Comparison of Inhaled Corticosteroids: An Update

H William Kelly, PharmD


The Annals of Pharmacotherapy. 2009;43(3):519-527. 

In This Article

Once-daily Dosing

Mometasone furoate was the first inhaled corticosteroid to obtain FDA-approved labeling for once-daily dosing as a starting dose. Budesonide DPI obtained FDA approval for once-daily dosing for patients who were initially stabilized on twice-daily dosing and budesonide inhalation suspension has been approved for initial once-daily dosing. Beclomethasone dipropionate HFA-MDI, ciclesonide HFA-MDI, flunisolide HFA-MDI, and fluticasone propionate HFA-MDI all have FDA-approved labeling for twice-daily dosing. The initial 2 pivotal trials for ciclesonide HFA-MDI in children 4–11 years old showed that once-daily dosing failed to produce conclusive evidence of efficacy. However, data from the 2 studies were published as an integrative analysis that reported significantly improved lung function over placebo treatment for the 2 higher doses.[60] The differences were quite small and of questionable clinical significance, with only 2.9% and 3.5% greater improvement shown in mean baseline FEV1 percent predicted for 80 and 160 µg once daily, respectively. However, a comparison of ciclesonide 80 µg twice daily with fluticasone propionate 88 µg twice daily in children 4–15 years of age with persistent asthma reported that both treatments improved prebronchodilator FEV1 significantly above baseline and were not significantly different from each other.[5]

It is unclear whether the differences in indications for once-daily versus twice-daily dosing represent real differences between the various inhaled corticosteroids or whether they are solely based on the dosing or entry criteria in the pivotal trials.[61] Most of the inhaled corticosteroids have demonstrated efficacy with once-daily dosing, although they are more effective in patients with more moderate-to-severe asthma when given twice daily.[2,62,63,64,65,66,67] Neither budesonide nor mometasone furoate has unique pharmacokinetic properties that would favor once-daily dosing. The pharmacokinetic profile of mometasone furoate is similar to that of fluticasone propionate, only with lower lipophilicity and distribution volumes that would not favor retention in the lung. Ciclesonide and flunisolide also undergo fatty acid esterification similar to that of budesonide, and des-ciclesonide has a distribution volume similar to that of fluticasone propionate.[11,14]


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