hoe-777 and hydrocortisone-aceponate

Nonhalogenated double esters of prednisolone or hydrocortisone 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.. 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%), hydrocortisone (1%), and two drug-free vehicles in 60 healthy volunteers. Test models are the skin blanching assay (occluded and nonoccluded mode), ultraviolet-induced erythema, and an irritant (sodium dodecyl sulfate) dermatitis. The benefit/risk ratio is derived from the activity in the former models and the reduction of skin thickness as determined previously.. Prednicarbate activity increases in a dose-dependent manner. Prednicarbate, 0.25%, and the hydrocortisone double esters appear to be equipotent to betamethasone 17-valerate in the skin blanching test and the ultraviolet-erythema test, but superior to hydrocortisone and the vehicles. Prednicarbate and its vehicle, however, do not reverse irritant dermatitis. The benefit/risk ratios of prednicarbate and hydrocortisone aceponate exceed those with betamethasone 17-valerate.. Prednicarbate and hydrocortisone aceponate are intermediate potent glucocorticoids that are superior to betamethasone 17-valerate because of the improved benefit/risk ratio. Patients with severe atopic dermatitis and those who relapse frequently should profit from the treatment with these newer glucocorticoids.

Topics: Administration, Topical; Adult; Anti-Inflammatory Agents; Betamethasone Valerate; Dose-Response Relationship, Drug; Double-Blind Method; Drug Eruptions; Female; Humans; Hydrocortisone; Male; Prednisolone; Reference Values; Skin

Topics: Administration, Cutaneous; Adult; Betamethasone Valerate; Double-Blind Method; Drug Evaluation; Erythema; Female; Humans; Hydrocortisone; Male; Prednisolone; Skin; Ultraviolet Rays; Vasoconstriction

With the advent of non-fluorinated double esters the spectrum of topical dermatotherapy with glucocorticoids seems to have broadened to include safer congeners. To assess the atrophogenicity potential of glucocorticoids, high-frequency ultrasound has been proposed. In a comparative trial using the DUB 20 system, 24 healthy volunteers applied hydrocortisone aceponate, the corresponding vehicle, prednicarbate ointment and betamethasone-17-valerate ointment over a period of 6 weeks. While both hydrocortisone aceponate and prednicarbate ointment induced no significant reduction in skin thickness, the onset of epidermal-dermal thinning with betamethasone-17-valerate was early and the extent marked. These findings imply an increased therapeutic index with the non-fluorinated double esters.

Topics: Administration, Topical; Anti-Inflammatory Agents; Atrophy; Betamethasone Valerate; Double-Blind Method; Humans; Hydrocortisone; Ointments; Prednisolone; Skin; Ultrasonography

Topics: Administration, Topical; Anti-Inflammatory Agents; Atrophy; Humans; Hydrocortisone; Prednisolone; Risk Factors; Skin

Topics: Administration, Cutaneous; Adult; Atrophy; Betamethasone Valerate; Clobetasol; Double-Blind Method; Glucocorticoids; Humans; Hydrocortisone; Pharmaceutical Vehicles; Prednisolone; Skin; Ultrasonography