Glab W N, Corby D G, Decker W J, Coldiron V R
J Toxicol Clin Toxicol. 1982 Apr;19(2):129-38. doi: 10.3109/15563658208990375.
In 1968 we first suggested that activated charcoal (AC) should be administered in the emergency treatment of propoxyphene overdosage. The dramatic increase in recent years of deaths involving propoxyphene has prompted us to again evaluate the efficacy of AC in preventing absorption of propoxyphene from the GI tract. Male rats (100-125 g) were administered propoxyphene hydrochloride (P-HCl, 350 mg/kg) or propoxyphene napsylate (P-N, 825 mg/kg) either dissolved or suspended in 5% acacia in H2O. After 30 min the rats were administered either AC at 10 times the drug dose or water. Surviving rats were sacrificed at 1, 2, 4, 8, 12, and 24 h; the brain, liver, and both kidneys were removed intact, weighed, and stored at -70 degrees C. After lyophilization, the tissues were analyzed for propoxyphene and its metabolite, norpropoxyphene, by GLC. There were significantly less deaths in rats that received P-HCl + AC or P-N + AC than rats that received either P-HCl or P-N alone (9 vs 19, p less than .01 and 5 vs 10, p less than .05 respectively). Tissue levels of propoxyphene and norpropoxyphene were similarly significantly reduced. These studies provide further evidence of the efficacy of AC in propoxyphene overdosage.
1968年,我们首次提出在丙氧芬过量的紧急治疗中应使用活性炭(AC)。近年来,涉及丙氧芬的死亡人数急剧增加,这促使我们再次评估AC在预防丙氧芬从胃肠道吸收方面的效果。将雄性大鼠(100 - 125克)给予盐酸丙氧芬(P - HCl,350毫克/千克)或萘磺酸丙氧芬(P - N,825毫克/千克),它们分别溶解或悬浮于5%阿拉伯胶的水溶液中。30分钟后,给大鼠给予药物剂量10倍的AC或水。存活的大鼠在1、2、4、8、12和24小时处死;完整取出脑、肝和双肾,称重并储存在 - 70摄氏度。冻干后,通过气相色谱法分析组织中的丙氧芬及其代谢物去甲丙氧芬。接受P - HCl + AC或P - N + AC的大鼠死亡数明显少于单独接受P - HCl或P - N的大鼠(分别为9只对19只,p <.01;5只对10只,p <.05)。丙氧芬和去甲丙氧芬的组织水平同样显著降低。这些研究进一步证明了AC在丙氧芬过量治疗中的有效性。