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啮齿动物实验性地西泮中毒:毒扁豆碱和纳洛酮作为潜在拮抗剂

Experimental diazepam intoxication in rodents: physostigmine and naloxone as potential antagonists.

作者信息

Walz M A, Davis W M

出版信息

Drug Chem Toxicol. 1979;2(3):257-67. doi: 10.3109/01480547908998247.

DOI:10.3109/01480547908998247
PMID:546626
Abstract

The ability of physostigmine and naloxone to reverse the loss of righting reflex (LRR) induced by diazepam was tested in mice and rats. Physostigmine was ineffective under our test conditions, but high doses of naloxone reduced the duration of LRR in both species. However, the LD50 of diazepam in mice was unaltered by 100 or 150 mg/kg of naloxone given 1 hr after LRR to model an antidotal situation. Use of a longer duration narcotic antagonist, naltrexone (172 mg/kg), in the same design likewise failed to elevate the LD50 for diazepam. These data give limited support to prior suggestions for clinical usefulness of naloxone, although not for physostigmine, in the management of intoxication caused by diazepam.

摘要

在小鼠和大鼠中测试了毒扁豆碱和纳洛酮逆转地西泮诱导的翻正反射丧失(LRR)的能力。在我们的测试条件下毒扁豆碱无效,但高剂量的纳洛酮缩短了两种动物的LRR持续时间。然而,在LRR后1小时给予100或150mg/kg纳洛酮以模拟解毒情况,小鼠地西泮的半数致死量(LD50)未改变。在相同设计中使用作用时间更长的麻醉拮抗剂纳曲酮(172mg/kg)同样未能提高地西泮的LD50。这些数据为先前关于纳洛酮(而非毒扁豆碱)在处理地西泮中毒方面临床实用性的建议提供了有限支持。

相似文献

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Experimental diazepam intoxication in rodents: physostigmine and naloxone as potential antagonists.啮齿动物实验性地西泮中毒:毒扁豆碱和纳洛酮作为潜在拮抗剂
Drug Chem Toxicol. 1979;2(3):257-67. doi: 10.3109/01480547908998247.
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Effects of physostigmine on benzodiazepine toxicity.毒扁豆碱对苯二氮䓬类药物毒性的影响。
Arch Int Pharmacodyn Ther. 1981 Sep;253(1):164-76.
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Intracerebroventricular physostigmine-induced analgesia: enhancement by naloxone, beta-funaltrexamine and nor-binaltorphimine and antagonism by dynorphin A (1-17).
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Interactions of cholinesterase inhibitors and corticosteroids with the hypnotic effect of benzodiazepines in mice.胆碱酯酶抑制剂和皮质类固醇与苯二氮䓬类药物对小鼠催眠作用的相互作用。
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Failure of naloxone or physostigmine to reverse nitrogen anesthesia in guinea pigs.纳洛酮或毒扁豆碱未能逆转豚鼠的氮气麻醉。
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Lack of physostigmine-diazepam antagonism.毒扁豆碱与地西泮无拮抗作用。
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Physostigmine: effectiveness as an antagonist of respiratory depression and psychomotor effects caused by morphine or diazepam.毒扁豆碱:作为吗啡或地西泮所致呼吸抑制及精神运动效应拮抗剂的有效性。
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Physostigmine, a highly potent antidote for acute experimental diazepam intoxication.毒扁豆碱,一种用于急性实验性地西泮中毒的高效解毒剂。
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Toxic interaction between choline and morphine.胆碱与吗啡之间的毒性相互作用。
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New and experimental therapeutic roles for naloxone and related opioid antagonists.纳洛酮及相关阿片类拮抗剂的新治疗作用与实验性治疗作用
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