Wajchenberg B L, Cesar F P, Luthold W W, Okada H, Borghi V C
Braz J Med Biol Res. 1986;19(1):39-47.
The effects of deflazacort (DFL), a new oxazoline derivative of prednisolone, were compared with those of prednisone (Pd) by measuring plasma cortisol (F) levels as an index of the function of the hypothalamic-pituitary-adrenal (HPA) axis. Twelve normal volunteers received each glucocorticoid for 16 to 24 days in a double-blind cross-over trial with random allocation of subjects to treatment with DFL (24 mg/day) and Pd (20 mg/day) in clinically equivalent doses, with a washout period from 20 to 45 days between administration of the glucocorticoids. The following tests were performed in a randomized sequence: cortisol (F) circadian rhythm, insulin tolerance test (ITT), lysine-vasopressin (LVP) and B1-24 ACTH stimulation. Despite basal F suppression by DFL, the relative maximum F response (maximum F increment above basal/basal x 100) was significantly greater than control for the ITT and ACTH tests and was similar to the control after intramuscular injection of LVP, suggesting that the responses were appropriate for the basal F levels, with the HPA being reset at a lower level. After Pd, despite higher basal F levels, the F diurnal rhythm disappeared and there was no significant response to ITT, LVP or ACTH, indicating that the limiting factor in the HPA response was the reduced adrenal F production independent of the effects on the steroid-sensitive tissues of the brain including the pituitary.
通过测量血浆皮质醇（F）水平作为下丘脑 - 垂体 - 肾上腺（HPA）轴功能指标，比较了泼尼松龙的新型恶唑啉衍生物地夫可特（DFL）与泼尼松（Pd）的作用。12名正常志愿者参与了一项双盲交叉试验，每人接受每种糖皮质激素治疗16至24天，受试者被随机分配接受临床等效剂量的DFL（24毫克/天）和Pd（20毫克/天）治疗，两种糖皮质激素给药之间有20至45天的洗脱期。按随机顺序进行了以下测试：皮质醇（F）昼夜节律、胰岛素耐量试验（ITT）、赖氨酸 - 血管加压素（LVP）和B1 - 24促肾上腺皮质激素（ACTH）刺激试验。尽管DFL使基础F水平受到抑制，但ITT和ACTH试验中相对最大F反应（高于基础值的最大F增加值/基础值×100）显著大于对照组，且肌肉注射LVP后与对照组相似，这表明这些反应与基础F水平相适应，HPA轴在较低水平重新设定。使用Pd后，尽管基础F水平较高，但F昼夜节律消失，对ITT、LVP或ACTH无明显反应，表明HPA反应的限制因素是肾上腺F生成减少，这与对包括垂体在内的脑内类固醇敏感组织的影响无关。
