Pulmicort Turbukhaler, 100 mcg/dose 200 doses

Pharmacotherapeutic group: glucocorticosteroid for topical use
ATC code: Pharmacological properties

Pharmacodynamics
Budesonide is a glucocorticosteroid with strong local anti-inflammatory effects.
The exact mechanism of action of glucocorticosteroids in the treatment of bronchial asthma is not fully understood. Anti-inflammatory effects, such as inhibition of release of inflammatory mediators and cytokine-mediated immune response, may be the most important. The affinity of budesonide for glucocorticosteroid receptors is 15 times greater than that of prednisolone.
The anti-inflammatory effect of budesonide is mediated by a reduction in the degree of airway obstruction during early and late allergic response. Budesonide reduces airway reactivity in response to histamine and methacholine inhalation.
The sooner budesonide treatment is initiated from the time of diagnosis of persistent bronchial asthma, the greater improvement in lung function should be expected.
A dose-dependent effect on plasma and urinary cortisol levels has been shown with Pulmicort Turbuhaler administration. At the recommended doses, the drug has significantly less effect on adrenal function than prednisone at 10 mg as shown in ACTH tests.
Use of budesonide at doses up to 400 mcg per day in children over 3 years of age did not result in systemic effects. Biochemical signs of the drug systemic effect may be observed when using the drug in the dose from 400 to 800 mcg per day. When the dose of 800 mcg per day is exceeded, systemic effects of the drug are common.
The use of glucocorticosteroids for the treatment of bronchial asthma may cause growth retardation.
Initially small, usually transient growth retardation (about 1 cm) has been noted, usually during the first year of treatment. Long-term studies in clinical settings have shown that children and adolescents treated with inhaled budesonide achieve, on average, the estimated adult height. However, in a long-term double-blind study primarily without titration of the budesonide dose to the lowest effective dose, the growth of children and adolescents receiving inhaled budesonide was on average 1.2 cm shorter than that of the placebo group when they reached adulthood (see Dosage and Growth Control recommendations in the Dosage and Administration and Precautions sections).
Therapy with inhaled budesonide once or twice daily has been shown to be effective in preventing physical effort asthma.

Pharmacokinetics

Absorption
Inhaled budesonide is rapidly absorbed. After inhalation with Turbuhaler, about 25-35% of the measured dose is absorbed into the lungs. Maximum plasma concentration is reached 30 minutes after inhalation. Systemic bioavailability of the drug is about 38% of the administered dose.

Metabolism and distribution
Binding to plasma proteins is on average 90%. The volume of distribution of budesonide is approximately 3 L/kg. After absorption budesonide undergoes intensive (over 90%) biotransformation in the liver to form metabolites with low glucocorticosteroid activity. The glucocorticosteroid activity of the major metabolites 6b-hydroxybudesonide and 16a-hydroxyprednisolone is less than 1% of the glucocorticosteroid activity of budesonide.

Evolution
Budesonide is metabolized mainly with participation of the CYP3A4 enzyme. Metabolites are excreted unchanged in the urine or in conjugated form. A small amount of unchanged budesonide is excreted in the urine. Budesonide has high systemic clearance (about 1.2 l/min). Pharmacokinetics of budesonide is proportional to the administered dose of the drug.
Pharmacokinetics of budesonide in children and patients with impaired renal function is unknown. In patients with liver disease the time of budesonide retention in the body may be prolonged.

Indications

Active ingredient

Composition

How to take, the dosage

Interaction

Special Instructions

Synopsis

Contraindications

Side effects

By frequency of occurrence, adverse effects are classified as follows: very frequently (> 1/10), frequently (> 1/100 to < 1/10), infrequently (> 1/1000 to < 1/100), rarely (> 1/10000 to < 1/1000), very rarely, including individual reports (< 1/10000), frequency not determined.

Patients taking the drug may experience the following side effects:

System-organ

grade

Frequency

Unwanted drug reaction

Infections and invasions

Often

Oropharyngeal candidiasis, pneumonia

(in patients with COPD)

Immune system disorders

Rarely

Immediate and delayed-type hypersensitivity reactions, including rash, contact dermatitis, urticaria,

anergic reaction/p>

angioedema, bronchospasm, and anaphylactic reaction

Mental disorders

Rarely

Nervousness, excitability,

depression, behavioral disorders

Respiratory system, chest organ disorders

/p>

and mediastinum

Often

Mild irritation of the pharyngeal mucosa, cough,

hoarseness of the voice

Rarely

Bronchospasm

Skin and subcutaneous tissue disorders

Rarely

Bleeding

Given the risk of oropharyngeal candidiasis, patients should rinse their mouth thoroughly with water after each inhalation of the drug.

In rare cases, symptoms due to systemic effects of glucocorticosteroids may occur, including adrenal hypofunction. Nausea, altered taste, hypercorticism, hypocorticism, cataracts, glaucoma, difficulty swallowing, stunted growth (in children and adolescents), and decreased bone density may also occur.

Overdose

Pregnancy use

Pregnancy

The results of animal studies have shown that glucocorticosteroids can cause fetal abnormalities, but these findings cannot be extrapolated to humans receiving glucocorticosteroids at recommended doses.

The use of budesonide in pregnant women has not increased the risk of fetal abnormalities; however, the risk cannot be completely ruled out, and the lowest effective dose of budesonide should be used during pregnancy, keeping in mind the possibility of worsening the course of bronchial asthma.

When prescribing the drug, the expected benefit to the mother must be balanced against the potential risk to the baby.

Breastfeeding

Budesonide is excreted with breast milk, but no effect on the infant is expected with the use of Pulmicort Turbukhaler in therapeutic doses. When prescribing the drug, the expected benefit to the mother and the potential risk to the baby should be considered.

Similarities