Markham A, Bryson H M
Adis International Limited, Auckland, New Zealand.
Drugs. 1995 Aug;50(2):317-33. doi: 10.2165/00003495-199550020-00008.
Deflazacort is an oxazoline derivative of prednisolone with anti-inflammatory and immunosuppressive activity. Both short (4 to 6 weeks) and longer term (13 to 52 weeks) studies have shown deflazacort to be as effective as prednisone or methylprednisolone in patients with rheumatoid arthritis. The drug was at least as effective as prednisone in children with juvenile chronic arthritis. Insufficient data are available to draw firm conclusions regarding the efficacy of deflazacort as treatment for patients with severe asthma, but the drug has demonstrated some efficacy as treatment for nephrotic syndrome and other applications such as Duchenne dystrophy, systemic lupus erythematosus, uveitis and transplantation. The overall incidence of adverse events in deflazacort recipients (16.5%) is lower than that recorded in patients treated with prednisone (20.5%) or methylprednisolone (32.7%) and similar to that in betamethasone recipients (15.3%). Gastrointestinal symptoms are the most frequently reported adverse events in deflazacort recipients; other adverse events associated with the drug include metabolic and nutritional disorders, central and peripheral nervous system disturbances and psychiatric disorders. In general, deflazacort appears to have less effect than prednisone on parameters which may be associated with the development of corticosteroid-induced osteoporosis. Further, the drug appears have less negative impact on growth rate in children with diseases requiring corticosteroid therapy. In a study of 2 months' duration in patients with conditions requiring corticosteroid treatment, moderate dosages of deflazacort produced no clinically relevant diabetogenic effects. Thus, deflazacort may be associated with less serious metabolic sequelae than prednisone but further well designed long term trials are required to confirm this. In the meantime, in adults, deflazacort should be reserved for use in those pre-disposed to, or who develop, intolerable metabolic sequelae during treatment with corticosteroids. In children, however, even though available efficacy data are minimal, deflazacort should be considered as an initial option in those requiring corticosteroid therapy since the adverse effects caused by this drug class are particularly debilitating in this patient group.
地夫可特是泼尼松龙的恶唑啉衍生物,具有抗炎和免疫抑制活性。短期(4至6周)和长期(13至52周)研究均表明,地夫可特在类风湿性关节炎患者中与泼尼松或甲泼尼龙疗效相当。在青少年慢性关节炎患儿中,该药物疗效至少与泼尼松相当。关于地夫可特治疗重度哮喘患者的疗效,现有数据不足,无法得出确切结论,但该药物已证明在治疗肾病综合征及其他病症(如杜氏肌营养不良症、系统性红斑狼疮、葡萄膜炎和移植)方面有一定疗效。接受地夫可特治疗的患者不良事件总发生率(16.5%)低于接受泼尼松(20.5%)或甲泼尼龙(32.7%)治疗的患者,与接受倍他米松治疗的患者(15.3%)相似。胃肠道症状是接受地夫可特治疗的患者最常报告的不良事件;与该药物相关的其他不良事件包括代谢和营养紊乱、中枢和外周神经系统障碍以及精神障碍。一般来说,地夫可特对可能与皮质类固醇诱导的骨质疏松症发展相关的参数影响似乎比泼尼松小。此外,该药物对需要皮质类固醇治疗的患儿生长速率的负面影响似乎较小。在一项针对需要皮质类固醇治疗的患者进行的为期2个月的研究中,中等剂量的地夫可特未产生临床相关的致糖尿病作用。因此,地夫可特可能比泼尼松引起的严重代谢后遗症更少,但需要进一步设计良好的长期试验来证实这一点。同时,在成人中,地夫可特应保留用于那些在皮质类固醇治疗期间易发生或已发生无法耐受的代谢后遗症的患者。然而,在儿童中,尽管现有疗效数据极少,但对于需要皮质类固醇治疗的患儿,地夫可特应被视为初始选择,因为该类药物引起的不良反应在该患者群体中尤其严重。