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Published in: Drugs 2/2000

01-02-2000 | Adis New Drug Profile

Dexmedetomidine

Authors: Nila Bhana, Karen L. Goa, Karen J. McClellan

Published in: Drugs | Issue 2/2000

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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.
Literature
1.
go back to reference Wheeler AP. Sedation, analgesia, and paralysis in the intensive care unit. Chest 1993 Aug; 104: 566–77PubMedCrossRef Wheeler AP. Sedation, analgesia, and paralysis in the intensive care unit. Chest 1993 Aug; 104: 566–77PubMedCrossRef
2.
go back to reference 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: 544–50PubMed 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: 544–50PubMed
3.
go back to reference Eisenach JC. Alpha-2 agonists and analgesia. Expert Opin Invest Drug 1994 Oct; 3: 1005–10CrossRef Eisenach JC. Alpha-2 agonists and analgesia. Expert Opin Invest Drug 1994 Oct; 3: 1005–10CrossRef
4.
go back to reference 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: 1339–44PubMedCrossRef 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: 1339–44PubMedCrossRef
5.
go back to reference 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: 193–9PubMedCrossRef 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: 193–9PubMedCrossRef
6.
go back to reference 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 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
7.
go back to reference Salonen M, Reid K, Maze M. Synergistic interaction between alpha2-adrenergic agonists and benzodiazepines in rats. Anesthesiology 1992 Jun;76: 1004–11PubMedCrossRef Salonen M, Reid K, Maze M. Synergistic interaction between alpha2-adrenergic agonists and benzodiazepines in rats. Anesthesiology 1992 Jun;76: 1004–11PubMedCrossRef
8.
go back to reference 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. 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.
go back to reference 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)CrossRef 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)CrossRef
10.
go back to reference 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.: 25CrossRef 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.: 25CrossRef
11.
go back to reference Bloor BC, Ward DS, Belleville JP, et al. Effects of intravenous dexmedetomidine in humans. II. Hemodynamic changes. Anesthesiology 1992 Dec; 77: 1134–42 Bloor BC, Ward DS, Belleville JP, et al. Effects of intravenous dexmedetomidine in humans. II. Hemodynamic changes. Anesthesiology 1992 Dec; 77: 1134–42
12.
go back to reference 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 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.
go back to reference 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 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
14.
go back to reference 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 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.
go back to reference 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: 835–41PubMedCrossRef 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: 835–41PubMedCrossRef
16.
go back to reference Aho M, Erkola O, Kallio A, et al. Dexmedetomidine infusion for maintenance of anesthesia in patients undergoing abdominal hysterectomy. Anesth Analg 1992 Dec; 75: 940–6PubMed Aho M, Erkola O, Kallio A, et al. Dexmedetomidine infusion for maintenance of anesthesia in patients undergoing abdominal hysterectomy. Anesth Analg 1992 Dec; 75: 940–6PubMed
17.
go back to reference Scheinin H, Karhuvaara S, Olkkola KT, et al. Pharmacodynam-ics and pharmacokinetics of intramuscular dexmedetomidine. Clin Pharmacol Ther 1992 Nov; 52: 537–46PubMedCrossRef Scheinin H, Karhuvaara S, Olkkola KT, et al. Pharmacodynam-ics and pharmacokinetics of intramuscular dexmedetomidine. Clin Pharmacol Ther 1992 Nov; 52: 537–46PubMedCrossRef
18.
go back to reference 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 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
19.
go back to reference Abbott Laboratories. Precedex™. Dexmedetomidine hydro-chloride injection prescribing Information. Abbott Laboratories, USA. 2000 Abbott Laboratories. Precedex™. Dexmedetomidine hydro-chloride injection prescribing Information. Abbott Laboratories, USA. 2000
20.
21.
go back to reference Cunningham FE, Baughman VL, Tonkovich L, et al. Pharmacokinetics of dexmedetomidine in patients with hepatic failure [abstract]. Clin Pharmacol Ther 1999 Feb; 65: 128CrossRef Cunningham FE, Baughman VL, Tonkovich L, et al. Pharmacokinetics of dexmedetomidine in patients with hepatic failure [abstract]. Clin Pharmacol Ther 1999 Feb; 65: 128CrossRef
22.
go back to reference Rodrigues AD, Roberts EM. The in vitro interaction of dexmedetomidine with human liver microsomal cytochrome P4502D6 (CYP2D6). Drug Metab Dispos 1997 May; 25: 651–5PubMed Rodrigues AD, Roberts EM. The in vitro interaction of dexmedetomidine with human liver microsomal cytochrome P4502D6 (CYP2D6). Drug Metab Dispos 1997 May; 25: 651–5PubMed
23.
go back to reference 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 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
24.
go back to reference 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 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.
go back to reference 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) 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.
go back to reference 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) 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.
go back to reference Abbott/Orion Precedex to be launched in 2000 for ICU market. FDC Rep Pink Sheet 2000 Jan 3; 62(1): 9 Abbott/Orion Precedex to be launched in 2000 for ICU market. FDC Rep Pink Sheet 2000 Jan 3; 62(1): 9
28.
go back to reference 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 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.
go back to reference 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 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.
go back to reference Abbott Laboratories. Dexmedetomidine hydrochloride integrated summary of safety. Abbott Laboratories, 1998 Abbott Laboratories. Dexmedetomidine hydrochloride integrated summary of safety. Abbott Laboratories, 1998
Metadata
Title
Dexmedetomidine
Authors
Nila Bhana
Karen L. Goa
Karen J. McClellan
Publication date
01-02-2000
Publisher
Springer International Publishing
Published in
Drugs / Issue 2/2000
Print ISSN: 0012-6667
Electronic ISSN: 1179-1950
DOI
https://doi.org/10.2165/00003495-200059020-00012

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