Salbutamol

Description (Salbutamol):

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Description of the active substance:

Salbutamol

Pharmacological action:

Bronchodilator.

• In therapeutic doses, it has a pronounced stimulating effect on beta2-adrenergic receptors of the bronchi, blood vessels and myometrium.
• Practically 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 relieving bronchial spasms, reduces resistance in the airways, increases vital capacity.
• It has a positive effect on mucociliary clearance (in chronic bronchitis it increases it by 36%), stimulates mucus secretion, activates the functions of the ciliated epithelium.
• It inhibits the release of inflammatory mediators from mast cells and basophils, in particular anti-IgE-induced histamine release, eliminates antigen-dependent suppression of mucociliary transport and the release of neutrophil chemotactic factor.
• Prevents the development of allergen-induced bronchospasm.
• It can cause a decrease in the number of beta-adrenergic receptors, including on lymphocytes.
• It has a number of metabolic effects: it 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 developing acidosis.
• In recommended therapeutic doses, it does not have a negative effect on the heart, does not cause an increase in blood pressure.
• To a lesser extent, compared to drugs of this group, it has a positive chrono- and inotropic effect.
• Causes dilation of the coronary arteries.
• It has a tocolytic effect – it reduces the tone and contractile activity of the myometrium.
• After oral administration of non-extended-release forms, the onset of effect occurs within 30 minutes, with a maximum effect at 2 hours when taking syrup and 2-3 hours when taking tablets; the duration is 4-6 hours for the solution.
• Extended-release forms of the drug, due to the gradual release of the active substance through the tablet coating, provide the necessary concentration in the plasma to maintain the therapeutic effect for 12-14 hours.

Indications:

• Orally – bronchospastic syndrome, bronchial asthma – prevention and relief, (chronic bronchitis, emphysema).
• Parenterally – bronchospastic syndrome (relief).

Parenterally with subsequent transition to oral administration:

1.     Threatened preterm labor with the onset of contractile activity;
2.     Isthmic-cervical insufficiency;
3.     Fetal bradycardia (depending on uterine contractions during cervical dilation and expulsion periods);
4.     Surgery on the pregnant uterus (circular suturing in case of internal cervical insufficiency).

Contraindications:

Hypersensitivity, pregnancy (when used as a bronchodilator), lactation period, childhood (under 6 years old – for tablets, under 2 years old – for oral solution and syrup).
For administration as a tocolytic (additionally) – infections of the birth canal, intrauterine fetal death, fetal developmental defects, bleeding due to placenta previa or placental abruption; threatened miscarriage (in the 1st-2nd trimesters of pregnancy).

Use with caution:

Tachyarrhythmia, severe CHF, arterial hypertension, thyrotoxicosis, pheochromocytoma, pregnancy, lactation period, ischemic heart disease (angina, myocardial infarction), myocarditis, heart defects, aortic stenosis, diabetes mellitus, epilepsy, seizures, gastrointestinal stenosis (including pyloroduodenal).

Side effects:

• Common - palpitations, tachycardia (during pregnancy - in mother and fetus), headache, tremor, nervous tension;
• Uncommon - dizziness, insomnia, muscle cramps, nausea, vomiting, sweating; rarely - allergic reactions (urticaria, skin rash, angioedema, paradoxical bronchospasm, erythema multiforme, Stevens Johnson syndrome, arrhythmia, chest pain, hypokalemia, psychoneurological disorders (psychomotor agitation, disorientation, memory impairment, aggressiveness, panic, hallucinations, suicide 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, hyperglycemia (alternating hypoglycemia), decreased or increased blood pressure, hypokalemia, insomnia, malaise, nausea, nervous tension, convulsions, tremor.

Treatment:

symptomatic, in case of overdose of tablet forms of the drug - gastric lavage, in case of tachyarrhythmia, cardioselective beta-blockers are administered (with caution due to the risk of bronchospasm).

Method of administration and dosage:

Orally:

• Adults and children over 12 years old - 2-4 mg 3-4 times a day, if necessary, the dose can be increased 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 - 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;
• maximum dose - 32 mg/day (16 mg every 12 hours);
• children 6-12 years old - 4 mg every 12 hours, maximum dose - 24 mg/day (12 mg every 12 hours).
• Swallow the tablets whole, without chewing.

Intravenous administration:

1. For severe bronchospasm, administer intravenously as a bolus over 2-5 minutes at 0.25 mg (4 mcg/kg), every 15 minutes if necessary, or by infusion at 0.005 mg/min, increasing the dose if needed at 15-30 minute intervals up to 0.01-0.02 mg/min.
2. To prepare a solution for intravenous administration with the required concentration of 0.01 mg/ml, dilute 5 mg of salbutamol solution in 500 ml of solvent (water for injection, 0.9% sodium chloride solution, or 5% dextrose solution).

As a tocolytic agent – administer intravenously by drip, 2.5-5 mg (1-2 ampoules) dissolved in 500 ml of 0.9% NaCl solution or 5% dextrose solution. The intravenous drip rate (20-40 drops/min) depends on the intensity of uterine contractions and the drug's tolerance (the pulse of the pregnant woman should not exceed 120 bpm). Afterward, oral maintenance therapy is administered at 2-4 mg, 4-5 times a day. The first tablet is taken 15-30 minutes before the infusion ends. The treatment course lasts for 14 days.

Special instructions:

Frequent use of salbutamol may lead to exacerbation of bronchospasm and sudden death, so breaks of several hours (6 hours) must be observed between doses. Shortening these intervals should only occur in exceptional cases. If the drug is prescribed during lactation, caution is advised (it is unknown if salbutamol passes into breast milk). Strictly controlled clinical studies on the teratogenicity of salbutamol have not been conducted. In some studies, polydactyly was observed in children whose mothers used salbutamol/ventolin/proventil during pregnancy (no clear causal relationship between its use and the occurrence of polydactyly has been established).

Experimental studies have shown a teratogenic effect of salbutamol:

• In mice, doses 11.5-115 times higher than the maximum recommended doses for inhalation in humans caused cleft palate;
• In rabbits, doses 2315 times higher than the maximum recommended for inhalation caused incomplete closure of the skull bones.

Adrenergic bronchodilators can be used during pregnancy, as the potential risk of placental hypoxemia for the fetus due to uncontrolled bronchial asthma significantly outweighs the risk of their use. However, caution is necessary during pregnancy, as they can cause tachycardia and hyperglycemia in the mother (especially if she has diabetes) and the fetus, and may lead to delayed labor, low blood pressure, acute heart failure, and pulmonary edema in the mother.

Interaction:

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% during 10-day therapy with the latter (it has no clinical significance, it is necessary to monitor the concentration of digoxin in the blood).

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

Theophylline and other xanthines, when used simultaneously, increase the likelihood of developing tachyarrhythmias;
inhalation anesthetics, levodopa - severe ventricular arrhythmias.

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

Incompatible with non-selective beta-blockers (which should also be taken into account when using ocular forms of beta-adrenergic blockers).

Concomitant administration with anticholinergics may contribute to an increase in intraocular pressure.

Diuretics and GCS enhance the hypokalemic effect of salbutamol.

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