Compared with othersedatives, some studies suggest dexmedetomidine may be associated with lessdelirium.[15] However, this finding is not consistent across multiple studies.[14] At the very least, when aggregating many study results together, use of dexmedetomidine appears to be associated with less neurocognitive dysfunction compared to other sedatives.[16] Whether this observation has a beneficial psychological impact is unclear.[15] From an economic perspective, dexmedetomidine is associated with lower ICU costs, largely due to a shorter time to extubation.[17]
Dexmedetomidine can also be used for procedural sedation such as during colonoscopy.[18] It can be used as an adjunct with other sedatives likebenzodiazepines,opioids, andpropofol to enhance sedation and help maintain hemodynamic stability by decreasing the requirement of other sedatives.[19][20] Dexmedetomidine is also used for procedural sedation in children.[21]
It has also been used as an adjunct infusion during general anesthesia. In this application, it has been shown to decrease post-operative delirium, pain, nausea and opioid use.[23][24][25][26]
Dexmedetomidine may be useful for the treatment of the negative cardiovascular effects of acuteamphetamines andcocaineintoxication andoverdose.[27][28] Dexmedetomidine has also been used as an adjunct toneuroaxial anesthesia for lower limb procedures.[29] It has been successfully used to treat opioid withdrawal symptoms.[30]
In 2022 it was approved by the FDA for the treatment of agitation in schizophrenia and bipolar disorder.[31]
There are no known contraindication to the use of dexmedetomidine. It has a biphasic effect on blood pressure with lower readings at lower drug concentrations and higher readings at higher concentrations.[32] Common side effects include: hypotension, hypertension, with slight decreases in heart rate, arrhythmias, and hypoxia.[33][34] Toxic doses may cause first-degree or second-degreeatrioventricular block. These adverse events usually occur briefly after administering a loading dose of the drug. Thus, adverse effects may be reduced by omitting a loading dose.[34]
Dexmedetomidine may enhance the effects of other sedatives and anesthetics when co-administered. Similarly, drugs that lower blood pressure and heart rate, such asbeta blockers, may also have enhanced effects when co-administered with dexmedetomidine.[35]
Intravenous dexmedetomidine exhibits linear pharmacokinetics with a rapiddistribution half-life of approximately 6minutes in healthy volunteers, and a longer and more variable distribution half-life in ICU patients.[49] The terminalelimination half-life of intravenous dexmedetomidine ranged 2.1 to 3.1hours in healthy adults and 2.2 to 3.7hours in ICU patients.[9] Theplasma protein binding of dexmedetomidine is about 94% (mostlyalbumin).[4]
Dexmedetomidine was developed byOrion Pharma and is marketed under the names dexdor and Precedex; in 1999 the US Food and Drug Administration (FDA) approved it as a short-term sedative and analgesic (<24 hours) for critically ill or injured people on mechanical ventilation in theintensive care unit. The rationale for its short-term use was due to concerns over withdrawal side effects such as rebound high blood pressure. These effects have not been consistently observed in research studies, however.[50]
Dexmedetomidine, under the brand name Dexdomitor (Orion Corporation), was approved in the European Union for use in cats and dogs in 2002, for sedation and induction of general anesthesia.[51] The FDA approved dexmedetomidine for use in dogs in 2006 and cats in 2007.[52] Dexmedetomidine has supplanted xylazine as a sedative for cats and dogs in several countries. Dexmedetomidine is usedoff-label in horses.[53]
In 2015, the European Medicines Agency and the FDA approved an oromucosal gel form of dexmedetomidine marketed as Sileo by pharmaceutical companyZoetis for use in dogs for relief of noise aversion.[54][55]
^abFaden J, Musselman M, Citrome L (February 2023). "Sublingual dexmedetomidine: repurposing an anesthetic as an anti-agitation agent".Expert Rev Neurother.23 (2):97–106.doi:10.1080/14737175.2023.2174430.PMID36707066.
^abMacLaren R, Preslaski CR, Mueller SW, Kiser TH, Fish DN, Lavelle JC, Malkoski SP (March 2015). "A randomized, double-blind pilot study of dexmedetomidine versus midazolam for intensive care unit sedation: patient recall of their experiences and short-term psychological outcomes".Journal of Intensive Care Medicine.30 (3):167–175.doi:10.1177/0885066613510874.PMID24227448.S2CID25036525.
^Ahmed SS, Unland T, Slaven JE, Nitu ME, Rigby MR (September 2014). "Successful use of intravenous dexmedetomidine for magnetic resonance imaging sedation in autistic children".Southern Medical Journal.107 (9):559–564.doi:10.14423/SMJ.0000000000000160.PMID25188619.S2CID43652106.
^Richards JR, Albertson TE, Derlet RW, Lange RA, Olson KR, Horowitz BZ (May 2015). "Treatment of toxicity from amphetamines, related derivatives, and analogues: a systematic clinical review".Drug and Alcohol Dependence.150:1–13.doi:10.1016/j.drugalcdep.2015.01.040.PMID25724076.
^abcdefghiMillan MJ, Dekeyne A, Newman-Tancredi A, Cussac D, Audinot V, Milligan G, Duqueyroix D, Girardon S, Mullot J, Boutin JA, Nicolas JP, Renouard-Try A, Lacoste JM, Cordi A (December 2000). "S18616, a highly potent, spiroimidazoline agonist at alpha(2)-adrenoceptors: I. Receptor profile, antinociceptive and hypothermic actions in comparison with dexmedetomidine and clonidine".J Pharmacol Exp Ther.295 (3):1192–1205.doi:10.1016/S0022-3565(24)39022-6.PMID11082457.
^abcJasper JR, Lesnick JD, Chang LK, Yamanishi SS, Chang TK, Hsu SA, Daunt DA, Bonhaus DW, Eglen RM (April 1998). "Ligand efficacy and potency at recombinant alpha2 adrenergic receptors: agonist-mediated [35S]GTPgammaS binding".Biochem Pharmacol.55 (7):1035–1043.doi:10.1016/s0006-2952(97)00631-x.PMID9605427.
^Vucicevic J, Srdic-Rajic T, Pieroni M, Laurila JM, Perovic V, Tassini S, Azzali E, Costantino G, Glisic S, Agbaba D, Scheinin M, Nikolic K, Radi M, Veljkovic N (July 2016). "A combined ligand- and structure-based approach for the identification of rilmenidine-derived compounds which synergize the antitumor effects of doxorubicin".Bioorg Med Chem.24 (14):3174–3183.doi:10.1016/j.bmc.2016.05.043.PMID27265687.
^abcPanzer O, Moitra V, Sladen RN (July 2009). "Pharmacology of sedative-analgesic agents: dexmedetomidine, remifentanil, ketamine, volatile anesthetics, and the role of peripheral mu antagonists".Critical Care Clinics.25 (3):451–69, vii.doi:10.1016/j.ccc.2009.04.004.PMID19576524.
^Huupponen E, Maksimow A, Lapinlampi P, Särkelä M, Saastamoinen A, Snapir A, et al. (February 2008). "Electroencephalogram spindle activity during dexmedetomidine sedation and physiological sleep".Acta Anaesthesiologica Scandinavica.52 (2):289–294.doi:10.1111/j.1399-6576.2007.01537.x.PMID18005372.S2CID34923432.
^Gozalo-Marcilla M, Gasthuys F, Luna SP, Schauvliege S (April 2018). "Is there a place for dexmedetomidine in equine anaesthesia and analgesia? A systematic review (2005-2017)".Journal of Veterinary Pharmacology and Therapeutics.41 (2):205–217.doi:10.1111/jvp.12474.PMID29226340.S2CID3691570.
^abLamont LA, Creighton CM (11 September 2024). "Sedatives and Tranquilizers". In Lamont L, Grimm K, Robertson S, Love L, Schroeder C (eds.).Veterinary Anesthesia and Analgesia, The 6th Edition of Lumb and Jones. Wiley Blackwell. pp. 338–344.ISBN978-1-119-83027-6.
^"Recent Animal Drug Approvals". U.S. Department of Health and Human Services. 2 June 2016. Archived fromthe original on 12 July 2016. Retrieved3 July 2016.For the treatment of noise aversion in dogs
