Higher doses of naloxone are needed in the synthetic opiod era
Higher doses of naloxone are needed in the synthetic opiod era
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DOI：
10.1186/s13011-019-0195-4
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发表时间：
2019-02-18
影响因子：
3.3
通讯作者：
Carlo, Dennis J.
中科院分区：
文献类型：
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作者：
Moss, Ronald B.;Carlo, Dennis J.
由于非法芬太尼的死亡人数急剧增加。我们检查了芬太尼的药理学，并回顾了用于治疗芬太尼过量的纳洛酮重复剂量的数据。在一定比例的阿片类药物过量中，芬太尼需要多次连续剂量的纳洛酮。此外，芬太尼似乎与其他阿片类药物不同，因为在过量受害者中发现的全身性水平很高，起效非常快。纳洛酮需要快速竞争，才能在中枢神经系统中击败芬太尼占据的大量阿片受体。综上所述，我们建议需要更高剂量的纳洛酮来对抗由于芬太尼等更有效的合成阿片类药物而导致的新时代的过量。
There has been a dramatic increase of deaths due to illicit fentanyl. We examined the pharmacology of fentanyl and reviewed data on the number of repeat doses of naloxone used to treat fentanyl overdoses. Multiple sequential doses of naloxone have been required in a certain percentage of opioid overdoses due to fentanyl. In addition, fentanyl appears to differ from other opioids as having a very rapid onset with high systemic levels found in overdose victims. A rapid competition is required by naloxone to out-compete large numbers of opioid receptors occupied by fentanyl in the CNS. Taken together, we propose that higher doses of naloxone are needed to combat the new era of overdoses due to the more potent synthetic opioids such as fentanyl.