Budesonide in asthma treatment

In the last few years, bronchial asthma is one of the most common chronic diseases of the respiratory organs, which determines its high medical and social significance. Inga translational glucocorticosteroids provide the most effective anti-inflammatory action, which determines the leading position control of bronchial asthma.

Given the increased risk of developing chronic respiratory diseases due to the increasing negative influence of external factors, the presence of behavioral risk factors (smoking) , failure to follow medical recommendations, the urgency of the problem of pharmacotherapy of asthma leaves no doubt. Research data shows that corticosteroids effectively reduce the severity of asthma symptoms, improve quality of life, reduce bronchial hyperactivity, and inhibit inflammation in the airways .

Glucocorticosteroid anti-inflammatory drugs for topical (inhalation) use antiallergic and immunosuppressive effects, increase the production of phospholipase A inhibitors, violate the arachidonic acid metabolism cascade – cyclic endoperacidia and prostaglandins.

These drugs reduce the level of inflammatory exudation and production of lymphokines; inhibit the release of inflammatory mediators from mast cells, increase the number of active β- adrenoreceptors, eliminating their desensitization (restore the response to bronchodilators, allowing to reduce the frequency of their use), reduce the bronchial mucous membrane swelling, mucus production, improve mucociliary transport.

Unlike systemic anti-inflammatory drugs, drugs used in the form of inhalation, have a higher selectivity, more pronounced local anti-inflammatory and low systemic activity, minimal mineralocorticoid activity.

Effect of inhalation corticitis Asthma is dose-dependent. Abrupt withdrawal of drugs can lead to a worsening course of the disease. According to various authors, approximately 10–30% of the nominal dose is deposited in the lung by the inhalation route.

The dose of the drug entering the respiratory tract depends on the structure of the drug molecule, its size and on the form of its delivery to the respiratory system. With inhalation, most of the dose of corticosteroid swallowed, absorbed from the gastrointestinal tract and rather quickly destroyed due to the effect of “first passage” through the liver. The amount of drug entering the systemic circulation from the gastrointestinal tract is small.

Part of the dose of inhalation corticitis can enter the systemic circulation by adsorption in the alveoli, while the drug enters the systemic circulation, bypassing the liver. Particle size during inhalation of corticoid determines the percentage of absorption in the airways.

Particles less than 0.3 microns in size are easily deposited in the alveoli, where they are rapidly absorbed into the blood. All inhalation corticosteroids have a high level of association with plasma proteins. The rate of their elimination from the body is large enough, which causes minimal severity of systemic side effects. Inhaled glucocorticosteroids (beclomethasone, budesonide, fluticasone, mometasone, and ciclesonide) differ in bioavailability and anti-inflammatory activity, lipophilicity.

High lipophilic inhalation corticosomes , such as budesonide, are captured faster and better from respiratory gaps and are retained longer in the tissues of the respiratory tract compared to non-inhalational GCS. high selectivity of budesonide, a better benefit / risk ratio, and a high therapeutic index of the drug.

Unlike other inhaled corticosoids budesonide is capable of forming intracellular fatty acid conjugates. Conjugated budesonide is hydrolyzed by intracellular lipases, gradually releasing free and pharmacologically active budesonide, which can lengthen the glucocorticoid activity of the drug.

The lipophilicity of budesonide conjugates with fatty acids is tens of times higher than that of intact budesonide and this causes the duration of budesonide in the tissues of the respiratory tract. Budesonide is the only corticosteroid with a possible single administration per day .

To ensure an adequate dosing regimen and determine the duration of therapy for patients with bronchial asthma, all of the above should be taken into account when choosing a corticoid . The effectiveness of treatment of bronchial asthma and COPD depends largely on how optimally chosen inhaler.

There are various forms of delivery of these drugs . Nebulizer therapy is available in use, especially in pediatrics, and does not require the coordination of inspiration with the activation of a drug inhaler.

The possibilities of high-dose bronchodilatory therapy in severe attacks of asthma, use at an early age in children have been expanded. A relatively homogeneous highly dispersed aerosol is generated through a nebulizer and, at the same time, propellants and lactose are absent. In our research

In order to study the experience of using corticosteroid budesonide (Pulmicort), the goal was to confirm the therapeutic efficacy and tolerability of the drug budesonide (Pulmicort) in treating children with asthma in a specialized department of a multidisciplinary hospital. Materials and methods: the study included 45 patients with asthma at the allergology department aged 3 to 15 years.

The inclusion criterion was a confirmed diagnosis of bronchial asthma in children. The diagnosis is verified on the basis of complaints, clinical, laboratory, radiological and functional research methods. Aggravated allergic history of the disease was detected in 83.6% of patients.

Patients were evaluated for asthma control using the Asthma questionnaire. Control Test , analysis of case histories of patients with asthma , analysis of the department’s annual report.

According to the annual report in the allergology department of the children’s clinical hospital, the number of patients with asthma was: in 2011 — 396 (48.5%), in 2012 — 366 (46.7% of the total number of patients), in 2013 — 387 (39, 7%).

Drug therapy was conducted in the mode of nebulization with budesonide (pulmicort) for 21 days, followed by transfer to the dosage forms of the drug at the outpatient stage of patient management. Monitoring the effectiveness of drug pharmacotherapy was carried out before and 20 days after the start of therapy.

Results: in the course of treatment, all patients showed positive dynamics against the background of daily inhalation of budesonide (pulmicort) through a compression nebulizer manufactured by OMRON in doses of 250–500 μg per day. Obligation of inhalation is strictly controlled. It was clinically noted: a decrease in the number of daytime symptoms, a decrease in cough, a decrease in the amount of sputum and wheezing during auscultation.

Significant differences were found before and after treatment (p˂0.05) of peak expiratory flow rates. It was noted good tolerability. Asthma results in the observation group Control Test on the 20th day of hospitalization they looked as follows: less than 20 points – asthma could not be controlled – 9 children (22%); from 20 to 24 points – incomplete control –31 children (69%); 25 points – full control over asthma – 5 children (9%). Children with Asthma Control Test below 20 points received in the stage of severe exacerbation of asthma (5 people)

Thus, the use of inhaled glucocorticosteroid drug budesonide (Pulmicort) with delivery through a compression nebulizer in doses of 250-500 mg / day in a multidisciplinary hospital provides an effective and safe treatment of asthma in patients aged 3 to 15 years. Control of asthma comes in a shorter time.

Budesonide exhibits pronounced anti-inflammatory activity. The drug is well tolerated, safe to use. The success of pharmacotherapy with bronchial asthma gives hope in the management of patients with chronic respiratory diseases.

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