2010/06/07

Salbutamol

International name:
Salbutamol (Salbutamol)

Group Affiliation:
Beta2-selective adrenoagonists

Description of the active substance (INN):
Salbutamol

Dosage form:
aerosol for inhalation dose capsules with the powder for inhalation, powder for inhalation dose, solution for inhalation

Mode of action:
Bronchodilator, in therapeutic doses has a marked stimulating action on beta 2-adrenergic receptors of the bronchi, blood vessels and myometrium. Virtually no effect on beta1-adrenergic receptors of the heart. Ingibiruet release from mast cells of histamine, leukotrienes, PgD2 etc. biologically active substances for a long time. Inhibits early and late bronchial reactivity. A pronounced effect of bronchodilators, warning or kupiruya bronchospasm, reduces the resistance in the airways, increases the VC. Increases mucociliary clearance (in case of chronic bronchitis and 36%), stimulates mucus secretion, activates the function of ciliated epithelium. Hinders release of inflammatory mediators from mast cells and basophils, in particular anti-IgE-induced release of histamine, prevents suppression of antigen mucocilliary transport and separation factor of chemotaxis neutrophils. Prevents the development of allergen-induced bronchospasm. Can lead to a decrease in the number of beta-adrenergic receptors, including on lymphocytes. It has a number of metabolic effects: reduces the concentration of K + in the plasma affects glycogenolysis and insulin release, has hyperglycemic (especially in patients with bronchial asthma) and the lipolytic effect, increases the risk of acidosis. In recommended therapeutic doses has no negative impact on the CAS does not cause blood pressure increase. To a lesser degree, compared with drugs of this group has a positive chrono-and inotropic effect. It was the expansion of the coronary arteries. After the inhaled form of the action develops quickly, the beginning of the effect - after 5 minutes, maximum - after 30-90 minutes (75% of the maximum effect is achieved within 5 min), duration - 3-6 hours

Indications:
Bronhospastichesky syndrome, bronchial asthma (including nocturnal - Extended form) - prevention and cupping, COPD (including chronic bronchitis, emphysema).

Contraindications:
Hypersensitivity, children's age (under 2 years - for a solution for oral administration and syrup, under 4 years - for the powder for inhalation and aerosol metered without a spacer). C care. Tachyarrhythmias, severe CHF, hypertension, hyperthyroidism, pheochromocytoma, pregnancy, lactation.

Side effects:
Often - palpitations, headache, tremor, anxiety, less often - cough, respiratory tract irritation, dizziness, dry mouth and throat, changes in taste sensations, seldom - bronchospasm (paradoxical or cause hypersensitivity to the drug), dermatitis, allergic reactions (in including angioedema, skin rash), facial flushing, discomfort or chest pain, drowsiness, fatigue, hypokalemia, arrhythmias, muscle cramps, nausea, rvota.Peredozirovka. Symptoms of acute poisoning by inhalation use: more frequent - hyperglycemia, hypokalemia, reduced blood pressure, lactic acidosis, tachycardia, muscle tremors, vomiting less frequent - excitement, hypercalcaemia, hypophosphataemia, leukocytosis, respiratory alkalosis, the rare - hallucinations, paranoia, seizures, tachyarrhythmias. Symptoms of chronic intoxication by inhalation use: more frequent - lowering blood pressure, tachycardia, tremor, vomiting less frequent - excitement, rare - convulsions, tachyarrhythmia. Treatment: symptomatic, with tachycardia enter cardioselective beta-blockers (with caution because of the risk of bronchospasm ).

Dosage and administration:
Inhalation: prevention: adults - to 0.1-0.2 mg (1-2 inhalations) 4 times during the day, children - up to 0.1-0.2 mg 4 times a day. Cupping - 0.1-0.2 mg for children and adults. Prevention of an asthma attack, or physical stress associated with exposure to allergen: 0.2 mg for 15-30 minutes before exposure to a provoking factor. May not be receiving more than 12 inhalations per day. Powder for inhalation: the input mode disk inhaler (tsiklohalera). To treat an attack - once, for the prevention of bronchospasm - 3-4 times a day. Single dose - 200-400 mg. Daily dose - 0.8-1 mg, if necessary the dose may be increased to 1.2-1.6 mg. For the prevention of bronchospasm induced by physical activity - 400 mcg. The kids, for removal of an attack of bronchospasm: a single dose - 200 micrograms; prevention - 200 mcg / d, the multiplicity of the introduction - 3-4. For prevention of bronchospasm induced by physical stress - 200 micrograms before anticipated exercise. If you experience unpleasant sensations in the mouth and back of the throat after inhalation should rinse your mouth with water. In a severe attack, the introduction of inhalation solution with the use of nebulizers of different designs within 5-15 min: initial dose - 2.5-5 mg 4 times a day. In asthmatic status dose may be increased to 40 mg / day.

Cautions:
Frequent use of salbutamol may exacerbate bronchospasm, a sudden death, in connection with which between-meal regular doses of the drug must take breaks in a few hours (6 h). Reduction of these intervals can only occur in exceptional cases. When using dosed aerosols must be clear that the following instructions: Shake spray cans before each use, precise synchronization of breath and proceeds of the drug, the most profound, intense and long enough breath, breath holding after inhalation of the drug 10 seconds. Patients (including young children) who find it difficult to perform correct breathing maneuver should be used for inhalation drug special device (spacer), which increases tidal volume and smoothing inaccuracies asynchronous breaths. If necessary, the appointment during lactation should cease to be careful (unknown, penetrates whether salbutamol in breast milk). strictly controlled clinical studies on the teratogenicity of salbutamol is not carried out. In separate studies revealed polydactyly in children at the background of reception mothers during pregnancy, salbutamol (an unambiguous causal link its occurrence to the drug intake is not installed). In experimental studies revealed the presence of teratogenic effects from salbutamol: in mice after sc administration (doses of 11.5-115 times the maximum recommended in humans for inhalation) noted the development of cleft palate, in rabbits at oral assignment (the dose of 2315 times exceeding the maximum for inhalation) - nezaraschenie skull. adrenergic bronchodilators may be used during pregnancy because the potential risk of placental hypoxemia the fetus against the background of uncontrolled asthma is much greater than the risk associated with their use. However, their use during pregnancy should be careful because it may cause tachycardia and hyperglycemia in the mother (especially if you have diabetes) and the fetus, and cause delay in the mother in labor, reduction of blood pressure, acute pulmonary edema, and NC.

Interaction:
Enhances the action of the central nervous system stimulants, tachycardia in patients with thyrotoxicosis, the likelihood of beats in the background taking cardiac glycosides. Theophylline and other xanthine, while the application increases the risk of tachyarrhythmias; means for inhalation anesthesia, levodopa - severe ventricular arrhythmias. MAO inhibitors and tricyclic antidepressants amplifying effect of salbutamol, may lead to a sharp decrease in BP. Incompatible (pharmacological antagonism) with non-selective beta-blockers (which must also be taken into account in applying eye forms of beta-adorenoblokatorov). Simultaneous with the appointment of anticholinergic drugs (including inhalants) can contribute to increased intraocular pressure. Diuretics and SCS reinforce gipokaliemicheskoe effect of salbutamol.