摘要:
阿片受体拮抗剂是一类特异性地拮抗阿片类激动剂的药物，能与激动剂竞争性地作用于阿片受体，从而降低或逆转激动剂的麻醉镇痛活性，并能消除因激动剂的使用所引起的呼吸抑制、胃肠功能紊乱等副作用。拮抗剂在临床上常作为镇痛药用量过度而产生的昏迷及副作用的解药。本论文主要综述了临床上常见的几种阿片受体拮抗剂的类型及临床应用，近年来，拮抗剂的应用取得较大发展，但仍存在一些不足，需进一步开展阿片受体拮抗剂的研究，以获得竞争性更强、副作用小，安全性高、合成工艺简单的专一性新型μ阿片受体拮抗剂，更好的应用于临床治疗。
Abstract: Opioid receptor antagonists are a class of specifically drugs for antagonizing the opioid on opioid receptors, thereby reducing or reversing the analgesic activity of narcotic agonists. Antagonists can also eliminate breathing suppression, gastrointestinal disorders and other side effects caused by the use of the agonist. Antagonists are used in clinic as side effects and coma antidote arising from excessive usage of analgesic. This paper summarizes several common clinical types of opioid receptor antagonists and clinical applications. In recent years, antagonists have achieved greater development, but there are still some deficiencies; further research of opioid receptor antagonists is needed to get more competitive, safer and simpler novel μ opioid receptor-specific antagonist, for better use in clinical treatment.