STUDIES OF ANALGESIC DRUGS. VIII. A NARCOTIC ANTAGONIST ANALGESIC WITHOUT PSYCHOTOMIMETIC EFFECTS.
STUDIES OF ANALGESIC DRUGS. VIII. A NARCOTIC ANTAGONIST ANALGESIC WITHOUT PSYCHOTOMIMETIC EFFECTS.
复制标题
镇痛药物的研究。
DOI：
10.1097/00132586-196504000-00022
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发表时间：
1964
期刊：
影响因子：
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通讯作者：
Louis R. Orkin
中科院分区：
文献类型：
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作者：
A. Keats;J. Telford;Louis R. Orkin
弱麻醉性拮抗剂29-羟基-5，9-二甲基-2-（3，3-二甲基烯丙基）-6，7-苯并吗喃（Win 20，228）对术后疼痛的镇痛作用，10-20 mg/70 kg Win 20，228与10 mg/70 kg吗啡相当。20 mg/70 kg Win 20，228产生的呼吸抑制程度与10 mg/70 kg吗啡相当。Win 20，228的主观效应在定性和定量上与吗啡相似。除了一名患者报告了“疯狂的想法”外，在其他患者或健康受试者中未观察到纳洛啡样拟精神病作用。Win 20，228对吗啡引起的呼吸抑制作用弱，而其呼吸抑制作用不被强麻醉性拮抗剂所拮抗。与吗啡相反，Win 20，228在剂量大于2 mg/kg时静脉注射产生心动过速和高血压。Win 20，228可能是第一个临床上有用的强效镇痛药，成瘾倾向最小。
The effects of 29-hydroxy-5,9-dimethyl-2-(3,3-dimethylallyl)-6,7-benzomorphan (Win 20,228) a weak narcotic antagonist, have been studied in man. In the treatment of postoperative pain 10-20 mg/70 kg of Win 20,228 produced analgesia equivalent to 10 mg/70 kg of morphine. The degree of respiratory depression produced by 20 mg/70 kg of Win 20,228 was comparable to that of 10 mg/70 kg of morphine. The subjective effects of Win 20,228 were qualitatively and quantitatively similar to those of morphine. Except for one patient who reported "crazy thoughts," nalorphine-like psychotomimetic effects were not observed in other patients or healthy subjects. Win 20,228 was shown to be a weak antagonist of morphine induced respiratory depression and the respiratory depression of Win 20,228 was not antagonized by potent narcotic antagonists. In contrast to morphine, Win 20,228 in doses greater than 2 mg/kg intravenously produced tachycardia and hypertension. Win 20,228 may represent the first clinically useful potent analgesic with minimal addiction liability.