Clinical Pharmacokinetic and Pharmacodynamic Profile of Inhaled Ciclesonide

Asthma is a chronic inflammatory disease of the airways, and inhaled corticosteroids (ICSs) are recommended as first-line therapy for persistent asthma of all severities. Ciclesonide is a novel ICS, which is administered as an aerosol solution in a metered-dose inhaler, using hydrofluoroalkane-134a...

Full description

Saved in:
Bibliographic Details
Published in:Clinical pharmacokinetics 2009-01, Vol.48 (4), p.243-252
Main Author: Nave, Rüdiger
Format: Article
Language:English
Subjects:
Administration, Inhalation
Anti-Inflammatory Agents - pharmacokinetics
Anti-Inflammatory Agents - pharmacology
Asthma
Asthma - drug therapy
Biological and medical sciences
Chemical properties
Ciclesonide
Dosage and administration
Drug Interactions
Drug therapy
General pharmacology
Humans
Internal Medicine
Lung - diagnostic imaging
Medical sciences
Medicine
Medicine & Public Health
Molecular Structure
Oropharynx - metabolism
Pharmacokinetics
Pharmacokinetics. Pharmacogenetics. Drug-receptor interactions
Pharmacology
Pharmacology. Drug treatments
Pharmacology/Toxicology
Pharmacotherapy
Pregnenediones - administration & dosage
Pregnenediones - pharmacokinetics
Pregnenediones - pharmacology
Protein Binding
Radionuclide Imaging
Review Article
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:Asthma is a chronic inflammatory disease of the airways, and inhaled corticosteroids (ICSs) are recommended as first-line therapy for persistent asthma of all severities. Ciclesonide is a novel ICS, which is administered as an aerosol solution in a metered-dose inhaler, using hydrofluoroalkane-134a as a propellant. Because of the high respirable particle fraction, high pulmonary deposition is obtained in patients, which constitutes the basis of effective therapeutic action. The parent compound, ciclesonide, is pharmacologically inactive and is activated in the target organ, the lung, to form its only pharmacologically active metabolite, desisobutyryl-ciclesonide (des-CIC). Low oral deposition combined with minimal formation of des-CIC in the oropharynx may minimize the typical oropharyngeal adverse events associated with ICSs. Low oral bioavailability, rapid clearance and high protein binding reduce pharmacologically relevant systemic exposure. The unique pharmacokinetic and pharmacodynamic profile of ciclesonide offers a rationale that supports the favourable risk-benefit profile observed in clinical trials in patients with persistent asthma.
ISSN:0312-5963
1179-1926
DOI:10.2165/00003088-200948040-00002