Fujimoto K, Momose T
Department of Anesthesiology, Nagoya National Hospital.
Masui. 1995 Sep;44(9):1233-7.
Studies were carried out to elucidate the efficacy and safety of E2078, a metabolically stable dynorphin analog, in patients with severe pain following lower abdominal surgery. E2078 was administered intramuscularly in a single dose of 1 to 15 mg. The efficacy was determined by evaluating the pain intensity score (PI) and global improvement rating (GIR) by the investigator. E2078 exhibited analgesic effect at doses of 10 mg or more. At the dose of 10 mg (n = 24). PI decreased from 3.0 to 1.3, and GIR was 83%. When the dose was increased to 12.5 mg (n = 15), PI improved from 3.0 to 1.3, and GIR was 100%. The improvement in PI, GIR and the duration of efficacy were 3.0 to 0.8, 100% and 6 hours 40 minutes with E2078 15 mg (n = 10), respectively. E2078 did not produce any adverse effects at doses of up to 15 mg. The results of the present study indicate that E2078 begins to exhibit analgesic effect at a dose of 10 mg, and at 15 mg its effect is comparable to that of pentazocine 15 mg.
开展了多项研究，以阐明代谢稳定的强啡肽类似物E2078在接受下腹部手术后出现严重疼痛的患者中的疗效和安全性。E2078通过肌肉注射给药，单次剂量为1至15毫克。疗效由研究者通过评估疼痛强度评分（PI）和整体改善评级（GIR）来确定。E2078在10毫克及以上剂量时表现出镇痛作用。在10毫克剂量时（n = 24），PI从3.0降至1.3，GIR为83%。当剂量增加到12.5毫克时（n = 15），PI从3.0改善至1.3，GIR为100%。使用15毫克E2078时（n = 10），PI、GIR的改善情况以及疗效持续时间分别为从3.0至0.8、100%和6小时40分钟。E2078在高达15毫克的剂量下未产生任何不良反应。本研究结果表明，E2078在10毫克剂量时开始表现出镇痛作用，在15毫克剂量时其效果与15毫克喷他佐辛相当。
