Department of Anesthesiology, Leiden University Medical Center, Leiden, The Netherlands.
Division of Applied Regulatory Science, Center for Drug Evaluation and Research, U.S. Food and Drug Administration, Silver Spring, Maryland.
Anesthesiology. 2023 Sep 1;139(3):342-353. doi: 10.1097/ALN.0000000000004622.
Opioids are effective analgesics, but they can have harmful adverse effects, such as addiction and potentially fatal respiratory depression. Naloxone is currently the only available treatment for reversing the negative effects of opioids, including respiratory depression. However, the effectiveness of naloxone, particularly after an opioid overdose, varies depending on the pharmacokinetics and the pharmacodynamics of the opioid that was overdosed. Long-acting opioids, and those with a high affinity at the µ-opioid receptor and/or slow receptor dissociation kinetics, are particularly resistant to the effects of naloxone. In this review, the authors examine the pharmacology of naloxone and its safety and limitations in reversing opioid-induced respiratory depression under different circumstances, including its ability to prevent cardiac arrest.
阿片类药物是有效的镇痛药,但它们可能有有害的不良反应,如成瘾和潜在致命的呼吸抑制。纳洛酮是目前唯一可用于逆转阿片类药物的负面影响的治疗方法,包括呼吸抑制。然而,纳洛酮的有效性,特别是在阿片类药物过量后,取决于被过量的阿片类药物的药代动力学和药效学。长效阿片类药物,以及那些在μ-阿片受体上具有高亲和力和/或慢受体解离动力学的药物,对纳洛酮的作用特别有抵抗力。在这篇综述中,作者研究了纳洛酮的药理学及其在不同情况下逆转阿片类药物引起的呼吸抑制的安全性和局限性,包括其预防心脏骤停的能力。