Department of Pharmacology, Institute of Medical Sciences, Banaras Hindu University, Varanasi, UP, India.
Department of Geriatric Medicine, Institute of Medical Sciences, Banaras Hindu University, Varanasi, UP, India.
Eur Arch Psychiatry Clin Neurosci. 2021 Apr;271(3):417-429. doi: 10.1007/s00406-019-01084-z. Epub 2019 Nov 19.
The motive of this article is to review the pharmacological and clinical aspects of esketamine (ESK), an NMDA-receptor antagonist approved recently by the FDA for treatment-resistant depression (TRD). PubMed/Medline database was searched using keywords 'esketamine' and 'depression', 'S-ketamine' and 'depression', and 'NMDA antagonist' and 'depression'. Individual trials were searched from ClinicalTrials.gov. We included English-language articles evaluating pharmacokinetics and pharmacodynamics of intranasal (IN) esketamine, along with clinical trial data related to its efficacy and safety in patients diagnosed with TRD. Compared to placebo, IN esketamine causes significant and rapid improvement in depression. Dizziness, vertigo, headache, increase in blood pressure are some of its common adverse effects. With the growing number of patients of TRD, additional effective and safe treatment is the need of the hour. Esketamine appears to be an effective therapy when combined with oral antidepressants in patients with TRD. It is of special value due to the rapid onset of its action. Long-term clinical studies are, however, needed to ascertain its safety profile.
本文旨在综述 NMDA 受体拮抗剂依他佐辛（ESK）的药理学和临床方面，该药最近获得 FDA 批准用于治疗抵抗性抑郁症（TRD）。通过关键词“esketamine”和“depression”、“S-ketamine”和“depression”以及“NMDA 拮抗剂”和“depression”，在 PubMed/Medline 数据库中进行了检索。从 ClinicalTrials.gov 中搜索了单独的试验。我们纳入了评估鼻内（IN）依他佐辛药代动力学和药效学的英文文章，以及与 TRD 患者的疗效和安全性相关的临床试验数据。与安慰剂相比，IN 依他佐辛可显著且快速改善抑郁症。常见的不良反应包括头晕、眩晕、头痛、血压升高。随着 TRD 患者数量的增加，额外的有效和安全的治疗方法是当前的需求。对于 TRD 患者，依他佐辛与口服抗抑郁药联合使用似乎是一种有效的治疗方法。由于其起效迅速，具有特殊价值。然而，需要进行长期的临床研究以确定其安全性。
