Systemic side effects

Alvesco® exhibits high total lung deposition and small airway distribution.1 These properties could increase the systemic availability of Alvesco® and increase unwanted side effects, but the specific pharmacological properties of Alvesco® prevent this.

Alvesco® targets the lung, thereby minimizing systemic corticosteroid exposure, even at the highest dose of 1,280 µg/day:2

  1. Protein-binding ensures that only a small proportion of Alvesco® reaches the systemic circulation, and that most of the drug is unavailable to exert systemic effects.3
  2. Alvesco® undergoes high first-pass metabolism.4
  3. Alvesco® is excreted via the gut.5

The effects of Alvesco® on cortisol suppression are comparable with that of placebo (Figure 1).2

232 fig 1Cortisol suppression Derom 2005
Figure 1: The effect of Alvesco® on serum cortisol levels is comparable to placebo. Adapted from Derom E, et al 2005.2

  1. Newman S, Salmon A, Nave R, et al. High lung deposition of 99mTc-labeled ciclesonide administered via HFA-MDI to patients with asthma. Respir Med 2006;100:375-84.
  2. Derom E, Van DV, V, Marissens S, et al. Effects of inhaled ciclesonide and fluticasone propionate on cortisol secretion and airway responsiveness to adenosine 5'monophosphate in asthmatic patients. Pulm Pharmacol Ther 2005;18:328-36.
  3. Rohatagi S, Luo Y, Shen L, et al. Protein binding and its potential for eliciting minimal systemic side effects with a novel inhaled corticosteroid, ciclesonide. Am J Ther 2005;12:201-9.
  4. Nave R, Bethke TD, van Marle SP, et al. Pharmacokinetics of [14C]ciclesonide after oral and intravenous administration to healthy subjects. Clin Pharmacokinet 2004;43:479-86.
  5. Alvesco® EU SmPC. Date of last revision: November 2012.
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