Salbutamol

General characteristics. Structure:

Active ingredient: 2 mg or 4 mg of salbutamol in 1 tablet.

The drug having broncholitic, tokolitichesky effect.

Pharmacological properties:

Pharmacodynamics. Vysokoselektivno stimulates beta2-adrenoceptors, activates intracellular adenylatecyclase. The broncholitic effect is caused by relaxation of smooth muscles of bronchial tubes. Catechol-au-methyltransferase does not collapse pulmonary and therefore works is long. Runs down a uterus, brakes sokratitelny activity of a myometrium, prevents premature birth.

Pharmacokinetics. At inhalation of 10-20% reaches small bronchial tubes and it is gradually soaked up, a part of a dose after a proglatyvaniye is absorbed from a GIT. When using tablets of the prolonged action well it is soaked up. Cmax  makes 30 ng/ml. Circulation duration in blood at the therapeutic level makes 3–9 h, then concentration gradually decreases. Linkng with proteins of plasma — 10%. Passes through a placenta, gets into breast milk. Is exposed to biotransformation in a liver. T1/2  is 3,8 h. It is removed irrespective of a way of introduction with urine and bile, it is preferential in not changed look (90%) or in the form of a glucuronide.

The maximum speed of action (removal of a bronchospasm) is reached at an inhalation way of introduction. Bronkhodilatation comes in the 4-5th minute, increases by 20th minute and reaches a maximum in 40–60 min.; duration of effect makes 4–5 h. The most expressed result is received after inhalation of 2 doses, further increase in a dose does not lead to growth of bronchial passability, but increases probability of development of by-effects (a tremor, a headache, dizziness). Positively influences mukotsiliarny clearance (at chronic bronchitis increases it by 36%), stimulates slime secretion, activates functions of a ciliary epithelium.

Slows down emission of mediators of an inflammation from mast cells and basophiles, in particular anti-IgE - the induced emission of a histamine, eliminates antigenzavisimy suppression of mukotsiliarny transport and allocation of a factor of a chemotaxis of neutrophils. Prevents development of the bronchospasm induced by allergen. Can cause a desensitization and a reduction of number of beta adrenoceptors, including on lymphocytes. Has a number of metabolic effects — reduces the content of potassium in plasma, influences a glycogenolysis and release of insulin, renders hyper glycemic (especially at patients with bronchial asthma) and the lipolytic effect, increases risk of development of acidosis.

Indications to use:

Prevention and stopping of a bronchospasm at bronchial asthma, a symptomatic treatment of a bronkhoobstruktivny syndrome (including chronic bronchitis, a chronic obstructive pulmonary disease, emphysema), night asthma (the prolonged tableted forms); threat of premature births (on durations of gestation from 16 to 38 weeks).

Route of administration and doses:

Is inhalation, inside, in / century. It is inhalation: for stopping of beginning suffocation attack — 100–200 mkg (1–2 breaths). In the absence of effect in 5 min. repeated inhalation is possible. The subsequent inhalations make with intervals of 4-6 h (as much as possible up to 6 times a day). For regular use — on 1–2 inhalations 2–4 time/day; prevention of a bronchospasm — za15-20 mines before contact with frosty air. Powder for inhalations: a single dose — 200–400 mg (in connection with lower bioavailability of a dose is twice higher). At a heavy attack administration of inhalation solution with use of various designs of nebulizers in techeniye5-15 mines is possible; the initial dose to adults and children is more senior than 18 months — 2,5 mg (if necessary — 5 mg) to 4 times a day; at appointment to children aged up to 18 months efficiency is doubtful (possibly development of a passing anoxemia, the oxygenotherapy is shown).

Inside, to adults and children 12 years — on 2–4 mg (2 mg — to elderly patients and patients with hypersensitivity) 3–4 times a day, the maximum single dose of 8 mg, the maximum daily dose of 32 mg are more senior; detyam6-12lt — 2 mg 3–4 times a day, the maximum dose — 24 mg/days, children are 2–6 years old — 1–2 mg (0,1 mg/kg) 3–4 times a day. Tablets of the prolonged action: to adults and children 12 years — on 4–8 mg each 12 h, the maximum dose of 32 mg/days are more senior (16 mg each 12 h), detyam6-12lt — 4 mg each 12 h, the maximum dose — 24 mg/days (12 mg each 12 h).

As tokolitichesky means: in/in kapelno — 2,5–5 mg (1–2 ampoules) dissolve 0,9% of solution of sodium of chloride or 5% of solution of a dextrose in 500 ml and enter kapelno, rate of administering depends on intensity of sokratitelny activity of a uterus and portability of drug (ChSS of the pregnant woman 120v 1 min.). Further the supporting peroral therapy is carried out by the tableted salbutamol forms: on 2–4 mg of 4-5 times a day. The first tablet is appointed za15-30min before the end of infusion. A course — 14 days.

Features of use:

For increase in efficiency of therapy of the patient it is necessary to train in the correct use of an inhaler and in an initiation of treatment to apply an inhaler under observation of medical personnel. Reception of high doses of salbutamol at an exacerbation of asthma leads to the fact that each subsequent attack of suffocation becomes more intensively previous (a ricochet syndrome). At a heavy attack of suffocation the break between inhalations has to be not less than 20 min. In the absence of the minimum effect of inhalation or emergence of the expressed tremor, tachycardia, disturbances of a heart rhythm further uncontrolled use of an inhaler is contraindicated, and the address to the doctor is necessary. The risk of complications increases both at the considerable duration of treatment, and at sharp drug withdrawal.

Special instructions. At use of the dosed aerosol accurate implementation of the following instructions is necessary: stirring of a barrel with an aerosol before each use, accurate synchronization of a breath and intake of drug, the deepest, intensive and rather long breath, breath holding after inhalation of drug on 10 pages. Patients, it is difficult for them to execute correctly respiratory maneuver, are recommended to use special devices (spacers) increasing respiratory volume and smoothing inaccuracies of an asynchronous breath for drug inhalation.

Side effects:

From a nervous system and sense bodys: tremor (usually brushes), concern, tension, hypererethism, dizziness, headache, sleep disorder, short-term spasms.

From cardiovascular system and blood (a hemopoiesis, a hemostasis): heartbeat, tachycardia (at pregnancy — at mother and a fruit), arrhythmia, expansion of peripheral vessels, decrease in DAD or increase the GARDEN, myocardium ischemia, heart failure, a cardiopathy.

From bodies of a GIT: nausea, vomiting, dryness or irritation in an oral cavity or a throat, appetite loss.

Others: a bronchospasm (paradoxical or caused by hypersensitivity to salbutamol), pharyngitis, the complicated urination, perspiration, increase in content in blood of glucose, free fatty acids, a hypopotassemia (dozozavisimy), allergic reactions in the form of an erythema, a face edema, the complicated breath, development of physical and mental medicinal dependence.

Interaction with other medicines:

Increases activity of stimulators of TsNS, a kardiotropnost of hormones of a thyroid gland. Theophylline and ephedrine exponentiate toxic effects. Corticosteroids, inhibitors of synthesis of PG, tricyclic antidepressants and blockers of MAO increase risk of development of cardiovascular complications, means for an inhalation anesthesia and a levodopa — heavy ventricular arrhythmias. Reduces efficiency of beta adrenoblockers (including ophthalmologic forms), anti-hypertensive means, anti-anginal effect of nitrates. Increases probability of glikozidny intoxication.

Contraindications:

Hypersensitivity, pregnancy (when using as bronchial spasmolytic), breastfeeding, children's age (up to 2 years — for intake and for the dosed aerosol without spacer, up to 4 years — for powder for inhalations, up to 18 months — for solution for inhalations).

For in/in introductions as a tokolitik (in addition): infections of patrimonial ways, pre-natal death of a fruit, fruit malformations, bleeding at placental presentation or premature placental detachment; the menacing abortion (in the I-II trimester of pregnancy).

Restrictions to use. A tachyarrhythmia, the expressed arterial hypertension and an ischemic heart disease, heavy heart failure, myocarditis, heart disease, an aortal stenosis, a thyrotoxicosis, a pheochromocytoma, a diabetes mellitus, the expressed liver and/or renal failure.

Overdose:

Symptoms: tachycardia (ChSS to 200 уд. / mines), trembling of ventricles, decrease in the ABP, increase in cordial emission, an anoxemia, acidosis, a hypopotassemia, a hyperglycemia, a muscular tremor, a headache, excitement, hallucinations, spasms.

Treatment: drug withdrawal and performing symptomatic therapy; purpose of beta adrenoblockers (selection) with bronchial asthma demands extreme care because of danger of heavy bronkhospastichesky reaction from patients.

Storage conditions:

To store at a temperature of 15-25 °C, in dry, protected from light and the place, unavailable to children. Period of validity 3 years. Not to use after the expiry date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets of 2 mg and 4 mg. 20 tablets in each blister, on one, two or three blisters together with the application instruction in cardboard packaging.