Liu Xiaotian, Li Yueqin, Kang Li, Wang Qian
Department of Anesthesiology, Children's Hospital of Soochow University, Suzhou, Jiangsu, People's Republic of China.
J Inflamm Res. 2021 Dec 30;14:7507-7527. doi: 10.2147/JIR.S346089. eCollection 2021.
Dexmedetomidine, a highly selective α2-adrenoceptor agonist, has sedative, anxiolytic, analgesic, sympatholytic, and opioid-sparing properties and induces a unique sedative response which shows an easy transition from sleep to wakefulness, thus allowing a patient to be cooperative and communicative when stimulated. Recent studies indicate several emerging clinical applications via different routes. We review recent data on dexmedetomidine studies, particularly exploring the varying routes of administration, experimental implications, clinical effects, and comparative advantages over other drugs. A search was conducted on the PubMed and Web of Science libraries for recent studies using different combinations of the words "dexmedetomidine", "route of administration", and pharmacological effect. The current routes, pharmacological effects, and application categories of dexmedetomidine are presented. It functions by stimulating pre- and post-synaptic α2-adrenoreceptors within the central nervous system, leading to hyperpolarization of noradrenergic neurons, induction of an inhibitory feedback loop, and reduction of norepinephrine secretion, causing a sympatholytic effect, in addition to its anti-inflammation, sleep induction, bowel recovery, and sore throat reduction effects. Compared with similar α2-adrenoceptor agonists, dexmedetomidine has both pharmacodynamics advantage of a significantly greater α2:α1-adrenoceptor affinity ratio and a pharmacokinetic advantage of having a significantly shorter elimination half-life. In its clinical application, dexmedetomidine has been reported to present a significant number of benefits including safe sedation for various surgical interventions, improvement of intraoperative and postoperative analgesia, sedation for compromised airways without respiratory depression, nephroprotection and stability of hypotensive hemodynamics, reduction of postoperative nausea and vomiting and postoperative shivering incidence, and decrease of intraoperative blood loss. Although the clinical application of dexmedetomidine is promising, it is still limited and further research is required to enhance understanding of its pharmacological properties, patient selection, dosage, and adverse effects.
右美托咪定是一种高选择性α2肾上腺素能受体激动剂,具有镇静、抗焦虑、镇痛、抗交感神经和节省阿片类药物的特性,并能诱导独特的镇静反应,即从睡眠到清醒的转换容易,从而使患者在受到刺激时能够配合并进行交流。最近的研究表明,通过不同途径有几种新出现的临床应用。我们回顾了右美托咪定研究的最新数据,特别探讨了不同的给药途径、实验意义、临床效果以及与其他药物相比的优势。在PubMed和Web of Science数据库中进行了搜索,以查找使用“右美托咪定”、“给药途径”和“药理作用”等不同组合词的近期研究。介绍了右美托咪定目前的给药途径、药理作用和应用类别。它通过刺激中枢神经系统内突触前和突触后的α2肾上腺素能受体发挥作用,导致去甲肾上腺素能神经元超极化,诱导抑制性反馈回路,并减少去甲肾上腺素分泌,从而产生抗交感神经作用,此外还具有抗炎、诱导睡眠、促进肠道恢复和减轻咽痛的作用。与类似的α2肾上腺素能受体激动剂相比,右美托咪定具有显著更高的α₂:α₁肾上腺素能受体亲和力比的药效学优势以及消除半衰期显著更短的药代动力学优势。在其临床应用中,据报道右美托咪定有许多显著益处,包括为各种手术干预提供安全镇静、改善术中和术后镇痛、为气道受损患者进行镇静而无呼吸抑制、肾保护和维持低血压血流动力学稳定、降低术后恶心呕吐和术后寒战发生率以及减少术中失血。尽管右美托咪定的临床应用前景广阔,但仍有局限性,需要进一步研究以加深对其药理特性、患者选择、剂量和不良反应的理解。