Ciclesonide

General information

Ciclesonide, a non-halogenated glucocorticoid, is converted locally in the airways to an active metabolite, desisobutyrylciclesonide, which has a 100-fold greater relative glucocorticoid receptor binding affinity than ciclesonide itself [ ]. The pharmacokinetic–pharmacodynamic profile of inhaled ciclesonide suggests a reduced potential for adverse systemic effects.

Ciclesonide is formulated in a hydrofluoroalkane-propelled metered-dose inhaler (MDI), and a daily dosing schedule of 160 micrograms was as active and safe in asthmatic patients as fluticasone propionate 88 micrograms twice daily [ ] or budesonide 200 micrograms twice daily [ ].

Mean intrapulmonary deposition of inhaled ciclesonide is 52%, while mean oropharyngeal deposition is 38% [ , ]. Oropharyngeal deposition of desisobutyrylciclesonide was more than one order of magnitude lower than that of budesonide when ciclesonide was administered in a dose of 800 micrograms in healthy volunteers [ ]. Low oropharyngeal deposition of ciclesonide and low conversion of ciclesonide to desisobutyrylciclesonide in the oropharynx [ , ] result in reduced local adverse reactions.

Drug studies