Effects
Glucocorticoids (ATC R03BA02) have anti-inflammatory, antiallergic, and immunosuppressive properties. The effects are based on binding to intracellular receptors, resulting in an influence on protein expression. In addition, glucocorticoids also exert extragenomic effects. All agents are lipophilic (virtually insoluble in water) and thus enter cells well across the cell membrane.
Indications
For the treatment of obstructive airway diseases:
- Bronchial asthma – inhaled glucocorticoids are among the 1st choice agents.
- Chronic bronchitis, chronic obstructive pulmonary disease (COPD) – not the standard therapy.
Dosage
According to the professional information. The drugs should be inhaled regularly and not only when needed. Inhalation methods include metered-dose inhalers, powder inhalers, and solutions. To reduce the risk of mouth sores, it is recommended to inhale immediately before eating and to rinse the mouth well with water after each use and then spit out the water. Mouth rinsing may also help prevent throat irritation and possibly reduce the risk of systemic effects.
Active Ingredients
The following active ingredients are approved in many countries:
- Budesonide inhalation (e.g., Pulmicort, generic, Symbicort).
- Ciclesonide (Alvesco)
- Fluticasone (e.g., Axotide, Seretide)
- Beclometasone (Qvar, Beclo Orion)
- Mometasone inhalation (Asmanex)
- Triamcinolone acetonide (not commercially available for this indication in many countries).
Contraindications
Inhaled glucocorticoids are contraindicated in hypersensitivity, untreated respiratory or eye infections, and in some cases in children. Refer to the drug label for complete precautions.
Interactions
Some agents are substrates of CYP450 isozymes, which degrade glucocorticoids in the liver and elsewhere. Concomitant administration of CYP inhibitors may increase systemic exposure and thus the risk for adverse reactions.
Adverse effects
The most common potential adverse effects include oral thrush due to immunosuppression, pharyngitis, headache, and hoarseness. The drugs may very rarely cause systemic glucocorticoid side effects. These include:
- Cushing’s syndrome, cushingoid symptoms.
- Inhibition of adrenal cortex function.
- Growth retardation in children and adolescents
- Decrease in bone density
- Cataracts, glaucoma
However, the amounts absorbed into the circulation are small and local therapy is much better tolerated than systemic.
