• 第15卷第2期

Buprenorphine Pivalate Has a Long-acting Antinociceptive Effects in Rats


台灣疼痛醫學雜誌第15卷第2期(2005-09-01)
 高振興(Cheng-Hsing Kao);劉巡宇(Shyun-Yeu Liu);郭珍妮(Jenny Que);林立青(Li-Ching Lin);鄭伯智(Bor-Chin Cheng);陳柄仁(Bing-Ren Chan);謝介平(Ja-Ping Shieh)
摘要
A long-acting analgesic is particularly desirable in patients with long-term pain. This study evaluates the antinociceptive effect and duration of action of a novel buprenorphine ester-buprenorphine pivalate-and shows whether this ester has a long-acting effect. The antinociceptive effects of buprenorphine HCl and pivalate were evaluated by using the plantar test in male Sprague-Dawley rats. We found that intramuscular injection of buprenorphine HCl 0.03, 0.1, and 0.3痠ol/kg in rats produced dose-related antinociceptive effects of 2, 3, and 4h, respectively. Intramuscular injection of buprenorphine pivalate 0.3, 3, and 30痠ol/kg also produced dose-related antinociceptive effects, but with longer durations of action of 48, 52 and 54h. Under an equi-molar basis of 0.3痠ol/kg, the durations of action of intramuscular buprenorphine HCl and buprenorphine pivalate were 4 and 48h, respectively. We conclude that intramuscular injection of buprenorphine pivalate produced a long-lasting antinociceptive effect which was much longer (12-fold) than intramuscular buprenorphine HCl.
並列摘要
患有長時間疼痛的病患皆應希望能有一個具長效作用的止痛劑來解除疼痛。為了延長一個強效止痛劑Buprenorphine之藥效,我們合成了一個Buprenorphine酯即三甲基乙酸Buprenorphine酯,本研究的目的在評估這個酯是否具有長效作用。使用雄性SD大白鼠以縮腳掌反射來測試Buprenorphine及其酯類之止痛作用,發現在大白鼠肌肉注射Buprenorphine HCl 0.03,0.01及0.3µmol/kg可產生2、3及4小時之止痛作用。而肌肉注射三甲基乙酸Buprenorphine酯0.3,3及30µmol/kg可產生較長效的止痛作用,達48、52及54小時。在相同的給藥劑量下(0.3µmol/kg),Buprenorphine HCl及三甲基乙酸Buperenorphine酯之止痛效期分別為4及48小時。我們作以下結論,在大鼠肌肉注射三甲基乙酸Buprenorphine酯可產生一個非常長的止痛作用,其效果為Buprenorphine HCl的12倍。

 

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