抗抑郁药物的手性:立体选择性综述。

IF 0.4 4区 医学 Q4 MEDICINE, RESEARCH & EXPERIMENTAL
Vinod Kumar Vashistha, Sonika Sethi, Inderjeet Tyagi, Dipak Kumar Das
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引用次数: 3

摘要

立体化学在药物设计中起着重要的作用,因为药物的对映体在其生物作用和药代动力学特征上经常变化。具有非活性或不安全对映体的药物外消旋物可导致有害影响。制造业仍然可以生产外消旋物,但这样的决定必须经过对与外消旋物相关的特定对映体的药理学和药代动力学特征的严格分析。抗抑郁药或抗抑郁药的药代动力学是立体选择性的,主要倾向于一种对映体。使用纯对映体提供(i)在某些药理作用方面比外消旋体更好的特异性,(ii)增强临床适应症,(iii)优化药代动力学。因此,控制抗抑郁药物药代动力学中的立体选择性对治疗抑郁症和精神疾病至关重要。本综述的目的是强调抗抑郁药的立体化学在设计和开发新的手性纯药物的背景下的重要性,使用外消旋体引起的潜在并发症,以及使用纯对映体的好处。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Chirality of antidepressive drugs: an overview of stereoselectivity.

Chirality of antidepressive drugs: an overview of stereoselectivity.

Chirality of antidepressive drugs: an overview of stereoselectivity.

Chirality of antidepressive drugs: an overview of stereoselectivity.

Stereochemistry plays an important role in drug design because the enantiomers of a drug frequently vary in their biological action and pharmacokinetic profiles. Racemates of a drug with either an inactive or an unsafe enantiomer can lead to detrimental effects. The manufacturing industry may still produce racemates, but such decisions must pass through rigorous analyses of the pharmacological and pharmacokinetic characteristics of the particular enantiomer related to the racemates. The pharmacokinetics of antidepressants or antidepressive agents is stereoselective and predominantly favors one enantiomer. The use of pure enantiomers offers (i) better specificity than the racemates in terms of certain pharmacological actions, (ii) enhanced clinical indications, and (iii) optimized pharmacokinetics. Therefore, controlling the stereoselectivity in the pharmacokinetics of antidepressive drugs is of critical importance in dealing with depression and psychiatric conditions. The objective of this review is to highlight the importance of the stereochemistry of antidepressants in the context of the design and development of new chirally pure pharmaceuticals, the potential complications caused by using racemates, and the benefits of using pure enantiomers.

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来源期刊
Asian Biomedicine
Asian Biomedicine 医学-医学:研究与实验
CiteScore
1.20
自引率
0.00%
发文量
24
审稿时长
6-12 weeks
期刊介绍: Asian Biomedicine: Research, Reviews and News (ISSN 1905-7415 print; 1875-855X online) is published in one volume (of 6 bimonthly issues) a year since 2007. [...]Asian Biomedicine is an international, general medical and biomedical journal that aims to publish original peer-reviewed contributions dealing with various topics in the biomedical and health sciences from basic experimental to clinical aspects. The work and authorship must be strongly affiliated with a country in Asia, or with specific importance and relevance to the Asian region. The Journal will publish reviews, original experimental studies, observational studies, technical and clinical (case) reports, practice guidelines, historical perspectives of Asian biomedicine, clinicopathological conferences, and commentaries Asian biomedicine is intended for a broad and international audience, primarily those in the health professions including researchers, physician practitioners, basic medical scientists, dentists, educators, administrators, those in the assistive professions, such as nurses, and the many types of allied health professionals in research and health care delivery systems including those in training.
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