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Dexmedetomidine

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Abstract

  • ▴ Dexmedetomidine is a potent α2-adrenoceptor agonist with 8 times higher affinity for the α2-adrenoceptorthan clonidine.

  • ▴ Dexmedetomidine has shown sedative, analgesic and anxiolytic effects after intravenous administration to healthy volunteers or postsurgical patients in the intensive care unit.

  • ▴ Dexmedetomidine produced a predictable haemo-dynamic decline (dose-dependently decreased arterial blood pressure and heart rate) in postsurgical patients coinciding with reductions in plasma catecholamines.

  • ▴ In phase III clinical trials, dexmedetomidine 0.2 to 0.7 µg/kg/h produced clinically effective sedation and significantly reduced the analgesic requirements of postsurgical ventilated intensive care unit patients. There was no clinically apparent respiratory depression after cessation of assisted ventilation.

  • ▴ Dexmedetomidine produced rapid and stable sedation in postsurgical ventilated patients while maintaining a high degree of patient reusability and anxiety reduction.

  • ▴ Dexmedetomidine was well tolerated in phase III studies. The most frequently observed adverse events were hypotension, bradycardia and nausea.

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References

  1. Wheeler AP. Sedation, analgesia, and paralysis in the intensive care unit. Chest 1993 Aug; 104: 566–77

    Article  PubMed  CAS  Google Scholar 

  2. Lawrence CJ, Prinzen FW, de LS. The effect of dexmedetomidine on the balance of myocardial energy requirement and oxygen supply and demand. Anesth Analg 1996 Mar; 82: 544–50

    PubMed  CAS  Google Scholar 

  3. Eisenach JC. Alpha-2 agonists and analgesia. Expert Opin Invest Drug 1994 Oct; 3: 1005–10

    Article  CAS  Google Scholar 

  4. Hunter JC, Fontana DJ, Hedley LR, et al. Assessment of the role of alpha-2-adrenoceptor subtypes in the antinociceptive, sedative and hypothermic action of dexmedetomidine in transgenic mice. Br J Pharmacol 1997 Dec; 122: 1339–44

    Article  PubMed  CAS  Google Scholar 

  5. Savola J-M, Virtanen R. Central alpha2-adrenoceptors are highly stereoselective for dexmedetomidine, the dextro enantiomer of medetomidine. Eur J Pharmacol 1991 Mar 26; 195: 193–9

    Article  PubMed  CAS  Google Scholar 

  6. Coughlan MG, Lee JG, Bosnjak ZJ, et al. Direct coronary and cerebral vascular responses to dexmedetomidine. Significance of endogenous nitric oxide synthesis. Anesthesiology 1992 Nov; 77: 998–1006

    CAS  Google Scholar 

  7. Salonen M, Reid K, Maze M. Synergistic interaction between alpha2-adrenergic agonists and benzodiazepines in rats. Anesthesiology 1992 Jun;76: 1004–11

    Article  PubMed  CAS  Google Scholar 

  8. Guo T-Z, MacMillan LB, Limbird LE, et al. The alpha2A-adrenoceptor mediates anesthesia and analgesia in mice receiving dexmedetomidine [abstr. A702.]. Anesthesiology 1997 Sep; 87 Suppl.

  9. Morrison P, Etropolski M, Bachand RT. Dose-ranging study to evaluate the effects of dexmedetomidine on sedation [abstract no A298]. Anesthesiology 1999; 91: 3A Abstracts of Scientific Papers 1999 Annual Meeting American Society of Anesthesiologists, 1999 Oct 9-13, Dallas (TX)

    Article  Google Scholar 

  10. Gravel N, Richardson C, Searle N, et al. Hemodynamic, cardiac and neurohormonal interactions of esmolol and dexmedetomidine in 36 healthy volunteers [abstract]. Anesth Analg 1999 Apr; 88 Suppl.: 25

    Article  Google Scholar 

  11. Bloor BC, Ward DS, Belleville JP, et al. Effects of intravenous dexmedetomidine in humans. II. Hemodynamic changes. Anesthesiology 1992 Dec; 77: 1134–42

    CAS  Google Scholar 

  12. Grounds M. Dexmedetomidine: phase HI results. Proceedings from the 19th International Symposium on Intensive Care and Emergency Medicine; 1999 Mar 16–19; Brussels: 15-8

  13. Belleville JP, Ward DS, Bloor BC, et al. Effects of intravenous dexmedetomidine in humans. I. Sedation, ventilation, and metabolic rate. Anesthesiology 1992 Dec; 77: 1125–33

    CAS  Google Scholar 

  14. Singer M. Dexmedetomidine: phase I/II results. Proceedings from the 19th International Symposium on Intensive Care and Emergency Medicine; 1999 Mar 16–19; Brussels: 11-3

  15. Talke P, Tayefeh F, Sessler DI, et al. Dexmedetomidine does not alter the sweating threshold, but comparably and linearly decreases the vasoconstriction and shivering thresholds. Anesthesiology 1997 Oct; 87: 835–41

    Article  PubMed  CAS  Google Scholar 

  16. Aho M, Erkola O, Kallio A, et al. Dexmedetomidine infusion for maintenance of anesthesia in patients undergoing abdominal hysterectomy. Anesth Analg 1992 Dec; 75: 940–6

    PubMed  CAS  Google Scholar 

  17. Scheinin H, Karhuvaara S, Olkkola KT, et al. Pharmacodynam-ics and pharmacokinetics of intramuscular dexmedetomidine. Clin Pharmacol Ther 1992 Nov; 52: 537–46

    Article  PubMed  CAS  Google Scholar 

  18. Khan ZP, Munday IT, Jones RM, et al. Effects of dexmedetomidine on isoflurane requirements in healthy volunteers. 1: pharmacodynamic and pharmacokinetic interactions. Br J Anaesth 1999 Sep; 83: 372–80

    CAS  Google Scholar 

  19. Abbott Laboratories. Precedex™. Dexmedetomidine hydro-chloride injection prescribing Information. Abbott Laboratories, USA. 2000

  20. Mantz J. Dexmedetomidine. Drugs Today 1999 Mar; 35(3): 151–7

    PubMed  CAS  Google Scholar 

  21. Cunningham FE, Baughman VL, Tonkovich L, et al. Pharmacokinetics of dexmedetomidine in patients with hepatic failure [abstract]. Clin Pharmacol Ther 1999 Feb; 65: 128

    Article  Google Scholar 

  22. Rodrigues AD, Roberts EM. The in vitro interaction of dexmedetomidine with human liver microsomal cytochrome P4502D6 (CYP2D6). Drug Metab Dispos 1997 May; 25: 651–5

    PubMed  CAS  Google Scholar 

  23. Bachand R, Scholz J, Pinaud M, et al. The effects of dexmedetomidine in patients in the intensive care setting [abstract no. 622]. Intensive Care Med 1999; 25 Suppl. 1: S160

    Google Scholar 

  24. Martin E, Lehot JJ, Manikis P, et al. Dexmedetomidine: a novel agent for patients in the intensive care setting [abstract no. 623]. Intensive Care Med 1999; 25 Suppl. 1

  25. Mantz J, Goldfarb G, Lehot J-J, et al. Dexmedetomidine efficacy for ICU postoperative sedation [abstract no. 197]. Anesthesiology 1999; 91, no 3A (Sep M9126) Abstracts of Scientific Papers 1999 Annual Meeting American Society Of Anesthiologists, 1999 Oct 9–13, Dallas (TX)

  26. Bachand RT, Werner L, Etropolski M, et al. A phase III study evaluating dexmedetomidine for sedation in postoperative patients [abstract no. 296]. Anesthesiology 1999; 91, no. 3A (Sep M9126) Abstracts of Scientific Papers 1999 Annual Meeting American Society of Anesthesiologists, 1999 Oct 9–13, Dallas (TX)

  27. Abbott/Orion Precedex to be launched in 2000 for ICU market. FDC Rep Pink Sheet 2000 Jan 3; 62(1): 9

    Google Scholar 

  28. Jokinen K, Etropolski M, Paluselli M, et al. Dexmedetomidine and patient management: midazolam study. Proceedings of the XXV Congreso Latinoamericano de Anestesiologia 1999 Nov 3–6: poster 509

  29. Jokinen J, Etropolski M, Paluselli M, et al. Dexmedetomidine and patient management: propofol study. Proceedings of the XXV Congreso Latinoamericano de Anestesiologia 1999 Nov 3–6 Nov: poster 510

  30. Abbott Laboratories. Dexmedetomidine hydrochloride integrated summary of safety. Abbott Laboratories, 1998

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Authors and Affiliations

  1. Adis International Limited, 41 Centorian Drive, Private Bag 65901, Mairangi Bay, Auckland 10, New Zealand

    Nila Bhana, Karen L. Goa & Karen J. McClellan

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  1. Nila Bhana
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  2. Karen L. Goa
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  3. Karen J. McClellan
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Correspondence to Nila Bhana.

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Bhana, N., Goa, K.L. & McClellan, K.J. Dexmedetomidine. Drugs 59, 263–268 (2000). https://doi.org/10.2165/00003495-200059020-00012

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  • DOI: https://doi.org/10.2165/00003495-200059020-00012

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