Salbutamol

General characteristics. Structure:

Structure on 1 cylinder / 1 a dose:
 
Active ingredient: salbutamol - 12,2 mg / 100 mkg; 
excipients: cetyloleate - 24,4 mg / 0,2 mg, fluorotrichloromethane (hla-Don-11) - 6000 mg / 49,2 mg, дифтордихлорметан (freon-12) - 10800 mg / 88,5 mg.

Description: Contents of a metal cylinder with the valve dosing a deystyoviya - the suspension which is under pressure and forming a spot of white color at a rasyopyleniya on a slide plate.

Pharmacological properties:

Pharmacodynamics. Salbutamol is the selection agonist of beta2-adrenoceptors. In terapevyotichesky doses he affects beta2-adrenoceptors of smooth muscles of bronchial tubes, rendering the expressed broncholitic effect, warns and stops a bronchospasm, increases the vital capacity of lungs. Prevents allocation of a histamine, the substance medyolenno reacting from mast cells and factors of a chemotaxis of neutrophils. Causes insignificant positive hrono-and the inotropic effect on a myocardium, expansion of coronary arteries, practically does not reduce arterial pressure. Okazyyovayet tokolitichesky action: lowers a tone and sokratitelny activity of a myometrium. Effect of drug begins in 5 minutes after inhalation introduction and prodolyozhatsya within 4-6 hours.
Has a number of metabolic effects: reduces the maintenance of K+ in plasma, okayozyvat гипергликемическкй (especially at patients with bronchial asthma) and the lipolytic effect, increases risk of development of acidosis.

Pharmacokinetics. After inhalation introduction from 10 to 20% of a dose gets into airways. Other part is late in the device or settles in a stomatopharynx and then проглатывает­ся. A part of a dose which remains in respiratory tracts is absorbed by tissues of lungs, without being exposed to metabolism in lungs, and gets to a blood stream. At hit in a system blood stream it can be metabolized in a liver and is removed preferential with urine in an invariable look.
Part of the dose which came to digestive tract is soaked up and подвергает­ся to intensive metabolism during the first passing through a liver.
Invariable drug and conjugate are removed preferential with urine.
The most part of a dose of salbutamol is removed within 72 hours. Degree the salbutamol svyazyvayoniya with proteins of plasma makes 10%.
The maximum concentration in a blood plasma - 30 ng/ml.
Elimination half-life - 3,7-5 h.

Indications to use:

The prevention and stopping of a bronchospasm at bronchial asthma, the hronicheyosky obstructive disease of lungs (HODL), chronic bronchitis and emphysema of lungs.

Route of administration and doses:

It is inhalation.
To adults and children 12 years are more senior: on 100-200 mkg of salbutamol (1-2 inhalations)
for stopping of attacks of suffocation.
In the absence of effect in 5 min. repeated inhalation is possible. The subsequent inhalation can be carried out not earlier than in 2 hours.
For control of the course of asthma of easy severity - on 1-2 doses 1-4 times a day and disease moderate severity - in the same dosage in a combination with druyogy antiasthmatic drugs.
For prevention of asthma of physical effort - in 20-30 min. prior to loading 1-2 doses on reception.
To children from 2 to 12 years: at development of an attack of bronchial asthma, and also for prevention of the attacks of bronchial asthma connected with influence of allergen or caused by an exercise stress, the recommended dose makes 100-200 mkg (1-2 ingayolyation).
The daily dose of salbutamol should not exceed 1200 mkg (12 inhalations).

At use of the dosed aerosol accurate implementation of the following instructions is necessary:
 1. Before use carefully to stir up a cylinder.
2. To put on the sprayer a cylinder, to uncover with the sprayer.
3. To make a deep exhalation.
4. To turn a cylinder upside down, to clasp a mouthpiece with lips, to make a strong breath iodnovremenno to press a cylinder bottom. At the same time there is a strong emission of an aerosol. To hold the breath for several seconds and, having taken away a mouthpiece from a mouth, to make медленныйвыдох.
5. After use to close a cover a mouthpiece for protection from pollution.
 
To patients (including to children of younger age), it is difficult for them to execute
correctly respiratory maneuver, is recommended to use special adaptation (spacer) increasing respiratory volume and sglazhiyovayushchiya of inaccuracy of an asynchronous breath for drug inhalation.

Features of use:

At patients with the heavy or unstable course of bronchial asthma the primeyoneniye of broikhodilatator should not be the main or only method of therapy.
If action of a usual dose of salbutamol becomes less effective or less long (effect of drug has to remain not less than 3 hours), the payotsiyent should see a doctor.
Frequent use of salbutamol can lead to strengthening of a bronchospasm, vneyozapny death in this connection between receptions of the next doses of drug it is necessary to deyolat breaks in several hours.
Increase in need for use of inhalation agonists of beta2-adrenoceptors with a short duration of action for control of symptoms of bronchial asthma testifies to an exacerbation of a disease. In such cases sleduyot to reconsider treatment planning of the patient and to resolve an issue of appointment or increase in a dose of inhalation or system glucocorticosteroids.
Therapy by agonists of beta2-adrenoceptors can lead to a hypopotassemia. Extra care is recommended to be shown at treatment of heavy attacks of bronkhiyoalny asthma as in these cases the hypopotassemia can amplify as a result of simultaneous use of derivatives of xanthine, glucocorticosteroids, diuretiyok, and also owing to a hypoxia. In such situations it is necessary to control potassium level in blood serum.

Side effects:

On frequency side effects can be divided into the following categories: very frequent (≥ 1/10), frequent (≥ 1/100 and <1/10), infrequent (≥ 1/1000 and <1/100), rare (≥ 1/10 000 and <1/100), very rare (<1/10 000).
From immune system: very seldom - hypersensitivity reactions, including a Quincke's disease, a small tortoiseshell, an erythema, a nose congestion, a bronchospasm.
From exchange processes: seldom - a hypopotassemia, and also reversible metayobolichesky disturbances, for example, increase in concentration of glucose in blood.
From the central nervous system: often - a tremor, a headache; not час­то - dizziness; very seldom - hypererethism, uneasiness, a sleep disorder, sleeplessness, fatigue.
From cardiovascular system: seldom - insignificant kompensatoryony increase in heart rate, increase in arterial pressure; very seldom - arrhythmia, including fibrillation of auricles, supraventricular tachycardia and premature ventricular contraction, arterial hypotension and a collapse; seldom - expansion of perifericheyosky vessels (a dermahemia of the person).
From respiratory system: very seldom - a paradoxical bronchospasm, cough.
From the alimentary system: not often - change of flavoring oshchushcheyoniya; seldom - dryness or irritation of a mucous membrane of an oral cavity and throat (farinyogit), nausea, vomiting.
From a musculoskeletal system: seldom - muscular spasms.

Interaction with other medicines:

Theophylline and other xanthines at simultaneous use with salbutamol increase probability of development of tachyarrhythmias; means for inhalation anesthesia, a levodopa - heavy ventricular arrhythmias.
It is not recommended to apply at the same time salbutamol and non-selective blockers of beta adrenoceptors, such as propranolol.
Monoamine oxidase inhibitors and tricyclic antidepressants strengthen effect of salbutamol and can lead to a sharp lowering of arterial pressure.
Salbutamol strengthens action of stimulators of the central nervous system, poyobochny action on heart of hormones of a thyroid gland.
Increases probability of development of glikozidny intoxication. Reduces an effektivyonost of hypotensive drugs, nitrates.
The hypopotassemia can amplify as a result of simultaneous use proizyovodny xanthine, glucocorticosteroids, diuretics.
Co-administration with anticholinergics (including ingalyatsiyoonny) can promote increase in intraocular pressure.

Contraindications:

Hypersensitivity to any component of drug, disturbance of a rhythm (a Bouveret's disease, polytopic ventricular premature ventricular contraction), myocarditis, heart diseases, an aortal stenosis, coronary heart disease, a heavy cordial nedostatochyonost, a dekompensirovanny diabetes mellitus, glaucoma, epipripadka, pilorodoudenal-ny narrowing, a renal or liver failure, pregnancy, a concomitant use of non-selective beta adrenoblockers, children's age up to 2 years.

Overdose:

Symptoms: nausea, vomiting, hyperexcitability, hallucinations, takhikaryodiya, trembling of ventricles, expansion of peripheral vessels, decrease in arterialyyony pressure, anoxemia, acidosis, hypopotassemia, hyperglycemia, muscular tremor, goyolovny pain.
Treatment: drug withdrawal, cardioselective beta adrenoblockers; simptomayotichesky therapy.
At suspicion on overdose it is necessary to control potassium level in a syvoyorotka of blood.

Storage conditions:

At a temperature not above 30 °C.
To protect from children. To store far from heating system and direct sunshine.

Issue conditions:

According to the recipe

Packaging:

Aerosol for inhalations dosed 100 mkg / a dose.
On 90 doses (12 ml) of drug in aluminum aerosol cans with the valve nayozhimny dosing the sprayer for antiasthmatic means and a cap. Each cylinder with the sprayer, a cap and the application instruction is placed in a pack from a cardboard.