Egsmose C, Lund B, Andersen R B
Department of Rheumatology, Hvidovre Hospital, Denmark.
Scand J Rheumatol. 1988;17(2):103-11. doi: 10.3109/03009748809098769.
Timegadine is a tri-substituted guanidine derivative which inhibits both arachidonate cyclo-oxygenase and lipoxygenase activity. In a 24-week randomized double-blind controlled trial, timegadine 500 mg/day was compared with naproxen 750 mg/day in two groups of 20 patients with active rheumatoid arthritis. In the timegadine group, significant improvements were seen in both biochemical and clinical markers of disease activity, i.e. ESR, serum IgG and IgM, leukocyte and platelet counts, duration of morning stiffness, Ritchie index, number of swollen joints, pain, and general condition. In the naproxen group, only the Ritchie index improved. Differences between treatments, when present, were always in favour of timegadine. Serum alkaline phosphatase rose during the first 8 weeks of treatment in the timegadine group. A transient rise was also seen in the naproxen group. The side effects reported were mainly gastrointestinal and allergic, the latter being more frequently found in the timegadine group. Timegadine is superior to naproxen in controlling disease activity in rheumatoid arthritis, and appears to possess disease-modifying properties.
替美加定是一种三取代胍衍生物，可抑制花生四烯酸环氧化酶和脂氧化酶的活性。在一项为期24周的随机双盲对照试验中，将两组各20例活动性类风湿性关节炎患者分别给予每日500毫克替美加定和每日750毫克萘普生进行比较。在替美加定组中，疾病活动的生化和临床指标均有显著改善，即血沉、血清免疫球蛋白G和M、白细胞和血小板计数、晨僵持续时间、里奇指数、关节肿胀数、疼痛及总体状况。在萘普生组中，仅里奇指数有所改善。治疗之间的差异（若存在）总是有利于替美加定。在替美加定组治疗的前8周血清碱性磷酸酶升高。萘普生组也出现短暂升高。报告的副作用主要是胃肠道和过敏方面的，后者在替美加定组中更常见。在控制类风湿性关节炎的疾病活动方面，替美加定优于萘普生，且似乎具有改善病情的特性。
