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鼠尾草叶大麻酚A的药代动力学与药效学:临床与法医学方面

Pharmacokinetics and Pharmacodynamics of Salvinorin A and : Clinical and Forensic Aspects.

作者信息

Brito-da-Costa Andreia Machado, Dias-da-Silva Diana, Gomes Nelson G M, Dinis-Oliveira Ricardo Jorge, Madureira-Carvalho Áurea

机构信息

IINFACTS-Institute of Research and Advanced Training in Health Sciences and Technologies, Department of Sciences, University Institute of Health Sciences (IUCS), CESPU, CRL, 4585-116 Gandra, Portugal.

UCIBIO-REQUIMTE, Laboratory of Toxicology, Department of Biological Sciences, Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal.

出版信息

Pharmaceuticals (Basel). 2021 Feb 3;14(2):116. doi: 10.3390/ph14020116.

Abstract

Epling and Játiva is a perennial mint from the Lamiaceae family, endemic to Mexico, predominantly from the state of Oaxaca. Due to its psychoactive properties, had been used for centuries by Mazatecans for divinatory, religious, and medicinal purposes. In recent years, its use for recreational purposes, especially among adolescents and young adults, has progressively increased. The main bioactive compound underlying the hallucinogenic effects, salvinorin A, is a non-nitrogenous diterpenoid with high affinity and selectivity for the k-opioid receptor. The aim of this work is to comprehensively review and discuss the toxicokinetics and toxicodynamics of and salvinorin A, highlighting their psychological, physiological, and toxic effects. Potential therapeutic applications and forensic aspects are also covered in this review. The leaves of can be chewed, drunk as an infusion, smoked, or vaporised. Absorption of salvinorin A occurs through the oral mucosa or the respiratory tract, being rapidly broken down in the gastrointestinal system to its major inactive metabolite, salvinorin B, when swallowed. Salvinorin A is rapidly distributed, with accumulation in the brain, and quickly eliminated. Its pharmacokinetic parameters parallel well with the short-lived psychoactive and physiological effects. No reports on toxicity or serious adverse outcomes were found. A variety of therapeutic applications have been proposed for which includes the treatment of chronic pain, gastrointestinal and mood disorders, neurological diseases, and treatment of drug dependence. Notwithstanding, there is still limited knowledge regarding the pharmacology and toxicology features of and salvinorin A, and this is needed due to its widespread use. Additionally, the clinical acceptance of salvinorin A has been hampered, especially due to the psychotropic side effects and misuse, turning the scientific community to the development of analogues with better pharmacological profiles.

摘要

埃普林鼠尾草是一种来自唇形科的多年生薄荷,原产于墨西哥,主要分布在瓦哈卡州。由于其具有精神活性,马萨特克人已经使用了几个世纪,用于占卜、宗教和药用目的。近年来,其在娱乐用途上的使用,尤其是在青少年和年轻人中,逐渐增加。致幻作用的主要生物活性化合物——Salvinorin A,是一种对κ-阿片受体具有高亲和力和选择性的非含氮二萜。这项工作的目的是全面回顾和讨论埃普林鼠尾草和Salvinorin A的毒代动力学和毒效动力学,突出它们的心理、生理和毒性作用。本综述还涵盖了潜在的治疗应用和法医方面。埃普林鼠尾草的叶子可以咀嚼、冲泡饮用、吸食或汽化。Salvinorin A通过口腔黏膜或呼吸道吸收,吞咽时在胃肠道系统中迅速分解为其主要无活性代谢物Salvinorin B。Salvinorin A迅速分布,在大脑中积累,并迅速消除。其药代动力学参数与短暂的精神活性和生理效应良好平行。未发现关于毒性或严重不良后果的报告。已经提出了埃普林鼠尾草的多种治疗应用,包括治疗慢性疼痛、胃肠道和情绪障碍、神经疾病以及药物依赖的治疗。尽管如此,关于埃普林鼠尾草和Salvinorin A的药理学和毒理学特征的知识仍然有限,鉴于其广泛使用,这是必要的。此外,Salvinorin A的临床接受度受到阻碍,特别是由于其精神副作用和滥用,促使科学界开发具有更好药理学特征的类似物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9a08/7913753/cf4fed50d2e0/pharmaceuticals-14-00116-g001.jpg

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