Mechanism of Action and Pharmacokinetics
The structure of beclomethasone is based on a steroid nucleus (cyclopentanoperhydrophenanthrene). The drug contains a chlorine atom at the 9-alpha position, making it a halogenated steroid with enhanced glucocorticoid activity.
The main challenge with inhaled steroids is the risk of systemic (resorptive) effects. The drug can be cleared from the airways by mucociliary clearance, deposited in the oral cavity, swallowed, and absorbed from the gastrointestinal tract into the bloodstream.
To minimize systemic effects, beclomethasone undergoes intensive presystemic elimination. The fraction of the drug reaching the GI tract is rapidly degraded during its first pass through the liver and does not reach the systemic circulation in an active form. Unlike systemic drugs (prednisolone, dexamethasone), beclomethasone acts topically.
Pharmacological Effects
The drug exerts pronounced anti-inflammatory, anti-allergic, and anti-edematous effects on the airway mucosa.
- Reduces eosinophilic infiltration of lung tissue.
- Decreases bronchial hyperreactivity.
- Improves pulmonary function test (PFT) parameters.
- Exerts a permissive effect: restores the sensitivity of bronchial receptors to bronchodilators, which is critical in severe asthma.
Indications
Because the drug's action develops gradually, it is intended exclusively for regular, systematic (maintenance) treatment rather than emergency relief.
- Pulmonology: Steroid-dependent bronchial asthma (most severe cases). Administered via aerosol inhalation.
- ENT pathology: Vasomotor and allergic rhinitis. Administered intranasally (as nasal sprays).
Adverse Effects and Contraindications
Due to its pharmacokinetic properties, systemic effects are virtually absent. Adverse effects are primarily local in nature:
- Voice apparatus: Dysphonia (hoarseness).
- Irritant effects: Cough, sneezing, throat irritation, and burning in the throat or larynx.
- Infectious complications: Prolonged use may lead to oral candidiasis (oral thrush) of the mouth and upper respiratory tract.
- Specific reaction: Paradoxical bronchospasm occurs rarely. Intravenous theophylline is used to relieve it.
Contraindications: Active pulmonary tuberculosis and the first trimester of pregnancy.
Administration and Prescription Writing
The drug is available as metered-dose aerosols (including dose optimizers) and dry powder inhalers (with dosing devices or diskhalers).
Maintenance dose is 100–200 mcg. Frequency is 2–4 times daily.
Prescription example: Rp.: Aeros. Beclomethasoni 0.05 mg - 1 dose D.t.d. N. 1 S. Inhale 2 puffs twice daily.