The physical, animal and human pharmacologic, and toxicologic properties of desonide, a new, topically active, antiinflammatory steroid
| Autor: | Frank J. Sanen, Jerry L. Leeling, Olfeo J. Lorenzetti, R. E. Hartnagel, Toni L. Hammes, Barrie M. Phillips, Paul J. Kraus, Lawrence F. Sancilio |
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| Rok vydání: | 1971 |
| Předmět: |
Male
Triamcinolone acetonide Chemical Phenomena Hydrocortisone medicine.medical_treatment Administration Topical Prednisolone Anti-Inflammatory Agents Absorption (skin) Pharmacology Toxicology Triamcinolone Acetonide Steroid Acetals Dogs Fluocinolone acetonide medicine Potency Animals Carbon Isotopes Granuloma Chemistry Liver Glycogen Rats Desonide Fluocinolone Acetonide Toxicity Female Rabbits medicine.drug |
| Zdroj: | Toxicology and applied pharmacology. 20(4) |
| ISSN: | 0041-008X |
| Popis: | Desonide, 16α-hydroxyprednisolone-16,17-acetonide, is a nonhalogenated steroid possessing physical properties predictive of potent topical antiinflammatory activity. Based on assay findings in 4 animal models (liver glycogen deposition, cotton pellet granuloma, ear edema, and ocular inflammation), desonide showed an average potency about 60 times that of hydrocortisone, which suggested that desonide should exhibit, on topical use, considerable antiinflammatory activity. Subsequently, desonide proved to be about as active as fluocinolone acetonide in human dose titration studies, having a more rapid onset than the reference steroid during the early phase of treatment. The absorption of desonide from a cream formulation applied to the skin of rabbits averaged 54% greater than that of triamcinolone acetonide (as predicted by the physical properties of desonide), an observation that may partially explain the apparently greater clinical activity of desonide. In view of the apparently greater clinical activity of desonide, this finding indicates that somewhat less steroid will be absorbed from clinically effective doses of desonide than from equieffective doses of triamcinolone acetonide. Desonide was only 6 times as toxic as hydrocortisone and one-fifteenth as toxic as triamcinolone acetonide on acute sc administration to rats. A cream formulation of desonide was virtually nontoxic on po administration to rats and dogs, and it elicited a low order of toxicity when administered topically in large doses to rabbits. |
| Databáze: | OpenAIRE |
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