摘要
阿片受体激动-拮抗剂是一类对阿片受体兼有激动和拮抗作用的药物。已经上市的这类药物主要包括喷他佐辛、布托啡诺、纳布啡、丁丙诺啡和地佐辛等。与吗啡、芬太尼等单纯阿片受体激动剂相比,该类药物具有镇痛效果较强,成瘾性较弱,咳嗽、瘙痒以及呼吸抑制等副作用少的优点。由于阿片受体激动-拮抗剂在不同内源性阿片受体(μ、κ、δ等)间具有不同的倾向性作用,基于不同受体亚型,可在情绪影响、药物依赖方面表现出不同甚至相反的作用,因此合理地使用这类药物可以有效地减少阿片类药物导致的不良反应以及药物滥用的发生。随着学界对内源性阿片各受体亚型及相关药物研究的深入,阿片受体激动-拮抗剂在改善阿片类药物不良反应和提高患者药物依从性方面有着广泛的应用空间和前景。
Opioid receptor agonist-antagonists are a class of drugs which have both agonistic and antagonistic effects on opioid receptors.These drugs already on the market mainly include pentazocine,butorphanol,nalbuphine,buprenorphine,dezocine and so on.Compared with pure opioid receptor agonists such as morphine and fentanyl,these drugs have strong analgesic effects,less addictive,and less side effects such as cough,itching and respiratory depression.Due to the different tendentious effects of opioid receptor agonists-antagonists among different endogenous opioid receptors(μ,κ,δ,etc.),different receptors of subtypes can exhibit different or even opposite effects in terms of affecting emotions and drug dependence.Therefore,the rational use of these drugs can effectively reduce the occurrence of adverse reactions and drug abuse caused by opioid drugs.With the deepening of research on various endogenous opioid receptor subtypes and related drugs in the academic community,opioid receptor agonistsantagonists have broad application space and prospects in improving adverse reactions to opioid drugs and enhancing patient drug compliance.
作者
陈泽权
肖国伟
敖健
蒋为薇
CHEN Zequan;XIAO Guowei;AO Jian;JIANG Weiwei(Dept.of Orthopaedics,Wushan County Hospital of Traditional Chinese Medicine,Chongqing 404700,China;Dept.of Pharmacy,the Second Affiliated Hospital of Chongqing Medical University,Chongqing 400010,China)
出处
《中国药房》
CAS
北大核心
2023年第18期2299-2304,共6页
China Pharmacy
基金
白求恩公益基金会“2022白求恩·求索-药学科研能力建设”项目(No.X2023-206)。
关键词
阿片受体激动-拮抗剂
内源性阿片受体
镇痛
不良反应
opioid receptor agonists-antagonists
endogenous opioid receptors
analgesia
adverse drug reactions
