新型药物艾司氯胺酮的特性与效能

Characteristics and efficacy of a noval drug Esketamine

氯胺酮最早于20世纪90年代在欧洲国家上市,最初被用作麻醉剂和战争创伤中的麻醉药,后由于其滥用导致精神运动、心血管系统等不良反应的限制,逐渐淡出临床工作中。艾司氯胺酮作为氯胺酮的右旋异构体,与其外消旋混合物相比,保留了药代动力学的特征,静脉注射后1分钟内便可达到峰值浓度,之后艾司氯胺酮及其代谢产物都主要通过肾脏排泄,不同的是艾司氯胺酮拥有更快的清除倾向和更大的总清除率;另外其药效动力学发生了变化,其镇静镇痛效力更强、所需剂量更小,达到相同麻醉效果用量仅为氯胺酮的1/2,且血流动力学变化更加平稳,锥体外系反应及其他不良反应也更加轻微。2019年艾司氯胺酮因其抗抑郁成果取得重大突破获得美国食品药品监督管理局(FDA)批准上市,自此作为一种新型药物重新进入临床麻醉工作视野中。目前艾司氯胺酮可用作麻醉诱导与维持、术后止痛、神经阻滞佐剂和抗抑郁等多种用途,复合用药时可减少丙泊酚和阿片类药物的使用量,更快创造插管条件,逆转阿片类药物的呼吸抑制,也可抑制瑞芬太尼诱发的痛觉过敏,同时具有镇静镇痛、产生意识消失和遗忘、抗炎抗应激、改善情绪等多重效能。本研究就艾司氯胺酮的药理学特性、临床应用等方面作如下综述,以供临床参考。

Ketamine was first marketed in European countries in the 1990s,and was initially used as a veterinary anesthetic and an anesthetic in war trauma,but gradually lost its clinical field of vision due to its abuse,psychomotor,cardiovascular system and other adverse reactions.Esketamine,as a dextral isomer of Ketamine,retains pharmacokinetic characteristics compared to its racemic mixture,reaching peak concentration within one minute after intravenous administration,after which esketamine and its metabolites are excreted mainly through the kidney,with the difference that esketamine has a faster clearance tendency and greater total clearance.In addition,its pharmacokinetics have changed,its sedative and analgesic effects are stronger,the dosage required is smaller,only half of ketamine can achieve the same anesthetic effect,and the hemodynamic changes are more stable,extrapyramidal reactions and other adverse reactions are less severe.In addition,in 2019,Esketamine was approved by the FDA for its major breakthrough in anti-depression results,and since then,it has re-entered the field of clinical anesthesia work as a novel drug.Esketamine can be used as anesthetic induction and maintenance drug,postoperative pain relief drug,nerve blocking adjuvant drug,antidepressant drug and so on.When it is combined,it can reduce the use of propofol and opioids,create intubation conditions faster,reverse respiratory depression caused by opioids,and inhibit the hyperalgesia induced by remifentanil.At the same time,it has multiple effects such as sedation and analgesia,inducing loss of consciousness and forgetting,anti-inflammatory and anti-stress,and improving mood.In this paper,the pharmacological properties and clinical applications of Esketamine as a novel drug,are summarized as follows for clinical reference.