Kim Hong K, Nelson Lewis S
University of Maryland School of Medicine, Department of Emergency Medicine , 110 South Paca St. 6th Floor, STE 200, Baltimore, MD 21201 , USA +1 415 846 8995 ; +1 410 328 8028 ;
Expert Opin Drug Saf. 2015 Jul;14(7):1137-46. doi: 10.1517/14740338.2015.1037274. Epub 2015 Apr 12.
Opioid overdose fatality has increased threefold since 1999. As a result, prescription drug overdose surpassed motor vehicle collision as the leading cause of unintentional injury-related death in the USA. Naloxone , an opioid antagonist that has been available for decades, can safely reverse opioid overdose if used promptly and correctly. However, clinicians often overestimate the dose of naloxone needed to achieve the desired clinical outcome, precipitating acute opioid withdrawal syndrome (OWS).
This article provides a comprehensive review of naloxone's pharmacologic properties and its clinical application to promote the safe use of naloxone in acute management of opioid intoxication and to mitigate the risk of precipitated OWS. Available clinical data on opioid-receptor kinetics that influence the reversal of opioid agonism by naloxone are discussed. Additionally, the legal and social barriers to take home naloxone programs are addressed.
Naloxone is an intrinsically safe drug, and may be administered in large doses with minimal clinical effect in non-opioid-dependent patients. However, when administered to opioid-dependent patients, naloxone can result in acute opioid withdrawal. Therefore, it is prudent to use low-dose naloxone (0.04 mg) with appropriate titration to reverse ventilatory depression in this population.
自1999年以来，阿片类药物过量致死率增长了两倍。因此，在美国，处方药过量已超过机动车碰撞，成为非故意伤害相关死亡的首要原因。纳洛酮作为一种已上市数十年的阿片类拮抗剂，如果及时、正确使用，能够安全地逆转阿片类药物过量。然而，临床医生常常高估实现预期临床效果所需的纳洛酮剂量，从而引发急性阿片戒断综合征（OWS）。
本文全面综述了纳洛酮的药理特性及其临床应用，以促进纳洛酮在阿片类药物中毒急性处理中的安全使用，并降低引发OWS的风险。文中讨论了影响纳洛酮逆转阿片激动作用的阿片受体动力学的现有临床数据。此外，还探讨了纳洛酮带回家计划面临的法律和社会障碍。
纳洛酮本质上是一种安全的药物，在非阿片类药物依赖患者中，大剂量使用时临床效应极小。然而，在阿片类药物依赖患者中使用时，纳洛酮可能导致急性阿片戒断。因此，对于这类人群，谨慎的做法是使用低剂量纳洛酮（0.04毫克）并进行适当滴定，以逆转呼吸抑制。
