Department of Pharmacology, University of Arizona, Tucson, Arizona.
Department of Pharmacology, University of Arizona, Tucson, Arizona
Pharmacol Rev. 2021 Oct;73(4):98-126. doi: 10.1124/pharmrev.120.000046.
Pain prevalence among adults in the United States has increased 25% over the past two decades, resulting in high health-care costs and impacts to patient quality of life. In the last 30 years, our understanding of pain circuits and (intra)cellular mechanisms has grown exponentially, but this understanding has not yet resulted in improved therapies. Options for pain management are limited. Many analgesics have poor efficacy and are accompanied by severe side effects such as addiction, resulting in a devastating opioid abuse and overdose epidemic. These problems have encouraged scientists to identify novel molecular targets and develop alternative pain therapeutics. Increasing preclinical and clinical evidence suggests that cannabis has several beneficial pharmacological activities, including pain relief. contains more than 500 chemical compounds, with two principle phytocannabinoids, Δ-tetrahydrocannabinol (Δ-THC) and cannabidiol (CBD). Beyond phytocannabinoids, more than 150 terpenes have been identified in different cannabis chemovars. Although the predominant cannabinoids, Δ-THC and CBD, are thought to be the primary medicinal compounds, terpenes including the monoterpenes -myrcene, -pinene, limonene, and linalool, as well as the sesquiterpenes -caryophyllene and -humulene may contribute to many pharmacological properties of cannabis, including anti-inflammatory and antinociceptive effects. The aim of this review is to summarize our current knowledge about terpene compounds in cannabis and to analyze the available scientific evidence for a role of cannabis-derived terpenes in modern pain management. SIGNIFICANCE STATEMENT: Decades of research have improved our knowledge of cannabis polypharmacy and contributing phytochemicals, including terpenes. Reform of the legal status for cannabis possession and increased availability (medicinal and recreational) have resulted in cannabis use to combat the increasing prevalence of pain and may help to address the opioid crisis. Better understanding of the pharmacological effects of cannabis and its active components, including terpenes, may assist in identifying new therapeutic approaches and optimizing the use of cannabis and/or terpenes as analgesic agents.
美国成年人的疼痛患病率在过去二十年中增加了 25%,导致医疗保健成本高昂,并影响了患者的生活质量。在过去的 30 年中,我们对疼痛回路和(细胞内)机制的理解呈指数级增长,但这种理解尚未带来更好的治疗方法。疼痛管理的选择有限。许多镇痛药疗效不佳,并且伴随着严重的副作用,如成瘾,导致毁灭性的阿片类药物滥用和过量流行。这些问题促使科学家们确定新的分子靶点并开发替代疼痛治疗方法。越来越多的临床前和临床证据表明,大麻具有多种有益的药理活性,包括缓解疼痛。大麻含有超过 500 种化学物质,其中两种主要的植物大麻素是 Δ-四氢大麻酚(Δ-THC)和大麻二酚(CBD)。除了植物大麻素外,在不同的大麻化学品种中还鉴定出 150 多种萜烯。尽管主要的大麻素 Δ-THC 和 CBD 被认为是主要的药用化合物,但萜烯包括单萜 - 薄荷脑、- 蒎烯、柠檬烯和芳樟醇,以及倍半萜 - 石竹烯和 - 葎草烯,可能对大麻的许多药理特性有贡献,包括抗炎和抗伤害作用。本综述的目的是总结我们目前对大麻萜烯化合物的认识,并分析大麻衍生萜烯在现代疼痛管理中的作用的现有科学证据。意义声明:几十年来的研究提高了我们对大麻多药治疗和相关植物化学物质的认识,包括萜烯。大麻持有合法化地位的改革和可用性(药用和娱乐用)的增加导致了大麻的使用,以对抗日益普遍的疼痛,并可能有助于解决阿片类药物危机。更好地了解大麻及其活性成分(包括萜烯)的药理作用可能有助于确定新的治疗方法,并优化大麻和/或萜烯作为镇痛剂的使用。