Department of Internal Medicine II, Rheumatology, Clinical Immunology & Osteology, Schlosspark-Klinik Teaching Hospital Charité University Medicine Berlin, Heubnerweg 2, 14059 Berlin, Germany.
Expert Rev Clin Immunol. 2012 Feb;8(2):123-33. doi: 10.1586/eci.11.95.
Glucocorticoids are indispensable for the treatment of systemic inflammatory diseases such as rheumatoid arthritis (RA), though their beneficial effects have to be balanced with potential complications arising from high doses, prolonged use or dose splitting. A glucocorticoid formulation (modified-release prednisone) has been developed to be taken in accordance with biological rhythms (chronotherapy). Morning symptoms of RA are caused by elevated nocturnal levels of proinflammatory cytokines, particularly IL-6. Endogenous cortisol levels may be insufficient to counter the inflammatory effects of IL-6. The early morning rise in cortisol can be supplemented with exogenous glucocorticoid replacement therapy if this is given as the recently developed chronotherapy formulation. There is no adverse impact of modified-release prednisone on the hypothalamic-pituitary-adrenal (HPA) axis; indeed, there might be evidence of a beneficial effect on HPA axis function. This review summarizes the development of modified-release prednisone, pharmacokinetic characteristics and clinical experience in patients with RA.
糖皮质激素在治疗全身性炎症性疾病（如类风湿关节炎）方面不可或缺，但为了平衡其疗效与大剂量、长期使用或分剂量使用相关的潜在并发症，需要采用适当的治疗方案。一种糖皮质激素制剂（控释泼尼松）已经根据生物节律（时间治疗学）开发出来，以便于使用。RA 的晨症是由夜间升高的促炎细胞因子（尤其是白细胞介素 6）引起的。内源性皮质醇水平可能不足以抵消白细胞介素 6 的炎症作用。如果使用最近开发的时间治疗学制剂给予外源糖皮质激素替代治疗，则可以补充外源性糖皮质激素替代治疗来补充清晨皮质醇的升高。控释泼尼松对下丘脑-垂体-肾上腺（HPA）轴没有不良影响；事实上，可能有证据表明对 HPA 轴功能有有益的影响。这篇综述总结了控释泼尼松的开发、药代动力学特征以及在 RA 患者中的临床应用经验。
