Joosten L A, Helsen M M, van den Berg W B
Department of Rheumatology, University Hospital Nijmegen, The Netherlands.
Agents Actions. 1990 Aug;31(1-2):135-42. doi: 10.1007/BF02003233.
We studied the effect of the local steroid preparation rimexolone on cartilage metabolism in arthritis and normal joints. Prolonged anti-inflammatory action was evident after intraarticular injection of a single dose of 450 micrograms into mice with monoarticular antigen-induced arthritis. Suppression of inflammation lasted for at least 21 days. A single dose of 25 micrograms of the anti-inflammatory steroid triamcinolone hexacetonide (THA) induced comparable suppression in the initial stage of the arthritis, but the suppressive action was of shorter duration. Both drugs significantly prevented osteophyte formation, which is a characteristic feature of this type of experimental arthritis. Although chondrocyte proteoglycan (PG) synthesis in patellar cartilage was significantly suppressed upon injection in normal joints, both steroids counteracted the severe suppression of PG synthesis in arthritic joints. These data indicate that although steroids may have significant side effects on chondrocytes, the overall effect on arthritic chondrocytes is beneficial. An advantage of rimexolone over THA is its prolonged retention, which may explain its sustained anti-inflammatory action, and the lack of systemic effects.
我们研究了局部用类固醇制剂瑞美索龙对关节炎关节和正常关节软骨代谢的影响。在单关节抗原诱导性关节炎小鼠中，关节腔内注射单剂量450微克后，明显出现了持久的抗炎作用。炎症抑制持续了至少21天。单剂量25微克的抗炎类固醇曲安奈德（THA）在关节炎初期诱导了类似的抑制作用，但抑制作用持续时间较短。两种药物均显著预防了骨赘形成，这是此类实验性关节炎的一个特征。尽管在正常关节注射后，髌软骨中的软骨细胞蛋白聚糖（PG）合成受到显著抑制，但两种类固醇都抵消了关节炎关节中PG合成的严重抑制。这些数据表明，尽管类固醇可能对软骨细胞有显著副作用，但对关节炎软骨细胞的总体影响是有益的。瑞美索龙相对于THA的一个优势是其保留时间延长，这可能解释了其持续的抗炎作用以及缺乏全身效应。
