Ciclesonide

Lipophilic inhaled glucocorticoid available as an aerosol for the treatment of bronchial asthma.

Ciclesonide is a non-halogenated glucocorticoid ester, a prodrug that has an ester group at the receptor binding site. Thus the molecule cannot dock to the glucocorticoid receptor. Only after inhalation endogenous esterases in the lung cleave the ester bond to carbon C-17 of the steroid backbone ("on-site" activation). This releases the active metabolite. Cclesonide binds intracellularly to glucocorticoid receptors or forms lipid conjugates which act as a depot. From this depot the active metabolite can be released slowly, which allows the administration once a day. After removal, the substance is metabolised mainly via CYP3A4 to hydroxylated inactive metabolites. Due to the local accumulation in the lung, the rate of local and systemic side effects (e.g. osteoporosis, skin atrophy) is kept comparatively low.

Ciclesonide is suitable for basic therapy of bronchial asthma. When used regularly, it reduces the allergic reactions in the bronchial tubes and hyperreactivity and leads to an improvement in the clinical picture.

The recommended dose as basic medication is 160 μg 1x/day. If necessary dose reduction to 80 μg/day.

Bronchospasm; furthermore, mainly mild local reactions of the oral mucosa (burning, itching). Very rarely cataract formation under long-term Ciclesonide therapy.

Children under 18, pregnant women (see product information)

Alvesco ®

1. Chapman KR et al (2005) Maintenance of asthma control by once-daily inhaled ciclesonide in adults with persistent asthma. Allergy 60: 330-337.
2. Noonan M et al (2001) Comparison of once-daily to twice-daily treatment with mometasone furoate dry powder inhaler. Ann Allergy Asthma Immunol 86: 36-43.
3. Postma DS et al (2001) Treatment of asthma by the inhaled corticosteroid ciclesonide given either in the morning or evening. Eur Respir J 17: 1083-1088.
4. Richter K et al (2005) Comparison of the oropharyngeal deposition of inhaled ciclesonide and fluticasone propionate in patients with asthma. J Clin Pharmacol 45: 146-152.
5. Stock, S et al (2005) Asthma: prevalence and cost of illness. Eur. Respir. J. 25: 47-53.