Comparison of clinical efficacy of inhaled glucocorticoids.
Ratios of clinical efficacy of inhaled steroids are determined by re-evaluation of 29 clinical studies including 6538 patients. The method is based on the calculation of the areas under the curves (AUCs) describing the increase of morning peak flow over baseline during the period of treatment with inhaled glucocorticoids. Dividing the AUC by the applied dose results in a normalized AUC for a dose of 1 mg. Effects of treatments are compared for pairs of glucocorticoids tested in carefully matched groups using the normalized AUCs. Additionally, the effect of the drug delivery system is taken into account according to the literature because of its influence on the effective dose deposed in the lung. Thus, ratios of treatment success are determined: fluticasone propionate (FP, CAS 80474-14-2) versus budesonide (Bud, CAS 51333-22-3) 1:0.309, FP versus beclomethasone dipropionate (BDP, CAS 5534-09-8)1:0.561, FP versus flunisolide (CAS 3385-03-3) 1:0.339, FP versus triamcinolone acetonide (TAAC, CAS 76-25-5) 1:0.206, BDP versus Bud 1:0.609. Ratios for clinical efficacy correspond with the ratios of relative receptor affinities of these pairs of glucocorticoids. Besides the dominant influence of the receptor mediated effect the influence of local metabolisation in case of BDP is discussed as well as the effect of tissue binding in case of FP.
Rohdewald
P J
PJ
Institut für Pharmazeutische Chemie der Westfälischen Wilhelms-Universität, Münster/Westf. (Germany).
D000280:Administration, Inhalation; D000818:Animals; D002986:Clinical Trials as Topic; D005938:Glucocorticoids / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D006801:Humans
D005938:Glucocorticoids