PREDNICARBATE ACTIVITY AND BENEFIT RISK RATIO IN RELATION TO OTHER TOPICAL GLUCOCORTICOIDS

Background. Nonhalogenated double esters of prednisolone or hydrocorti sone applied topically to the skin have a low atrophogenic potential. However, activity and benefit/risk ratio and therefore the superiority over conventional topical glucocorticoids are not well defined. Metho ds: The activities of cream preparations with prednicarbate (0.025% to 0.25%), hydrocortisone aceponate, and hydrocortisone buteprate (0.1%) are compared to the effects of betamethasone 17-valerate (0.1%), hydr ocortisone (1%), and two drug-free vehicles in 60 healthy volunteers. Test models are the skin blanching assay (occluded and nonoccluded mod e), ultraviolet-induced erythema, and an irritant (sodium dodecyl sulf ate) dermatitis. The benefit/risk ratio is derived from the activity i n the former models and the reduction of skin thickness as determined previously. Results: Prednicarbate activity increases in a dose-depend ent manner. Prednicarbate, 0.25%, and the hydrocortisone double esters appear to be equipotent to betamethasone 17-valerate in the skin blan ching test and the ultraviolet-erythema test, but superior to hydrocor tisone and the vehicles. Prednicarbate and its vehicle, however, do no t reverse irritant dermatitis. The benefit/risk ratios of prednicarbat e and hydrocortisone aceponate exceed those with betamethasone 17-vale rate. Conclusions. Prednicarbate and hydrocortisone aceponate are inte rmediate potent glucocorticoids that are superior to betamethasone 17- valerate because of the improved benefit/risk ratio. Patients with sev ere atopic dermatitis and those who relapse frequently should profit f rom the treatment with these newer glucocorticoids.