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Dexmedetomidine
Systematic (IUPAC) name
(S)-4-[1-(2,3-dimethylphenyl)ethyl]-3H-imidazole
Identifiers
CAS number 113775-47-6
ATC code N05CM18
PubChem 68602
DrugBank APRD00578
Chemical data
Formula C 13H16N2  
Mol. mass 200.28 g/mol
Pharmacokinetic data
Bioavailability  ?
Protein binding 94%
Metabolism near complete hepatic metabolism to inactive metabolites
Half life 2 hours
Excretion urinary
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes by intravenous infusion only

Dexmedetomidine is a sedative medication used by intensive care units and anesthesiologists, and is marketed under the brand name Precedex (Hospira, Inc.) in the United States. It is relatively unique in its ability to provide sedation without causing respiratory depression. Like clonidine, its mechanism of action is agonism of alpha-2 receptors in certain parts of the brain.[1] It is the S-enantiomer of medetomidine.[2]

Dexmedetomidine has sedative, analgesic, sympatholytic, and anxiolytic effects that blunt many of the cardiovascular responses in the perioperative period. It reduces the volatile anesthetic, sedative and analgesic requirements of the patient without causing significant respiratory depression.[3]

Recent research has suggested dexmedetomidine to be an effective treatment for the dangerous cardiovascular symptoms of cocaine intoxication and overdose.[4] It also seemed to be superior to lorazepam for ventilated patients in the intensive care unit.[5] Compared to midazolam, dexmedetomidine was similarly effective for sedation, but shortened the time to extubation, was associated with less delirium, and experience more bradycardia and less tachycardia and hypertension.[6]

References

  1. ^ Cormack JR, Orme RM, Costello TG. The role of alpha2-agonists in neurosurgery. Journal of Clinical Neuroscience. 2005 May;12(4):375-8.
  2. ^ "Dexmedetomidine - Substance Summary". National Library of Medicine. http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=7847580. Retrieved 2009-01-26.  
  3. ^ Paris A, Tonner PH. Dexmedetomidine in anaesthesia. Current Opinion in Anaesthesiology. 2005 Aug;18(4):412-8.
  4. ^ Menon DV, Wang Z, Fadel PJ, Arbique D, Leonard D, Li JL, Victor RG, Vongpatanasin W. "Central sympatholysis as a novel countermeasure for cocaine-induced sympathetic activation and vasoconstriction in humans". J Am Coll Cardiol 2007; 50(7): 626-33. PMID 17692748
  5. ^ Pandharipande PP, Pun BT, Herr DL, et al.. "Effect of sedation with dexmedetomidine vs lorazepam on acute brain dysfunction in mechanically ventilated patients: the MENDS randomized controlled trial." JAMA 2007; 298(22): 2644-53. PMID 18073360
  6. ^ Riker RR, Shehabi Y, Bokesch PM, Ceraso D, Wisemandle W, Koura F, Whitten P, Margolis BD, Byrne DW, Ely EW, Rocha MG; for the SEDCOM (Safety and Efficacy of Dexmedetomidine Compared With Midazolam) Study Group. "Dexmedetomidine vs Midazolam for Sedation of Critically Ill Patients: A Randomized Trial " JAMA; Early release online February 2, 2009.
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