[Topical anti-inflammatory activity of dexamethasone 17-valerate (author's transl)].
The anti-inflammatory activity of dexamethasone 17-valerate ointment (DV-17, 0.12%) was investigated by topical application in mice and rats, and the effects compared with those of dexamethasone (DX, 0.12%), betamethasone 17-valerate (BV-17, 0.12%), beclomethasone 17,21-dipropionate (BE, 0.025%) and hydrocortisone 17-butyrate (HC, 0.1%) which were prepared with the same ointment base. DV-17 inhibited markedly the superficial inflammation such as increased vascular permeability induced by intradermal injection of histamine or bradykinin in rats and edema induced by a drop of croton oil into the mouse ear. DV-17 also inhibited significantly rat paw edema induced by carrageenin, yeast, nystatin and mustard. The inhibitory activity of DV-17 on those acute inflammatory responses was similar to that of DX and BV-17. In the inhibitory activity on carrageenin induced paw edema, DV-17 was less potent than that of DX when given orally, however was similar to DX in topical application. DV-17 also inhibited granulation tissue proliferation by subcutaneous paper disk implantation and nontreated foot swelling in adjuvant arthritic rats, but the inhibitory activity of DV-17 on the inflammation of these distant areas was lower than that of DX. On the other hand, systemic effects such as decrease in weight of adrenal or thymus and body weight loss were most evident in the case of DX and lower with DV-17. DV-17 prolonged wound healing and inhibited the delayed-type hypersensitivity induced by picryl chloride. The activity was equivalent to that of DX and BV-17. From the above results, it may be considered that DV-17 possesses potent anti-inflammatory activity, whereas it has fewer side effects and is a useful glucocorticoid for external application.
D000287:Administration, Topical; D000818:Animals; D000893:Anti-Inflammatory Agents; D001169:Arthritis, Experimental / Q000188:drug therapy; D002199:Capillary Permeability / Q000187:drug effects; D003907:Dexamethasone / Q000031:analogs & derivatives* / Q000494:pharmacology / Q000627:therapeutic use; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy; D006097:Granulation Tissue / Q000502:physiology; D006968:Hypersensitivity, Delayed / Q000188:drug therapy; D008297:Male; D051379:Mice; D009929:Organ Size / Q000187:drug effects; D011817:Rabbits; D051381:Rats; D014945:Wound Healing / Q000187:drug effects
D000893:Anti-Inflammatory Agents; D003907:Dexamethasone; C030949:dexamethasone 17-valerate