The asthma drug salbutamol. Are there side effects? Composition and impact

(SALBUTAMOL)

Registration number- LSR-006937/10

Tradename- Salbutamol

International non-proprietary name- Salbutamol

Chemical Name:
bis(1RS)-2-[(1,1-dimethylethyl)amino]-1-ethanol] sulfate. Dosage form- dosed aerosol for inhalation

The composition of the drug:
Active substance: salbutamol sulfate 0.1208 mg per dose (equivalent to 0.1 mg salbutamol).
Excipients: oleyl alcohol, ethanol (rectified ethyl alcohol), propellant R 134a (1,1,1,2-tetrafluoroethane, HFA 134a). The preparation does not contain chlorofluorocarbon propellants.

Description:
The drug is a white or almost white suspension, under pressure in an aluminum cylinder with a metering valve, equipped with an inhaler nozzle with a protective cap; the drug is sprayed in the form of an aerosol jet upon exiting the balloon.

Pharmacotherapeutic group:


Bronchodilator - selective beta 2-agonist.

ATX code: R03AC02.

PHARMACOLOGICAL PROPERTIES
Pharmacodynamics.
Salbutamol is a selective ß 2 -adrenergic agonist. In therapeutic doses, it acts on the ß 2 -adrenergic receptors of the smooth muscles of the bronchi, having a slight effect on the ß 1 -adrenergic receptors of the myocardium. It has a pronounced bronchodilating effect, preventing or stopping bronchospasm, reduces resistance in the airways. Increases the vital capacity of the lungs.
In the recommended therapeutic doses, it does not adversely affect the cardiovascular system, does not cause an increase in blood pressure. To a lesser extent, compared with drugs of this group, it has a positive chrono- and inotropic effect. Causes expansion of the coronary arteries. It has a number of metabolic effects: it reduces the concentration of potassium in plasma, affects glycogenolysis and insulin secretion, has a hyperglycemic (especially in patients with bronchial asthma) and lipolytic effect, increasing the risk of acidosis.
After the use of inhalation forms, the action develops quickly, the onset of the effect is after 5 minutes, the maximum is after 30-90 minutes (75% of the maximum effect is achieved within 5 minutes), the duration is 4-6 hours.
Pharmacokinetics.
After inhalation, 10-20% of the dose of salbutamol reaches the lower respiratory tract. The rest of the dose remains in the inhaler or settles on the mucous membrane of the oropharynx and is then swallowed. The fraction deposited on the mucous membrane of the respiratory tract is absorbed into the lung tissues and blood, but is not metabolized in the lungs.
The degree of binding of salbutamol to plasma proteins is about 10%.
Salbutamol is metabolized in the liver and excreted mainly in the urine unchanged and in the form of phenolic sulfate. The swallowed part of the inhalation dose is absorbed from the gastrointestinal tract and undergoes active metabolism during the "first pass" through the liver, turning into phenolic sulfate. Unchanged salbutamol and the conjugate are excreted primarily in the urine.
The half-life of salbutamol is 4-6 hours. It is excreted by the kidneys partly unchanged and partly as an inactive metabolite 4 "-O-sulfate (phenolic sulfate). A small part is excreted in the bile (4%), with feces. Most of the dose of salbutamol is excreted in within 72 hours

INDICATIONS FOR USE
1. Bronchial asthma:
- relief of attacks of bronchial asthma, including exacerbation of severe bronchial asthma;
- prevention of attacks of bronchospasm associated with exposure to an allergen or caused by physical activity;
- use as one of the components in long-term maintenance therapy of bronchial asthma.
2. Chronic obstructive pulmonary disease (COPD), accompanied by reversible airway obstruction, chronic bronchitis.

CONTRAINDICATIONS
- Hypersensitivity to any component of the drug.
- Children's age up to 2 years.

CAREFULLY
if there is a history of tachyarrhythmia, myocarditis, heart defects, aortic stenosis, coronary heart disease, severe chronic heart failure, arterial hypertension, thyrotoxicosis, pheochromocytoma, decompensated diabetes mellitus, glaucoma, epileptic seizures, renal or hepatic insufficiency, simultaneous use of non-selective ß-blockers , pregnancy, lactation.

USE IN PREGNANCY AND LACTATION
Salbutamol can be prescribed to pregnant women only if the expected benefit to the patient outweighs the potential risk to the fetus. The possibility of salbutamol penetration into breast milk is not excluded, therefore it is not recommended to prescribe it to nursing women, unless the expected benefit to the patient herself outweighs the potential risk to the child. There is no data on whether salbutamol present in breast milk has a harmful effect on the newborn.

METHOD OF APPLICATION AND DOSES
Salbutamol aerosol for inhalation dosed 100 mcg/dose is intended for inhalation only.
Only a doctor can decide whether to increase the dose or frequency of the drug.
It is not recommended to use the drug more than 4 times a day. The need for frequent use of maximum doses of the drug or a sudden increase in dose indicates a deterioration in the course of the disease.
Adults (including elderly patients) . Long-term maintenance therapy for bronchial asthma and COPD as part of complex therapy: the recommended dose is up to 200 mcg (2 inhalations) 4 times a day.
Prevention of attacks of bronchospasm associated with exposure to an allergen or caused by exercise: the recommended dose is 200 mcg (2 inhalations) 10-15 minutes before exposure to a provoking factor.
Children. Long-term maintenance therapy for bronchial asthma and COPD as part of complex therapy: the recommended dose is up to 200 mcg (2 inhalations) 4 times a day.
Relief of an attack of bronchospasm: the recommended dose is 100-200 mcg (1-2 inhalations).
Prevention of attacks of bronchospasm associated with exposure to an allergen or caused by exercise: the recommended dose is 100-200 mcg (1-2 inhalations) 10-15 minutes before exposure to a provoking factor.

Rules for the use of the drug:
Preparation for the first application:
Before the first use of the drug, remove the protective cap from the inhaler nozzle. Then vigorously shake the canister with vertical motions, turn the canister upside down with the inhaler nozzle and make two sprays into the air to make sure that the valve works adequately. With a break in the use of the drug for several days, one spray into the air should be done after thoroughly shaking the can.
Application:
1. Remove the protective cap from the inhaler nozzle. Make sure that the inner and outer surfaces of the inhaler nozzle are clean.
2. Shake the can vigorously with vertical movements.
3. Turn the balloon upside down with the inhaler nozzle, hold the balloon vertically between the thumb and middle and index fingers so that the thumb is under the inhaler nozzle.
4. Exhale as deeply as possible, then place the inhaler nozzle in your mouth between your teeth and cover it with your lips without biting.
5. Starting to inhale through the mouth, press the top of the balloon to dispense the dose of the drug, while continuing to inhale slowly and deeply.

6. Hold your breath, remove the inhaler nozzle from your mouth and remove your finger from the top of the balloon. Continue to hold your breath as much as possible.
7. If necessary, perform the next inhalation. To do this, wait about 30 seconds, holding the balloon vertically. After that, perform inhalation in accordance with the instructions in paragraphs 2-6.
Close the inhaler nozzle with a protective cap.
IMPORTANT:
Perform actions in accordance with paragraphs 4, 5 and 6 slowly. It is important that immediately before the dose is given, start inhaling as slowly as possible. The first few times you should use the drug after training in front of a mirror. If a “cloud” appears on the sides of the mouth, then it is necessary to start again from point 2.
Cleaning:
The inhaler nozzle should be cleaned at least once a week.
1. Remove the protective cap from the inhaler nozzle, and remove the inhaler nozzle from the balloon.
2. Thoroughly rinse the inhaler nozzle and protective cap under warm running water.
3. Dry the inhaler cap and protective cap thoroughly inside and out.
4. Put the inhaler nozzle on the balloon and the valve stem, close the free opening of the inhaler nozzle with a protective cap.
Do not place the can in water!

SIDE EFFECT
By frequency, side effects can be divided into the following categories: very often (> 1/10), often (> 1/100 and<1/10), нечасто (>1/1000 and<1/100), редко (>1/10 000 and<1/100), очень редко (<1/10 000) встречающиеся.
From the side of the immune system: rarely - dermatitis; very rarely - hypersensitivity reactions, including angioedema, skin rash;
From the side of metabolic processes: rarely - hypokalemia.
From the side of the nervous system: often - tremor, headache, anxiety; rarely - dizziness, drowsiness, fatigue; very rarely - hyperactivity.
From the side of the cardiovascular system: often - tachycardia, palpitations; rarely - the expansion of peripheral vessels with flushing of the skin, discomfort or pain in the chest; very rarely - arrhythmia, including atrial fibrillation, supraventricular tachycardia, extrasystole, lowering blood pressure and collapse.
From the respiratory system: rarely - cough, irritation of the respiratory tract; very rarely - bronchospasm (paradoxical or caused by hypersensitivity to the drug).
From the gastrointestinal tract: rarely - dryness and irritation of the mucous membrane of the oral cavity and pharynx, changes in taste sensations, nausea, vomiting.
From the musculoskeletal system: rarely - muscle cramps.

OVERDOSE
Overdose symptoms: more frequent - hypokalemia, lowering blood pressure, tachycardia, muscle tremor, nausea, vomiting; less frequent - agitation, hyperglycemia, respiratory alkalosis, hypoxemia, headache; rare - hallucinations, convulsions, tachyarrhythmia, ventricular flutter, peripheral vasodilation.
With an overdose of salbutamol, cardioselective ß-blockers are the best antidotes. However, ß-adrenergic blockers must be used with caution (risk of developing bronchospasm).
The use of large doses of salbutamol can cause hypokalemia, therefore, if an overdose is suspected, the concentration of potassium in the blood serum should be monitored.

INTERACTIONS WITH OTHER DRUGS
It is not recommended to use salbutamol and non-selective ß-adrenergic blockers, such as propranolol, at the same time.
Salbutamol is not contraindicated in patients receiving monoamine oxidase inhibitors (MAOIs).
Enhances the effect of stimulants of the central nervous system.
Theophylline and other xanthines, when used simultaneously, increase the likelihood of developing tachyarrhythmias; means for inhalation anesthesia, levodopa - severe ventricular arrhythmias.
Simultaneous use with m-anticholinergics (including inhalation) may increase intraocular pressure. Diuretics and glucocorticosteroids enhance the hypokalemic effect of salbutamol.

SPECIAL INSTRUCTIONS
Patients should be instructed on the correct use of Salbutamol. The correct use of the drug and the precise implementation of the instructions is necessary in order to ensure that salbutamol enters the bronchi. At the beginning of treatment, the drug should be used under the supervision of medical personnel and after training in front of a mirror.
As with the use of other inhalation drugs, the therapeutic effect may decrease when the balloon is cooled. Therefore, before use, the balloon with the drug must be warmed up to room temperature (warm the balloon with your hands for several minutes, you can not use other methods!).
The contents of the cylinders are under pressure, so the cylinders must not be heated, broken, pierced or incinerated, even when they are empty.
In case of discomfort in the mouth and sore throat after inhalation, the mouth should be rinsed with water.
Bronchodilators should not be the sole or main component of the treatment of unstable or severe bronchial asthma.
If the effect of the usual dose of the drug becomes less effective or less prolonged (the effect of the drug should last at least 3 hours), the patient should consult a doctor. Increasing the dose or frequency of salbutamol intake should be carried out only under the supervision of a physician. Reducing the interval between taking the following doses is possible only in exceptional cases and must be strictly justified. An increase in the need for the use of inhaled ß 2 -adrenergic agonists with a short duration of action for the treatment of bronchial asthma indicates an exacerbation of the disease. In such cases, the patient's treatment plan should be reviewed. Taking high doses of salbutamol during exacerbation of bronchial asthma can cause the "rebound" syndrome (each subsequent attack becomes more intense). In case of a severe attack of suffocation, the interval between inhalations should be at least 20 minutes.
The risk of complications increases both with a significant duration of treatment, and with a sharp withdrawal of the drug. Long-term use of salbutamol should be accompanied by the use of anti-inflammatory drugs for basic therapy.
Sudden and progressive worsening of bronchial asthma can pose a threat to the patient's life, therefore, in such cases, it is necessary to urgently address the issue of prescribing or increasing the dose of glucocorticosteroids. In such patients, daily monitoring of peak expiratory flow is recommended.
Salbutamol should be used with caution in patients with thyrotoxicosis.
Therapy with ß 2 -adrenergic agonists, especially when administered parenterally or by nebulizer, can lead to hypokalemia. Particular caution is recommended in the treatment of severe attacks of bronchial asthma, since in these cases hypokalemia may increase as a result of the simultaneous use of xanthine derivatives, glucocorticosteroids, diuretics, and also due to hypoxia. In such cases, it is necessary to control the concentration of potassium in the blood serum.
Influence on the ability to drive a car and / or other mechanisms.
Since Salbutamol can cause side effects such as convulsions and dizziness, it is recommended that you exercise increased caution at the first dose or refuse to drive vehicles and engage in other potentially hazardous activities.

RELEASE FORM
Aerosol for inhalation dosed 100 mcg / dose. 200 doses (12 ml each) in aluminum monoblock cylinders with internal protection, sealed with a dosing valve and equipped with an inhaler nozzle with a protective cap. Each cylinder, together with a nozzle and a protective cap, as well as instructions for use, is placed in a pack.

SHELF LIFE
2 years. Do not use after the expiration date.

STORAGE CONDITIONS
Store below 25°C. Do not freeze.
Keep out of the reach of children!
Keep away from heating system and direct sunlight.
Protect from drops and impacts.

TERMS AND CONDITIONS OF DISCOUNT FROM PHARMACIES
On prescription.

MANUFACTURER:
ZAO Binnopharm
Address: Russia, 124460, Moscow, Zelenograd, passage 4th Zapadny, 3, building 1

ORGANIZATION ACCEPTING CLAIMS:
ZAO Binnopharm
Address: Russia, 124460, Moscow, Zelenograd, passage 4th Zapadny, 3, building 1.

The drug "Salbutamol" refers to bronchodilator drugs. One of the representatives of selective beta2-adrenergic agonists. It is most often used to smooth out attacks caused by bronchial asthma.

In this article, we will look at why doctors prescribe Salbutamol, including instructions for use, analogues and prices for this drug in pharmacies. Real REVIEWS of people who have already used Salbutamol can be read in the comments.

Composition and form of release

Salbutamol is produced 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).

  • The main substance is salbutamol sulfate (124 mg = 100 g of pure substance).
  • Additional substances - propellant GR106642X. The preparation does not contain chlorofluorocarbon freons.

Pharmacological action: salbutamol is a bronchodilator, a selective β2-adrenergic agonist (selective β2-adrenergic receptor antagonist).

What helps Salbutamol?

There are several medical indications for the use of Salbutamol aerosol, which are aimed at improving airway patency for air and restoring the function of external respiration, these include:

  • Complex treatment of bronchial asthma together with glucocorticosteroids.
  • Short-term expansion of the bronchi (up to 4 hours) with improved breathing, a decrease in the severity of shortness of breath with the development of obstructive syndrome.
  • Relief of attacks of shortness of breath in the development of bronchial asthma, which is characterized by an allergic reaction with bronchospasm, and other obstructive pulmonary pathology.

Also, the drug is used to prevent attacks of shortness of breath associated with a narrowing of the lumen of the bronchial tree.

Pharmacodynamics and pharmacokinetics

Beta-agonist with a predominant effect on β2-adrenergic receptors (localized, in particular, in the bronchi, myometrium, blood vessels). Prevents and relieves bronchospasm; reduces airway resistance, increases lung capacity.

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.

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.

Instructions for use

For each individual form of this drug, a special method of using Salbutamol is prescribed:

  • 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 prescribing the drug Salbutamol in the form of an aerosol, one or two presses on the valve are recommended (i.e. 1-2 doses per dose). For the relief of an attack, as a rule, this is enough. If within 5-10 minutes the effect does not occur, repeated administration of the drug in the same dose is allowed. The next inhalation is possible after 4-6 hours, but not more than six times a day. The drug in the form of tablets for adults is prescribed three times a day (1 tablet per dose).

Before using Salbutamol aerosol, you need to check the expiration date of this drug. If the inhaler is new or has not been used for several days, you need to shake it and make one spray into the air to check the health.

  • Remove the cover from the dispenser;
  • Take the inhaler upright;
  • Shake the inhaler for 20 seconds;
  • Take a deep breath and press the dispenser to your lips;
  • Make a spray while inhaling deeply through your mouth;
  • Hold your breath after inhaling;
  • If necessary, repeat the procedure after a few seconds;
  • Close the lid after use.

The plastic adapter needs to be cleaned regularly. To clean, remove the metal container and wash the adapter in warm soapy water. Rinse thoroughly, dry the adapter and assemble the device. Close the lid after assembly.

Contraindications

You can not use the drug in such cases:

  1. The threat of miscarriage in the I-II trimesters of pregnancy;
  2. Toxicosis or bleeding in the III trimester of pregnancy;
  3. Premature placental abruption;
  4. Children's age up to 2 years;
  5. Hypersensitivity to the components of the drug.

Side effects

When using Salbutamol, it is possible to develop disorders from some body systems:

  • Central nervous system: dizziness, headache, vomiting, nausea;
  • Cardiovascular system: moderate tachycardia, transient expansion of peripheral vessels;
  • Allergic reactions: in some cases - allergic reactions in the form of skin rash, angioedema, arterial hypotension, urticaria, collapse;
  • Metabolism: hypokalemia;
  • Other: tension, internal trembling, tremor of the hands; rarely - muscle cramps, paradoxical bronchospasm.

Salbutamol's analogs

Structural analogues for the active substance:

  • Aloprol;
  • Astalin;
  • Ventolin;
  • Ventolin Nebula;
  • Volmax;
  • Salamol;
  • Salamol Eco;
  • Salmo;
  • Salben;
  • Salbuvent;
  • Salbutamol Teva;
  • Salbutamol hemisuccinate;
  • Salbutamol sulfate;
  • Salgim;
  • Saltos;
  • Sterineb Salamol;
  • Cibutol Cyclocaps.

Attention: the use of analogues must be agreed with the attending physician.

Prices

The average price of SALBUTAMOL, an aerosol in pharmacies (Moscow) is 55 rubles.

1 ml of the drug contains the active substance - salbutamol 0.8 mg (2 mg in 1 vial)

Release form

Solution for inhalation 2.5 ml in a bottle - 10 bottles in a package

pharmachologic effect

Bronchodilator drug.

Salbutamol is a selective beta2-adrenergic agonist. In therapeutic doses, it acts on beta2-adrenergic receptors of the smooth muscles of the bronchi, providing a pronounced bronchodilator effect, prevents and relieves bronchospasm, and increases the vital capacity of the lungs. Prevents the release of histamine, a slow reacting substance from mast cells and neutrophil chemotaxis factors. It causes a slight positive chrono- and inotropic effect on the myocardium, dilation of the coronary arteries, and practically does not reduce blood pressure. It has a tocolytic effect: it lowers the tone and contractile activity of the myometrium. The action of the drug begins 5 minutes after inhalation and lasts for 4-6 hours.

It has a number of metabolic effects: it reduces the content of K + in plasma, has a hyperglycemic (especially in patients with bronchial asthma) and lipolytic effect, increases the risk of acidosis.

Indication for use

  • prevention and relief of bronchospasm in bronchial asthma;
  • symptomatic treatment of broncho-obstructive syndrome (including chronic bronchitis and emphysema);
  • chronic obstructive pulmonary disease.

Dosage and administration

The drug is used by inhalation only with the help of a nebulizer of any design. The nebulizer turns the solution into an aerosol for inhalation. When used, the solution should be at room temperature (cold solution may cause a coughing effect). Before using the drug, you must carefully study the instructions for use of the nebulizer:

Prepare the nebulizer for use.

Put the drug solution into the nebulizer. Do not mix the solution with other drugs. The solution can be diluted with distilled water or 0.9% sodium chloride.

After the end of inhalation, remove the remaining solution and wash the nebulizer. When using a solution of Salbutamol through a nebulizer, the initial dose of the drug for adults and children over 12 years of age is 2.5 mg, but can be increased to 5 mg. Inhalations are carried out every 4-6 hours during the first 24-48 hours of therapy or until the clinical picture stabilizes. Improvement is observed after inhalation, usually after 10-15 minutes. In severe exacerbation of chronic obstructive pulmonary disease, the frequency of administration of the drug can be significantly increased - it is possible to prescribe the drug every 30-60 minutes until a clinical effect is achieved (in adults up to 40 mg per day).

Use in children from 18 months to 12 years: to relieve an attack of bronchospasm: a single dose of 2 mg per inhalation up to 4 times a day under the supervision of specialists. For prophylaxis 2 mg/day.

Contraindications

  • Hypersensitivity to the components of the drug,
  • coronary artery disease,
  • severe heart failure
  • rhythm disturbances (paroxysmal tachycardia, polytopic ventricular extrasystole),
  • myocarditis,
  • heart defects,
  • aortic stenosis,
  • decompensated diabetes,
  • glaucoma,
  • epileptic seizures
  • pyloroduodenal constriction,
  • diseases of the kidneys and liver with a violation of their function,
  • pregnancy,
  • concomitant use of non-selective beta-blockers,
  • children's age up to 18 months.

special instructions

In patients with severe or unstable asthma, the use of bronchodilators should not be the main or only therapy.

If the effect of the usual dose of the drug becomes less effective, the patient should consult a doctor.

If paradoxical bronchospasm occurs, it is necessary to stop it immediately with another dosage form of salbutamol or a fast-acting inhaled bronchodilator, stop treatment and prescribe therapy with other drugs.

Storage conditions

In a dry, dark place, at a temperature not exceeding 25°C. Keep out of the reach of children.

Many severe pathologies of the upper respiratory organs, such as asthma, can go into a chronic stage, and may be accompanied by periodic relapses. Salbutamol for inhalation is an effective inexpensive remedy that allows you to quickly alleviate the condition, relieve an attack of suffocation and shortness of breath.

Description of the drug

Salbutamol is a bronchodilator drug belonging to the beta-2-adrenergic agonists. Available in the form of a powder, solution, and aerosol for inhalation procedures. It is used according to the appointment of a specialist.

The main component is salbutamol, in addition to it, the aerosol contains propellant R134a, ethyl and oleyl alcohol. The solution additionally contains succinic acid and purified water.

The active substance can be found in other preparations - syrups, capsules, and injection solutions.

The aerosol is a white liquid with a slight odor. It is contained in an aluminum cylinder equipped with a nozzle and a valve that allows dosed delivery of the medicinal substance. One spray contains 0.1 mg of the active ingredient.

A clear solution with a slightly yellowish tint is used for inhalation through a nebulizer.

Possessing bronchodilator properties, the drug has a relaxing effect on the smooth muscles of the bronchi, relieves spasms, expands the gaps, improves the patency of the bronchial tree and the functioning of the lungs.

Properties of inhalations

Using Salbutamol in solution or aerosol for inhalation, you can quickly improve the patient's condition:

  • relieve bronchospasm;
  • eliminate shortness of breath;
  • improve the patency of the bronchial tract;
  • increase the vital capacity of the lungs;
  • prevent and stop bronchospasm, including allergic;
  • activate the production of mucus and start the process of sputum discharge;
  • protect mucous membranes.

During inhalation procedures using a nebulizer, approximately 20% of the substance penetrates to the small branches of the bronchi. Some of the drug enters the stomach. The substance is metabolized in the liver, excreted unchanged.

Regular use of the drug can reduce potassium levels and lead to hypoglycemia.

Indications for appointment

Salbutamol in the form of an inhaler has shown high efficacy in the treatment of various severe respiratory diseases. However, this remedy should not be used as a self-medication.

Indications for use are:

  • emphysema;
  • bronchospasm of various origins;
  • inflammation of the bronchi in a chronic form;
  • obstruction;
  • asthmatic bronchitis.

In addition, the drug is used in pediatric practice during preterm labor, if the condition threatens the life of the fetus and is accompanied by bradycardia.

Salbutamol is an excellent remedy for asthma attacks, which can be used as a preventive measure at any stage of the disease, including complicated ones. In addition, it is approved for long-term use as maintenance therapy for bronchial inflammation.

Methods of use and doses

According to the instructions for use, the aerosol is intended for inhalation of the substance into the oral cavity using a special valve and sprayer. The solution for inhalation is used in a nebulizer.


Before the procedure, the protective cap is removed from the atomizer, the mouthpiece is inserted into the oral cavity, tightly covering it with lips. The patient takes a deep breath while simultaneously pressing the valve button. This will help the drug to penetrate deeper into the respiratory organs.

The dosage depends on the age characteristics of the patient.

With bronchospasm, as well as an asthma attack, the aerosol is applied once:

  • Adults and adolescents from 12 years of age, 0.1-02 mg (1-2 clicks). The optimal dosage to eliminate a severe choking attack is to use two inhalations at a time (2 presses on the nebulizer), every 6 hours. The daily maintenance dose should not exceed 800 mcg.
  • Children aged 2 to 6 years are prescribed a dosage of 100 mcg, no more than 3 times a day.

In order to prevent spasms and asthma attacks, as well as before possible interaction with the allergen, the drug is applied 10-15 minutes before the expected contact:

  • adults - 0.2 mg (two procedures);
  • children - 0.1 mg.

Before physical activity, the aerosol must be sprayed three to four times a day:

  • adults - 0.2 mg;
  • children - 0.1 mg.

In childhood, the procedure is carried out by parents. If the patient is unable to take a deep breath, a special device (spacer) can be used.

Solution for nebulizer

The medicine Salbutamol-native is used by inhalation through any nebulizer. A nebulizer is a device that turns medicine into an aerosol.

Salbutamol in a solution for inhalation through a nebulizer is an effective way to eliminate asthma attacks and reduce inflammation. With the help of aerosol intake of the drug, a high therapeutic result can be achieved, especially in the treatment of children.

It is necessary to use a medication at room temperature, since a cold agent can provoke a cough, and hot one can cause a burn.

Before use, the nebulizer should be prepared: rinse all nozzles and dry thoroughly. The solution is poured into a special container, the mask is attached to the tube, and then it is tightly pressed to the face.

The device is turned on and the procedure is started. Inhalations are carried out according to the testimony of a specialist, according to the prescribed dosage. The substance begins to act after 10-15 minutes.

Inhalation procedures are carried out every 4-6 hours during the first two days: this will help stabilize the clinical picture of the disease. In severe attacks, the time interval can be reduced: to relieve symptoms, inhalations can be carried out every half an hour or an hour.

  • for adolescents over 12 years of age and adults, the dose starts at 2.5 mg every 4-6 hours. The dosage, if necessary, can be increased by a doctor up to 5 mg;
  • in children from 1.5 to 12 years old, 2 mg four times a day is used, under the supervision of the attending physician. For preventive purposes, the appointment of 2 mg per day is allowed.

Do not combine the solution with other medicinal substances. It is allowed to dilute the medicine with 0.9% saline or distilled water.

Contraindications

Before use, you should read the annotation to the drug. Contraindications for use are:

  • hypersensitivity to the components of the drug;
  • aortic stenosis;
  • heart failure and other severe heart diseases;
  • arrhythmia;
  • myocardial damage;
  • type 2 diabetes;
  • serious diseases of the liver and kidneys;
  • increased intraocular pressure;
  • period of pregnancy;
  • children's age up to one and a half years.

Extreme caution must be exercised if the patient has hypertension, thyrotoxicosis, as well as neoplasms in the adrenal glands.

Side effects

Subject to the dosage prescribed by the doctor and proper use, the drug usually does not cause negative reactions. However, in some cases, side effects are observed:

  • tremor of the limbs;
  • convulsive syndromes;
  • increased heartbeat;
  • sleep disorders;
  • cough;
  • redness of the skin of the face;
  • negative reactions from the brain - anxiety, headaches, dizziness;
  • runny nose;
  • change in taste sensations;
  • lowering blood pressure;
  • inflammatory processes in the pharynx;
  • irritation of the upper ENT organs;
  • allergic reactions;
  • hypoglycemia;
  • dry mouth;
  • dermatitis;
  • increased sweating.

If negative effects have developed due to misuse of the drug, as well as overdose, treatment is stopped and symptomatic therapy is carried out.

During pregnancy and lactation

To date, there are no accurate data on the safety of the use of the substance by pregnant women.

The tool should not be used in the first and second trimesters of bearing a child, especially if there is a threat of miscarriage. It is also forbidden to use Salbutamol at the risk of bleeding and toxicosis in the later stages of pregnancy. However, in case of emergency, the attending physician, comparing the benefits and harms, may decide to prescribe an aerosol.

The drug is able to penetrate into the mother's milk, so for the duration of treatment it is necessary to transfer the child to artificial feeding.

drug interaction

Aerosol for inhalation Salbutamol may be alternated with other anti-asthma drugs.

The combined use of antihistamines, expectorants and mucolytic herbal remedies, as well as corticosteroids, is allowed.

The combination with theophylline can lead to cardiac arrhythmia and tachycardia.

The use of tricyclic antidepressants can enhance the effect of the drug and lower blood pressure.

With the simultaneous use of drugs with beta-blockers, bronchospasm may occur.

special instructions

At the moment, data on the negative impact of the drug on the ability to drive a car is not available. However, for the period of therapy, it is better to abandon work that requires special care and concentration.

Overdose can lead to bronchospasm, in isolated cases - death.

If it is necessary to use high doses of the drug, the attending physician should review the overall treatment plan.

Against the background of the use of the drug, it is important to include glucocorticosteroids in the treatment, as well as systematically monitor the function of breathing.

Salbutamol is able to affect the heart and provoke the development of arrhythmia.

Sometimes inhalation of a substance leads to a sharp deterioration in respiratory abilities. In this case, other short-term bronchodilators are used.

In situations of vital necessity, the medicine can be prescribed during pregnancy.

Terms and conditions of storage

The drug is valid for 2 years at a temperature not exceeding 30 degrees. It is necessary to store the bottle in a dry, dark place, avoiding damage to the bottle, overheating and freezing.

Price

Salbutamol is sold in pharmacy chains by prescription of a medical specialist. The price of a solution for inhalation Salbutamol-native is 136 rubles, in the form of an aerosol of 100 mcg (200 doses), the agent can be purchased for 115 rubles.

Salbutamol is a highly effective drug that can eliminate intense cough, bronchospasm, asthma attack and other manifestations of bronchopulmonary diseases. The use of the drug in the form of inhalation will help stabilize the clinical picture of the disease and achieve a positive result within the first day. However, the medication must be used after visiting a medical institution: it has quite serious contraindications, and can provoke a number of severe side effects.

1 dose of the drug contains:

Active substance: salbutamol sulfate (in terms of 100% substance) 0.1208 mg (equivalent to 0.1 mg salbutamol).

Excipients: oleyl alcohol 0.0625 mg, ethanol (rectified ethyl alcohol) 2.02 mg, propellant R 134a (1,1,1,2-tetrafluoroethane, HFA 134a) 56.91 mg. The preparation does not contain chlorofluorocarbon propellants.

Description of the dosage form

Aerosol for inhalation dosed in the form of a white or almost white suspension.

pharmachologic effect

Salbutamol is a selective b 2 -adrenergic agonist. In therapeutic doses, it acts on the b 2 -adrenergic receptors of the smooth muscles of the bronchi, having a slight effect on the b 1 -receptors of the myocardium. It has a pronounced bronchodilating effect, preventing or stopping bronchospasm, reduces resistance in the airways. Increases the vital capacity of the lungs.

In the recommended therapeutic doses, it does not adversely affect the cardiovascular system, does not cause an increase in blood pressure. To a lesser extent, compared with drugs of this group, it has a positive chrono- and inotropic effect. Causes expansion of the coronary arteries. It has a number of metabolic effects: it reduces the concentration of potassium in plasma, affects glycogenolysis and insulin secretion, has a hyperglycemic (especially in patients with bronchial asthma) and lipolytic effect, increasing the risk of acidosis.

After the use of inhalation forms, the action develops quickly, the onset of the effect is after 5 minutes, the maximum is after 30-90 minutes (75% of the maximum effect is achieved within 5 minutes), the duration is 4-6 hours.

Pharmacokinetics

absorption and metabolism

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 deposited in the respiratory tract is absorbed into the lung tissues and blood, but is not metabolized in the lungs.

The swallowed part of the inhalation dose is absorbed from the gastrointestinal tract and undergoes intensive metabolism during the "first pass" through the liver, turning into inactive 4 "-O-sulfate (phenolic sulfate).

Distribution

The binding of salbutamol to plasma proteins is 10%.

breeding

With the / in the introduction of T1 / 2 salbutamol is 4-6 hours.

Unchanged salbutamol and the conjugate are excreted primarily in the urine. Only a small part of the administered dose of salbutamol is excreted in the feces.

Most of the dose of salbutamol administered intravenously, orally, or by inhalation is excreted within 72 hours.

Indications for use Salbutamol

1. Bronchial asthma:

Relief of attacks of bronchial asthma, including exacerbation of severe bronchial asthma;

Prevention of attacks of bronchospasm associated with exposure to an allergen or caused by exercise;

Use as one of the components in long-term maintenance therapy of bronchial asthma.

2. Chronic obstructive pulmonary disease (COPD), accompanied by reversible airway obstruction, chronic bronchitis.

Contraindications to the use of Salbutamol

Hypersensitivity to any component of the drug

Children's age up to 2 years

The drug should be used with caution if patients have a history of tachyarrhythmia, myocarditis, heart defects, aortic stenosis, coronary heart disease, severe chronic heart failure, arterial hypertension, thyrotoxicosis, pheochromocytoma, decompensated diabetes mellitus, glaucoma, seizures, renal or hepatic failure , simultaneous use of non-selective b-blockers, pregnancy, lactation.

Salbutamol Use in pregnancy and children

Contraindicated during pregnancy and lactation. Children under 2 years.

Salbutamol side effects

By frequency, side effects can be divided into the following categories: very often (≥ 1/10), often (≥ 1/100 and< 1/10), нечасто (≥ 1/1000 и < 1/100), редко (≥ 1/10 000 и < 1/100), очень редко (< 1/10 000) встречающиеся.

From the immune system: rarely - dermatitis, very rarely - hypersensitivity reactions, including angioedema, skin rash.

On the part of metabolic processes: rarely - hypokalemia.

From the nervous system: often - tremor, headache, anxiety; rarely - dizziness, drowsiness, fatigue; very rarely - hyperactivity.

From the side of the cardiovascular system: often - tachycardia, palpitations; rarely - the expansion of peripheral vessels with flushing of the skin, discomfort or pain in the chest; very rarely - arrhythmia, including atrial fibrillation, supraventricular tachycardia, extrasystole, lowering blood pressure and collapse.

From the respiratory system: rarely - cough, irritation of the respiratory tract; very rarely - bronchospasm (paradoxical or caused by hypersensitivity to the drug).

From the gastrointestinal tract: rarely - dryness and irritation of the mucous membrane of the oral cavity and pharynx, changes in taste sensations, nausea, vomiting.

From the musculoskeletal system: rarely - muscle cramps.

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

Enhances the effect of stimulants of the central nervous system.

Theophylline and other xanthines, when used simultaneously, increase the likelihood of developing tachyarrhythmias; means for inhalation anesthesia, levodopa - severe ventricular arrhythmias.

Simultaneous use with m-anticholinergics (including inhalation) may increase intraocular pressure.

Diuretics and glucocorticosteroids enhance the hypokalemic effect of salbutamol.

Dosage of Salbutamol

Inhalation in the form of a metered-dose aerosol, dry powders for inhalation or through a nebulizer: It is not allowed to take more than 1200-1600 mcg of salbutamol per day! For the relief of asthma attacks, adults are prescribed 200 mcg once (1-2 inhalations). Children are prescribed 100 mcg once for the relief of asthma attacks. If there is no effect, repeated inhalation is possible after 5 minutes. Subsequent inhalations are performed at intervals of 4-6 hours. in particular, to improve the penetration of basic anti-asthma drugs to the distal parts of the bronchial tree - 100-200 mcg 15-20 minutes before inhalation of sodium cromoglycate, sodium nedocromil or inhaled glucocorticoid. Prevention of bronchospasm - 15-20 minutes before contact with frosty air, an allergen , another trigger for 100-200 mcg. Powder for inhalation is administered using a powder inhaler (diskhaler, cyclohaler). The usual doses are 200-400 mcg 2 times a day (maximum dose 1600 mcg / day). In a severe attack, an inhalation solution (in nebulas) can be administered using various nebulizers for 5-15 minutes, the interval between inhalations is 4 hours ( the maximum dose is 1600 mcg / day). If you experience discomfort in the mouth and sore throat, rinse your mouth with water after inhalation. Tablets for oral administration: Tablets are swallowed whole without chewing. As an aid in case of ineffectiveness of inhalation forms: 2 mg 3-4 times a day. If necessary, the dose of the drug can be increased to 4-8 mg 3-4 times a day. In elderly patients, the dose is 2 mg 3 to 4 times a day. Children aged 2 to 6 years are prescribed 1 to 2 mg of the drug 3 to 4 times a day; at the age of 6 - 12 years - 2 mg 3 - 4 times a day; older than 12 years - 2 - 4 mg 3 - 4 times a day. Prolonged forms and two-layer tablets: adults and children - 8 mg every 12 hours; the maximum dose is 32 mg / day. Forms for intravenous infusion: In the treatment of the threat of preterm labor, as well as for the prevention and treatment of placental insufficiency. The contents of 1-2 ampoules (2.5-5 mg) of the drug are diluted in 250-500 ml of isotonic solution or 5% glucose solution. The rate of intravenous drip is 10-40 drops per minute, depending on the intensity of the contractile activity of the uterus and on the tolerance of the drug (the pulse of a pregnant woman should not be more than 120 beats per minute). Infusion is carried out in the supine position. Tolerability control is required: heart rate (HR) and blood pressure (BP) of the mother, fetal heart rate. After the end of intravenous infusion, maintenance therapy is continued with oral administration of the drug at a dose of 2-4 mg 3-4 times a day, until the uterus contractions completely stop. The first tablet is prescribed 15-30 minutes before the end of the infusion. The course of treatment is 14 days.

Precautionary measures

The patient should be instructed on the correct use of the Salbutamol inhaler.

Bronchodilators should not be the sole or main component of the treatment of unstable or severe bronchial asthma.

If the action of the usual dose of Ventolin becomes less effective or less prolonged (the effect of the drug persists for at least 3 hours), the patient should consult a doctor.

An increased need for the use of inhaled beta2-adrenergic agonists with a short duration of action to control the symptoms of bronchial asthma indicates an exacerbation of the disease. In such cases, the treatment plan should be reviewed. A sudden and progressive worsening of the course of bronchial asthma can pose a threat to the patient's life, therefore, in such situations, it is urgent to decide whether to prescribe or increase the dose of GCS. In such patients, daily monitoring of peak expiratory flow is recommended.

Use the drug with caution in patients with thyrotoxicosis.

Therapy with beta2-adrenergic agonists, especially when administered parenterally or by nebulizer, can lead to hypokalemia. Particular caution is recommended in the treatment of severe attacks of bronchial asthma, since in these cases hypokalemia may increase as a result of the simultaneous use of xanthine derivatives, corticosteroids, diuretics, and also due to hypoxia. In such situations, it is necessary to control the level of potassium in the blood serum.

Influence on the ability to drive vehicles and control mechanisms
Since Salbutamol can cause side effects such as convulsions and dizziness, it is recommended that you exercise increased caution at the first dose or refuse to drive vehicles and engage in other potentially hazardous activities.