Alvesco

Mode of action

Following inhalation, Alvesco® is rapidly absorbed by the cells of the respiratory tract and lung,1 where it is converted into activated desisobutyryl-ciclesonide (des-CIC).2 Des-CIC has a high glucocorticoid receptor (GR) affinity3 and its influence on DNA transcription results in high anti-inflammatory activity, through activation of anti-inflammatory genes and down-regulation of pro-inflammatory genes.

Des-CIC forms reversible lipid conjugates in the lung,4 creating a reservoir capable of releasing active metabolite and prolonging the anti-inflammatory effects of Alvesco®. This allows for once-daily dosing.5 

VIDEO: Watch the mode of action of Alvesco® below or download it from here to share with colleagues.

The mode of action of Alvesco®

The mode of action of Alvesco®


References

  1. Nonaka T, Nave R, McCracken N, et al. Ciclesonide uptake and metabolism in human alveolar type II epithelial cells (A549). BMC Pharmacol 2007;7:12.
  2. Mutch E, Nave R, McCracken N, et al. The role of esterases in the metabolism of ciclesonide to desisobutyryl-ciclesonide in human tissue. Biochem Pharmacol 2007;73:1657-64.
  3. Stoeck M, Riedel R, Hochhaus G, et al. In vitro and in vivo anti-inflammatory activity of the new glucocorticoid ciclesonide. J Pharmacol Exp Ther 2004;309:249-58.
  4. Nave R, Meyer W, Fuhst R, et al. Formation of fatty acid conjugates of ciclesonide active metabolite in the rat lung after 4-week inhalation of ciclesonide. Pulm Pharmacol Ther 2005;18:390-6.
  5. Wilson AM, Duong M, Pratt B, et al. Anti-inflammatory effects of once daily low dose inhaled ciclesonide in mild to moderate asthmatic patients. Allergy 2006;61:537-42.
Loading ...