新型免疫抑制剂来氟米特药效学实验研究

Pharmacodynamic study of leflunomide——a new immunosuppressant

为验证来氟米特 (L FM)的免疫抑制作用 ,应用 BAL B/ C小鼠自身溶血性贫血、Wistar大鼠佐剂性关节炎及 C5 7BL / 6 - >BAL B/ C小鼠心肌移植模型 ,观察了 L FM对抗自身红细胞抗体产生、炎症及移植排斥反应的预防和治疗作用。结果表明 :(1) L FM 10 mg/ kg预防给药可明显抑制抗自身红细胞抗体的产生 ,治疗组 30 mg/ kg可使升高的自身抗体水平显著降低 ;(2 ) L FM 10、2 0 mg/ kg预防给药可显著抑制关节的原发和继发性肿胀 ,2 0 mg/ kg治疗给药可使已肿胀的关节显著消退 ;(3) L FM 2 0 mg/ kg可使小鼠心肌移植存活时间显著延长。实验证明 L FM在自身免疫病和器官移植等方面均具有良好的免疫抑制作用。

Experimental autoimmune haemolytic anaemia in BALB/C mice, adjuvant arthritis in Wistar rats and murine split heart transplantation model from C57BL/6 to BALB/C mice were used to evaluate the immunosuppressive effects of leflunomide (LFM). Three aspects of results have been obtained. (1) LFM 10mg/kg/day effectively prevented the production of anti erythrocyte auto antibodies and the treatment of LFM 30mg/(kg·day) led to a remarkable depression of the raised autoantibodies level. (2) 10 and 20mg/(kg·day) of LFM significantly inhibited the primary and secondary paw edema of the arthritis rats and LFM 20mg/(kg·day) reduced the paw edema of the established adjuvant arthrisis. (3) LFM 20mg/(kg·day) significantly prolonged the survival time of split transplanted hearts. In conclusion, LFM showed good immunesuppressive effects in autoimmune diseases and organ transplantation in mice and rats.