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Revision as of 10:01, 1 November 2011 editBeetstra (talk | contribs)Edit filter managers, Administrators172,031 edits Script assisted update of identifiers for the Chem/Drugbox validation project (updated: 'DrugBank').← Previous edit		Latest revision as of 04:38, 26 December 2024 edit undoWhywhenwhohow (talk | contribs)Autopatrolled, Extended confirmed users, Pending changes reviewers49,153 edits infobox
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			{{Short description|Anxiolytic, sedative, and pain medication}}
	{{Drugbox
			{{Infobox drug
	| Watchedfields = changed		| Watchedfields = changed
	| verifiedrevid = 443632909		| verifiedrevid = 458436659
			| image = Dexmedetomidine.svg
	| IUPAC_name = (''S'')-4--3H-imidazole
			| width =
	| image = Dexmedetomidine skeletal.svg
			| alt =
			| caption =
	<!--Clinical data-->		<!--Clinical data-->
	| tradename =		| tradename = Precedex, others
	| Drugs.com = {{drugs.com|monograph|dexmedetomidine-hydrochloride}}		| Drugs.com = {{drugs.com|monograph|dexmedetomidine-hydrochloride}}
			| MedlinePlus =
	| pregnancy_AU = <!-- A / B1 / B2 / B3 / C / D / X -->
			| DailyMedID = Dexmedetomidine
	| pregnancy_US = <!-- A / B / C / D / X -->
			| pregnancy_AU = B1
	| pregnancy_category =
			| pregnancy_category =
	| legal_AU = <!-- Unscheduled / S2 / S4 / S8 -->
			| routes_of_administration = ], ], ], ]<ref name="FadenMusselmanCitrome2023" />
			| ATC_prefix = N05
			| ATC_suffix = CM18
			| ATC_supplemental =
			<!--Legal status-->
			| legal_AU = S4
			| legal_AU_comment = <ref>{{cite web |title=DEXMEDETOMIDINE FRESENIUS (Fresenius Kabi Australia Pty Ltd) |url=https://www.tga.gov.au/resources/prescription-medicines-registrations/dexmedetomidine-fresenius-fresenius-kabi-australia-pty-ltd |website=] |archive-url=https://web.archive.org/web/20230318045443/https://www.tga.gov.au/resources/prescription-medicines-registrations/dexmedetomidine-fresenius-fresenius-kabi-australia-pty-ltd |archive-date=2023-03-18 |url-status=live}}</ref>
			| legal_BR = C1
			| legal_BR_comment = <ref>{{Cite web |author=Anvisa |author-link=Brazilian Health Regulatory Agency |date=2023-03-31 |title=RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial |trans-title=Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control|url=https://www.in.gov.br/en/web/dou/-/resolucao-rdc-n-784-de-31-de-marco-de-2023-474904992 |url-status=live |archive-url=https://web.archive.org/web/20230803143925/https://www.in.gov.br/en/web/dou/-/resolucao-rdc-n-784-de-31-de-marco-de-2023-474904992 |archive-date=2023-08-03 |access-date=2023-08-16 |publisher=] |language=pt-BR |publication-date=2023-04-04}}</ref>
	| legal_UK = <!-- GSL / P / POM / CD -->		| legal_UK = <!-- GSL / P / POM / CD -->
	| legal_US = <!-- OTC / Rx-only -->		| legal_US = Rx-only
			| legal_US_comment = <ref name="Precedex FDA label">{{cite web | title=Precedex- dexmedetomidine hydrochloride injection, solution | website=DailyMed | date=2 March 2022 | url=https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=4419162d-81d4-49bd-96de-1729440bdb74 | access-date=8 April 2022 | archive-date=8 April 2022 | archive-url=https://web.archive.org/web/20220408230944/https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=4419162d-81d4-49bd-96de-1729440bdb74 | url-status=live }}</ref><ref name="Igalmi FDA label">{{cite web | title=Igalmi- dexmedetomidine film | website=DailyMed | date=14 December 2022 | url=https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=99476e8c-2527-4cb0-9d67-9f9cd91343c6 | access-date=21 January 2023}}</ref>
	| legal_status =
			| legal_EU = Rx-only
	| routes_of_administration = by intravenous infusion only
			| legal_EU_comment = <ref>{{cite web | title=Sileo EPAR | website=European Medicines Agency | date=7 July 2015 | url=https://www.ema.europa.eu/en/medicines/veterinary/EPAR/sileo | access-date=21 June 2024}}</ref><ref>{{cite web | title=Dexdomitor EPAR | website=European Medicines Agency (EMA) | date=14 December 2009 | url=https://www.ema.europa.eu/en/medicines/veterinary/EPAR/dexdomitor | access-date=26 December 2024}}</ref><ref>{{cite web | title=Dexdomitor PI | website=Union Register of medicinal products | date=5 September 2002 | url=https://ec.europa.eu/health/documents/community-register/html/v033.htm | access-date=26 December 2024}}</ref>
			| legal_status = Rx-only
	<!--Pharmacokinetic data-->		<!--Pharmacokinetic data-->
	| bioavailability =		| bioavailability =
	| protein_bound = 94%		| protein_bound = 94% (mostly ])<ref name="Precedex FDA label" />
	| metabolism = near complete hepatic metabolism to inactive metabolites		| metabolism = Near complete hepatic metabolism to inactive metabolites
	| elimination_half-life = 2 hours		| elimination_half-life = 2–4 hours<ref name="Weerink_2017" />
	| excretion = urinary		| excretion = ]
	<!--Identifiers-->		<!--Identifiers-->
			| index2_label = as HCl
	| CASNo_Ref = {{cascite|correct|CAS}}
	| CAS_number_Ref = {{cascite|correct|??}}		| CAS_number_Ref = {{cascite|correct|??}}
	| CAS_number = 113775-47-6		| CAS_number = 113775-47-6
	| ATC_prefix = N05
	| ATC_suffix = CM18
	| ATC_supplemental =
	| PubChem = 68602		| PubChem = 68602
	| DrugBank_Ref = {{drugbankcite|correct|drugbank}}		| DrugBank_Ref = {{drugbankcite|correct|drugbank}}
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	| KEGG_Ref = {{keggcite|correct|kegg}}		| KEGG_Ref = {{keggcite|correct|kegg}}
	| KEGG = D00514		| KEGG = D00514
			| KEGG2_Ref = {{keggcite|correct|kegg}}
			| KEGG2 = D01205
	| ChEBI_Ref = {{ebicite|correct|EBI}}		| ChEBI_Ref = {{ebicite|correct|EBI}}
	| ChEBI = 4466		| ChEBI = 4466
	| ChEMBL_Ref = {{ebicite|correct|EBI}}		| ChEMBL_Ref = {{ebicite|correct|EBI}}
	| ChEMBL = 778		| ChEMBL = 778
			| synonyms = MPV-1440;
	<!--Chemical data-->		<!--Chemical data-->
			| IUPAC_name = (''S'')-4--3''H''-imidazole
	| C=13 | H=16 | N=2
			| C=13 | H=16 | N=2
	| molecular_weight = 200.28 g/mol
	| smiles = n1cc(nc1)(c2c(c(ccc2)C)C)C		| SMILES = Cc2cccc((C)c1ccn1)c2C
	| InChI = 1/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
	| InChIKey = CUHVIMMYOGQXCV-NSHDSACABZ
	| StdInChI_Ref = {{stdinchicite|correct|chemspider}}		| StdInChI_Ref = {{stdinchicite|correct|chemspider}}
	| StdInChI = 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		| StdInChI = 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
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	| StdInChIKey = CUHVIMMYOGQXCV-NSHDSACASA-N		| StdInChIKey = CUHVIMMYOGQXCV-NSHDSACASA-N
	}}		}}
	'''Dexmedetomidine''' ('''Precedex''') is a ] medication used by intensive care units and anesthetists. It is relatively unique in its ability to provide sedation without causing ]. Like ], it is an ] of ]s in certain parts of the brain.<ref name=Cormack2005/>
			'''Dexmedetomidine''', sold under the brand name '''Precedex''' among others, is a ] used for ].<ref name="Precedex FDA label" /> ]s use dexmedetomidine for similar purposes in treating cats, dogs, and horses.<ref>{{cite journal | vauthors = Marly-Voquer C, Schwarzwald CC, Bettschart-Wolfensberger R | title = The use of dexmedetomidine continuous rate infusion for horses undergoing transvenous electrical cardioversion--A case series | journal = The Canadian Veterinary Journal | volume = 57 | issue = 1 | pages = 70–75 | date = January 2016 | pmid = 26740702 | pmc = 4677613 }}</ref><ref>{{Cite web |url=http://www.dexdomitor.com/ |title = Dexdomitor |access-date=2013-08-02 |archive-url=https://web.archive.org/web/20130927122231/http://www.dexdomitor.com/ |archive-date=2013-09-27 |url-status=dead }}</ref> It is also used in humans to treat acute ] associated with ] or ].<ref name="Igalmi FDA label" /> It is administered as an ] or ] ] or as a ] or ] film.<ref name="FadenMusselmanCitrome2023">{{cite journal | vauthors = Faden J, Musselman M, Citrome L | title = Sublingual dexmedetomidine: repurposing an anesthetic as an anti-agitation agent | journal = Expert Rev Neurother | volume = 23 | issue = 2 | pages = 97–106 | date = February 2023 | pmid = 36707066 | doi = 10.1080/14737175.2023.2174430 | url = }}</ref>
			Similar to ], dexmedetomidine is a ] drug that acts as an ] of ]s in certain parts of the brain.<ref name="Cormack2005" /> It was developed by ].
	==Indications==		==Medical uses==
	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 α<sub>2</sub>-receptor stimulation with resulting hypotension, combined with its high cost relative to generic medications like propofol, fentanyl and midazolam which can achieve similar clinical effects
	===Intensive care unit sedation===		===Intensive care unit sedation===
			Studies suggest dexmedetomidine for sedation in ] adults may reduce time to ] and ICU stay.<ref>{{cite journal | vauthors = Pasin L, Greco T, Feltracco P, Vittorio A, Neto CN, Cabrini L, Landoni G, Finco G, Zangrillo A | display-authors = 6 | title = Dexmedetomidine as a sedative agent in critically ill patients: a meta-analysis of randomized controlled trials | journal = PLOS ONE | volume = 8 | issue = 12 | pages = e82913 | date = 2013-01-01 | pmid = 24391726 | pmc = 3877008 | doi = 10.1371/journal.pone.0082913 | doi-access = free | bibcode = 2013PLoSO...882913P }}</ref><ref name="Chen CD010269">{{cite journal | vauthors = Chen K, Lu Z, Xin YC, Cai Y, Chen Y, Pan SM | title = Alpha-2 agonists for long-term sedation during mechanical ventilation in critically ill patients | journal = The Cochrane Database of Systematic Reviews | volume = 1 | pages = CD010269 | date = January 2015 | issue = 1 | pmid = 25879090 | pmc = 6353054 | doi = 10.1002/14651858.CD010269.pub2 }}</ref>
	Compared to ], dexmedetomidine was similarly effective for sedation, but shortened the time to ]. It was associated with less ], ] and ]. but more ]. <ref name=Riker2009/> It also seemed to be superior to lorazepam for ] patients in the ].<ref name=Pandha2007/> Compared to midazolam, dexmedetomidine is superior due to reduced intensive care costs. The reduced costs are due to a reduction in ] stay as well as reduced ].<ref name=OConnor2009/>
			Compared with other ]s, some studies suggest dexmedetomidine may be associated with less ].<ref name="MacLaren 167–175">{{cite journal | vauthors = MacLaren R, Preslaski CR, Mueller SW, Kiser TH, Fish DN, Lavelle JC, Malkoski SP | title = 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 = Journal of Intensive Care Medicine | volume = 30 | issue = 3 | pages = 167–175 | date = March 2015 | pmid = 24227448 | doi = 10.1177/0885066613510874 | s2cid = 25036525 }}</ref> However, this finding is not consistent across multiple studies.<ref name="Chen CD010269" /> 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.<ref>{{cite journal | vauthors = Li B, Wang H, Wu H, Gao C | title = Neurocognitive dysfunction risk alleviation with the use of dexmedetomidine in perioperative conditions or as ICU sedation: a meta-analysis | journal = Medicine | volume = 94 | issue = 14 | pages = e597 | date = April 2015 | pmid = 25860207 | pmc = 4554047 | doi = 10.1097/MD.0000000000000597 }}</ref> Whether this observation has a beneficial psychological impact is unclear.<ref name="MacLaren 167–175"/> From an economic perspective, dexmedetomidine is associated with lower ICU costs, largely due to a shorter time to extubation.<ref>{{cite journal | vauthors = Turunen H, Jakob SM, Ruokonen E, Kaukonen KM, Sarapohja T, Apajasalo M, Takala J | title = Dexmedetomidine versus standard care sedation with propofol or midazolam in intensive care: an economic evaluation | journal = Critical Care | volume = 19 | pages = 67 | date = February 2015 | issue = 1 | pmid = 25887576 | pmc = 4391080 | doi = 10.1186/s13054-015-0787-y | doi-access = free }}</ref>
	===Procedural sedation===		===Procedural sedation===
			Dexmedetomidine can also be used for procedural sedation such as during colonoscopy.<ref>{{cite journal | vauthors = Dere K, Sucullu I, Budak ET, Yeyen S, Filiz AI, Ozkan S, Dagli G | title = A comparison of dexmedetomidine versus midazolam for sedation, pain and hemodynamic control, during colonoscopy under conscious sedation | journal = European Journal of Anaesthesiology | volume = 27 | issue = 7 | pages = 648–652 | date = July 2010 | pmid = 20531094 | doi = 10.1097/EJA.0b013e3283347bfe | s2cid = 24778669 | doi-access = free }}</ref> It can be used as an adjunct with other sedatives like ]s, ]s, and ] to enhance sedation and help maintain hemodynamic stability by decreasing the requirement of other sedatives.<ref name=Paris2005/><ref>{{cite journal | vauthors = Giovannitti JA, Thoms SM, Crawford JJ | title = Alpha-2 adrenergic receptor agonists: a review of current clinical applications | journal = Anesthesia Progress | volume = 62 | issue = 1 | pages = 31–39 | date = 2015-01-01 | pmid = 25849473 | pmc = 4389556 | doi = 10.2344/0003-3006-62.1.31 }}</ref> Dexmedetomidine is also used for procedural sedation in children.<ref>{{cite journal | vauthors = Ahmed SS, Unland T, Slaven JE, Nitu ME, Rigby MR | title = Successful use of intravenous dexmedetomidine for magnetic resonance imaging sedation in autistic children | journal = Southern Medical Journal | volume = 107 | issue = 9 | pages = 559–564 | date = September 2014 | pmid = 25188619 | doi = 10.14423/SMJ.0000000000000160 | s2cid = 43652106 }}</ref>
			It can be used for sedation required for ] in patients with a difficult airway.<ref>{{cite journal | vauthors = He XY, Cao JP, He Q, Shi XY | title = Dexmedetomidine for the management of awake fibreoptic intubation | journal = The Cochrane Database of Systematic Reviews | issue = 1 | pages = CD009798 | date = January 2014 | volume = 2020 | pmid = 24442817 | pmc = 8095023 | doi = 10.1002/14651858.cd009798.pub2 }}</ref>
			===Adjunct in general anesthesia===
			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.<ref name="pmid22546966">{{cite journal | vauthors = Blaudszun G, Lysakowski C, Elia N, Tramèr MR | title = Effect of perioperative systemic α2 agonists on postoperative morphine consumption and pain intensity: systematic review and meta-analysis of randomized controlled trials | journal = Anesthesiology | volume = 116 | issue = 6 | pages = 1312–22 | date = June 2012 | pmid = 22546966 | doi = 10.1097/ALN.0b013e31825681cb | s2cid = 3117071 | doi-access = free }}</ref><ref name="pmid23524149">{{cite journal | vauthors = Kim SY, Kim JM, Lee JH, Song BM, Koo BN | title = Efficacy of intraoperative dexmedetomidine infusion on emergence agitation and quality of recovery after nasal surgery | journal = British Journal of Anaesthesia | volume = 111 | issue = 2 | pages = 222–8 | date = August 2013 | pmid = 23524149 | doi = 10.1093/bja/aet056 | doi-access = free }}</ref><ref name="pmid20705788">{{cite journal | vauthors = Patel A, Davidson M, Tran MC, Quraishi H, Schoenberg C, Sant M, Lin A, Sun X | title = Dexmedetomidine infusion for analgesia and prevention of emergence agitation in children with obstructive sleep apnea syndrome undergoing tonsillectomy and adenoidectomy | journal = Anesthesia and Analgesia | volume = 111 | issue = 4 | pages = 1004–10 | date = October 2010 | pmid = 20705788 | doi = 10.1213/ANE.0b013e3181ee82fa | s2cid = 35590020 | doi-access = free }}</ref><ref name="pmid35957999">{{cite journal | vauthors = Tang Y, Song Y, Tian W, Chen G, Gu Y | title = A systematic review and meta-analysis on the efficacy and safety of dexmedetomidine combined with sevoflurane anesthesia on emergence agitation in children | journal = Translational Pediatrics | volume = 11 | issue = 7 | pages = 1156–1170 | date = July 2022 | pmid = 35957999 | pmc = 9360810 | doi = 10.21037/tp-22-172 | doi-access = free }}</ref>
	Dexmedetomidine has sedative, ], ], and ] effects that blunt many of the cardiovascular responses in the ] period. It reduces the requirements for ]s, sedatives and analgesics without causing significant ].<ref name=Paris2005/>
	===Other===		===Other===
			Dexmedetomidine may be useful for the treatment of the negative cardiovascular effects of acute ] and ] ] and ].<ref name=Menon2007/><ref name="Richards_2015">{{cite journal | vauthors = Richards JR, Albertson TE, Derlet RW, Lange RA, Olson KR, Horowitz BZ | title = Treatment of toxicity from amphetamines, related derivatives, and analogues: a systematic clinical review | journal = Drug and Alcohol Dependence | volume = 150 | pages = 1–13 | date = May 2015 | pmid = 25724076 | doi = 10.1016/j.drugalcdep.2015.01.040 }}</ref> Dexmedetomidine has also been used as an adjunct to ] for lower limb procedures.<ref>{{cite journal | vauthors = Mahendru V, Tewari A, Katyal S, Grewal A, Singh MR, Katyal R | title = A comparison of intrathecal dexmedetomidine, clonidine, and fentanyl as adjuvants to hyperbaric bupivacaine for lower limb surgery: A double blind controlled study | journal = Journal of Anaesthesiology Clinical Pharmacology | volume = 29 | issue = 4 | pages = 496–502 | date = October 2013 | pmid = 24249987 | pmc = 3819844 | doi = 10.4103/0970-9185.119151 | doi-access = free }}</ref> It has been successfully used to treat opioid withdrawal symptoms.<ref name="pmid22346054">{{cite journal | vauthors = Upadhyay SP, Mallick PN, Elmatite WM, Jagia M, Taqi S | title = Dexmedetomidine infusion to facilitate opioid detoxification and withdrawal in a patient with chronic opioid abuse | journal = Indian Journal of Palliative Care | volume = 17 | issue = 3 | pages = 251–4 | date = September 2011 | pmid = 22346054 | pmc = 3276827 | doi = 10.4103/0973-1075.92353 | doi-access = free }}</ref>
	Dexmedetomidine may be useful for the treatment of the deleterious cardiovascular effects of acute ] ] and ].<ref name=Menon2007/> 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.<ref name=Jackson2006/>
			In 2022 it was approved by the FDA for the treatment of agitation in schizophrenia and bipolar disorder.<ref name="FDA_2022">{{Cite web |title=FDA Okays First Sublingual Med for Agitation in Schizophrenia, BD |url=http://www.medscape.com/viewarticle/971866 |access-date=2022-04-11 |website=Medscape |language=en |archive-date=2022-04-11 |archive-url=https://web.archive.org/web/20220411224254/https://www.medscape.com/viewarticle/971866 |url-status=live }}</ref>
	==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.<ref name=Dosing/>
	==See also==		==Side effects==
			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.<ref>{{cite journal | vauthors = Ebert TJ, Hall JE, Barney JA, Uhrich TD, Colinco MD | title = The effects of increasing plasma concentrations of dexmedetomidine in humans | journal = Anesthesiology | volume = 93 | issue = 2 | pages = 382–394 | date = August 2000 | pmid = 10910487 | doi = 10.1097/00000542-200008000-00016 | s2cid = 20795504 | doi-access = free }}</ref> Common side effects include: hypotension, hypertension, with slight decreases in heart rate, arrhythmias, and hypoxia.<ref>{{cite web | url=https://www.drugs.com/sfx/dexmedetomidine-side-effects.html | title=Dexmedetomidine Side Effects: Common, Severe, Long Term }}</ref><ref name="Gertler_2001">{{cite journal | vauthors = Gertler R, Brown HC, Mitchell DH, Silvius EN | title = Dexmedetomidine: a novel sedative-analgesic agent | journal = Proceedings | volume = 14 | issue = 1 | pages = 13–21 | date = January 2001 | pmid = 16369581 | pmc = 1291306 | doi = 10.1080/08998280.2001.11927725 }}</ref> Toxic doses may cause first-degree or second-degree ]. 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.<ref name="Gertler_2001"/>
	* ], another α<sub>2</sub>-receptor agonist used in ].
	* ], a ] mixture of R and S-] of Dexmedetomidine used in small animal anesthesia.<ref name=PubChem/>
	* ], a similar compound used largely in large animal anesthesia.
	==References==		== Interactions ==
			Dexmedetomidine may enhance the effects of other sedatives and anesthetics when co-administered. Similarly, drugs that lower blood pressure and heart rate, such as ]s, may also have enhanced effects when co-administered with dexmedetomidine.<ref name="Keating 1119–1130"/>
	{{Reflist|colwidth=30em|refs=
			== Pharmacology==
	<ref name=Cormack2005>{{cite journal|author=Cormack JR, Orme RM, Costello TG|title=The role of alpha2-agonists in neurosurgery|journal=Journal of Clinical Neuroscience|year=2005|volume=12|issue=4|pages=375–8|doi=10.1016/j.jocn.2004.06.008|pmid=15925765|url=}}</ref>
			=== Pharmacodynamics ===
			{| class="wikitable floatright"
			|+ Dexmedetomidine at targets<ref name="BindingDB">{{cite web | last=Liu | first=Tiqing | title=BindingDB BDBM50085683 (+)-4-((S)-alpha,2,3-trimethylbenzyl)imidazole::4--1H-imidazole::CHEMBL778::DEXMEDETOMIDINE::MPV 1440 | website=BindingDB | url=https://www.bindingdb.org/rwd/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50085683 | access-date=11 September 2024}}</ref><ref name="PDSPKiDatabase">{{cite web | title=PDSP Database | website=UNC | url=https://pdsp.unc.edu/databases/pdsp.php?receptorDD=&receptor=&speciesDD=&species=&sourcesDD=&source=&hotLigandDD=&hotLigand=&testLigandDD=&testFreeRadio=testFreeRadio&testLigand=Dexmedetomidine&referenceDD=&reference=&KiGreater=&KiLess=&kiAllRadio=all&doQuery=Submit+Query | language=zu | access-date=11 September 2024}}</ref>
			! Site
			! ''K''<sub>i</sub> (nM)
			! Species
			! Ref
			|-
			| ]
			| 5
			| Human
			| <ref name="RossJetterMcDonnell2000">{{cite journal | vauthors = Ross TM, Jetter MC, McDonnell ME, Boyd RE, Connelly CD, Martinez RP, Lewis MA, Codd EE, Raffa RB, Reitz AB | display-authors = 6 | title = alpha(2) Adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-Imidazo)-1,3-dimethyl-6,7-dihydrothianaphthene as a high-affinity ligand for the alpha(2D) adrenergic receptor | journal = Journal of Medicinal Chemistry | volume = 43 | issue = 5 | pages = 765–768 | date = March 2000 | pmid = 10715142 | doi = 10.1021/jm990569e |url=https://www.bindingdb.org/rwd/jsp/dbsearch/Summary_ki.jsp?entryid=50009620&ki_result_id=50118025&reactant_set_id=50118025&energyterm=kJ/mole&kiunit=nM&icunit=nM }}</ref>
			|-
			| ]
			| 200
			| Human
			| <ref name="MillanDekeyneNewman-Tancredi2000" />
			|-
			| ]
			| 316
			| Human
			| <ref name="MillanDekeyneNewman-Tancredi2000" />
			|-
			| ]
			| 79
			| Human
			| <ref name="MillanDekeyneNewman-Tancredi2000" />
			|-
			| ]
			| 0.015–16
			| Human
			| <ref name="BoydPressRasmussen1999">{{cite journal | vauthors = Boyd RE, Press JB, Rasmussen CR, Raffa RB, Codd EE, Connelly CD, Bennett DJ, Kirifides AL, Gardocki JF, Reynolds B, Hortenstein JT, Reitz AB | display-authors = 6 | title = Alpha(2) adrenoceptor agonists as potential analgesic agents. 1. (Imidazolylmethyl)oxazoles and -thiazoles | journal = Journal of Medicinal Chemistry | volume = 42 | issue = 25 | pages = 5064–5071 | date = December 1999 | pmid = 10602691 | doi = 10.1021/jm990005a |url=https://www.bindingdb.org/rwd/jsp/dbsearch/Summary_ki.jsp?entryid=50003533&ki_result_id=51152970&reactant_set_id=51152970&energyterm=kJ/mole&kiunit=nM&icunit=nM }}</ref><ref name="JasperLesnickChang1998" /><ref name="MillanDekeyneNewman-Tancredi2000" /><ref name="VucicevicSrdic-RajicPieroni2016">{{cite journal | vauthors = 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 | title = A combined ligand- and structure-based approach for the identification of rilmenidine-derived compounds which synergize the antitumor effects of doxorubicin | journal = Bioorg Med Chem | volume = 24 | issue = 14 | pages = 3174–3183 | date = July 2016 | pmid = 27265687 | doi = 10.1016/j.bmc.2016.05.043 | url = }}</ref>
			|-
			| ]
			| 2.0–34
			| Human
			| <ref name="JasperLesnickChang1998">{{cite journal | vauthors = Jasper JR, Lesnick JD, Chang LK, Yamanishi SS, Chang TK, Hsu SA, Daunt DA, Bonhaus DW, Eglen RM | title = Ligand efficacy and potency at recombinant alpha2 adrenergic receptors: agonist-mediated GTPgammaS binding | journal = Biochem Pharmacol | volume = 55 | issue = 7 | pages = 1035–1043 | date = April 1998 | pmid = 9605427 | doi = 10.1016/s0006-2952(97)00631-x | url = }}</ref><ref name="MillanDekeyneNewman-Tancredi2000">{{cite journal | vauthors = Millan 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 | title = S18616, a highly potent, spiroimidazoline agonist at alpha(2)-adrenoceptors: I. Receptor profile, antinociceptive and hypothermic actions in comparison with dexmedetomidine and clonidine | journal = J Pharmacol Exp Ther | volume = 295 | issue = 3 | pages = 1192–1205 | date = December 2000 | pmid = 11082457 | doi = | url = }}</ref>
			|-
			| ]
			| 15–95
			| Human
			| <ref name="JasperLesnickChang1998" /><ref name="MillanDekeyneNewman-Tancredi2000" /><ref name="CrassousCardinalettiCarrieri2007">{{cite journal | vauthors = Crassous PA, Cardinaletti C, Carrieri A, Bruni B, Di Vaira M, Gentili F, Ghelfi F, Giannella M, Paris H, Piergentili A, Quaglia W, Schaak S, Vesprini C, Pigini M | display-authors = 6 | title = Alpha2-adrenoreceptors profile modulation. 3.1 (R)-(+)-m-nitrobiphenyline, a new efficient and alpha2C-subtype selective agonist | journal = Journal of Medicinal Chemistry | volume = 50 | issue = 16 | pages = 3964–3968 | date = August 2007 | pmid = 17630725 | doi = 10.1021/jm061487a |url=https://www.bindingdb.org/rwd/jsp/dbsearch/Summary_ki.jsp?entryid=50020830&ki_result_id=50069440&reactant_set_id=50069440&energyterm=kJ/mole&kiunit=nM&icunit=nM }}</ref>
			|-
			<!-- | ]
			| 0.015
			| Rodent
			| <ref name="RossJetterMcDonnell2000" /><ref name="BoydPressRasmussen2001">{{cite journal | vauthors = Boyd RE, Press JB, Rasmussen CR, Raffa RB, Codd EE, Connelly CD, Li QS, Martinez RP, Lewis MA, Almond HR, Reitz AB | title = Alpha(2) adrenoceptor agonists as potential analgesic agents. 3. Imidazolylmethylthiophenes | journal = J Med Chem | volume = 44 | issue = 6 | pages = 863–872 | date = March 2001 | pmid = 11300868 | doi = 10.1021/jm0003891 | url = }}</ref>
			|- -->
			| ]
			| 200
			| Bovine
			| <ref name="MillanDekeyneNewman-Tancredi2000" />
			|-
			| ]
			| 50
			| Rat
			| <ref name="MillanDekeyneNewman-Tancredi2000" />
			|-
			| ]
			| >1,000
			| Human
			| <ref name="MillanDekeyneNewman-Tancredi2000" />
			|}
			Dexmedetomidine is a highly ] ] ]. It possesses an α<sub>2</sub>:α<sub>1</sub> selectivity ratio of 1620:1, making it 8{{nbsp}}times more selective for the α<sub>2</sub>-adrenergic receptor than the related drug ].<ref>{{Cite journal | vauthors = Scott-Warren VL, Sebastian J |date=2016 |title=Dexmedetomidine: its use in intensive care medicine and anaesthesia |journal=BJA Education |volume=16 |issue=7 |pages=242–246 |doi=10.1093/bjaed/mkv047 |doi-access=free }}</ref><ref name="WeerinkStruysHannivoort2017">{{cite journal | vauthors = Weerink MA, Struys MM, Hannivoort LN, Barends CR, Absalom AR, Colin P | title = Clinical Pharmacokinetics and Pharmacodynamics of Dexmedetomidine | journal = Clin Pharmacokinet | volume = 56 | issue = 8 | pages = 893–913 | date = August 2017 | pmid = 28105598 | pmc = 5511603 | doi = 10.1007/s40262-017-0507-7 | url = }}</ref> Unlike ]s and other ]s such as ], dexmedetomidine is able to achieve its effects without causing ]. Dexmedetomidine induces sedation by decreasing activity of ] ]s in the ] in the ], thereby increasing the downstream activity of inhibitory ] (GABA) neurons in the ].<ref name="WeerinkStruysHannivoort2017" /><ref name="Nelson_2003">{{cite journal | vauthors = Nelson LE, Lu J, Guo T, Saper CB, Franks NP, Maze M | title = The alpha2-adrenoceptor agonist dexmedetomidine converges on an endogenous sleep-promoting pathway to exert its sedative effects | journal = Anesthesiology | volume = 98 | issue = 2 | pages = 428–436 | date = February 2003 | pmid = 12552203 | doi = 10.1097/00000542-200302000-00024 | s2cid = 5034487 | doi-access = free }}</ref> In contrast, other sedatives like propofol and ]s directly increase activity of GABAergic neurons.<ref name="Panzer_2009">{{cite journal | vauthors = Panzer O, Moitra V, Sladen RN | title = Pharmacology of sedative-analgesic agents: dexmedetomidine, remifentanil, ketamine, volatile anesthetics, and the role of peripheral mu antagonists | journal = Critical Care Clinics | volume = 25 | issue = 3 | pages = 451–69, vii | date = July 2009 | pmid = 19576524 | doi = 10.1016/j.ccc.2009.04.004 }}</ref> Through action on this endogenous sleep-promoting pathway the sedation produced by dexmedetomidine more closely mirrors natural ] (specifically stage 2 ] (NREM)), as demonstrated by ] studies.<ref name="WeerinkStruysHannivoort2017" /><ref name="Nelson_2003" /><ref>{{cite journal | vauthors = Huupponen E, Maksimow A, Lapinlampi P, Särkelä M, Saastamoinen A, Snapir A, Scheinin H, Scheinin M, Meriläinen P, Himanen SL, Jääskeläinen S | display-authors = 6 | title = Electroencephalogram spindle activity during dexmedetomidine sedation and physiological sleep | journal = Acta Anaesthesiologica Scandinavica | volume = 52 | issue = 2 | pages = 289–294 | date = February 2008 | pmid = 18005372 | doi = 10.1111/j.1399-6576.2007.01537.x | s2cid = 34923432 }}</ref> As such, dexmedetomidine provides less ] than benzodiazepines.<ref name="Panzer_2009"/> Dexmedetomidine also has ] effects at the ] level and other supraspinal sites.<ref name="Panzer_2009"/>
	<ref name=Dosing>{{cite web|author=|title=Dosing Guidelines for Precedex®|doi=|pmid=|url=http://www.precedex.com/wp-content/uploads/2010/02/Dosing_Guide.pdf|accessdate=2010-11-21}}</ref>
			=== Pharmacokinetics ===
	<ref name=Jackson2006>{{cite journal|author=Jackson KC, Wang Z, Wohlt P, Fine PG|title=Dexmedetomidine a novel analgesic with palliative medicine potential|journal=J Pain and Palliative Care Pharmacotherapy|year=2006|volume=20|issue=2|pages=23–7|doi=10.1080/J354v20n02_05|pmid=16702133|url=}}</ref>
			Intravenous dexmedetomidine exhibits linear pharmacokinetics with a rapid ] of approximately 6{{nbsp}}minutes in healthy volunteers, and a longer and more variable distribution half-life in ICU patients.<ref>{{cite journal | vauthors = Venn RM, Karol MD, Grounds RM | title = Pharmacokinetics of dexmedetomidine infusions for sedation of postoperative patients requiring intensive caret | journal = British Journal of Anaesthesia | volume = 88 | issue = 5 | pages = 669–675 | date = May 2002 | pmid = 12067004 | doi = 10.1093/bja/88.5.669 | doi-access = free }}</ref> The terminal ] of intravenous dexmedetomidine ranged 2.1 to 3.1{{nbsp}}hours in healthy adults and 2.2 to 3.7{{nbsp}}hours in ICU patients.<ref name="Weerink_2017">{{cite journal | vauthors = Weerink MA, Struys MM, Hannivoort LN, Barends CR, Absalom AR, Colin P | title = Clinical Pharmacokinetics and Pharmacodynamics of Dexmedetomidine | journal = Clinical Pharmacokinetics | volume = 56 | issue = 8 | pages = 893–913 | date = August 2017 | pmid = 28105598 | pmc = 5511603 | doi = 10.1007/s40262-017-0507-7 }}</ref> The ] of dexmedetomidine is about 94% (mostly ]).<ref name="Precedex FDA label" />
			Dexmedetomidine is ] by the ], largely by ] (34%) as well as by ] via ] and other ] ]s.<ref name="Weerink_2017" /> As such, it should be used with caution in people with ] or ].<ref name="Keating 1119–1130">{{cite journal | vauthors = Keating GM | title = Dexmedetomidine: A Review of Its Use for Sedation in the Intensive Care Setting | journal = Drugs | volume = 75 | issue = 10 | pages = 1119–1130 | date = July 2015 | pmid = 26063213 | doi = 10.1007/s40265-015-0419-5 | s2cid = 20447722 | doi-access = free }}</ref>
	<ref name=Menon2007>{{cite journal|author=Menon DV, Wang Z, Fadel PJ, Arbique D, Leonard D, Li JL, Victor RG, Vongpatanasin W|title=Central sympatholysis as a novel countermeasure for cocaine-induced sympathetic activation and vasoconstriction in humans|journal=J Am Coll Cardiol|year=2007|volume=50|issue=7|pages=626–33|doi=10.1016/j.jacc.2007.03.060|pmid=17692748|url=}}</ref>
			The majority of metabolized dexmedetomidine is ] in the ] (~95%).{{Medical citation needed|date=October 2021}}
	<ref name=OConnor2009>{{cite journal|last1=O'Connor|first1=M|last2=Bucknall|first2=T|last3=Manias|first3=E|title=Sedation Management in Australian and New Zealand Intensive Care Units: Doctors' and Nurses' Practices and Opinions|journal=Am J Crit Care|year=2009|volume=19|issue=3|pages=285–95|doi=10.4037/ajcc2009541|pmid=19770414|url=}}</ref>
			It can also be ] ].<ref name="FDA_2022" />
	<ref name=Pandha2007>{{cite journal|last1=Pandharipande|first1=PP|last2=Pun|first2=BT|last3=Herr|first3=DL|last4=Maze|first4=M|last5=Girard|first5=TD|last6=Miller|first6=RR|last7=Shintani|first7=AK|last8=Thompson|first8=JL|last9=Jackson|first9=JC|title=Effect of sedation with dexmedetomidine vs lorazepam on acute brain dysfunction in mechanically ventilated patients: the MENDS randomized controlled trial|journal=JAMA|volume=298|issue=22|pages=2644–53|year=2007|doi=10.1001/jama.298.22.2644|pmid=18073360|url=}}</ref>
			== History ==
	<ref name=Paris2005>{{cite journal|author=Paris A, Tonner PH|title=Dexmedetomidine in anaesthesia|journal=Current Opinion in Anaesthesiology|year=2005|volume=18|issue=4|pages=412–8|doi=10.1097/01.aco.0000174958.05383.d5|pmid=16534267}}</ref>
			Dexmedetomidine was developed by ] 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 the ]. 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.<ref>{{cite journal | vauthors = Shehabi Y, Ruettimann U, Adamson H, Innes R, Ickeringill M | title = Dexmedetomidine infusion for more than 24 hours in critically ill patients: sedative and cardiovascular effects | journal = Intensive Care Medicine | volume = 30 | issue = 12 | pages = 2188–2196 | date = December 2004 | pmid = 15338124 | doi = 10.1007/s00134-004-2417-z | s2cid = 26258023 | doi-access = free }}</ref>
			==Veterinary use==
	<ref name=PubChem>{{PubChem|5311068}}</ref>
			Dexmedetomidine, under the brand name Dexdomitor (]), was approved in the European Union for use in cats and dogs in 2002, for sedation and induction of general anesthesia.<ref name="Gozalo-Marcilla 2018">{{cite journal | vauthors = Gozalo-Marcilla M, Gasthuys F, Luna SP, Schauvliege S | title = Is there a place for dexmedetomidine in equine anaesthesia and analgesia? A systematic review (2005-2017) | journal = Journal of Veterinary Pharmacology and Therapeutics | volume = 41 | issue = 2 | pages = 205–217 | date = April 2018 | pmid = 29226340 | doi = 10.1111/jvp.12474 | s2cid = 3691570 }}</ref> The FDA approved dexmedetomidine for use in dogs in 2006 and cats in 2007.<ref>{{cite web |title=Freedom of Information Summary {{!}} Supplemental New Animal Drug Application {{!}} NADA 141-267 {{!}} Dexdomitor |url=https://animaldrugsatfda.fda.gov/adafda/app/search/public/document/downloadFoi/828 |publisher=Food and Drug Administration |access-date=2018-07-01 |date=16 August 2010 |archive-date=2021-08-28 |archive-url=https://web.archive.org/web/20210828060527/https://animaldrugsatfda.fda.gov/adafda/app/search/public/document/downloadFoi/828 |url-status=live }}</ref>
			In 2015, the European Medicines Agency and the FDA approved an oromucosal gel form of dexmedetomidine marketed as Sileo by pharmaceutical company ] for use in dogs for relief of noise aversion.<ref>{{cite web |url=https://www.fda.gov/AnimalVeterinary/Products/ApprovedAnimalDrugProducts/ucm363948.htm |title=Recent Animal Drug Approvals |author=<!--Staff writer(s); no by-line.--> |date=2 June 2016 |publisher=U.S. Department of Health and Human Services |access-date=3 July 2016 |quote=For the treatment of noise aversion in dogs |archive-date=12 July 2016 |archive-url=https://web.archive.org/web/20160712163311/http://www.fda.gov/AnimalVeterinary/Products/ApprovedAnimalDrugProducts/ucm363948.htm |url-status=live }}</ref><ref>{{cite journal | vauthors = | title = Veterinary medicines: product update | journal = The Veterinary Record | volume = 177 | issue = 5 | pages = 116–117 | date = August 2015 | pmid = 26231872 | doi = 10.1136/vr.h4051 | s2cid = 42312260 }}</ref>
	<ref name=Riker2009>{{cite journal|author=Riker RR, Shehabi Y, Bokesch PM, Ceraso D, Wisemandle W, Koura F, Whitten P, Margolis BD, Byrne DW, Ely EW, Rocha MG|title=Dexmedetomidine vs Midazolam for Sedation of Critically Ill Patients: A Randomized Trial|journal=]|year=2009|volume=301|issue=5|pages=489–99|doi=10.1001/jama.2009.56|pmid=19188334|url=}}</ref>
			==References==
	}}
			{{Reflist|refs=
			<ref name=Cormack2005>{{cite journal | vauthors = Cormack JR, Orme RM, Costello TG | title = The role of alpha2-agonists in neurosurgery | journal = Journal of Clinical Neuroscience | volume = 12 | issue = 4 | pages = 375–378 | date = May 2005 | pmid = 15925765 | doi = 10.1016/j.jocn.2004.06.008 | s2cid = 79899746 }}</ref>
	==External links==
	*
			<ref name=Menon2007>{{cite journal | vauthors = Menon DV, Wang Z, Fadel PJ, Arbique D, Leonard D, Li JL, Victor RG, Vongpatanasin W | display-authors = 6 | title = Central sympatholysis as a novel countermeasure for cocaine-induced sympathetic activation and vasoconstriction in humans | journal = Journal of the American College of Cardiology | volume = 50 | issue = 7 | pages = 626–633 | date = August 2007 | pmid = 17692748 | doi = 10.1016/j.jacc.2007.03.060 | doi-access = free }}</ref>
			<ref name=Paris2005>{{cite journal | vauthors = Paris A, Tonner PH | title = Dexmedetomidine in anaesthesia | journal = Current Opinion in Anesthesiology | volume = 18 | issue = 4 | pages = 412–418 | date = August 2005 | pmid = 16534267 | doi = 10.1097/01.aco.0000174958.05383.d5 | s2cid = 20014479 }}</ref>
			}}
	{{Adrenergic agonists}}
	{{Hypnotics and sedatives}}		{{Hypnotics and sedatives}}
			{{Anxiolytics}}
	]
			{{Adrenergic receptor modulators}}
	]
			{{Phenethylamines}}
	]
			{{Portal bar | Medicine}}
			]
	]
			]
	]
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	]
			]
			]
			]
			]
			]
			]
			]
			]