类阿片
止痛药
不利影响
背景(考古学)
癌症疼痛
上瘾
医学
重症监护医学
麻醉
镇静
慢性疼痛
芬太尼
药理学
精神科
癌症
内科学
受体
古生物学
生物
作者
M. T. Smith,Dehui Kong,Andy Kuo,Mohammad Zafar Imam,Craig M. Williams
标识
DOI:10.1021/acs.jmedchem.0c01915
摘要
Strong opioid analgesics, including morphine, are the mainstays for treating moderate to severe acute pain and alleviating chronic cancer pain. However, opioid-related adverse effects, including nausea or vomiting, sedation, respiratory depression, constipation, pruritus (itch), analgesic tolerance, and addiction and abuse liability, are problematic. In addition, the use of opioids to relieve chronic noncancer pain is controversial due to the "opioid crisis" characterized by opioid misuse or abuse and escalating unintentional death rates due to respiratory depression. Hence, considerable research internationally has been aimed at the "Holy Grail" of the opioid analgesic field, namely the discovery of novel and safer opioid analgesics with improved opioid-related adverse effects. In this Perspective, medicinal chemistry strategies are addressed, where structurally diverse nonmorphinan-based opioid ligands derived from natural sources were deployed as lead molecules. The current state of play, clinical or experimental status, and novel opioid ligand discovery approaches are elaborated in the context of retaining analgesia with improved safety and reduced adverse effects, especially addiction liability.
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