Instruction for use: Salbutamol (Salbutamolum)

Chemical name: alpha 1 - [[(1,1-dimethylethyl) amino] methyl] -4-hydroxy-1,3-benzenedimethanol (as sulfate or hemisuccinate)

Pharmacotherapeutic group:

Beta-adrenergic agonist

Tocolytics

The nosological classification (ICD-10)

J42 Chronic bronchitis, unspecified

recurrent bronchitis, Bronchitis asthma, wheeze bronchitis, chronic Bronchitis, Inflammatory airways disease, bronchi disease, Qatar smoker, Cough in inflammatory diseases of the lung and bronchus, Exacerbation of Chronic Bronchitis, Chronic bronchitis, Chronic obstructive pulmonary disease, Chronical bronchitis, Chronic bronchitis smokers, Chronic spastic bronchitis, allergic Bronchitis

J43 Emphysema

Interstitial emphysema, Emphysema, Chronic lung disease, Chronic obstructive pulmonary disease, Obstructive pulmonary emphysema, Chronic pulmonary emphysema, Chronic obstructive pulmonary emphysema

J44.9 Chronic obstructive pulmonary disease, unspecified

Obstructive pulmonary diseases, Bronchial obstruction, bronchial obstruction, Exacerbation of chronic obstructive pulmonary disease, reversible airflow obstruction, Reversible airway obstruction, panbronchiolitis, Panbronhit, COPD, Chronic pulmonary infection, Chronic infection of the lower respiratory tract, Chronic obstructive pulmonary disease, Chronic obstructive pneumonia, Chronic lung disease, Chronic obstructive pulmonary disease, Chronic bronchopulmonary disease, Chronic broncho-pulmonary diseases, Airway obstruction

J45 Asthma

Asthma physical effort, status asthmaticus, Bronchial asthma, Asthma lung flow, Bronchial asthma with obstruction of sputum discharge, Bronchial asthma heavy currents, Bronchial asthma physical effort, hypersecretory asthma, Hormone-dependent form of bronchial asthma, Relief of asthma attacks in bronchial asthma, Non-allergic asthma, nocturnal asthma, Exacerbation of asthma, Asthma attacks, Endogenous forms of asthma, Night asthma, Cough with bronchial asthma

J46 Status asthmaticus

Asthmatic attack, status asthmaticus, Bronchospasm in bronchial asthma

J98.8.0 * Bronchospasm

Bronchospasm in bronchial asthma, Bronchospasm when exposed to an allergen, bronchospastic reactions, bronchospastic status, bronhospastichesky syndrome, Diseases accompanied by bronchospastic syndrome, reversible bronchospasm, spasmodic cough

O60 Premature birth

Pregnancy prematurity, The birth premature, Preterm labor pains, Premature contractions prehospital, Immobilization of the uterus before the cesarean section, Immobilization of the uterus, Acute tocolysis, Threatening premature labor, Premature discharge of water, Preventing premature births, The threat of premature birth

CAS Cade 154-42-7

Characteristics

Salbutamol sulphate - a white crystalline powder and odorless. Easily soluble in water (1: 4), slightly soluble in ethanol, chloroform and ether.

Pharmacology

Pharmacological effect

tocolytic, bronchodilator.

Highly selective beta2-adrenergic receptors stimulates, activates the intracellular adenylate cyclase. Bronchodilator effect is due to the relaxation of the smooth muscle of the bronchi. Not destroyed lung catechol-O-methyltransferase and therefore the duration. Relaxes the uterus, inhibits the contractile activity of the myometrium, prevents premature births.

Inhalation 10-20% reaches the bronchial tubes and is gradually absorbed, the dose is absorbed after ingestion of the gastrointestinal tract. When using long-acting tablets are well absorbed. Cmax was 30 ng / ml. Duration blood circulation in a therapeutic level of 3-9 hours, then gradually decreasing concentration. Binding to plasma proteins - 10%. It passes through the placenta, enters the breast milk. Treated biotransformation in the liver. T1 / 2 -. 3.8 hours is displayed regardless of the mode of administration in the urine and bile, mainly in unchanged form (90%) or in the form of glucuronide.

Maximum speed of action (removal of bronchospasm) achieved by inhalation route of administration. Bronchodilation occurs already in 4-5 minutes, increased to 20 minutes, and reaches its maximum after 40-60 minutes; duration of effect of 4-5 hours. The most pronounced effect is obtained after inhalation of 2 doses, further increasing the dose does not lead to an increase in bronchial obstruction, but increases the likelihood of side effects (tremor, headache, dizziness). Positive effect on mucociliary clearance (in chronic bronchitis increases by 36%), stimulates the secretion of mucus, activates the function of the ciliated epithelium. Inhibits release of inflammatory mediators from mast cells and basophils, in particular anti-IgE-induced release of histamine, removes suppression of antigen mucociliary transport and neutrophil chemotactic factor of selection. It prevents the development of allergen-induced bronchospasm. May cause desensitization and reduction of the number of beta-adrenergic receptors, including lymphocytes. It has a number of metabolic effects - reduces the content of potassium in the plasma affects glycogenolysis and insulin release, has a hyperglycemic (especially in asthmatic patients) and lipolytic effect, increases the risk of acidosis.

Indications

Prevention and relief of bronchospasm in bronchial asthma, symptomatic treatment of bronchial obstruction syndrome (including chronic bronchitis, chronic obstructive pulmonary disease, emphysema), asthma, night (long-acting tablet form); threat of premature birth (in terms of pregnancy from 16 to 38 weeks).

Contraindications

Hypersensitivity, pregnancy (when used as a bronchodilator), breastfeeding, children's age (up to 2 years - for intake and dispensing aerosol without spacer to 4 years - for the powder for inhalation, to 18 months - for a solution for inhalation). For in / in the introduction as antioxytocic (optional): the birth canal infection, intrauterine fetal death, fetal malformations, bleeding, placenta previa or premature detachment of the placenta; threatening miscarriage (in the I-II trimester).

Restrictions apply

Tachyarrhythmia, severe hypertension and coronary heart disease, severe heart failure, myocarditis, heart disease, aortic stenosis, hyperthyroidism, pheochromocytoma, diabetes, severe liver and / or kidney failure.

Pregnancy and breast-feeding

Category effects on the fetus by FDA - C.

Side effects of Salbutamol

From the nervous system and sensory organs: tremor (usually hands), anxiety, tension, irritability, dizziness, headache, insomnia, intermittent convulsions.

Cardio-vascular system and blood (blood, hemostasis): palpitations, tachycardia (during pregnancy - the mother and fetus), arrhythmias, peripheral vascular expansion, reduction or increase Sad Dad, myocardial ischemia, heart failure, cardiomyopathy.

From the digestive tract: nausea, vomiting, dryness or irritation in the mouth or throat, loss of appetite.

Other: bronchospasm (paradoxical or caused by hypersensitivity to salbutamol), throat, difficulty urinating, sweating, increased blood glucose, free fatty acids, hypokalemia (dose-dependent), allergic reactions such as erythema, edema of the face, difficulty breathing, development of physical and mental drug dependence.

Interaction

Increases the activity of the central nervous system stimulants, kardiotropnyh thyroid hormones. Ephedrine and theophylline potentiate toxic effects. Corticosteroids, PG synthesis inhibitors, tricyclic antidepressants and MAO blockers increase the risk of cardiovascular events, means for inhalation anesthesia and levodopa - severe ventricular arrhythmias. Reduces the effectiveness of beta-blockers (including ophthalmic form), antihypertensive agents, antianginal effect of nitrates. It increases the glycoside intoxication.

Overdose

Symptoms: tachycardia (heart rate to 200 beats / min.), Ventricular flutter, decreased blood pressure, increased cardiac output, hypoxemia, acidosis, hypokalemia, hyperglycemia, muscle tremor, headache, agitation, hallucinations, seizures.

Treatment: removal of preparation and holding of symptomatic therapy; appointment of beta-blockers (selective) in patients with bronchial asthma patients requires extreme caution because of the risk of severe bronchospastic reactions.

Routes of administration

Inhalation, inside, in / in.

Precautions

To improve the efficiency of patient care should be trained in proper use of the inhaler and the beginning of treatment to use an inhaler under medical supervision. Receiving high doses of salbutamol during exacerbation of asthma leads to the fact that each subsequent attack becomes more intense suffocation previous (rebound syndrome). In severe asthma attacks break between inhalations should not be less than 20 minutes. In the absence of a minimum effect from inhalation or appearance of pronounced tremor, tachycardia, uncontrolled use of further violations of cardiac rhythm inhaler contraindicated and need access to a doctor. The risk of complications increases with a long duration of treatment, and at the abrupt cancellation of the drug.

special instructions

When using aerosol dosage must be clear that the following instructions: Shake aerosol spray before each use, the precise synchronization of inspiration and income of the drug, the most profound, intense and long enough breath, holding your breath after inhalation of the drug for 10 seconds. Patients who find it difficult to perform correct breathing maneuver, it is recommended to use the drug for inhalation special attachments (spacers), increasing tidal volume and smoothing inaccuracies asynchronous breaths.