Prednicarbate activity and benefit/risk ratio in relation to other topical glucocorticoids.
BACKGROUND
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.


METHODS
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.


RESULTS
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.


CONCLUSIONS
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.
Schäfer-Korting
M
M
Pharmakologisches Institut für Naturwissenschaftler, Johann Wolfgang Goethe-Universität, Frankfurt, Germany.
Korting
H C
HC
Kerscher
M J
MJ
Lenhard
S
S
D000287:Administration, Topical; D000328:Adult; D000893:Anti-Inflammatory Agents / Q000494:pharmacology* / Q000627:therapeutic use; D001624:Betamethasone Valerate / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D004311:Double-Blind Method; D003875:Drug Eruptions / Q000188:drug therapy; D005260:Female; D006801:Humans; D006854:Hydrocortisone / Q000031:analogs & derivatives / Q000494:pharmacology; D008297:Male; D011239:Prednisolone / Q000031:analogs & derivatives* / Q000494:pharmacology / Q000627:therapeutic use; D012016:Reference Values; D012867:Skin / Q000187:drug effects*
D000893:Anti-Inflammatory Agents; C063919:hydrocortisone aceponate; C033014:hydrocortisone 17-butyrate 21-propionate; D001624:Betamethasone Valerate; D011239:Prednisolone; C035287:prednicarbate; D006854:Hydrocortisone