Inoue K, Fujisawa H, Motonaga A, Inoue Y, Kyoi T, Ueda F, Kimura K
Research Laboratories, Nippon Shinyaku Co., Ltd., Kyoto, Japan.
Biol Pharm Bull. 1994 Dec;17(12):1577-83. doi: 10.1248/bpb.17.1577.
The anti-inflammatory effects of etodolac (Eto) were compared with those of 6 other anti-inflammatory drugs: indomethacin (Ind), diclofenac Na (Dic), piroxicam (Pir), naproxen (Nap), ketoprofen (Ket) and aspirin (Asp). Eto inhibited carrageenin-induced edema in rats, adjuvant-induced arthritis in rats, acetic acid-induced writhing in mice and brewer's yeast-induced hyperalgesia and fever in rats. In the adjuvant arthritis test, the ED30 value (1.88 mg/kg) on day 3 and ED50 values (adjuvant-injected paw: 1.18 mg/kg and non-injected paw: 0.96 mg/kg) on day 18 for Eto were comparable to those for Dic (2.16, 1.72 and 1.28) when given prophylactically and the ED50 values for Eto (adjuvant-injected paw: 1.61 and non-injected paw: 1.20 mg/kg) were comparable to those for Ket (1.24 and 1.22) when used therapeutically. The analgesic activity of Eto (ED50 value: 3.67 mg/kg) in the acetic acid-induced writhing test was greater than that of Nap (9.83) or Asp (31.6) and less than that of Ind (0.71), Dic (1.54), Pir (0.92) or Ket (1.34). In the antipyretic test, the minimum effective dose (MED: 1 mg/kg) for Eto was comparable to that for Ind (1.0), Nap (1.0) or Ket (1.0). Eto was less potent in inhibiting carrageenin-induced edema (ED30 value: 6.99 mg/kg) and inflammatory pain (ED50 value: 9.24 mg/kg) than the other drugs (Ind: 2.32 and 3.47, Dic: 0.69 and 3.80, Pir: 1.31 and 1.94, Nap: 1.83 and 2.78, Ket: 1.12 and 0.63), except for Asp (167 and 51.8).(ABSTRACT TRUNCATED AT 250 WORDS)
将依托度酸(Eto)的抗炎作用与其他6种抗炎药物进行了比较:吲哚美辛(Ind)、双氯芬酸钠(Dic)、吡罗昔康(Pir)、萘普生(Nap)、酮洛芬(Ket)和阿司匹林(Asp)。Eto可抑制角叉菜胶诱导的大鼠水肿、佐剂诱导的大鼠关节炎、醋酸诱导的小鼠扭体反应以及啤酒酵母诱导的大鼠痛觉过敏和发热。在佐剂性关节炎试验中,预防性给药时,Eto在第3天的ED30值(1.88mg/kg)和第18天的ED50值(注射佐剂的足爪:1.18mg/kg,未注射佐剂的足爪:0.96mg/kg)与Dic(2.16、1.72和1.28)相当;治疗性使用时,Eto的ED50值(注射佐剂的足爪:1.61mg/kg,未注射佐剂的足爪:1.20mg/kg)与Ket(1.24和1.22)相当。在醋酸诱导的扭体试验中,Eto的镇痛活性(ED50值:3.67mg/kg)大于Nap(9.83)或Asp(31.6),小于Ind(0.71)、Dic(1.54)、Pir(0.92)或Ket(1.34)。在解热试验中,Eto的最小有效剂量(MED:1mg/kg)与Ind(1.0)、Nap(1.0)或Ket(1.0)相当。Eto在抑制角叉菜胶诱导的水肿(ED30值:6.99mg/kg)和炎性疼痛(ED50值:9.24mg/kg)方面比其他药物(Ind:2.32和3.47,Dic:0.69和3.80,Pir:1.31和1.94,Nap:1.83和2.78,Ket:1.12和0.63)效力低,但Asp除外(167和51.8)。(摘要截短为250字)