Centre for Evidence-Based Medicine, Nuffield Department of Primary Care Health Sciences, University of Oxford, Radcliffe Observatory Quarter, Woodstock Road, Oxford, OX2 6GG, UK.
Oxford Medical School, John Radcliffe Hospital, University of Oxford, Oxford, OX3 9DU, UK.
Br J Clin Pharmacol. 2021 Oct;87(10):3790-3812. doi: 10.1111/bcp.14786. Epub 2021 Mar 20.
The growing demand for analgesia, coupled with an increasing need to treat opioid dependence and overdose, has escalated the development of novel opioids. We aimed to quantify the number of opioid drugs developed and to catalogue them based on their pharmacology.
We conducted a systematic search of seven sources in November 2020, including the WHO's Anatomical Therapeutic Classification index, the British National Formulary, the IUPHAR/BPS Guide to Pharmacology, the International Narcotics Control Board Index of Names of Narcotic Drugs, the WHO's International Nonproprietary Names MedNet service, Martindale's Extra Pharmacopoeia and the Merck Index, to include opioid drugs that targeted or had an effect or coeffect at one or more opioid receptors. We extracted chemical and nonproprietary names, drug stems, molecular formulas, molecular weights, receptor targets, actions at opioid receptors and classes based on their origins. We used descriptive statistics and calculated medians and interquartile ranges where appropriate.
We identified 233 opioid drugs and created an online resource (https://www.catalogueofopioids.net/). There were 10 unique drug stems, and "-fentanil" accounted for one-fifth (20%) of all opioids. Most of the drugs (n = 133) targeted mu-opioid receptors and the majority (n = 191) were agonists at one or more receptors. Most (82%) were synthetic opioids, followed by semisynthetic opioids (16%) and alkaloids (3%).
This catalogue centralizes and disseminates information that could assist researchers, prescribers and the public to improve the safe use of opioids.
镇痛需求不断增长,加上治疗阿片类药物依赖和过量的需求不断增加,推动了新型阿片类药物的发展。本研究旨在量化已开发的阿片类药物数量,并根据其药理学对其进行分类。
我们于 2020 年 11 月对七个来源进行了系统检索,包括世界卫生组织的解剖治疗学药物分类索引、英国国家处方集、国际药理学联合会/英国药理学学会药物指南、国际麻醉品管制局麻醉品名称索引、世界卫生组织国际非专利名称 MedNet 服务、马廷代尔额外药典和默克索引,以纳入针对或对一个或多个阿片受体具有作用或协同作用的阿片类药物。我们提取了化学名称和非专利名称、药物词干、分子式、分子量、受体靶点、阿片受体作用和起源分类。我们使用描述性统计和适当的中位数和四分位间距计算。
我们确定了 233 种阿片类药物,并创建了一个在线资源(https://www.catalogueofopioids.net/)。有 10 个独特的药物词干,其中“-fentanil”占所有阿片类药物的五分之一(20%)。大多数药物(n=133)靶向μ-阿片受体,大多数(n=191)药物在一个或多个受体上是激动剂。大多数(82%)是合成阿片类药物,其次是半合成阿片类药物(16%)和生物碱(3%)。
该目录集中并传播了信息,可帮助研究人员、处方者和公众提高阿片类药物的安全使用。