Kawczak Piotr, Feszak Igor, Bączek Tomasz
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Medical University of Gdańsk, 80-416 Gdańsk, Poland.
Institute of Health Sciences, Pomeranian University in Słupsk, 76-200 Słupsk, Poland.
Biomedicines. 2024 Oct 9;12(10):2283. doi: 10.3390/biomedicines12102283.
Research over the past years has compared the enantiomers (S)-ketamine (esketamine) and (R)-ketamine (arketamine) of the previously known racemic mixture called ketamine (R/S-ketamine). Esketamine has been found to be more potent, offering three times stronger analgesic effects and 1.5 times greater anesthetic efficacy than arketamine. It provides smoother anesthesia with fewer side effects and is widely used in clinical settings due to its neuroprotective, bronchodilatory, and antiepileptic properties. Approved by the FDA and EMA in 2019, esketamine is currently used alongside SSRIs or SNRIs for treatment-resistant depression (TRD). On the other hand, arketamine has shown potential for treating neurological disorders such as Alzheimer's, Parkinson's, and multiple sclerosis, offering possible antidepressant effects and anti-inflammatory benefits. While esketamine is already in clinical use, arketamine's future depends on further research to address its safety, efficacy, and optimal dosing. Both enantiomers hold significant clinical value, with esketamine excelling in anesthesia, and arketamine showing promise in neurological and psychiatric treatments.
过去几年的研究比较了先前已知的外消旋混合物氯胺酮（R/S-氯胺酮）的对映体（S）-氯胺酮（艾氯胺酮）和（R）-氯胺酮（阿氯胺酮）。已发现艾氯胺酮效力更强，镇痛效果比阿氯胺酮强三倍，麻醉效果比阿氯胺酮高1.5倍。它能提供更平稳的麻醉，副作用更少，因其具有神经保护、支气管扩张和抗癫痫特性而在临床环境中广泛使用。艾氯胺酮于2019年获得美国食品药品监督管理局（FDA）和欧洲药品管理局（EMA）批准，目前与选择性5-羟色胺再摄取抑制剂（SSRIs）或5-羟色胺-去甲肾上腺素再摄取抑制剂（SNRIs）联合用于治疗抵抗性抑郁症（TRD）。另一方面，阿氯胺酮已显示出治疗诸如阿尔茨海默病、帕金森病和多发性硬化症等神经疾病的潜力，具有可能的抗抑郁作用和抗炎益处。虽然艾氯胺酮已在临床使用，但阿氯胺酮的未来取决于进一步研究以解决其安全性、有效性和最佳剂量问题。两种对映体都具有重要的临床价值，艾氯胺酮在麻醉方面表现出色，而阿氯胺酮在神经和精神疾病治疗方面显示出前景。
