Clinical Medicine Insights: Pediatrics

Background: Ciclesonide is an inhaled corticosteroid administered by a metered dose inhaler (MDI) to treat bronchial asthma. After inhalation, the inactive ciclesonide is converted by esterases in the airways to active metabolite desisobutyryl-ciclesonide (des-CIC).

Aim: To compare the pharmacokinetic (PK) parameters of des-CIC in children after administration of therapeutic dose of ciclesonide with and without spacer (AeroChamber PlusTM).

Methods: Open-label, 3 period, cross over, repeated dose, PK study in 37 children with mild to moderate stable asthma (age: 6–11 y; body weight: 20–53 kg). During each 7-day treatment period, ciclesonide was inhaled once in the morning: A) 160 µg MDI with spacer, B) 80 µg MDI with spacer, and C) 160 µg MDI without spacer. Serum PK parameters of ciclesonide and des-CIC were determined on Day 7 of each period. The primary PK parameters were the AUC τ and Cmax for des-CIC.

Results: Inhaling ciclesonide with spacer led to a dose proportional systemic exposure (AUC τ) of des-CIC (0.316 µg*h/L for 80 µg and 0.663 µg*h/L for 160 µg). The dose-normalized systemic exposure for des-CIC (based on AUC τ) was 27% higher after inhalation of ciclesonide 80 µg or 160 µg with spacer than without spacer; the corresponding Cmax values for des-CIC were, respectively, 63% and 55% higher with spacer. No clinically relevant abnormalities or adverse drug reactions were observed.

Conclusions: Inhalation of therapeutic ciclesonide dose with spacer led to a slight increase in the systemic exposure of des-CIC, which does not warrant dose adjustment.