右美托咪定药理学作用的研究进展

doi:10.3969/j.issn.1004-616x.2026.02.011

摘要/Abstract

摘要： 右美托咪定（DEX）是一种特异性α₂肾上腺素能受体激动剂，具有镇痛、镇静而无呼吸抑制的特点，常用于重症监护室成年患者的短期镇静。近年研究发现DEX还展现出显著的抗炎、抗氧化、抗凋亡和调节自噬作用，随着药理机制的深入研究，DEX在临床中的应用将更加广泛。本文综述了DEX的药理机制、临床应用现状、药物不良反应和优化策略，以期为优化其临床应用提供有益借鉴。

关键词: 右美托咪定, 镇静, 镇痛, 抗炎, 抗氧化, 药理机制

中图分类号:

R971.3

师敏婕, 耿溶辰, 赵昱舜, 刘建豪, 詹天豪, 邓紫丰, 刘江正, 孔德钦. 右美托咪定药理学作用的研究进展[J]. 癌变·畸变·突变, 2026, 38(2): 156-159,165.

[1] TAO Z X, LI P P, ZHAO X D. Progress on the mechanisms and neuroprotective benefits of dexmedetomidine in brain diseases[J]. Brain Behav, 2024, 14(11):e70116.
[2] 姚允泰,李立环.右美托咪定在心血管麻醉和围术期应用的专家共识(2018)[J].临床麻醉学杂志, 2018, 34(9):914-917.
[3] AARNES T K, DENT B T, LAKRITZ J, et al. Pharmacokinetics and pharmacodynamics of intramuscular dexmedetomidine in dogs[J]. Am J Vet Res, 2023, 84(4):ajvr.22.10.0184.
[4] RUUSKANEN J O, PEITSARO N, KASLIN J V M, et al. Expression and function of alpha-adrenoceptors in zebrafish:drug effects, m RNA and receptor distributions[J]. J Neurochem, 2005, 94(6):1559-1569.
[5] GOGOI S, SAIKIA D, DEY S. Addition of clonidine or dexmedetomidine with bupivacaine to prolong caudal analgesia in children undergoing infraumbilical surgery[J]. Cureus, 2022, 14(3):e23110.
[6] LIU M W, ZHANG Y, XIONG G F, et al. Dexmedetomidine for the treatment of sepsis-associated encephalopathy:Mechanism and prospects[J]. Biomed Pharmacother, 2025, 188:118209.
[7] TABARI M, MORADI A, REZAIEH G A, et al. Effects of midazolam and dexmedetomidine on cognitive dysfunction following open-heart surgery:a comprehensive review[J]. Brain Behav, 2025, 15(4):e70421.
[8] SUN S J, WANG J M, WANG J X, et al. Fetal and maternal responses to dexmedetomidine intrathecal application during cesarean section:a meta-analysis[J]. Med Sci Monit, 2020, 26:e918523.
[9] KIVISTÖK T, KALLIO A, NEUVONEN P J. Pharmacokinetics and pharmacodynamics of transdermal dexmedetomidine[J]. Eur J Clin Pharmacol, 1994, 46(4):345-349.
[10] LI A W, YUEN V M Y, GOULAY-DUFAY S, et al. Pharmacokinetics and pharmacodynamics of dexmedetomidine[J]. Drug Dev Ind Pharm,2016, 42(12):1917-1927.
[11] WEERINK M A S, STRUYS M M R F, HANNIVOORT L N, et al.Clinical pharmacokinetics and pharmacodynamics of dexmedetomidine[J]. Clin Pharmacokinet, 2017, 56(8):893-913.
[12] TALKE P, ANDERSON B J. Pharmacokinetics and pharmacodynamics of dexmedetomidine-induced vasoconstriction in healthy volunteers[J].Br J Clin Pharmacol, 2018, 84(6):1364-1372.
[13] KHAN Z P, FERGUSON C N, JONES R M. Alpha-2 and imidazoline receptor agonists Their pharmacology and therapeutic role[J]. Anaesthesia,1999, 54(2):146-165.
[14] SHEHABI Y, HOWE B D, BELLOMO R, et al. Early sedation with dexmedetomidine in critically ill patients[J]. N Engl J Med, 2019, 380(26):2506-2517.
[15] CHRYSOSTOMOU C, SCHMITT C G. Dexmedetomidine:sedation,analgesia and beyond[J]. Expert Opin Drug Metab Toxicol, 2008, 4(5):619-627.
[16] 杜诗斌,李璟,李晓勤,等.右美托咪定对大鼠脊髓背角突触传递的影响[J]. 2016(10):1232-1235.
[17] WEAVER V M, KIM N S, LEE B K, et al. Differences in urine cadmium associations with kidney outcomes based on serum creatinine and cystatin C[J]. Environ Res, 2011, 111(8):1236-1242.
[18] MOHAN A M, SHARMA A, GOYAL S, et al. Comparison of caudal dexmedetomidine and midazolam as an adjuvant to ropivacaine for postoperative pain relief in children undergoing infra-umbilical surgeries:a randomized controlled trial[J]. Asian J Anesthesiol, 2023, 61(2):89-101.
[19] NAGARAJU A, SAHU L, DAS S, et al. Comparative evaluation of dexmedetomidine and dexamethasone as adjuvants in supraclavicular brachial plexus block[J]. Cureus, 2023, 15(5):e38775.
[20] YAMAGUCHI Y, HOSOKAWA S, HARAGUCHI G, et al. The anti-inflammatory effects and clinical potential of dexmedetomidine in pulmonary arterial hypertension[J]. J Pharmacol Exp Ther, 2023, 385(2):88-94.
[21] KHO W, VON HAEFEN C, PAESCHKE N, et al. Dexmedetomidine restores autophagic flux, modulates associated microRNAs and the cholinergic anti-inflammatory pathway upon LPS-treatment in rats[J]. J Neuroimmune Pharmacol, 2022, 17(1/2):261-276.
[22] BAO N R, DAI D. Dexmedetomidine protects against ischemia and reperfusion-induced kidney injury in rats[J]. Mediators Inflamm, 2020,2020:2120971.
[23] POON W H, LING R R, YANG I X, et al. Dexmedetomidine for adult cardiac surgery:a systematic review, meta-analysis and trial sequential analysis[J]. Anaesthesia, 2023, 78(3):371-380.
[24] 刘娟.右美托咪定改善高脂肝细胞氧化应激损伤的作用机制研究[D].成都:成都医学院, 2020.
[25] ZHANG Y J, WEI H, WANG M M, et al. Dexmedetomidine alleviates ferroptosis following hepatic ischemia-reperfusion injury by upregulating Nrf2/GPx4-dependent antioxidant responses[J]. Biomed Pharmacother,2023, 169:115915.
[26] SUN L N, NIU K, GUO J, et al. Dexmedetomidine attenuates postoperative spatial memory impairment after surgery by reducing cytochrome C[J]. BMC Anesthesiol, 2023, 23(1):85.
[27] LIN Y, WEI Y, WEI Y H, et al. Dexmedetomidine alleviates oxidative stress and mitochondrial dysfunction in diabetic peripheral neuropathy via the microRNA-34a/SIRT2/S1PR1 axis[J]. Int Immunopharmacol,2023, 117:109910.
[28] CHEN X H, CHEN D T, CHEN P Z, et al. Dexmedetomidine attenuates apoptosis and neurological deficits by modulating neuronal NADPH oxidase 2-derived oxidative stress in neonates following hypoxic brain injury[J]. Antioxidants, 2022, 11(11):2199.
[29] LEWIS K, ALSHAMSI F, CARAYANNOPOULOS K L, et al.Dexmedetomidine vs other sedatives in critically ill mechanically ventilated adults:a systematic review and meta-analysis of randomized trials[J]. Intensive Care Med, 2022, 48(7):811-840.
[30] LIU X T, LI Y Q, KANG L, et al. Recent advances in the clinical value and potential of dexmedetomidine[J]. J Inflamm Res, 2021, 14:7507-7527.
[31] WEN J X, DING X Y, LIU C, et al. A comparation of dexmedetomidine and midazolam for sedation in patients with mechanical ventilation in ICU:a systematic review and meta-analysis[J]. PLoS One, 2023, 18(11):e0294292.
[32] ZHENG T, PEI Z, HUANG X J. Progress and frontiers of research on dexmedetomidine in perioperative medicine:a bibliometric analysis[J].Drug Des Devel Ther, 2024, 18:6017-6029.
[33] SAXENA P, GILL R K, SAROA R, et al. Comparison of nebulized ropivacaine(0.75%)with nebulized dexmedetomidine on the hemodynamic response on intubation in patients undergoing surgery under general anesthesia:a comparative randomized double-blind placebo-controlled study[J]. Saudi J Anaesth, 2024, 18(1):31-39.
[34] WANG D, DOU W, HU J H, et al. Pre-operative dexmedetomidine nasal spray and emergence agitation in adults undergoing ear, nose and throat surgery:a randomised controlled trial[J]. Anaesthesia, 2025, 80(12):1519-1527.
[35] ZHAO J N, KONG M, QI B, et al. Comparison of the morphine-sparing effect of intraoperative dexmedetomidine with and without loading dose following general anesthesia in multiple-fracture patients:a prospective, randomized, controlled clinical trial[J]. Medicine, 2016, 95(33):e4576.
[36] MUNHALL C C, WARNER B K, NGUYEN S A, et al. Use of dexmedetomidine for controlled hypotension in middle ear surgery:a systematic review and meta-analysis[J]. Am J Otolaryngol, 2023, 44(4):103917.
[37] SUN Q, LI P F, LIU C, et al. Effects of dexmedetomidine and sevoflurane on optic nerve sheath diameter and postoperative nausea and vomiting in patients undergoing microvascular decompression:a retrospective cohort study[J]. BMC Anesthesiol, 2025, 25(1):293.
[38] CAI Q, LIU G Q, HUANG L S, et al. The role of dexmedetomidine in tumor-progressive factors in the perioperative period and cancer recurrence:a narrative review[J]. Drug Des Devel Ther, 2022, 16:2161-2175.
[39] SHI M J, LIU J Z, YU W H, et al. Repurposing the anesthetic dexmedetomidine:a novel antidote for sulfur mustard analog-induced acute lung injury via multi-mechanism modulation[J]. Int Immunopharmacol, 2026, 170:116069.
[40] PORTELLI K, KANDRAJU H, RYU M, et al. Efficacy and safety of dexmedetomidine for analgesia and sedation in neonates:a systematic review[J]. J Perinatol, 2024, 44(2):164-172.
[41] COLLIER T E, FARRELL L B, KILLIAN A D, et al. Effect of adjunctive dexmedetomidine in the treatment of alcohol withdrawal compared to benzodiazepine symptom-triggered therapy in critically ill patients:the EvADE study[J]. J Pharm Pract, 2022, 35(3):356-362.
[42] KEATING G M. Dexmedetomidine:a review of its use for sedation in the intensive care setting[J]. Drugs, 2015, 75(10):1119-1130.
[43] BURLACU C C, NEAG M A, MITRE A O, et al. The role of miRNAs in dexmedetomidines neuroprotective effects against brain disorders[J]. Int J Mol Sci, 2022, 23(10):5452.
[44] AOUAD M T, ZEENI C, AL NAWWAR R, et al. Dexmedetomidine for improved quality of emergence from general anesthesia:a dose-finding study[J]. Anesth Analg, 2019, 129(6):1504-1511.
[45] 杨杰.右美托咪定类似物的设计合成、药理学活性及成药性的研究[D].成都:四川大学, 2021.
[46] 贺渝淼,李默晗,马超,等.超长效镇痛药物的研发与转化[J].协和医学杂志, 2024, 15(2):251-257.

右美托咪定药理学作用的研究进展

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