Department of Pharmacy Practice, Harrison School of Pharmacy, Auburn University, Auburn, Alabama, USA.
J Clin Pharmacol. 2022 May;62(5):577-593. doi: 10.1002/jcph.2001. Epub 2022 Jan 5.
Kratom (Mitragyna speciosa) consists of over 40 alkaloids, with 2 of them, mitragynine and 7-OH-mitragynine (7-OH-MG) being the main psychoactive compounds. Mitragynine and 7-OH-mitragynine each target opioid receptors and have been referred to as atypical opioids. They exert their pharmacologic effects on the mu, delta, and kappa opioid receptors. In addition, they affect adrenergic, serotonergic, and dopaminergic pathways. Kratom has been touted as an inexpensive, legal alternative to standard opioid replacement therapy such as methadone and buprenorphine. Other uses for kratom include chronic pain, attaining a "legal high," and numerous central nervous system disorders, including anxiety, depression, and posttraumatic stress disorder. Kratom induces analgesia and mild euphoria, with a lower risk of respiratory depression or adverse central nervous system effects compared to traditional opioid medications. Nonetheless, kratom has been associated with both physical and psychological dependence, with some individuals experiencing classic opioid withdrawal symptoms upon abrupt cessation. Kratom use has been linked to serious adverse effects, including liver toxicity, seizures, and death. These risks are often compounded by polysubstance abuse. Further, kratom may potentiate the toxicity of coadministered medications through modulation of cytochrome P450, P-glycoprotein, and uridine diphosphate glucuronosyltransferase enzymes. In 2016, the US Drug Enforcement Administration took steps to classify kratom as a federal schedule 1 medication; however, due to public resistance, this plan was set aside. Until studies are conducted that define kratom's role in treating opioid withdrawal and/or other central nervous system conditions, kratom will likely remain available as a dietary supplement for the foreseeable future.
译文：咔特（Mitragyna speciosa）包含超过 40 种生物碱，其中 2 种，即Mitragynine和 7-羟基-Mitragynine（7-OH-MG）是主要的精神活性化合物。Mitragynine和 7-羟基-Mitragynine 分别靶向阿片受体，并被称为非典型阿片类药物。它们对μ、δ和κ阿片受体发挥药理作用。此外，它们还影响肾上腺素能、血清素能和多巴胺能途径。咔特被吹捧为一种廉价的、合法的替代标准阿片类药物替代疗法，如美沙酮和丁丙诺啡。咔特的其他用途包括慢性疼痛、获得“合法快感”以及许多中枢神经系统疾病，包括焦虑、抑郁和创伤后应激障碍。咔特诱导镇痛和轻度欣快，与传统阿片类药物相比，呼吸抑制或不良中枢神经系统作用的风险较低。尽管如此，咔特与身体和心理依赖都有关联，一些人在突然停药时会出现典型的阿片类药物戒断症状。咔特的使用与严重的不良反应有关，包括肝毒性、癫痫发作和死亡。这些风险通常因多物质滥用而加剧。此外，咔特可能通过调节细胞色素 P450、P-糖蛋白和尿苷二磷酸葡萄糖醛酸转移酶来增强联合用药的毒性。2016 年，美国缉毒局采取措施将咔特列为联邦附表 1 药物；然而，由于公众的反对，该计划被搁置。在进行定义咔特在治疗阿片类药物戒断和/或其他中枢神经系统疾病方面的作用的研究之前，咔特在可预见的未来可能仍然作为膳食补充剂供应。
