Corticosteroid pharmacokinetic/pharmacodynamic parameters and their relationship to safety and efficacy.
All inhaled corticosteroids (ICSs) exert their pharmacologic effects through the same mechanism. This review examines pharmacokinetic profiles of ICSs to explain the variations in efficacy and adverse effects seen with these agents and identify ideal properties for an optimal ICS. For optimum efficacy and safety, the ideal ICS would have high pulmonary bioavailability with pulmonary activation for targeted delivery, negligible oral bioavailability, high plasma protein binding, rapid systemic clearance, and sustained pulmonary residence to permit once-daily dosing.
Derendorf
Hartmut
H
Department of Pharmaceutics, University of Florida, P.O. Box 100494, Gainesville, FL 32610-0494, USA.
D000280:Administration, Inhalation; D001249:Asthma / Q000188:drug therapy*; D005938:Glucocorticoids / Q000008:administration & dosage / Q000493:pharmacokinetics*; D006801:Humans; D016896:Treatment Outcome
D005938:Glucocorticoids