MEDICAL SPECIALIST Dr. Martin S Pine

This content has been written and checked for quality and accuracy. Content Administrator Updated on: 17/10/2023. Next review: 17/04/2024

Ventolin – concentrate, syrup, tablets

Indications for use

Inside – bronchospastic syndrome, bronchial asthma (including nighttime – prolonged forms) – prevention and relief, COPD (including chronic bronchitis, pulmonary emphysema).

Parenteral – bronchospastic syndrome (relief).

Parenteral with the subsequent transition to oral administration): threatening premature birth with the appearance of contractile activity; isthmic-cervical insufficiency; fetal bradycardia (depending on uterine contractions during periods of uterine cervix dilatation and expulsion); operations on the pregnant uterus (the imposition of a circular suture in case of insufficiency of the internal uterine pharynx).

Active ingredient, group

Salbutamol (Salbutamol), Beta2-selective adrenergic agonist.

Dosage form

Concentrate for preparation of solution for infusion, syrup, tablets, film-coated tablets, prolonged-release tablets, prolonged-release film-coated tablets.

Contraindications

Hypersensitivity, pregnancy (when used as a bronchodilator), lactation, childhood (under 6 years old – for tablets, under 2 years old – for oral solution and syrup).

For intravenous administration as a tocolytic (optional) – infections of the birth canal, intrauterine fetal death, fetal malformations, bleeding with placenta previa or premature placental abruption; threatening miscarriage (in the I-II trimester of pregnancy). C caution. Tachyarrhythmia, severe CHF, arterial hypertension, thyrotoxicosis, tachyarrhythmia, pheochromocytoma, pregnancy, lactation period, coronary artery disease (angina pectoris, myocardial infarction), myocarditis, heart defects, aortic stenosis, diabetes mellitus, epilepsy, convulsions, including stenosis. pyloroduodenal).

How to use: dosage and course of treatment

Inside: adults and children over 12 years old – 2-4 mg 3-4 times a day, if necessary, it is possible to increase the dose to 8 mg 4 times a day. The maximum daily dose is 32 mg. Children 6-12 years old – 2 mg 3-4 times a day, the maximum dose is 24 mg / day; 2-6 years old – 1-2 mg (0.1 mg / kg) 3-4 times a day.

Extended-release tablets: adults and children over 12 years old – 4-8 mg every 12 hours; the maximum dose is 32 mg / day (16 mg every 12 hours); children 6-12 years old 4 mg every 12 hours, the maximum dose is 24 mg / day (12 mg every 12 hours). The tablets are swallowed whole without chewing.

Intravenous – for severe bronchospasm, intravenous bolus for 2-5 minutes at 0.25 mg (4 μg / kg), if necessary, every 15 minutes or by infusion, at 0.005 mg / min, with an increase in the dose, if necessary, at intervals of 15-30 minutes up to 0.01-0.02 mg / min. To prepare a solution for intravenous administration of the required concentration of 0.01 mg / ml, 5 mg salbutamol solution is diluted with 500 ml of a solvent (water for injection, 0.9% sodium chloride solution, 5% dextrose solution).

As a tocolytic agent – intravenous drip, 2.5-5 mg (1-2 ampoules) are dissolved in 500 ml of 0.9% NaCl solution or 5% dextrose solution. The rate of intravenous drip (20-40 drops / min) depends on the intensity of uterine contractile activity and on the tolerance of the drug (the pulse of a pregnant woman should not be more than 120 / min). Further, oral maintenance therapy is carried out – 2-4 mg 4-5 times a day. The first tablet is prescribed 15-30 minutes before the end of the infusion. The course of treatment is 14 days.

Pharmachologic effect

Bronchodilator. In therapeutic doses, it has a pronounced stimulating effect on the beta2-adrenergic receptors of the bronchi, blood vessels and myometrium. Virtually no effect on beta1-adrenergic receptors of the heart.

Inhibits the release of histamine, leukotrienes, PgD2 and other biologically active substances from mast cells for a long time.

Suppresses early and late bronchial reactivity. It has a pronounced bronchodilator effect, preventing or arresting spasms of the bronchi, reduces resistance in the airways, and increases VC. It has a positive effect on mucociliary clearance (in chronic bronchitis it increases it by 36%), stimulates mucus secretion, and activates the functions of the ciliated epithelium.

It inhibits the release of inflammatory mediators from mast cells and basophils, in particular anti-IgE-induced release of histamine, eliminates antigen-dependent suppression of mucociliary transport and the release of neutrophil chemotaxis factor. Prevents the development of allergen-induced bronchospasm.

May cause a decrease in the number of beta-adrenergic receptors, incl. on lymphocytes. Has a number of metabolic effects: reduces the concentration of K + in plasma, affects glycogenolysis and insulin secretion, has a hyperglycemic (especially in patients with bronchial asthma) and lipolytic effect, increases the risk of acidosis.

In the recommended therapeutic doses, it does not adversely affect the CVS, does not cause an increase in blood pressure. To a lesser extent in comparison with drugs of this group, it has a positive chrono- and inotropic effect. Causes expansion of the coronary arteries. Has a tocolytic effect – reduces the tone and contractile activity of the myometrium.

After oral administration of non-prolonged lecforms, the onset of effect is within 30 minutes, maximum – 2 hours when taking syrup and 2-3 hours when taking tablets, duration – 4-6 hours for solution. Prolonged forms of the drug, due to the gradual release of the active substance through the tablet shell, provide the necessary plasma concentration to maintain the therapeutic effect for 12-14 hours.

Side effects

1. Often – palpitations, tachycardia (during pregnancy – in the mother and fetus), headache, tremors, nervous tension;
2. Less common – dizziness, insomnia, muscle cramps, nausea, vomiting, sweating;
3. Rarely – allergic reactions (urticaria, skin rash, angioedema, paradoxical bronchospasm, erythema multiforme, Stevens-Johnson syndrome, arrhythmia, chest pain, hypokalemia, neuropsychiatric disorders (including psychomotor agitation, disorientation, memory impairment, aggressiveness, panic, hallucinations, suicidal attempts, schizophrenia-like disorders, urinary retention.Overdose.Symptoms of acute poisoning: angina pectoris, tachycardia (with a heart rate of up to 200 beats per minute), palpitations, arrhythmia, dizziness, dry mouth, fatigue, headache ( replacing hypoglycemia), decrease or increase in blood pressure, hypokalemia, insomnia, malaise, nausea, nervous tension, convulsions, tremors.

Special instructions

Frequent use of salbutamol can lead to increased bronchospasm, sudden death, in connection with which, between taking the next doses of the drug, it is necessary to take breaks of several hours (6 hours). Reduction of these intervals can take place only in exceptional cases.

If it is necessary to prescribe the drug during lactation, you should stop using caution (it is not known whether salbutamol penetrates into breast milk).

There have been no strictly controlled clinical studies to study the teratogenicity of salbutamol. In some studies, polydactyly was revealed in children against the background of the intake of salbutamol by mothers during pregnancy (an unambiguous causal relationship of its occurrence with the intake of the drug has not been established). In experimental studies, the presence of a teratogenic effect in salbutamol was found: in mice, with SC administration (doses 11.5-115 times higher than the maximum recommended for humans for inhalation administration), the development of a cleft palate was noted; in rabbits when administered orally (doses 2315 times higher than the maximum for inhalation) – non-closure of the skull bones.

Adrenergic bronchodilators can be used during pregnancy, since the potential risk of placental hypoxemia for the fetus against the background of uncontrolled bronchial asthma significantly outweighs the risk associated with their use. However, when using them during pregnancy, care should be taken, since it can cause tachycardia and hyperglycemia in the mother (especially in the presence of diabetes mellitus) and the fetus, as well as cause delayed labor in the mother, lower blood pressure, acute NK and pulmonary edema.

Interaction

It enhances the effect of CNS stimulants, tachycardia in patients with thyrotoxicosis and the likelihood of developing extrasystole while taking cardiac glycosides.

A single use of salbutamol reduces the concentration of digoxin by 16-22% against the background of 10-day therapy with the latter (it has no clinical significance, the concentration of digoxin in the blood should be monitored).

The likely increase in heart rate and blood pressure while taking salbutamol may necessitate a dose adjustment of antihypertensive and antianginal drugs.

Theophylline and other xanthines with simultaneous use increase the likelihood of developing tachyarrhythmias; means for inhalation anesthesia, levodopa – severe ventricular arrhythmias.

MAO inhibitors and tricyclic antidepressants, enhancing the effect of salbutamol, can lead to a sharp decrease in blood pressure.

Incompatible (pharmacological antagonism) with non-selective beta-blockers (which must also be taken into account when using ophthalmic forms of beta-blockers).

Simultaneous administration with anticholinergics (including inhalation) can increase intraocular pressure.
Diuretics and corticosteroids enhance the hypokalemic effect of salbutamol.