[Dexmedetomidine. Pharmacokinetics and Pharmacodynamics]

Overview

Journal Anaesthesist

Specialty Anesthesiology

Date 2012 Dec 11

PMID 23223843

Citations 11

Authors

H Ihmsen

T I Saari

Affiliations

Soon will be listed here.

Abstract

Dexmedetomidine is a highly selective, potent α₂-adrenoceptor agonist which was approved in 2011 by the European Medicines Agency for sedation of patients in intensive care units (ICU). Dexmedetomidine exhibits sedative as well as analgesic and anxiolytic effects. Recent studies suggest that dexmedetomidine may be an alternative to midazolam in long-term ICU sedation. This review summarizes the pharmacokinetics and pharmacodynamics of dexmedetomidine particularly in ICU patients and with special regard to covariate effects. Although dexmedetomidine is currently approved only for use in adults the pharmacokinetics and pharmacodynamics in children will also be addressed as there are numerous studies on this off-label use.

Citing Articles

Nalmefene vs. dexmedetomidine for prevention of postoperative hyperalgesia in patients undergoing laparoscopic gynecological surgery with remifentanil infusion: A randomized double-blind controlled trial.

Jia Z, Chen Y, Gao T, Yuan Y, Zheng Y, Xie Y Front Pharmacol. 2023; 14:1131812.

PMID: 36762101 PMC: 9905252. DOI: 10.3389/fphar.2023.1131812.

Recent Advances in the Clinical Value and Potential of Dexmedetomidine.

Liu X, Li Y, Kang L, Wang Q J Inflamm Res. 2022; 14:7507-7527.

PMID: 35002284 PMC: 8724687. DOI: 10.2147/JIR.S346089.

Effect of dexmedetomidine on hemodynamic changes and inflammatory responses in patients undergoing off-pump coronary-artery bypass grafting.

Zhai W, Yang L, Sun P, Li Y, Han J, Wang G Exp Ther Med. 2020; 20(6):250.

PMID: 33178348 PMC: 7651881. DOI: 10.3892/etm.2020.9380.

Comparison of midazolam and low-dose dexmedetomidine in flexible bronchoscopy: A prospective, randomized, double-blinded study.

Magazine R, Venkatachala S, Goneppanavar U, Surendra V, Guddattu V, Chogtu B Indian J Pharmacol. 2020; 52(1):23-30.

PMID: 32201443 PMC: 7074428. DOI: 10.4103/ijp.IJP_287_19.

Dexmedetomidine-based monitored conscious sedation combined local anesthesia for levator resection in a 10-year-old child with Marcus Gunn jaw-winking synkinesis: A case report.

Tu Y, Gao F Medicine (Baltimore). 2018; 96(51):e9369.

PMID: 29390531 PMC: 5758233. DOI: 10.1097/MD.0000000000009369.

References

Talke P, Richardson C, Scheinin M, Fisher D . Postoperative pharmacokinetics and sympatholytic effects of dexmedetomidine. Anesth Analg. 1997; 85(5):1136-42. DOI: 10.1097/00000539-199711000-00033. View

Albrecht S, Ihmsen H, Hering W, Geisslinger G, Dingemanse J, Schwilden H . The effect of age on the pharmacokinetics and pharmacodynamics of midazolam. Clin Pharmacol Ther. 1999; 65(6):630-9. DOI: 10.1016/S0009-9236(99)90084-X. View

Devlin J, Mallow-Corbett S, Riker R . Adverse drug events associated with the use of analgesics, sedatives, and antipsychotics in the intensive care unit. Crit Care Med. 2010; 38(6 Suppl):S231-43. DOI: 10.1097/CCM.0b013e3181de125a. View

Venn R, Hell J, Grounds R . Respiratory effects of dexmedetomidine in the surgical patient requiring intensive care. Crit Care. 2000; 4(5):302-8. PMC: 29047. DOI: 10.1186/cc712. View

Diedrich D, Brown D . Analytic reviews: propofol infusion syndrome in the ICU. J Intensive Care Med. 2011; 26(2):59-72. DOI: 10.1177/0885066610384195. View

Bach A, Motsch J, Schmidt H, Bottiger B, Bohrer H, Martin E . In-use contamination of propofol. A clinical study. Eur J Anaesthesiol. 1997; 14(2):178-83. DOI: 10.1046/j.1365-2346.1997.00106.x. View

Venn R, Karol M, Grounds R . Pharmacokinetics of dexmedetomidine infusions for sedation of postoperative patients requiring intensive caret. Br J Anaesth. 2002; 88(5):669-75. DOI: 10.1093/bja/88.5.669. View

Devlin J, Lau A, Tanios M . Propofol-associated hypertriglyceridemia and pancreatitis in the intensive care unit: an analysis of frequency and risk factors. Pharmacotherapy. 2005; 25(10):1348-52. DOI: 10.1592/phco.2005.25.10.1348. View

Hosokawa K, Shime N, Kato Y, Taniguchi A, Maeda Y, Miyazaki T . Dexmedetomidine sedation in children after cardiac surgery. Pediatr Crit Care Med. 2009; 11(1):39-43. DOI: 10.1097/PCC.0b013e3181b062d7. View

10.

Czaja A, Zimmerman J . The use of dexmedetomidine in critically ill children. Pediatr Crit Care Med. 2009; 10(3):381-6. DOI: 10.1097/PCC.0b013e3181a3191f. View

11.

McKeage K, Perry C . Propofol: a review of its use in intensive care sedation of adults. CNS Drugs. 2003; 17(4):235-72. DOI: 10.2165/00023210-200317040-00003. View

12.

Dyck J, Maze M, Haack C, Vuorilehto L, Shafer S . The pharmacokinetics and hemodynamic effects of intravenous and intramuscular dexmedetomidine hydrochloride in adult human volunteers. Anesthesiology. 1993; 78(5):813-20. DOI: 10.1097/00000542-199305000-00002. View

13.

Dyck J, Maze M, Haack C, AZARNOFF D, Vuorilehto L, Shafer S . Computer-controlled infusion of intravenous dexmedetomidine hydrochloride in adult human volunteers. Anesthesiology. 1993; 78(5):821-8. DOI: 10.1097/00000542-199305000-00003. View

14.

Venn R, Bradshaw C, Spencer R, Brealey D, Caudwell E, Naughton C . Preliminary UK experience of dexmedetomidine, a novel agent for postoperative sedation in the intensive care unit. Anaesthesia. 1999; 54(12):1136-42. DOI: 10.1046/j.1365-2044.1999.01114.x. View

15.

Iirola T, Vilo S, Aantaa R, Wendelin-Saarenhovi M, Neuvonen P, Scheinin M . Dexmedetomidine inhibits gastric emptying and oro-caecal transit in healthy volunteers. Br J Anaesth. 2011; 106(4):522-7. DOI: 10.1093/bja/aer004. View

16.

Ebert T, Hall J, BARNEY J, Uhrich T, Colinco M . The effects of increasing plasma concentrations of dexmedetomidine in humans. Anesthesiology. 2000; 93(2):382-94. DOI: 10.1097/00000542-200008000-00016. View

17.

Kauppila T, Kemppainen P, Tanila H, Pertovaara A . Effect of systemic medetomidine, an alpha 2 adrenoceptor agonist, on experimental pain in humans. Anesthesiology. 1991; 74(1):3-8. DOI: 10.1097/00000542-199101000-00002. View

18.

Lin L, Guo X, Zhang M, Qu C, Sun Y, Bai J . Pharmacokinetics of dexmedetomidine in Chinese post-surgical intensive care unit patients. Acta Anaesthesiol Scand. 2011; 55(3):359-67. DOI: 10.1111/j.1399-6576.2010.02392.x. View

19.

Martin J, Parsch A, Franck M, Wernecke K, Fischer M, Spies C . Practice of sedation and analgesia in German intensive care units: results of a national survey. Crit Care. 2005; 9(2):R117-23. PMC: 1175921. DOI: 10.1186/cc3035. View

20.

Kivisto K, Kallio A, Neuvonen P . Pharmacokinetics and pharmacodynamics of transdermal dexmedetomidine. Eur J Clin Pharmacol. 1994; 46(4):345-9. DOI: 10.1007/BF00194403. View