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Dexmedetomidine

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Dexmedetomidine
Clinical data
AHFS/Drugs.comMonograph
Routes of
administration		by intravenous infusion only
ATC code
Pharmacokinetic data
Protein binding94%
Metabolismnear complete hepatic metabolism to inactive metabolites
Elimination half-life2 hours
Excretionurinary
Identifiers
  • (S)-4-[1-(2,3-dimethylphenyl)ethyl]-3H-imidazole
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.119.391 Edit this at Wikidata
Chemical and physical data
FormulaC13H16N2
Molar mass200.28 g/mol g·mol−1
3D model (JSmol)
  • n1cc(nc1)[C@H](c2c(c(ccc2)C)C)C
  • InChI=1S/C13H16N2/c1-9-5-4-6-12(10(9)2)11(3)13-7-14-8-15-13/h4-8,11H,1-3H3,(H,14,15)/t11-/m0/s1 checkY
  • Key:CUHVIMMYOGQXCV-NSHDSACASA-N checkY
 ☒NcheckY (what is this?)  (verify)

Dexmedetomidine (Precedex) is a sedative medication used by intensive care units and anesthetists. It is relatively unique in its ability to provide sedation without causing respiratory depression. Like clonidine, it is an agonist of α2-adrenergic receptors in certain parts of the brain.[1] It is the S-enantiomer of medetomidine,[2] used in veterinary medicine.

Indications

Dexmedetomidine is indicated for sedation of critically ill or injured patients in an intensive care unit setting. Its indication in the US was recently expanded to include nonintubated patient requiring sedation for surgery or procedures short-term. It is also useful as an adjunct for sedation and general anesthesia in the setting of certain operations and invasive medical procedures, such as colonoscopy. There are no absolute contraindications to the use of dexmedetomidine. Limiting its usefulness is the caution that the drug cannot be bolused due to concerns about peripheral α2-receptor stimulation with resulting hypotension, combined with its current high cost relative to generic medications such as propofol, fentanyl and midazolam which can achieve similar clinical effects.

Intensive care unit sedation

Compared to midazolam, dexmedetomidine was similarly effective for sedation, but shortened the time to extubation. It was associated with less delirium, tachycardia and hypotension. but more bradycardia. [3] It also seemed to be superior to lorazepam for ventilated patients in the intensive care unit.[4] Compared to midazolam, dexmedetomidine is superior due to reduced intensive care costs. The reduced costs are due to a reduction in intensive care unit stay as well as reduced mechanical ventilation.[5]

Procedural sedation

Dexmedetomidine has sedative, analgesic, sympatholytic, and anxiolytic effects that blunt many of the cardiovascular responses in the perioperative period. It reduces the requirements for volatile anesthetics, sedatives and analgesics without causing significant respiratory depression.[6]

Other

Dexmedetomidine may be useful for the treatment of the deleterious cardiovascular effects of acute cocaine intoxication and overdose.[7] Dexmedetomidine may also offer a new paradigm in the pharmacologic treatment of symptoms of distress (intractable pain, agitation or delirium) at the end of life. Recently, an investigator initiated IND was approved by the FDA to examine the use of dexmedetomidine in treating cancer patients at the end of life who are suffering from intractable pain, agitation or delirium.[8]

Dosage and administration

Intravenous infusion of dexmedetomidine is commonly initiated with a 1 mcg/kg loading dose, administered over 10 minutes, followed by a maintenance infusion of 0.2–1.0 mcg/kg/hour. There may be great individual variability in the hemodynamic effects (especially on heart rate and blood pressure), as well as the sedative effects of this drug. For this reason, the dose must be carefully adjusted to achieve the desired clinical effect.[9]

Pricing and Patent life

Dexmedetomidine is currently more expensive than off-patent sedatives, such as propofol and midazolam (median per-patient drug acquisition cost was reported as $1166 for dexmedetomidine vs $60 for midazolam in one study). [10] Dexmedetomidine is expected to lose patent protection in the United States in 2013 at which time the acquisition cost of this drug will likely decrease. [11]

See also

References

  1. ^ Cormack JR, Orme RM, Costello TG (2005). "The role of alpha2-agonists in neurosurgery". Journal of Clinical Neuroscience. 12 (4): 375–8. doi:10.1016/j.jocn.2004.06.008. PMID 15925765.{{cite journal}}: CS1 maint: multiple names: authors list (link)
  2. ^ a b CID 5311068 from PubChem
  3. ^ Riker RR, Shehabi Y, Bokesch PM, Ceraso D, Wisemandle W, Koura F, Whitten P, Margolis BD, Byrne DW, Ely EW, Rocha MG (2009). "Dexmedetomidine vs Midazolam for Sedation of Critically Ill Patients: A Randomized Trial". JAMA. 301 (5): 489–99. doi:10.1001/jama.2009.56. PMID 19188334.{{cite journal}}: CS1 maint: multiple names: authors list (link)
  4. ^ Pandharipande, PP; Pun, BT; Herr, DL; Maze, M; Girard, TD; Miller, RR; Shintani, AK; Thompson, JL; Jackson, JC (2007). "Effect of sedation with dexmedetomidine vs lorazepam on acute brain dysfunction in mechanically ventilated patients: the MENDS randomized controlled trial". JAMA. 298 (22): 2644–53. doi:10.1001/jama.298.22.2644. PMID 18073360.
  5. ^ O'Connor, M; Bucknall, T; Manias, E (2009). "Sedation Management in Australian and New Zealand Intensive Care Units: Doctors' and Nurses' Practices and Opinions". Am J Crit Care. 19 (3): 285–95. doi:10.4037/ajcc2009541. PMID 19770414.
  6. ^ Paris A, Tonner PH (2005). "Dexmedetomidine in anaesthesia". Current Opinion in Anaesthesiology. 18 (4): 412–8. doi:10.1097/01.aco.0000174958.05383.d5. PMID 16534267.
  7. ^ Menon DV, Wang Z, Fadel PJ, Arbique D, Leonard D, Li JL, Victor RG, Vongpatanasin W (2007). "Central sympatholysis as a novel countermeasure for cocaine-induced sympathetic activation and vasoconstriction in humans". J Am Coll Cardiol. 50 (7): 626–33. doi:10.1016/j.jacc.2007.03.060. PMID 17692748.{{cite journal}}: CS1 maint: multiple names: authors list (link)
  8. ^ Jackson KC, Wang Z, Wohlt P, Fine PG (2006). "Dexmedetomidine a novel analgesic with palliative medicine potential". J Pain and Palliative Care Pharmacotherapy. 20 (2): 23–7. doi:10.1080/J354v20n02_05. PMID 16702133.{{cite journal}}: CS1 maint: multiple names: authors list (link)
  9. ^ "Dosing Guidelines for Precedex®" (PDF). Retrieved 2010-11-21.
  10. ^ Dasta JF, Kane-Gill SL, Pencina M; et al. (2010). "A cost-minimization analysis of dexmedetomidine compared with midazolam for long-term sedation in the intensive care unit". Crit Care Med. 38 (2): 497–503. PMID 19789442. {{cite journal}}: Explicit use of et al. in: |author= (help)CS1 maint: multiple names: authors list (link)
  11. ^ Wunsch H (2011). "Weighing the Costs and Benefits of a Sedative". JAMA. 307 (11): 1195–1197. doi:10.1001. {{cite journal}}: Check |doi= value (help)
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