerate the pulmonary diffusion of salbutamol taken by inhalation. However, pressing the metered-dose inhaler repeatedly and releasing doses into the inhalation chamber may reduce the total inhaled dose, and the patient must inhale the medication directly (or, if necessary, after each series of two consecutive presses) from the inhalation chamber after each press of the inhaler. In the future, taking the drug should be repeated in successive cycles. A severe acute attack of bronchial asthma requires hospitalization. In this case, treatment consists of oxygen therapy and systemic corticosteroid therapy. Method of application: Inhalation administration using a device in the form of a sealed canister equipped with a mouthpiece. In order to use the device correctly, the physician is advised to ensure that the patient is using the inhaler correctly. If a patient is found to have a lack of synchronization between inhalation and pressing the inhaler, the use of an inhalation chamber is indicated. Also in such patients it is possible to use other more adapted types of dosage forms of salbutamol. In children and infants who require treatment with Salbutamol inhalation suspension in the form of an aerosol, it is advisable to use an inhalation chamber equipped with a spacer. The inhaler is not equipped with a dose counter.
Use during pregnancy and lactation
Pregnancy Salbutamol In clinical practice, there are a sufficient number of documented examples of the use of the drug during pregnancy, which allows us to conclude that salbutamol is safe to use during pregnancy. Therefore, the use of salbutamol during pregnancy by inhalation is acceptable. When taking the drug during pregnancy: A rapid heartbeat in the fetus may be observed against the background of tachycardia in the mother. In exceptional cases, the persistence of a rapid heartbeat after birth is noted. Similarly, in exceptional cases, postnatal changes in glycemic levels are noted. If the drug is taken before delivery, the peripheral vasodilatory effect of beta-2 mimetics should be taken into account. 1,1,1,2-tetrafluoroethane: propellant gas Reproduction studies performed in animals have not shown any harmful effects caused by 1,1,1,2-tetrafluoroethane, which is contained in this medicinal product. However, the effects of taking 1,1,1,2-tetrafluoroethane in pregnant women have not been established. Lactation Beta-2 mimetics pass into breast milk. The penetration of the displacing gas and its metabolites into breast milk when taking the drug has not been established. Fertility There is no information on the effects of salbutamol on fertility in humans. Preclinical studies did not reveal any undesirable effects on fertility in animals.
Precautionary measures
Special instructions Inform the patient about the need to immediately seek medical help if the previously observed relief does not occur during the development of an attack of bronchial asthma. An increased need for the use of bronchodilators, in particular beta-2 agonists, may be a sign of exacerbation of bronchial asthma or obstructive bronchopneumopathy. If the patient's need for long-acting and short-acting beta-2-mimetic bronchodilators by inhalation increases significantly over several days, one should be concerned (especially if the peak flow meter readings decrease and/or become irregular) of respiratory decompensation, and in asthmatics, the possibility development of status asthmaticus. Therefore, the physician should inform the patient of the need to seek immediate medical attention in such a case without intentionally exceeding the maximum prescribed doses. In such a situation, it is necessary to reconsider the indications for use. A sudden and progressive exacerbation of bronchial asthma can be life-threatening. In such a situation, it is necessary to consider either corticosteroid therapy or an increase in the dosage of existing corticosteroid therapy. In addition, in adult patients with asthma, inhaled corticosteroid therapy should be used when beta-2 mimetic agonists are needed more than once per week. In this case, it is necessary to inform the patient that improvement in his clinical condition should not be a consequence of changes in therapy, in particular, discontinuation of inhaled corticosteroids without medical advice. As with the use of other drugs for inhalation therapy, immediately after using the drug, paradoxical bronchospasm may develop, which manifests itself in more pronounced difficulty breathing and increased wheezing. Bronchospasm requires treatment with an alternative form of the drug or another bronchodilator for inhalation therapy (if available). The use of Salbutamol by inhalation should be stopped immediately and, if necessary, another fast-acting bronchodilator should be prescribed to continue treatment. Medicines with sympathomimetic effects, which include salbutamol, can cause disturbances in the functioning of the cardiovascular system. According to data obtained during the post-registration period of use of the drug, as well as in the literature, cases of myocardial ischemia associated with the use of salbutamol were noted. Patients with severe underlying cardiopathy (eg, coronary artery disease, arrhythmia, or severe heart failure) should be advised to contact their physician if chest pain or other symptoms suggestive of exacerbation of heart disease occur. Attention should be paid to assessing symptoms such as shortness of breath and chest pain, which can be the result of both heart disease and diseases of the respiratory system. Precautions for use In case of bronchial infection or profuse bronchorrhea, appropriate treatment should be provided to promote optimal diffusion of the drug in the respiratory tract. Salbutamol should be administered with caution to patients taking significant doses of other sympathomimetic drugs. Taking salbutamol in normal doses by inhalation using a device in the form of a sealed can usually does not cause adverse reactions in patients suffering from hyperthyroidism, coronary circulatory disorders, obstructive cardiomyopathy, ventricular arrhythmia, arterial hypertension, diabetes mellitus, unlike salbutamol, which is taken by nebulizer orally or by injection, which should be administered with caution to such patients. Therapy with beta-2 mimetics in high doses (especially when administered parenterally or by nebulizer) can lead to potentially severe hypokalemia, which can cause cardiac arrhythmias. In such cases, it is recommended to monitor the level of potassium in the blood serum, in particular, with the simultaneous use of xanthine derivatives, corticosteroids, diuretics, due to hypoxia, as well as in patients with a high risk of developing arrhythmias (prolonged QT interval or therapy that can prolong the QT interval). Like other beta-2 adrenergic agonists, salbutamol may cause an increase in blood glucose levels. Cases of ketoacidosis have been reported in patients with diabetes. Concomitant use of corticosteroids may enhance this effect. Extremely rare cases of lactic acidosis associated with the use of increased doses of short-acting beta-2 agonists, administered intravenously or by inhalation using a nebulizer, have been reported, mainly in patients undergoing therapy to relieve exacerbation of bronchial asthma). Elevated levels of lactic acid may cause difficulty breathing or compensatory hyperventilation, which may be misinterpreted as a sign of unsuccessful asthma treatment due to inappropriate increases in the dosage of short-acting beta-agonists. Therefore, the risk of developing lactic acidosis should be closely monitored, especially in severe cases. Athletes: Athletes should be aware that this medicinal product contains an active substance that may show positive results in anti-doping control tests.
Interaction with other drugs
Combinations not recommended + Non-selective beta-blockers It is not recommended to prescribe salbutamol in combination with non-selective beta-blockers such as propranolol as concomitant therapy. + Halogen drugs for anesthesia (halothane) During obstetric surgical operations, there is an increase in the inertia of the uterus with the risk of bleeding; In addition, there is a risk of developing serious ventricular arrhythmias with increased cardiac reactivity. Combinations requiring precautions during use + Antidiabetic drugs: Beta-2 mimetics are associated with an increase in glycemia, which may be interpreted as a decrease in the effect of antidiabetic therapy, therefore, it may be necessary to change antidiabetic therapy (see section "Precautions") . Increased monitoring of blood and urine status is recommended.
Contraindications
An allergic reaction to one of the components of the drug. Intolerance to this drug (unexpected cough or development of bronchospasm immediately after taking the drug). In this case, treatment should be stopped and other therapy or other methods of administration should be prescribed.
Compound
Active substance: salbutamol sulfate 120.5 mcg per dose (equivalent to 100 mcg salbutamol). Excipients: propellant GR106642X (1,1,1,2-tetrafluoroethane, also known as HFA 134a or norflurane). Does not contain CFCs.
Overdose
Signs and symptoms of salbutamol overdose are transient phenomena, expressed in increased pharmacodynamic effects of beta-2 agonists (see sections "Precautions" and "Side effects"). An overdose of salbutamol may result in hypokalemia. Therefore, in case of overdose, monitoring of serum potassium concentration is necessary. Cases of nausea, vomiting and hyperglycemia have been reported mainly in children and in cases where overdose resulted from oral administration of salbutamol. Cases of lactic acidosis have been reported with increased doses of rapidly acting beta-2 agonists. Therefore, in case of overdose, it is necessary to monitor the concentration of lactate in the blood serum, as well as the risk of developing lactic acidosis, in particular in the case of persistence or worsening of tachypnea, despite the disappearance of symptoms of bronchospasm such as wheezing, which may be associated with the development of metabolic acidosis. Necessary actions: observation and symptomatic treatment.
Side effect
Adverse 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
Storage conditions
At temperatures not exceeding 30 °C, do not freeze, do not expose to sunlight. Keep out of the reach of children. Like most other aerosol inhalers, Salbutamol may be less effective at low temperatures. When the canister cools down, it is recommended to remove it from the plastic case and warm it with your hands for a few minutes. The can cannot be disassembled, pierced or thrown into fire, even if it is empty.
