Salbutamol

Pharmacological properties

salbutamol is a selective β2-adrenergic receptor agonist. in therapeutic doses, acts on β2-adrenergic receptors of the bronchial muscles with minimal or complete absence of action on β1-adrenergic receptors of the heart.

Pharmacokinetics After inhalation, 10 to 20% of the administered dose reaches the lower respiratory tract. The rest remains in the transport system or in the oropharynx, from where it is swallowed. The portion of the dose that reaches the airways is absorbed into the lung tissue and enters the bloodstream, but is not metabolized in the lungs.

The onset of action of the drug occurs at 4-5 minutes after inhalation, the duration of action is 4-6 hours.

After entering the systemic circulation, the drug is metabolized in the liver, excreted mainly by the kidneys in an unchanged form and in the form of a phenol sulfate metabolite.

The dose of the drug, which from the nasopharynx enters the digestive system, is absorbed into the digestive tract, goes through the first stage of metabolism in the liver to the phenolsulfate compound, then excreted by the kidneys.

Indications

The drug is indicated for the relief of asthma attacks, as well as for the treatment of patients with hobl.

Application

The drug nebutamol is intended for inhalation by inhalation through the mouth with a nebulizer and is used under the supervision of a physician.

Do not administer solution by injection or swallow.

Adults (including elderly patients)

The usual initial dose of salbutamol by inhalation is 2–2.5 mg. It can be increased to 4–5 mg. You can repeat inhalation 4 times a day.

For the treatment of adult patients with severe obstruction of the respiratory tract, the dose can be increased to 40 mg / day, however, such treatment should be carried out in a hospital under the supervision of a doctor.

Children

The usual initial dose of salbutamol by inhalation is 2–2.5 mg. It can be increased to 4–5 mg. You can repeat inhalation 4 times a day.

The clinical efficacy of salbutamol by nebulization before the age of 18 months has not been established.

Since transient hypoxemia is possible, the need for additional oxygen therapy should be considered.

Nebutamol is usually used undiluted. However, if inhalation needs to be carried out for a long time (10 min), the contents of the container can be diluted with sterile physiological solution.

Aerosol inhalation can be carried out using a special facial mask or mouthpiece. Periodic ventilation of the room where inhalation is performed should be carried out. If there is a risk of hypoxia due to hypoventilation, inhaled air should be enriched with oxygen.

Increasing the dose and frequency of use of the drug can only be done by a doctor, given the possibility of side effects when the dose is exceeded.

Instructions for use of the drug Nebutamol.

1. Prepare a nebulizer for use.

2. Open the polymer bag and remove the single-dose container. Do not remove the container from the bag unless necessary.

3. Shake the container. Leave other containers in a plastic bag and place them in a cardboard box.

4. Holding the container by the top edge, rotate the other edge to open the container.

5. Insert the container into the nebulizer with the open edge down and press gently. Make sure that the entire drug flows into the nebulizer.

6. Assemble the nebulizer and use as intended.

Rinse the nebulizer after use, dispose of the remaining product.

Contraindications

A history of hypersensitivity to any component of the drug. although salbutamol in the form of a solution for intravenous injection and sometimes in the form of tablets and suppositories is used in the management of preterm labor, salbutamol in the form of an aerosol for inhalation is not used for these indications. do not use salbutamol in case of a miscarriage.

Side effects

The following are classified by organs and systems and according to frequency of occurrence. incidence rate is classified as: very often (≥1 / 10), often (≥1 / 100 and 1/10), infrequently (≥1 / 1000 and 1/100), rarely (≥1 / 10,000 and 1/1000) , very rarely (1/10 000), including isolated cases. in general, very frequent and frequent side effects are determined according to clinical studies, while rare and very rare - according to spontaneous reports.

On the part of the immune system: very rarely - hypersensitivity reactions, including angioedema, urticaria, bronchospasm, hypotension and collapse.

Metabolic disorders: rarely - hypokalemia. Potentially severe hypokalemia may result from treatment with β agonists₂-adrenoreceptors; very rarely - lactic acidosis. In patients with AD in the acute stage, who are treated with salbutamol administered intravenously or via a nebulizer, lactic acidosis can occur in very rare cases.

From the nervous system: often - tremors, headache, very rarely - hyperactivity.

From the cardiovascular system: often - tachycardia; infrequently - increased palpitations; very rarely - cardiac arrhythmias, including ventricular fibrillation, supraventricular tachycardia and extrasystole, peripheral vasodilation, frequency not determined - myocardial ischemia.

From the respiratory system: very rarely - paradoxical bronchospasm.

As with other inhaled drugs, paradoxical bronchospasm with increased choking is possible. In this case, it is necessary to immediately prescribe alternative forms of the drug or other fast-acting inhaled bronchodilators. Nebutamol should be immediately canceled, the patients condition assessed and, if necessary, alternative therapy initiated.

From the digestive tract: infrequently - irritation of the mucous membrane of the oral cavity and pharynx.

From the musculoskeletal system: infrequently - muscle cramps.

special instructions

Nebutamol is required to be used by inhalation through the mouth and should not be administered by injection or swallow.

Treatment for AD must be carried out according to a phased program, the patients condition must be evaluated clinically and using functional pulmonary tests.

Increased use of inhaled β agonists₂-adrenoreceptors indicates a deterioration in control of AD. In this case, the patients therapy must be reviewed, because the deterioration of the course of asthma is a life-threatening condition that requires the onset or increase in the use of GCS. Risk patients are advised to monitor their maximum expiratory flow daily.

Patients receiving Nebutamol at home should be warned of the following: if the effective dose of the drug does not bring relief from treatment or the duration of this relief decreases, you should consult a doctor and not increase the dose or frequency of its use on your own.

Nebutamol is used with caution for treatment in patients using other high-dose sympathomimetics.

The use of sympathomimetics, including salbutamol, has an effect on the cardiovascular system. According to post-licensed use and published literature, there is evidence of rare cases of myocardial ischemia associated with salbutamol. Patients with heart conditions (e.g., coronary heart disease, arrhythmia, or severe heart failure) who receive salbutamol should seek medical attention if they have chest pain or other symptoms that indicate an exacerbation of heart disease.Attention should be paid to assessing symptoms such as shortness of breath and chest pain, which can be a consequence of both heart disease and respiratory system disease.

With caution, salbutamol is prescribed to patients with thyrotoxicosis.

In the treatment of patients with a combination of salbutamol in the nebulas and ipratropium bromide, cases of the development of acute angle-closure glaucoma have sometimes been observed. Therefore, the combination of salbutamol in nebulas with anticholinergics that are administered by nebulization should be used with caution. Patients are required to give appropriate instructions regarding the proper use of the drug and to warn that sprayed aerosol should be avoided in the eyes.

The result of treatment with β agonists₂β-adrenoreceptors can be severe hypokalemia, which is mainly observed with parenteral forms or a nebulizer. Particular attention is paid to patients with severe acute asthma, because hypokalemia can be potentiated by the concomitant use of xanthine derivatives, steroids, diuretics and hypoxia. In this situation, it is recommended to check the level of potassium in the blood plasma.

Like other β agonists₂-adrenoreceptors, Nebutamol can lead to reversible metabolic changes, for example, to an increase in blood glucose.

Compensation of such changes in patients with diabetes mellitus is not always possible, therefore, there are separate reports on the development of ketoacidosis in these patients. The simultaneous use of corticosteroids can exacerbate this condition.

Very rarely, in patients with AD in the exacerbation stage who were treated with high doses of salbutamol, used intravenously or through a nebulizer, cases of the development of lactic acidosis were reported. An increase in blood lactate levels can cause the development of suffocation and compensatory hyperventilation of the lungs, can be mistakenly regarded as insufficient anti-asthma treatment and, in turn, lead to inappropriate intensification of treatment with short-acting β-agonists₂-adrenoreceptors. Therefore, it is recommended to control the level of lactate in the blood plasma of such patients and, accordingly, the presence of metabolic acidosis in them.

Use during pregnancy and lactation. Salbutamol during pregnancy is prescribed only when the expected benefit to the mother is higher than the possible risk to the fetus.

Since salbutamol can be excreted in breast milk, it is not recommended to prescribe it during breastfeeding, unless the expected benefit to the mother outweighs the potential risk to the baby.

Children. The clinical effectiveness of salbutamol by nebulization before the age of 18 months has not been established, therefore, the use of the drug is not recommended.

The ability to influence the reaction rate when driving vehicles or working with other mechanisms. There is no data on the effect, in case of side effects from the nervous system (tremor), driving or working with mechanisms must be limited.

Interactions

Salbutamol is not prescribed simultaneously with such a non-selective β-adrenergic receptor blocker as propranolol.

Salbutamol is not contraindicated for use by patients using MAO inhibitors.

Overdose

The most common signs and symptoms of an overdose of nebutamol are transient changes pharmacologically induced by beta-agonists (e.g. tachycardia, tremor, headache).

As a result of an overdose of salbutamol, hypokalemia can occur, therefore, it is necessary to control the level of potassium in the blood plasma.

Treatment consists of stopping salbutamol and prescribing appropriate symptomatic therapy, such as cardioselective β-adrenoreceptor blockers, to treat patients with cardiac symptoms (e.g. tachycardia). Preparations of the group of β-adrenergic receptor blockers should be prescribed with caution to patients with a history of bronchospasm.

Storage conditions

At a temperature not exceeding 25 ° C. Avoid freezing and exposure to direct sunlight.