Salbutamol

Brand Moskhimpharmpreparaty

In stock 1182 Items

Available since: 2019-09-19

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Clinical Pharmacology

Bronchodilator - beta-2-adrenergic selective.

Pharmacodynamics
Salbutamol is a beta2-adrenoreceptor selective agonist. In therapeutic doses, it acts on the beta2-adrenoreceptors of the smooth muscles of the bronchi, providing a pronounced bronchodilator effect, warns and suppresses bronchospasm, increases lung capacity. Prevents the release of histamine, a slow-reacting mast cell substance and neutrophil chemotactic factors. Causes a slight positive chrono-and inotropic effect on the myocardium, the expansion of the coronary arteries, practically does not reduce blood pressure. It has a tocolytic effect: 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 plasma K + levels, has hyperglycemic (especially in patients with bronchial asthma) and the lipolytic effect, increases the risk of developing acidosis.

Pharmacokinetics
After inhalation of 10 to 20% of the dose enters the respiratory tract. The rest is retained in the device or deposited in the oropharynx and then swallowed. Part of the dose that remains in the respiratory tract is absorbed by the tissues of the lungs, not being metabolized in the lungs, and enters the bloodstream. If it enters the systemic circulation, it can be metabolized in the liver and excreted mainly in the urine unchanged.
Part of the dose received in the gastrointestinal tract is absorbed and subjected to intensive metabolism during the first passage through the liver.
Constant drug and conjugate excreted mainly in the urine.
Most of the salbutamol dose is excreted within 72 hours. The degree of binding of salbutamol to plasma proteins is 10%.
The maximum plasma concentration is 30 ng / ml.
The elimination half-life is 3.7-5 hours.

Indications

Prevention and relief of bronchospasm in bronchial asthma, chronic obstructive lung disease (COPD), chronic bronchitis and pulmonary emphysema.

Composition

The composition of 1 bottle / 1 dose:

active ingredient: salbutamol - 12.2 mg / 100 μg;
excipients: cetyl oleate - 24.4 mg / 0.2 mg, fluorotrichloromethane (freon-11) -6000 mg / 49.2 mg, difluorodichloromethane (freon-12) - 10,800 mg / 88.5 mg.

Salbutamol is marketed under different brands and generic names, and comes in different dosage forms:

Brand name	Manufacturer	Country	Dosage form
Salbutamol	Moskhimpharmpreparaty	Russia	inhalation spray
			inhalation spray
Salbutamol-Teva	Teva	Israel	inhalation spray
Ventolin	GlaxoSmithKline	UK	inhalation spray
Salamol Eco Light Breath	Teva	Israel	inhalation spray

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Dosage and Administration

Adults and children over 12 years old - 100-200 mcg each Salbutamol (1-2 inhalation doses) for stopping asthma attacks.
To control the course of asthma of mild severity - 1-2 doses 1-4 times per day and moderate severity of the disease - in the same dosage in combination with other anti-asthma drugs.
For the prevention of physical asthma - 20-30 minutes before the load of 1-2 doses per dose.
Children from 2 to 12 years with the development of an attack of bronchial asthma, as well as to prevent attacks of bronchial asthma associated with allergen exposure or exercise, the recommended dose is 100-200 mcg (1 or 2 inhalations).
The daily dose of salbutamol should not exceed 800 micrograms (8 inhalations).

Adverse reactions

From the side of the central nervous system: tremor of the hands (a typical side effect for all beta2-adrenergic mimetics), headache, dizziness, irritability, anxiety, sleep disturbances, insomnia. The drug can cause arousal and increased motor activity in children.
Since the cardiovascular system: the expansion of peripheral vessels (flushing of the skin of the face), a slight compensatory increase in heart rate, increased blood pressure. Arrhythmias may occur (including atrial fibrillation, supraventricular tachycardia, and extrasystole).
Allergic reactions: in rare cases - angioedema, urticaria, erythema, nasal congestion, bronchospasm, hypotension, collapse.
From the digestive system: nausea, vomiting, dyspepsia.
On the part of the respiratory system: paradoxical bronchospasm, irritation of the oral mucosa and pharynx (pharyngitis), cough.
Metabolism: possible hypokalemia (may pose a serious danger to the patient), reversible hyperglycemia.
Other: muscle cramps.

Contraindications

- Heart rhythm disorders (paroxysmal tachycardia, polytopic ventricular premature beats), tachyarrhythmias.
- Myocarditis.
- Heart defects, aortic stenosis.
- Coronary heart disease.
- Thyrotoxicosis.
- Decompensated diabetes.
- Glaucoma.
- Epilepsy.
- Pyloroduodenal constriction.
- Liver failure.
- Renal failure.
- Pregnancy.
- Simultaneous reception of non-selective beta-blockers.
- Children's age up to 2 years.
- Hypersensitivity to any component of the drug.
Be wary appoint the drug in the following cases:
- Chronic heart failure.
- Hyperthyroidism.
- Arterial hypertension.
- Pheochromocytoma.

Drug interactions

Theophylline and other xanthines with simultaneous use with salbutamol increase the likelihood of developing tachyarrhythmias; means for inhalation anesthesia, levodopa - severe ventricular arrhythmias. It is not recommended to use both Salamol Eco and non-selective beta-adrenoreceptor blockers such as propranolol. Monoamine oxidase inhibitors and tricyclic antidepressants increase the effects of salbutamol and can lead to a sharp decrease in pressure. Salbutamol enhances the action of central nervous system stimulants, side effects of thyroid hormones, and cardiac glycosides. Reduces the effectiveness of antihypertensive drugs, nitrates. Hypokalemia may be enhanced by the simultaneous use of xanthine derivatives, glucocorticosteroids, diuretics. Simultaneous administration with anticholinergic agents (including inhalants) may contribute to an increase in intraocular pressure.

Pregnancy and Lactation

The drug is contraindicated for use in pregnancy. During lactation (breastfeeding) prescribed only in cases where the expected benefit to the mother outweighs any potential risk to the child.

Special instructions

In patients with severe or unstable bronchial asthma, the use of bronchodilators should not be the main or only method of therapy. If the effect of the usual dose of Salamol Eco becomes less effective or less prolonged (the effect of the drug should be maintained for at least 3 hours), the patient should consult a doctor.Frequent use of salbutamol can lead to increased bronchospasm, sudden death, and therefore it is necessary to take breaks of several hours between taking the next dose of the drug. The increased need for the use of inhaled β-2 adrenoreceptor agonists with a short duration of action to control symptoms of bronchial asthma indicates an exacerbation of the disease. In such cases, the patient’s treatment plan should be reviewed and the issue of administering or increasing the dose of inhaled or systemic glucocorticosteroids (GCS) should be decided. Therapy with β-2-adrenoreceptor agonists can lead to hypokalemia. Particular caution is recommended when treating severe attacks of bronchial asthma, since in these cases hypokalemia may increase as a result of the simultaneous use of xanthine derivatives, GCS, diuretics, and also due to hypoxia. In such situations, it is necessary to control the level of potassium in the serum. Spray with Salamol Eco can not be pierced, disassembled or thrown into the fire, even if it is empty. Like most other inhalants in aerosol packages, Salamol Eco may be less effective at low temperatures. When cooling the cartridge, it is recommended to get it out of the plastic case and warm it with your hands for a few minutes.

Overdosage

Symptoms: nausea, vomiting, irritability, hallucinations, tachycardia, ventricular flutter, dilated peripheral vessels, decreased blood pressure, hypoxemia, acidosis, hypokalemia, hyperglycemia, muscle tremor, headache.
Treatment: drug withdrawal, cardioselective beta-blockers; symptomatic therapy. If overdose is suspected, the level of serum potassium should be monitored.

Brand name: Salbutamol
Active ingredient: Salbutamol
Dosage form: Inhalation aerosol dosed at 100 mcg / dose. At 90 doses (12 ml) of the drug in aluminum aerosol cans with a valve pressure dosing, spray for anti-asthma drugs and a cap. Each cylinder with a spray cap and instructions for use are placed in a stack of cardboard.
Manufacturer: Moskhimpharmpreparaty
Country of Origin: Russia