Salbutamol is a bronchodilator, a selective beta-2-adrenergic receptor stimulant, which is used to relieve bronchospasm, incl. with bronchial asthma. It is not a secret for people suffering from bronchial asthma that the fastest way to stop an attack is to take a bronchodilator. medicine. Until the middle of the 20th century, adrenaline was used for this purpose, which, along with the expansion of the bronchi, caused severe tachycardia and hypertension. This was due to the fact that adrenaline acted indiscriminately both on beta-1 receptors, "responsible" for the work of the heart, and on beta-2 receptors, "supervising" the bronchi. Such non-selectivity of action for many patients (primarily for those suffering from cardiovascular diseases) is unacceptable. This necessitated the creation of a group of drugs that would act primarily on beta-2-adrenergic receptors. The “flagship” of this group of drugs was Salbutamol, first synthesized by GlaxoSmithKline and given the trade name Ventolin. Subsequently, many companies began to produce Ventolin generics, incl. under trade name"Salbutamol". Today, this drug is the first line drug for the elimination of symptoms of suffocation. The inhalation method of administering beta-2-adrenergic agonists in bronchial asthma is optimal: in this way, the active component of the drug enters directly into the area of ​​therapeutic effect - the respiratory tract. The advantage of this method of administration is the speed of development of the pharmacological effect, the insignificance of the therapeutic dose, and the reduced risk of developing unwanted side reactions. With the help of Salbutamol, it is possible to successfully stop bronchospasms, reduce resistance in the respiratory tract, and increase VC.

The drug prevents the release of the mediator of allergic reactions histamine. The frequency and strength of heart contractions are only slightly affected. Arterial pressure does not decrease. Salbutamol in injectable form is rapidly absorbed into the systemic circulation, while its plasma content remains at a low, barely detectable level. When taken orally, it is quickly and completely absorbed in the digestive tract. The drug undergoes metabolic transformations only in the liver, it is not metabolized in the lungs, and therefore its elimination depends on the route of administration. The half-life is 2-7 hours. Elimination from the body is carried out by the kidneys and, to a lesser extent, by the intestines. The drug is contraindicated in a number of conditions associated with pregnancy, with hypersensitivity of the body to active ingredient. If it is necessary to use Salbutamol in pregnant women, it is necessary to carefully weigh all the risks to the mother and fetus and correlate them with the expected benefits of pharmacotherapy. Increasing the dose and frequency of use of the drug is carried out under medical supervision. During the entire course of medication in patients with severe bronchial asthma, the content of potassium ions in the blood is monitored to prevent the development of hypokalemia, the risk of which increases with oxygen starvation. When sharing Salbutamol with non-selective beta-blockers, mutual leveling is possible pharmacological effects. When combining the drug with theophylline, an increase in heart rate and rhythm disturbances is possible. Co-administration of Salbutamol with glucocorticosteroids increases the risk of hypokalemia.

Pharmacology

Beta-agonist with a predominant effect on β 2 -adrenergic receptors (localized, in particular, in the bronchi, myometrium, blood vessels). Prevents and relieves bronchospasm; reduces airway resistance, increases lung capacity. Prevents the release of histamine, a slow reacting substance from mast cells and neutrophil chemotaxis factors. Compared with other drugs in this group, it has a less pronounced positive chrono- and inotropic effect on the myocardium. It causes expansion of the coronary arteries, practically does not reduce blood pressure. It has a tocolytic effect, lowering the tone and contractile activity of the myometrium.

Pharmacokinetics

When using an aerosol, rapid absorption of salbutamol into the blood is observed; however, its plasma concentrations, when used at recommended doses, are very low or do not reach the limit of detection.

After oral administration, salbutamol is well absorbed from the gastrointestinal tract. Plasma protein binding is 10%. Metabolized during the "first pass" through the liver and possibly in the intestinal wall; the main metabolite is an inactive sulfate conjugate. Salbutamol is not metabolized in the lungs, thus its final metabolism and excretion after inhalation depends on the route of administration, which determines the ratio between inhaled and inadvertently ingested salbutamol.

T1 / 2 from blood plasma is 2-7 hours. Salbutamol is rapidly excreted in the urine in the form of metabolites and unchanged substance; in small amounts excreted with feces.

Release form

90 doses - aluminum aerosol cans with a dosing valve (1) - packs of cardboard.

Dosage

Inside as a bronchodilator for adults and children over 12 years old - 2-4 mg 3-4 times / day, if necessary, the dose can be increased to 8 mg 4 times / day. Children aged 6-12 years - 2 mg 3-4 times / day; children 2-6 years old - 1-2 mg 3 times / day.

When administered by inhalation, the dose depends on the dosage form, 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.

Interaction

With the 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.

Side effects

From the side of the cardiovascular system: transient expansion 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 skin rash, urticaria, arterial hypotension, collapse.

Other: tremor of the hands, internal trembling, tension; rarely - paradoxical bronchospasm, muscle cramps.

Indications

Prevention and relief of bronchospasm in all forms of bronchial asthma. Reversible obstruction respiratory tract in chronic bronchitis and emphysema, broncho-obstructive syndrome in children.

Threatening 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 prophylactic purposes during operations on the pregnant uterus (imposition of a circular suture in case of insufficiency of the internal os of the uterus).

Contraindications

The threat of miscarriage in the I and II trimesters of pregnancy, premature detachment of the placenta, bleeding or toxicosis in the III trimester of pregnancy; childhood up to 2 years; hypersensitivity to salbutamol.

Application features

Use during pregnancy and lactation

Salbutamol is contraindicated in case of a threatened miscarriage in the I and II trimesters of pregnancy, premature detachment of the placenta, bleeding or toxicosis in the III trimester of pregnancy.

If it is necessary to use salbutamol during pregnancy, the expected benefit of treatment for the mother and the potential risk to the fetus should be correlated. Currently, there is insufficient data on the safety of salbutamol in early pregnancy. Salbutamol is excreted in breast milk, therefore, if necessary, use during lactation should also evaluate the expected benefits of treatment for the mother and possible risk for a child.

Use in children

Contraindicated in children under 2 years of age.

special instructions

Use with caution in tachyarrhythmias and other cardiac arrhythmias, arterial hypertension, myocarditis, heart defects, aortic stenosis, diabetes, thyrotoxicosis, glaucoma, acute heart failure (subject to close medical supervision).

An increase in the dose or frequency of salbutamol intake should be carried out 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.

Salbutamol: instructions for use and reviews

Latin name: Salbutamol

ATX code: R03AC02

Active substance: Salbutamol (Salbutamol)

Producer: OAO Moskhimfarmpreparaty im. ON THE. Semashko, CJSC Binnopharm, CJSC Altayvitaminy ( the Russian Federation), TEVA (Israel)

Description and photo update: 12.08.2019

Salbutamol is a selective β 2 -agonist, bronchodilator.

Release form and composition

Dosage form - dosed aerosol for inhalation: suspension, the spraying of which on a glass slide leaves a white spot (10 ml in a bottle with a nozzle, 1 bottle in a box; 12 ml in an aluminum aerosol can complete with a spray nozzle, in a cardboard box 1 set; 12 ml in an aluminum aerosol can complete with a metering valve, an inhalation nozzle and a safety cap, in a cardboard box 1 set; 7.02 g or 15.2 g in an aluminum aerosol can, complete with a metering valve and applicator, in a cardboard box 1 set).

1 dose of the drug contains:

  • active substance: Salbutamol - 0.1 mg;
  • auxiliary components: cetyl oleate, fluorotrichloromethane (chladone-11), difluorodichloromethane (chladone-12).

Pharmacological properties

Pharmacodynamics

Salbutamol is a selective beta2-adrenergic agonist. In therapeutic doses, the drug acts on the beta2-adrenergic receptors of the smooth muscles of the bronchi and slightly affects the beta1-adrenergic receptors of the heart muscle. Salbutamol has a pronounced bronchodilating effect. It prevents or stops bronchospasm, reduces airway resistance and increases lung capacity.

At recommended doses, Salbutamol does not increase blood pressure and does not negative impact on the heart and blood vessels. Compared with other drugs in this group, it exhibits a positive inotropic and chronotropic effect to a lesser extent. Salbutamol dilates the coronary arteries.

Metabolic effects of the drug: has a lipolytic and hyperglycemic effect, affects the secretion of insulin and glycogenolysis, reduces the plasma concentration of potassium.

Salbutamol begins to act within 5 minutes after inhalation, the maximum effect is achieved after 30-90 minutes, and the duration of its action is from 4 to 6 hours.

Pharmacokinetics

After inhalation administration of the drug, approximately 10-20% of the dose taken reaches the lower respiratory tract. The remaining 80–90% of salbutamol remains in the inhaler or enters the oropharyngeal mucosa and is swallowed. The fraction of the drug that has settled on the mucous membrane of the respiratory tract is absorbed into the blood and lung tissues, but is not metabolized in the lungs.

Salbutamol is approximately 10% bound to plasma proteins. Its metabolism occurs in the liver, and the drug is excreted mainly in the urine in the form of phenolic sulfate and unchanged. Part of the dose swallowed with saliva is absorbed from the digestive tract and is actively metabolized, undergoing a "first pass" effect through the liver, with the formation of phenolic sulfate. The elimination half-life is 4-6 hours. Salbutamol conjugate and unchanged salbutamol are excreted mainly in the urine. An insignificant part of the drug (about 4%) is excreted in the bile, and some more in the feces. Excretion of most salbutamol occurs within 72 hours.

Indications for use

  • bronchial asthma - prevention and relief of bronchospasm;
  • Chronical bronchitis;
  • chronic obstructive pulmonary disease (COPD);
  • emphysema.

Contraindications

  • coronary artery disease;
  • rhythm disturbances (polytopic ventricular extrasystole, paroxysmal tachycardia);
  • myocarditis;
  • aortic stenosis;
  • heart defects;
  • severe heart failure;
  • decompensated diabetes mellitus;
  • epileptic seizures;
  • glaucoma;
  • renal and / or liver failure;
  • pyloroduodenal narrowing;
  • period of pregnancy;
  • simultaneous reception of non-selective β-blockers, including propranolol;
  • age up to two years;
  • hypersensitivity to the components of the drug.

Instructions for use of Salbutamol: method and dosage

Aerosol for inhalation Salbutamol is intended for inhalation use.

The use of an aerosol requires compliance with certain recommendations. Before each procedure, it is necessary to shake the can thoroughly, put a sprayer on it, remove the cap from the sprayer. Turning the balloon upside down, take a deep breath and, clasping the mouthpiece with your lips, press the bottom of the balloon with a strong breath. After a strong injection of the drug, you should hold your breath for a few seconds. Then pull the mouthpiece out of your mouth and exhale slowly.

After each use, the mouthpiece must be closed with a lid.

For young children and patients unable to perform a correct breathing maneuver, a spacer can be used to smooth out asynchronous inspiratory inaccuracies and increase tidal volume.

  • relief of asthma attacks: 1-2 doses (0.1-0.2 mg), in the absence of a sufficient effect, inhalation can be repeated after 5 minutes. The next injection is only after 120 minutes or more;
  • mild to moderate asthma: 1-2 doses 1-4 times a day. Additionally, to control asthma of moderate severity, the patient is prescribed anti-asthma drugs;
  • prevention of physical effort asthma: 1-2 doses 20-30 minutes before exercise.

For the prevention of asthma attacks (allergen exposure, physical activity), the treatment of asthma attacks in children aged 2 to 12 years, it is recommended to use 1-2 doses.

Maximum daily dose- 12 inhalations (1.2 mg).

Side effects

  • respiratory system: very rarely - cough, paradoxical bronchospasm;
  • immune system: very rarely - nasal congestion, urticaria, erythema, bronchospasm, angioedema and other hypersensitivity reactions;
  • metabolic processes: rarely - hypokalemia, reversible metabolic disorders (including an increase in the level of glucose concentration in the blood);
  • cardiovascular system: rarely - increased blood pressure(BP), a slight increase in heart rate of a compensatory nature; very rarely - arterial hypotension, arrhythmia (including supraventricular tachycardia, atrial fibrillation, extrasystole), collapse; rarely - flushing of the skin of the face (dilation of peripheral vessels);
  • nervous system: often - headache, tremor; infrequently - dizziness; very rarely - sleep disturbance, fatigue, irritability, insomnia, anxiety;
  • musculoskeletal system: rarely - muscle cramps;
  • digestive system: infrequently - a violation of taste sensations; rarely - nausea, vomiting, irritation or dryness of the oral mucosa, pharyngitis.

Overdose

With an overdose of Salbutamol, the following symptoms are observed: more often - vomiting, nausea, lowering blood pressure, muscle tremor, tachycardia, hypokalemia; less often - headache, respiratory alkalosis, agitation, lack of oxygen in the blood, hyperglycemia; rarely - tachyarrhythmia, peripheral vasodilation, ventricular flutter, convulsions, hallucinations.

The best antidote for an overdose of the drug are cardioselective beta-blockers, but they should be used with caution, as the risk of bronchospasm is high.

When taking high doses of Salbutamol, it is necessary to control the serum concentration of potassium (due to the possible development of hypokalemia).

special instructions

In the treatment of severe or unstable asthma, Salbutamol should not be the only or main treatment.

The therapeutic effect of the drug should last at least 3 hours. If the effect or duration of action decreases, you should consult a doctor.

Between inhalations, a break of at least 120 minutes must be observed, since more frequent use of the drug increases the risk of increased bronchospasm and sudden death.

The insufficient effect of the recommended dosing to control the symptoms of bronchial asthma may indicate an exacerbation of the disease and the need to revise the treatment plan with an additional appointment or increase in the dose of inhaled / systemic glucocorticosteroids.

Due to the risk of hypokalemia, against the background of the use of β 2 -adrenergic agonists, special care should be taken in severe asthma attacks. Patients need to ensure regular monitoring of the level of potassium in the blood serum, since due to hypoxia and concomitant therapy with xanthine derivatives, diuretics and glucocorticosteroids, hypokalemia may increase.

The effect of Salbutamol on the ability of patients to manage vehicles and mechanisms have not been established.

Use during pregnancy and lactation

During pregnancy and lactation, Salbutamol is used with caution and only if the expected benefit to the mother outweighs the possible risk to the fetus or child.

The probability of excretion of salbutamol with breast milk is not excluded, however, there are no data on the effect of salbutamol on the body of a newborn.

Application in childhood

According to the instructions, Salbutamol is contraindicated in children under two years of age.

drug interaction

When used simultaneously with Salbutamol:

  • xanthines (including theophylline) - increase the risk of developing tachyarrhythmia;
  • levodopa, means for inhalation anesthesia - cause severe ventricular arrhythmias;
  • antihypertensive drugs, nitrates - reduce their therapeutic effect;
  • glucocorticosteroids, xanthine derivatives, diuretics - increase the risk of hypokalemia;
  • thyroid hormones increase their side effects on the heart;
  • tricyclic antidepressants, monoamine oxidase inhibitors - enhance the effect of Salbutamol and a sharp decrease in blood pressure;
  • anticholinergics (including inhalers) - may increase intraocular pressure.

Salbutamol enhances the effect of drugs that stimulate the central nervous system.

The use of the drug also increases the risk of developing glycoside intoxication.

Analogues

Analogues of Salbutamol are: Ventolin, Astalin, Saltos, Salbutabs, Ventolin Nebula, Salamol Steri-Neb, Salbutamol-Teva, Salamol Eco Easy breath, Salbutamol-MHFP, Salbutamol-aeronative, Salbutamol-native, Cibutol Cyclocaps.

Terms and conditions of storage

Store in a place protected from direct sunlight, away from the heating system at temperatures up to 30 °C. Keep away from children.

Shelf life - 2 years.

Formula: C13H21NO3, chemical name: (RS)-2-tert-Butylamino-1-(4-hydroxy-3-hydroxymethyl-phenyl)-ethanol.
Pharmacological group: vegetotropic agents / adrenomimetic agents / beta-agonists; organotropic agents / agents that regulate function genitourinary system and reproduction/tocolytics.
Pharmachologic effect: tocolytic, bronchodilator.

Pharmacological properties

Salbutamol has a highly selective stimulating effect on beta2-adrenergic receptors, activates adenylate cyclase located in cells. The bronchodilator effect of salbutamol is due to the relaxation of the smooth muscles of the bronchi. Salbutamol acts for a long time, as it is not destroyed in the lungs by catechol-O-methyltransferase. Salbutamol slows down the contractile activity of the myometrium, relaxes the uterus, and prevents premature birth. When inhaled, 10–20% of salbutamol reaches the small bronchi, where it is gradually absorbed into the systemic circulation, part of the dose is absorbed into gastrointestinal tract when swallowed. Salbutamol is well absorbed when using tablets. long-acting. The maximum concentration is 30 ng / ml. The duration of circulation of salbutamol in the blood (in therapeutic concentration) is 3-9 hours, after which the content of the drug gradually decreases. Salbutamol binds to plasma proteins by 10%.

It is excreted in breast milk and passes through the placenta. In the liver, salbutamol undergoes biotransformation. The half-life is 3.8 hours. Regardless of the route of administration, it is excreted in the bile and urine, mainly unchanged (about 90%) or in the form of a glucuronide.

Removal of bronchospasm is achieved faster with inhalation administration of salbutamol. The expansion of the bronchi already occurs at the 4–5th minute, increases by the 20th minute, becomes maximum after 40–60 minutes; the duration of the effect is 4-5 hours. The most pronounced result is achieved with inhalation of 2 doses of salbutamol, a further increase in the dose does not lead to an increase in bronchial patency, but the possibility of developing adverse reactions (headache, tremor, dizziness) increases.

Salbutamol has a positive effect on mucociliary clearance (increases it by 36% in chronic bronchitis), activates the functions ciliated epithelium stimulates mucus secretion. Slows down the release of inflammatory mediators from basophils and mast cells (for example, anti-IgE-induced release of histamine), eliminates antigen-dependent release of neutrophil chemotaxis factor and suppression of mucociliary transport. Salbutamol prevents the occurrence of bronchospasm caused by an allergen. It can cause a reduction in the number and desensitization of beta-adrenergic receptors, including those on lymphocytes. Salbutamol has a number of metabolic effects - it reduces the concentration of potassium in the plasma, acts on the release of insulin and glycogenolysis, has a lipolytic and hyperglycemic (especially in patients with bronchial asthma) effect, and increases the likelihood of developing acidosis.

Indications

Relief and prevention of bronchospasm in bronchial asthma; nocturnal asthma (tablet prolonged forms); symptomatic therapy of broncho-obstructive syndrome (including chronic bronchitis, emphysema, chronic obstructive pulmonary disease); threat premature birth(with gestation periods from 16 to 38 weeks).

Method of application of salbutamol and doses

Salbutamol is administered by inhalation, intravenously, orally (regardless of food intake). Inhalation: relief of an incipient asthma attack - 100–200 mcg (1–2 breaths); after 5 minutes, repeated inhalation is possible in the absence of effect; further inhalations are made at intervals of 4-6 hours (no more than 6 inhalations per day); regular use - 2-4 times / day, 1-2 inhalations; prevention of bronchospasm - use 15–20 minutes before contact with frosty air. Powder for inhalation: a single dose is 200-400 mg (doses twice as high due to lower bioavailability). During a severe attack, it is possible to administer an inhalation solution using various designs of nebulizers for 5-15 minutes; The initial dose for patients older than 18 months is 2.5 mg (if necessary, 5 mg is possible) up to 4 times a day. Inside, for patients over 12 years old - 3-4 times a day for 2-4 mg, the maximum single dose is 8 mg, daily - 32 mg; children 6–12 years old - 3–4 times a day, 2 mg, maximum dose is 24 mg / day, children 2-6 years old - 3-4 times a day, 1-2 mg (0.1 mg / kg). Prolonged tablets: patient over 12 years old - every 12 hours 4-8 mg, the maximum dose is 32 mg / day (every 12 hours 16 mg), children 6-12 years old - every 12 hours 4 mg, the maximum dose is 24 mg / day days (every 12 hours, 12 mg). As a tocolytic agent: intravenously drip - 2.5-5 mg diluted in 500 ml of 5% dextrose solution or 0.9% sodium chloride solution, the rate of administration of salbutamol depends on the tolerability of the drug and the intensity of the contractile activity of the uterus. Further, maintenance oral treatment with salbutamol in the form of tablets is carried out: 4-5 times a day, 2-4 mg; the first tablet is taken 15-30 minutes before the end of the infusion; the duration of treatment is 14 days.

When using a metered-dose aerosol, the following instructions must be observed: before each use, shake the aerosol can, clearly synchronize the intake of the drug and inhale, take the deepest, longest and most intense breath possible, after inhaling the drug, hold your breath for 10 seconds. For patients who find it difficult to perform a correct breathing maneuver, it is recommended to use spacers (special devices) for inhalation of the drug, which smooth out inaccuracies of asynchronous inspiration and increase tidal volume. To increase the effectiveness of treatment, the patient must be taught the correct use of the inhaler, at the beginning of therapy, use the inhaler under the supervision of medical personnel. The use of salbutamol in exacerbation of asthma in high doses leads to an increase in the intensity of the subsequent asthma attack (rebound syndrome). In severe asthma attacks, the interval between salbutamol inhalations should be at least 20 minutes. In the absence of minimal effects from inhalation or the development of tachycardia, severe tremor, arrhythmias, further uncontrolled use of the inhaler is contraindicated, you should consult a doctor. The risk of complications increases with a significant duration of therapy, as well as abrupt withdrawal of the drug.

Contraindications for use

hypersensitivity, breast-feeding, pregnancy (for use as a bronchodilator), children's age (up to 4 years - for powder for inhalation, up to 2 years - for a metered aerosol without a spacer and for oral administration, up to 18 months - for a solution for inhalation); additionally for intravenous administration as a tocolytic: intrauterine fetal death, infections of the birth canal, fetal malformations, bleeding in premature placental abruption or placenta previa; threatened miscarriage (in the 1st and 2nd trimester of pregnancy).

Application restrictions

tachyarrhythmia, coronary disease heart, expressed arterial hypertension, heart disease, myocarditis, severe heart failure, aortic stenosis, thyrotoxicosis, diabetes mellitus, pheochromocytoma, severe renal and/or liver failure.

Use during pregnancy and lactation

The use of salbutamol is contraindicated during pregnancy and lactation.

Side effects of salbutamol

Nervous system: anxiety, tremor (usually of the hands), tension, dizziness, irritability, sleep disturbances, headache, short-term convulsions;
circulatory system: tachycardia (including in the fetus during pregnancy), palpitations, arrhythmia, increased or decreased blood pressure, peripheral vasodilation, heart failure, myocardial ischemia, cardiopathy;
digestive system: nausea, irritation or dryness in the mouth or throat, vomiting, loss of appetite;
others: pharyngitis, bronchospasm (caused by hypersensitivity to salbutamol or paradoxical), sweating, difficulty urinating, increased blood glucose, free fatty acids, dose-dependent hypokalemia, the development of mental and physical drug dependence, allergic reactions in the form of swelling of the face, erythema, difficulty breathing.

Interaction of salbutamol with other substances

Salbutamol increases the cardiotropism of thyroid hormones, the activity of stimulants of the central nervous system. Ephedrine and theophylline enhance the toxic effects of salbutamol. Prostaglandin synthesis inhibitors, corticosteroids, MAO blockers and tricyclic antidepressants increase the possibility of complications from the circulatory system, levodopa and inhalation anesthesia - severe ventricular arrhythmias. Salbutamol reduces the effectiveness of antihypertensive drugs, beta-blockers (including ophthalmic forms), the antianginal effect of nitrates. Salbutamol increases the risk of glycoside intoxication when used together.

Overdose

With an overdose of salbutamol, a decrease in blood pressure, tachycardia (pulse rate up to 200 beats per minute), ventricular flutter, increased cardiac output, acidosis, hypoxemia, hyperglycemia, hypokalemia, headache, muscle tremor, agitation, convulsions, hallucinations develop. It is necessary: ​​the abolition of salbutamol and symptomatic treatment; the use of selective beta-blockers in patients with bronchial asthma due to the risk of developing a severe bronchospastic reaction requires extreme caution.

Trade names of drugs with the active substance salbutamol

Aloprol
Astalin
Ventolin®
Ventolin® Easy Breathing
Ventolin® Nebules
Volmax®
Salamol
Salamol Steri-Neb
Salamol Eco
Salamol Eco Easy Breath
Salmo
Salben®
Salbuvent
Salbutamol
Salbutamol base

Content

In 1967, British scientists developed Salbutamol, a chemical compound that can affect smooth muscle organs of the respiratory tract, uterus, affect the level of potassium in the blood. A bronchodilator created on its basis belongs to the group of selective β2-adrenergic receptor agonists - substances that can affect the body's receptors that are sensitive to the hormone adrenaline. Today, Salbutamol is the main treatment for respiratory diseases.

Composition and form of release

The drug was created on the basis of salbutamol sulfate, an odorless white crystalline powder that dissolves easily in water. There are many dosage forms of a bronchodilator - tablets of regular and prolonged action, syrup, aerosol, powder for inhalation, solution for inhalation, injections. Aerosol cans have a metering valve and spray 1 dose (0.1 mg) of the drug when pressed. The drug does not contain chlorofluorocarbon freons, its excipients are ethanol, hydrofluoroalkane, hydrofluorocarbon. The quantitative composition of different forms is given below:

Mechanism of action

Therapeutic doses of a bronchodilator, stimulating β2-adrenergic receptors, have anti-inflammatory, mucolytic (promoting sputum thinning), bronchodilator (relaxing bronchial muscles) effects. The use of Salbutamol prevents and relieves bronchospasm, including allergic and exercise-induced, stimulates the production of mucus in the respiratory tract, enhances the respiratory function of the lungs.

The bronchodilator has a tocolytic effect - it lowers the tone, reduces the contractile activity of the myometrium (the muscular layer of the uterus), and is used to prevent premature birth. It has a metabolic effect - it helps to reduce the concentration of potassium in the blood, the breakdown of glycogen to glucose, the secretion of insulin, the blocking of histamine factors, glycogenolysis (the breakdown of glycogen to glucose). Therapeutic doses do not have a β1-adrenergic effect on the heart, they inhibit chemotaxis (activity) of bone marrow cells.

Any form of substance is quickly absorbed by the blood, metabolized by the liver, intestines. The time of circulation of the substance together with the blood can reach 9 hours. Removal of bronchospasm occurs faster with the inhalation route of administration. It is possible to enhance the effect of a bronchodilator by introducing 2 doses, a further increase in the amount does not affect the state of bronchial patency, but contributes to the occurrence of side effects.

Long-acting tablets due to gradual intake active substance the necessary therapeutic plasma concentration is maintained through the shell for 12–14 hours. After taking non-prolonged dosage forms, the maximum effect is observed after 30 minutes, the action lasts when taken:

  • syrup - 2 hours;
  • tablets - 2-4 hours;
  • solution for injection - 4-6 hours.

Salbutamol - a hormonal drug or not

Many hormonal medications effective in the treatment of chronic diseases of the respiratory tract, which include bronchial asthma. They are analogues of the natural steroid hormones produced by the adrenal glands - cortisone and cortisol. The need for their appointment arises with a neglected, progressive form of the disease.

Inhalers with hormones gradually slow down the development inflammatory process reduce the frequency and severity of exacerbations. Salbutamol with bronchitis eliminates an attack of shortness of breath that has already occurred, relaxing the muscles of the bronchi by stimulating their receptors. The drug is a means of rapid, but short-term relief of spasm, belongs to the category of bronchodilators, and not hormonal drugs.

Indications for use

The drug is used for diseases of the respiratory tract, accompanied by spastic conditions of the bronchi, as tocolytics in gynecology and a means of normalizing the level of potassium in the blood. It effectively eliminates the symptoms that have arisen or prevents their occurrence, including when in contact with provoking factors, under the following conditions:

  • bronchial asthma of any etiology;
  • Chronical bronchitis;
  • chronic obstructive pulmonary disease;
  • the threat of premature birth, accompanied by contractile activity of the uterus;
  • hyperkalemia.

Method of application and dosage

The size of the prescribed dose depends on the age of the patient, the nature of the disease, the dosage form of the bronchodilator. The amount of active ingredient in tablets, injection solution, syrup, aerosol is different, so changing the dosage form is possible only by agreement with the doctor. Salbutamol for children 6-12 years old is shown in the amount of half the dose for an adult, for babies 2-6 years old, the amount of medication is selected individually. Optimal is the use of a bronchodilator on demand during an attack of bronchospasm.

Salbutamol tablets

Orally, the drug is taken to expand the bronchi due to the ineffectiveness of inhalation forms and with the threat of premature birth. Adults and children from 12 years of age are prescribed 1 tablet with an active substance content of 2 mg (in acute forms of the disease - 4 mg) 3-4 times a day. Children 6-12 years old are shown a dose of 2 mg 3-4 times, 2-6 years old - 1 mg 3 times a day. Long-acting tablets coated with a special shell containing 8 mg of the active substance are able to gradually release it, providing the necessary concentration in plasma for 12-14 hours.

As a tocolytic agent to suppress premature contractions, 1 tablet is prescribed every 2-3 hours during the first day, then for 2 days - 1 tablet every 4 hours, then for several days until the contractile activity of the uterus stops completely, 1 tablet every 6 hours. In multiple pregnancies, oral administration of the drug as a means of prophylactic tocolytic therapy is ineffective.

Powder for inhalation

Salbutamol for inhalation in the form of a powder is administered using an individual portable disk inhaler - a cyclohaler. If it is necessary to stop attacks of bronchial asthma, 1-2 doses of 200-400 mcg are prescribed once, for the prevention of exacerbation - 1-2 doses 3-4 times a day, depending on the expected degree of influence of the provoking factor. The maximum daily dose (800-1000 mcg) can be increased to 1200-1600 mcg if necessary.

Spray can

The most convenient and commonly used form of the drug is an inhalation aerosol, administered by inhalation through the oropharynx. Shake the can before first use and perform one test spray into the air. Children under 4 years of age are inhaled through an intermediate reservoir - a spacer. An adult requires 1-2 injections per oral cavity, children - only one.

If there is no reaction of the body 10 minutes after ingestion, it is allowed to make 1 more injection, after which no longer use the medicine for 4-6 hours. The number of doses during the day should be no more than 8. For the prevention of bronchospasm, 1-2 inhalations are used 15-30 minutes before physical activity or exposure to an allergen. With a weak perception of the drug and exacerbation of the disease, the doctor may increase the dose.

special instructions

The use of β2-adrenergic agents by healthy people leads to bronchial dilatation and, as a result, an increase in resistance to physical activity, therefore, in professional sports, the use of a bronchodilator agent can be regarded as doping. Alcohol should be avoided during treatment. Both with long-term treatment with the drug, and with its sudden cancellation, there is a risk of complications.

The need for a bronchodilator should not be more than 4 times a day. An increase in the frequency of use may be due to an aggravation of the disease, in which case it is recommended to reconsider approaches to its treatment. Frequent use bronchodilators can lead to increased bronchospasm and even sudden death, so between doses you need to take breaks up to 6 hours. Reducing the reception interval is possible in exceptional situations and must be justified.

Salbutamol during pregnancy

None of the tocolytics was created specifically to prevent preterm labor, therefore, all drugs that affect the contractile activity of the uterus have multiple organ (characterized by disruption of 2 or more systems of the child's body) side effects. When they are used, transplacental transfer of active substances takes place.

Among other tocolytics, β2-agonists are relatively safe for the child, but they also cross the placenta and can cause fetal tachycardia, provoke hyperinsulinemia ( elevated level insulin), hypoglycemia (low glucose levels). The use of a bronchodilator during pregnancy should be after an assessment of the expected benefits and possible risks.

drug interaction

When prescribing a bronchodilator, one should take into account its effect on the pharmacology of other drugs used to treat concomitant diseases. The simultaneous use of Salbutamol with other medicines causes the following effects:

  • enhances the effect of stimulants of the central nervous system (Phenamine, Cytiton, Strychnine);
  • when interacting with xanthines (Eufillin, Theophylline) increases the likelihood of developing tachyarrhythmia;
  • simultaneous use with inhalation anesthesia (Aerran, Foran, Halothane) and antiparkinsonian drugs (Levodop, Cognitive, Nacom) can lead to severe ventricular arrhythmias;
  • joint reception with non-selective β-blockers (Propranolol, Levobunolol, Sotalol) weakens the bronchodilator effect;
  • simultaneous use with m-cholinergic receptor blockers (Pirenzepine, Tripitramine) may increase intraocular pressure;
  • diuretics (Mercuzal, Diuver) glucocorticosteroids (Prednisone, Hydrocortisone, Betamethasone) should not be taken in conjunction with Salbutamol with low potassium levels in the blood (hypokalemia);
  • co-administration with monoamine oxidase inhibitors (Moclobemide, Selegiline) is not contraindicated.

Side effects

Allergic reactions in the form of urticaria, angioedema, paradoxical bronchospasm against the background of the use of Salbutamol are rarely recorded. When prescribing the drug during pregnancy, it should be remembered that undesirable effects can be observed simultaneously in the mother and fetus. Often a bronchodilator causes:

  • extrasystole (type of arrhythmia), tachycardia;
  • dizziness, headache;
  • nervous tension, insomnia;
  • panic, memory impairment, aggressiveness;
  • tremor, muscle cramps;
  • sweating;
  • vomiting, nausea;
  • hypokalemia;
  • arterial hypotension - lowering blood pressure;
  • urinary retention.

Overdose

Symptoms of Salbutamol poisoning are tachycardia (up to 200 beats per minute), arrhythmia, fatigue, dry mouth, dizziness. In case of an overdose, blood pressure decreases or rises, excitability, insomnia, hallucinations, muscle cramps, tremors, acidosis (acid-base imbalance with excess acid), hypoxemia (low oxygen content in the blood) occur. In the presence of hypoxia (oxygen starvation), hypoglycemia is replaced by hyperglycemia. With signs of poisoning, symptomatic treatment is carried out.

Contraindications

Take the drug with hypersensitivity to its components should not be. It is contraindicated as a bronchodilator during pregnancy and lactation, for children under 2 years of age in the form of tablets, up to 4 years of age - powder for inhalation. As a tocolytic, you can not use the drug for infections of the birth canal, malformations and death of the fetus, premature detachment of the placenta, toxicosis, threatened abortion. Contraindications to prescribing the drug are:

  • stenosis of the aortic mouth;
  • blockage of the lumen of the cardiac artery;
  • coronary artery disease;
  • myocarditis - inflammation of the heart muscle;
  • arterial hypertension;
  • hyperthyroidism, thyrotoxicosis - increased function, high level thyroid hormones;
  • hypokalemia;
  • glaucoma.

Terms of sale and storage

Salbutamol is included in list B of medicines, the storage of which is recommended in iron cabinets and safes with the inscription "Strong". Keep the drug away from fire and sources high temperature, at home - with temperature regime not higher than 30°C, out of the reach of children. It is impossible to freeze and store the medicine in direct sunlight - this helps to reduce its effectiveness. Pharmacies bronchodilator dispensed by prescription.

Analogues

There are commercially available bronchodilators that have a similar pharmachologic effect created on the basis of both salbutamol phosphate and alternative active ingredients. Some analogues of Salbutamol are presented below:

  1. Ventolin (Great Britain) is a bronchodilator drug in the form of an aerosol for inhalation based on salbutamol phosphate, used to relieve asthma attacks. The drug is contraindicated in diabetes mellitus, impaired renal function, during the 1st trimester of pregnancy.
  2. Clenbuterol (Moldova) is a powerful β2-agonist based on clenbuterol hydrochloride in the form of a syrup. It is indicated for the symptomatic treatment of bronchial asthma and chronic respiratory diseases. It is prescribed as an additional remedy against the background of corticosteroid therapy;
  3. Berotek (Germany) is an oral inhalation solution based on fenoterol hydrobromide, effective in the symptomatic treatment and prevention of asthma attacks. To dilute the solution, physiological saline is used, spraying can be carried out using any commercially available inhaler.
  4. Foradil (Switzerland) - capsules with powder for inhalation based on formoterol fumarate for use with an aerolizer inhaler, which is included in the package. The drug is prescribed for the purpose of stopping and preventing bronchospasm. The capsule is placed in the inhaler, pierced, the mouthpiece of the aerolizer is inserted into the oral cavity, the powder is sprayed with a deep breath of the patient.
  5. Onbrez Brizhaler (Switzerland) - capsules with powder for inhalation in a gelatin shell, the active substance is a selective beta-2 adrenoreceptor agonist indacaterol maleate. The drug has a long-term, up to 24 hours, effect with a single dose. Relaxes the smooth muscles of the bronchi, relieves spasm.
  6. Volmax (Great Britain) - tablets based on salbutamol sulfate of regular (2-3 hours) and prolonged (12-14 hours) action. Used as a bronchodilator and tocolytic agent. The drug is contraindicated during lactation, as a bronchodilator during pregnancy.
  7. Aloprol (Yugoslavia) - a concentrate for the preparation of a solution for infusions based on salbutamol sulfate. Introduced intravenously in severe bronchospasm, for 2-5 minutes, if necessary - every 15 minutes. It can be used as a tocolytic, intravenously, drip, the rate of administration is 20-40 drops per minute.
  8. Infortispir Respimat (Germany) is an inhalation solution based on olodaterol. Used to reduce airway obstruction, improve quality of life, exercise tolerance in patients chronic diseases lungs and bronchi.

Salbutamol price

In pharmacies of the Moscow region, the drug and its synonyms are widely presented in the form of an aerosol for inhalation by domestic and foreign manufacturers. The cost of a bronchodilator varies depending on the form of release, the country of production and the margins of suppliers. When ordering medicines in online pharmacies, you should take into account the cost of delivery.

Name

price, rub.

Where can I buy

Salbutamol-Nativ, Russia, solution for inhalation in ampoules, No. 10

Salbutamol-Teva, Israel, inhalation aerosol, 200 doses

Pharmacy "Ozerki", Bratislavskaya str., 12

Salbutamol, Russia, Aerosol for inhalation, 90 doses

Pharmacy "Zhivika", Mitinskaya st., 36

Salbutamol, Ireland, inhalation aerosol, 300 doses

Pharmacy "Europharm", Butyrskaya St., 86b

Salbutamol is a selective β 2 -agonist that has a pronounced bronchodilating effect, relieves or prevents bronchospasm, reduces airway resistance and increases lung capacity.

Release form and composition

Salbutamol is available in the form of an aerosol for dosed inhalation: a white or almost white suspension, when exiting the cylinder, it is sprayed in the form of an aerosol jet (12 ml (200 doses) is contained under pressure in an aluminum monoblock cylinder with internal protection, sealed with a metering valve and equipped with a nozzle - inhaler with a protective cap; in a cardboard box 1 bottle).

Composition of 1 dose of the drug:

  • Active ingredient: salbutamol sulfate - 0.1208 mg (corresponds to 0.1 mg of salbutamol);
  • Additional components: oleyl alcohol, propellant R 134a (1,1,1,2-tetrafluoroethane, HFA 134a), ethanol (rectified ethyl alcohol).

The product does not contain chlorofluorocarbon propellants.

Indications for use

  • Bronchial asthma (stopping of attacks of bronchial asthma, including a period of exacerbation when it occurs in severe form; use as one of the components in long-term maintenance treatment of bronchial asthma; prevention of attacks of bronchospasm caused by exercise or exposure to an allergen);
  • Chronic obstructive pulmonary disease (COPD) accompanied by chronic bronchitis, reversible airway obstruction.

Contraindications

  • Age up to 2 years;
  • Hypersensitivity to the components of the drug.

With extreme caution, it is required to use Salbutamol (due to the possible occurrence of complications) in combination with non-selective β-blockers, as well as in the following diseases (including history data):

  • Heart defects;
  • Myocarditis;
  • tachyarrhythmia;
  • Severe form of chronic heart failure;
  • Coronary artery disease;
  • aortic stenosis;
  • Arterial hypertension;
  • Pheochromocytoma;
  • thyrotoxicosis;
  • Decompensated diabetes mellitus;
  • Renal or liver failure;
  • epileptic seizures;
  • Glaucoma.

During pregnancy and lactation, the use of the drug is permissible only if the intended benefit to the woman outweighs the possible threat to the fetus and child. The possibility of salbutamol passing into breast milk cannot be ruled out, but there is also no reliable information confirming it. harmful action on the child's body.

Method of application and dosage

The drug is intended exclusively for inhalation administration.

Inhalation more than 4 times a day is not recommended. The need to increase the frequency of use of the drug or to suddenly increase the dose is a confirmation of the worsening of the course of the disease.

  • Relief of an attack of bronchospasm: 100-200 mcg (1-2 inhalations);
  • COPD and long-term maintenance treatment for bronchial asthma (as part of combination therapy): in a single dose of not more than 200 mcg (2 inhalations) 4 times a day;
  • Prevention of attacks of bronchospasm caused by physical activity or exposure to an allergen: 10-15 minutes before the action of an irritating factor or physical activity, children are administered 100-200 mcg (1-2 inhalations), adults - 200 mcg (2 inhalations).

The decision to increase the dose or frequency of use of the drug is made only by the attending physician.

Elderly people do not need dose adjustment.

Before using Salbutamol for the first time, it is necessary to remove the protective cap from the inhaler nozzle, shake the can vigorously up and down and make 2 sprays into the air to check for adequate valve operation. At a break in the use of the aerosol after vigorous shaking, one spray should be made into the air.

To administer the drug, after removing the protective cap from the inhaler nozzle and checking the cleanliness of its inner and outer surfaces, the balloon is carefully shaken. Then hold it in a vertical position (nozzle down) between the thumb, middle and index fingers, while thumb should be located under the nozzle-inhaler.

After exhaling as deeply as possible, the nozzle is placed in the mouth between the teeth, covering it with the lips, but not biting. After that, a slow and deep breath is taken through the mouth, dispensing a dose of the drug by pressing the top of the balloon. To achieve the maximum effect of the drug, it is required to inhale air as slowly as possible. Holding the breath as far as possible, the nozzle is removed from the mouth and the finger is removed from the top of the balloon.

If necessary, the next inhalation is carried out after 30 seconds, holding the balloon vertically. After completion of the procedure, the inhaler nozzle is closed with a protective cap.

It is advisable to use Salbutamol for the first few times after training in front of a mirror; in case of a “cloud” appearing on the sides of the mouth, inhalation should be carried out first.

It is recommended to clean the inhaler nozzle at least once every seven days; for this, it and the protective cap are removed from the cylinder and washed thoroughly under warm running water. Then, having dried the washed parts inside and out, the nozzle is placed on the cylinder and the valve stem, closing its free opening with a protective cap.

The balloon must not be placed in water.

Side effects

  • Cardiovascular system: often - palpitations, tachycardia; rarely - pain or discomfort in the chest, expansion of peripheral vessels, accompanied by flushing of the skin; very rarely - lowering blood pressure and collapse, extrasystole, supraventricular tachycardia, arrhythmia (including atrial fibrillation);
  • Nervous system: often - anxiety, headache, tremor; rarely - drowsiness, dizziness, fatigue; extremely rarely - hyperactivity;
  • Respiratory system: rarely - irritation of the respiratory tract, cough; very rarely - bronchospasm (paradoxical or provoked by hypersensitivity to the agent);
  • Immune system: rarely - dermatitis; extremely rarely - hypersensitivity reactions (including skin rash, angioedema);
  • Gastrointestinal tract: rarely - irritation and dryness of the mucous membrane of the pharynx and mouth, vomiting, nausea, changes in taste sensations;
  • Metabolic processes: rarely - hypokalemia;
  • Musculoskeletal system: rarely - muscle cramps.

Signs of an overdose of salbutamol include: more frequent - tachycardia, lowering blood pressure, hypokalemia, vomiting, nausea, muscle tremor; less frequent - headache, agitation, respiratory alkalosis, hyperglycemia, hypoxemia; rare - peripheral vasodilation, ventricular flutter, tachyarrhythmia, convulsions, hallucinations. The best antidotes of the drug are cardioselective ß-blockers, but they must be used with extreme caution due to the threat of developing bronchospasm.

The introduction of high doses of the drug can lead to the appearance of hypokalemia, as a result, if an overdose is suspected, it is necessary to control the level of potassium in the blood.

special instructions

The therapeutic effect of Salbutamol may decrease when the balloon is cooled, therefore, before use, the balloon must be warmed in the hands for several minutes, the use of other methods is unacceptable!

Cylinders (including empty ones) must not be pierced, broken, heated or incinerated because their contents are under pressure.

In severe or unstable asthma, bronchodilators should not be used as monotherapy drugs.

If a sore throat or unpleasant taste sensations appear after inhalation, the mouth should be rinsed with water.

The patient should contact the attending physician if the effect of the usual dose of the drug decreases or becomes shorter (the therapeutic effect usually lasts for 3 hours or more). An increase in the dose or frequency of administration of salbutamol should be carried out only as directed and under the supervision of a physician.

The introduction of large doses during an exacerbation of bronchial asthma can provoke a "rebound" syndrome (each subsequent attack will be more intense).

The interval between inhalations in case of a severe asthma attack should be at least 20 minutes.

With a sudden cancellation of treatment or if the course is too long, the risk of complications increases.

Patients receiving Salbutamol for a long period should simultaneously use anti-inflammatory drugs for basic therapy.

With a progressive and sharp worsening of bronchial asthma, it is necessary to immediately decide whether to start taking or increase the dose of glucocorticosteroids (daily monitoring of peak expiratory flow should be carried out).

In the treatment of severe attacks of bronchial asthma, the threat of developing hypokalemia is aggravated as a result of the combined use of salbutamol with diuretics, glucocorticosteroids, xanthine derivatives, and also due to hypoxia (it is necessary to control the concentration of potassium in the serum).

At the beginning of the course of treatment with the drug, due to the risk of dizziness and convulsions, it is necessary to exercise increased caution when driving vehicles and operating other complex mechanisms.

drug interaction

Possible interaction reactions of salbutamol with other drugs:

  • Xanthines (theophylline, etc.) - the threat of developing tachyarrhythmias is aggravated;
  • Stimulants of the central nervous system - the effect of these drugs is enhanced;
  • Levodopa, means for inhalation anesthesia - the risk of severe ventricular arrhythmias increases;
  • Glucocorticosteroids, diuretics - the hypokalemic effect of salbutamol is enhanced;
  • M-anticholinergics (including inhalation) - an increase in intraocular pressure is possible.

The drug can be used in combination with monoamine oxidase inhibitors.

Terms and conditions of storage

Store away from direct sunlight and heating system, out of the reach of children, at a temperature not exceeding 25 °C. Do not freeze.

Shelf life - 2 years.