Page last updated: 2024-12-06

detomidine

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

Detomidine is a selective α2-adrenergic agonist, used as a sedative and analgesic in veterinary medicine. It was synthesized in the 1970s and its mechanism of action involves binding to α2-adrenergic receptors in the central nervous system, leading to the suppression of sympathetic nerve activity. This results in sedation, analgesia, muscle relaxation, and a decrease in heart rate and blood pressure. Detomidine is primarily used for sedation and analgesia in horses, cattle, and other animals, particularly during procedures such as surgery, dentistry, and transportation. It is also used for the treatment of colic in horses. Its importance lies in its ability to provide effective sedation and analgesia with a relatively short duration of action, making it a valuable tool for veterinarians. Research on detomidine continues to investigate its efficacy and safety in different species and for various applications, including its potential use in human medicine.'

detomidine: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID56032
CHEMBL ID2110829
SCHEMBL ID247340
MeSH IDM0122426

Synonyms (46)

Synonym
detomidinum [inn-latin]
1h-imidazole, 4-((2,3-dimethylphenyl)methyl)-
detomidine
detomidine [inn:ban]
4-(2,3-dimethylbenzyl)imidazol
detomidina [inn-spanish]
76631-46-4
detomidine (inn)
D07795
5-[(2,3-dimethylphenyl)methyl]-1h-imidazole
AKOS006271731
detomidina
unii-7n8k34p2xh
7n8k34p2xh ,
detomidinum
FT-0601981
1h-imidazole, 4-((2,3-dimethylphenyl)methyl)
4-(2,3-dimethylbenzyl)imidazole
detomidine [mi]
detomidine [inn]
SCHEMBL247340
HY-B0163
CS-1995
4-(2,3-dimethyl-benzyl)-1h-imidazole
DTXSID00227457 ,
4-(2',3'-dimethylbenzyl)imidazole
CHEMBL2110829
4-(2,3-dimethylbenzyl)-1h-imidazole
4-(2,3-dimethylbenzyl)imidazole hydrochloride
4-(2,3-dimethylbenzyl)-1h-imidazole #
AB01566879_01
SR-01000945281-1
sr-01000945281
dexdor (t)
BCP29001
1h-imidazole, 4-((2,3-dimethylphenyl)methyl)-;4-(2,3-dimethylbenzyl)imidazol;detomidina;4-(2,3-dimethylbenzyl)-1h-imidazole
Q3045367
DB11556
4721B
SB38652
A917401
EN300-27192520
detomidina (inn-spanish)
detomidinum (inn-latin)
dtxcid00149948
AKOS040745170

Research Excerpts

Overview

Detomidine is an alpha 2 adrenergic agonist, similar to clonidine. Detomidine was found to be a partial agonist producing about 43% of maximum inhibition obtained by medetomidine.

ExcerptReferenceRelevance
"Detomidine is an alpha 2 adrenergic agonist, similar to clonidine."( Parenteral exposure to detomidine and butorphanol.
Reid, FM; Tracey, JA, 1994
)
1.32
"Detomidine was found to be a partial agonist producing about 43% of maximum inhibition obtained by medetomidine."( Ocular hypotensive effects of medetomidine and its analogs.
Elko, EE; Jin, Y; Wilson, S; Yorio, T, 1991
)
1.29
"Detomidine is a potent non-narcotic sedative agent which is currently in the process of being approved for veterinary clinical use in the United States. "( Immunoassay detection of drugs in racing horses. IX. Detection of detomidine in equine blood and urine by radioimmunoassay.
Houtz, PK; Sturma, L; Tai, CL; Tai, HH; Taylor, DG; Wang, CJ; Weckman, TJ; Wood, T; Woods, WE; Yang, JM, 1989
)
1.96
"1. Detomidine is a novel veterinary sedative analgesic which is thought to act by stimulation of alpha 2 adrenoreceptors. "( Dose-related effects of detomidine on autonomic responses in the horse.
Bagwell, CA; Cravens, WM; Kamerling, SG, 1988
)
1.2

Actions

ExcerptReferenceRelevance
"For detomidine, the increase of mean thresholds compared to placebo was 5.4 +/- 1.7 times control levels with the electrical current test compared to 2.0 +/- 0.2 times for the mechanical pressure test (p = 0.040)."( A comparison of the antinociceptive effects of xylazine, detomidine and romifidine on experimental pain in horses.
Doherr, MG; Lanz, F; Moens, Y; Schatzmann, U, 2003
)
1.05

Treatment

ExcerptReferenceRelevance
"Detomidine-treated, halothane-anesthetized horses given atropine i.v. "( Effect of low-dose atropine administration on dobutamine dose requirement in horses anesthetized with detomidine and halothane.
Greene, SA; Keegan, RD; Weil, AB, 1997
)
1.95

Pharmacokinetics

detomidine was distributed rapidly and eliminated with a half-life (t1/2(el) of approximately 30 min. The study characterizes the pharmacokinetic (PK) and pharmacodynamic (PD) relationships of the α2-adrenergic receptor agonists detomazine (DET), medetomidine (MED) and dexmedetomalid (DEX)

ExcerptReferenceRelevance
" The mean peak concentration in the horse (51."( Single-dose pharmacokinetics of detomidine in the horse and cow.
Salonen, JS; Vähä-Vahe, T; Vainio, O; Vakkuri, O, 1989
)
0.56
" administration, detomidine was distributed rapidly and eliminated with a half-life (t1/2(el)) of approximately 30 min."( Pharmacokinetics of detomidine and its metabolites following intravenous and intramuscular administration in horses.
Grimsrud, KN; Mama, KR; Stanley, SD; Thomasy, SM, 2009
)
1.02
"These pharmacokinetic parameters provide information necessary for determination of peak plasma concentrations and clearance of detomidine in mature horses."( Pharmacokinetics of detomidine and its metabolites following intravenous and intramuscular administration in horses.
Grimsrud, KN; Mama, KR; Stanley, SD; Thomasy, SM, 2009
)
0.88
"Median back-extrapolated time zero plasma concentration was significantly lower and median plasma half-life and median mean residence time were significantly longer when detomidine was administered after exercise compared to administration at rest."( Pharmacokinetics of detomidine administered to horses at rest and after maximal exercise.
Hinchcliff, KW; Hubbell, JA; Muir, WW; Robertson, JT; Sams, RA; Schmall, LM, 2009
)
0.87
"The present study characterizes the pharmacokinetic (PK) and pharmacodynamic (PD) relationships of the α2-adrenergic receptor agonists detomidine (DET), medetomidine (MED) and dexmedetomidine (DEX) in parallel groups of horses from in vivo data after single bolus doses."( Pharmacokinetic and pharmacodynamic analysis comparing diverse effects of detomidine, medetomidine, and dexmedetomidine in the horse: a population analysis.
Ait-Oudhia, S; Durbin-Johnson, BP; Grimsrud, KN; Jusko, WJ; Mama, KR; Rezende, ML; Rocke, DM; Stanley, SD, 2015
)
0.85
" Blood samples were collected for quantification via liquid chromatography with mass spectrometry and pharmacokinetic analysis."( Pharmacokinetics of detomidine following intravenous or oral-transmucosal administration and sedative effects of the oral-transmucosal treatment in dogs.
Hopfensperger, M; Knych, HK; Messenger, KM; Papich, MG, 2016
)
0.76
"To determine the sedative effects and pharmacokinetic profile of detomidine when administered intravaginally as a gel formulation to horses."( Evaluation of the sedative effects and pharmacokinetics of detomidine gel administered intravaginally to horses.
Cox, SK; Doherty, TJ; Knych, HK; Moorhead, KA; Seddighi, R; Sun, X, 2019
)
0.99
" Characteristics of sedation and selected pharmacodynamic parameters were compared between groups using a non-parametric Mann-Whitney U test."( Xylazine or detomidine in dairy calves: a comparison of clinically relevant pharmacodynamic parameters under sedation.
Brehm, W; Gittel, C; Hillmann, A; Michaele, A; Roth, S; Wippern, M, 2021
)
1

Compound-Compound Interactions

The aim of this study was to compare the effects of methadone combined with detomidine or acepromazine on the quality of sedation and its influence over dissociative anesthesia in healthy horses. Increasing the dose ofdetomidine from 10 to 20 µg/kg increased the degree of sedated when administered with the same dose of buprenorphine.

ExcerptReferenceRelevance
" Increasing the dose of detomidine from 10 to 20 µg/kg increased the degree of sedation when administered with the same dose of buprenorphine (7."( Assessment of the sedative effects of buprenorphine administered with 20 microg/kg detomidine in horses.
Love, EJ; Murrell, J; Taylor, PM; Waterman-Pearson, AE; Whay, HR, 2011
)
0.9
"The effects of buprenorphine (5 μg kg(-1) ) (Group B, n = 46) or placebo (5% glucose solution) (Group C, n = 38) in combination with detomidine (10 μg kg(-1) ) were compared in standing horses undergoing minor clinical procedures."( Evaluation of sedation for standing clinical procedures in horses using detomidine combined with buprenorphine.
Coumbe, K; Henson, F; Scott, D; Taylor, A; Taylor, P, 2014
)
0.84
"To evaluate the antinociceptive effects of intravenous methadone combined with detomidine or acepromazine in adult horses."( Antinociceptive effects of methadone combined with detomidine or acepromazine in horses.
Crosignani, N; Lopes, C; Luna, SP; Pantoja, JC; Puoli, JN; Quarterone, C; Rosa, AC; Taylor, PM, 2016
)
0.91
"To compare sedative and analgesic properties of buprenorphine or morphine for standing procedures combined with a detomidine continuous rate infusion (CRI)."( Preliminary investigation comparing a detomidine continuous rate infusion combined with either morphine or buprenorphine for standing sedation in horses.
Love, EJ; MacFarlane, PD; Murrell, JC; Potter, JJ; Taylor, PM; Tremaine, H, 2016
)
0.92
"The objective of the study was to evaluate the duration of the effects of sedation with detomidine and detomidine combined with a low dose of butorphanol on the movement patterns of horses."( A kinematic comparison of the locomotor pattern of horses sedated with detomidine alone and in combination with low doses of butorphanol.
Frigerio, MA; Gómez Cisneros, D; López-Sanromán, J; Manso-Díaz, G; Santiago Llorente, I, 2019
)
0.97
"The objective of this study was to compare intravenous (IV) xylazine and detomidine as sedatives in combination with midazolam and ketamine for induction of anaesthesia in horses undergoing field castration."( Comparison of xylazine and detomidine in combination with midazolam/ketamine for field castration in Quarter Horses.
Bass, L; Damone, J; Mama, K; Rao, S; Smith, MC, 2020
)
1.09
"The aim of this study was to compare the effects of methadone combined with detomidine or acepromazine on the quality of sedation and its influence over dissociative anesthesia in healthy horses."( Effect of Methadone Combined With Acepromazine or Detomidine on Sedation and Dissociative Anesthesia in Healthy Horses.
Alonso, BB; Bisetto, SP; Carregaro, AB; Censoni, JB; Reginato, GM; Ueda, GI, 2020
)
1.04

Bioavailability

The objective of the study was to determine the absorption, bioavailability and sedative effect of detomidine administered to horses as an oromucosal gel compared to intravenous and intramuscular administration. The mean maximum plasma concentration ofdetomidine, time to maximum concentration and bioavailability for treatment IVG was 8.

ExcerptReferenceRelevance
"The objective of the study was to determine the absorption, bioavailability and sedative effect of detomidine administered to horses as an oromucosal gel compared to intravenous and intramuscular administration of detomidine injectable solution."( Bioavailability of detomidine administered sublingually to horses as an oromucosal gel.
Aspegrén, J; Hyyppä, S; Kaukinen, H; Salonen, JS; Tamm, L, 2011
)
0.91
" The bioavailability of detomidine was approximately 34% with GEL."( Sublingual administration of detomidine to calves prior to disbudding: a comparison with the intravenous route.
Hänninen, L; Hokkanen, AH; Norring, M; Raekallio, MR; Raussi, S; Rinne, VM; Salla, K; Scheinin, M; Vainio, OM; Viitasaari, E, 2014
)
1
" The mean maximum plasma concentration of detomidine, time to maximum concentration and bioavailability for treatment DET-VAG were 39."( Sedative effects and pharmacokinetics of detomidine when administered intravenously and intravaginally as a gel in alpacas.
Chow, NS; Doherty, TJ; Knych, HK; Seddighi, R; Sun, X, 2020
)
1.09

Dosage Studied

Eight domestic goats (Capra hircus) were anesthetized with a combination of carfentanil citrate and detomidine HCl each at a dosage of 60 micrograms/kg. Detomidine induced sedation and antinociception, but only antinOCiception was dosage dependent. The dose-response curve of detomidine was shifted to the right in a parallel manner by the selective alpha 2-antagonist idazoxan.

ExcerptRelevanceReference
" The dose-response curves of medetomidine and its analogs showed that the ranked order of intrinsic activity at lowering IOP was medetomidine greater than or equal to MPV-1440 greater than detomidine greater than MPV-1441 and MPV-305 BII."( Ocular hypotensive effects of medetomidine and its analogs.
Elko, EE; Jin, Y; Wilson, S; Yorio, T, 1991
)
0.85
" With the exception of a greater hypertensive response, detomidine at the dosages studied, produced cardiovascular effects that were very similar to those of the recommended dosage of xylazine."( Cardiovascular effects of detomidine, a new alpha 2-adrenoceptor agonist, in the conscious pony.
Garner, HE; Krause, GF; Sarazan, RD; Starke, WA, 1989
)
0.82
" dosing occurred."( Single-dose pharmacokinetics of detomidine in the horse and cow.
Salonen, JS; Vähä-Vahe, T; Vainio, O; Vakkuri, O, 1989
)
0.56
" The present study was undertaken to determine the direction, time course, and dose-response relationship of detomidine on specific autonomic responses in the unanaesthetized horse."( Dose-related effects of detomidine on autonomic responses in the horse.
Bagwell, CA; Cravens, WM; Kamerling, SG, 1988
)
0.79
" The dose-response curve of detomidine was shifted to the right in a parallel manner by the selective alpha 2-antagonist idazoxan."( Effect of detomidine on the release and turnover of noradrenaline in rat brain.
Kaisila, M; MacDonald, E; Virtanen, R, 1986
)
0.97
" A 1% solution of detomidine HCl was injected into the epidural catheter at a dosage of 60 micrograms/kg of body weight, and was expanded to a 10-ml volume with sterile water to induce selective caudal epidural analgesia (CEA)."( Caudal analgesia induced by epidural or subarachnoid administration of detomidine hydrochloride solution in mares.
Muir, WW; Skarda, RT, 1994
)
0.86
"The cardiorespiratory effects of thiamylal (10 mg/kg of body weight, IV) and the effects of preanesthetic medication with diazepam, acepromazine, detomidine, or xylazine administered prior to a thiamylal dosage of 6 mg/kg, IV, were evaluated in 6 adult horses."( Effects of diazepam, acepromazine, detomidine, and xylazine on thiamylal anesthesia in horses.
Mason, DE; Muir, WW, 1993
)
0.76
" An initial hand-injection of detomidine hydrochloride and butorphanol tartrate at a ratio of 1:1 on a microg:microg basis was administered intramuscularly, with a dosage range of 50-70 mg (12."( Standing sedation in African elephants (Loxodonta africana) using detomidine-butorphanol combinations.
Fontenot, DK; Miller, MA; Neiffer, DL; Pye, GW; Robbins, PK; Stetter, M; Weber, M, 2005
)
0.85
" Repeat dosing was required in 24% of Group B and 32% of Group C (p < 0."( Evaluation of sedation for standing clinical procedures in horses using detomidine combined with buprenorphine.
Coumbe, K; Henson, F; Scott, D; Taylor, A; Taylor, P, 2014
)
0.63
" Detomidine induced sedation and antinociception, but only antinociception was dosage dependent."( Sedation and mechanical antinociception after intravenous administration of detomidine in donkeys: a dosage-effect study.
Castillo-Alcala, F; Lizarraga, I; Robinson, LS; Varner, KM, 2015
)
1.56
" The dosage of MK-467 needs to be investigated to minimise the effect of MK-467 on MAP."( Detomidine and the combination of detomidine and MK-467, a peripheral alpha-2 adrenoceptor antagonist, as premedication in horses anaesthetized with isoflurane.
de Vries, A; Mykkänen, AK; Pakkanen, SA; Raekallio, MR; Salla, KM; Scheinin, M; Vainio, OM; Vuorilehto, L, 2015
)
1.86
" The SS did not differ among dosage groups, and the time-dose interaction was not statistically significant."( Oral Transmucosal Detomidine Gel in New Zealand White Rabbits (
Durrant, JR; Fish, RE; Griffith, EH; Long, CT; McKeon, GP; Messenger, KM; Shive, HR; Williams, MD, 2017
)
0.79
" The intravenous pharmacokinetics of butorphanol dosed individually compared with co-administration with detomidine had approximately a twofold larger clearance (646 ± 137 vs."( The intravenous pharmacokinetics of butorphanol and detomidine dosed in combination compared with individual dose administrations to exercised horses.
Bright, J; Hannan, C; Hillyer, L; Hincks, PR; Machnik, M; Paine, SW; Pearce, CM; Scarth, JP, 2020
)
1.02
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (300)

TimeframeStudies, This Drug (%)All Drugs %
pre-199056 (18.67)18.7374
1990's81 (27.00)18.2507
2000's67 (22.33)29.6817
2010's68 (22.67)24.3611
2020's28 (9.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 44.78

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index44.78 (24.57)
Research Supply Index6.04 (2.92)
Research Growth Index4.67 (4.65)
Search Engine Demand Index85.25 (26.88)
Search Engine Supply Index2.42 (0.95)

This Compound (44.78)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials98 (30.43%)5.53%
Reviews1 (0.31%)6.00%
Case Studies17 (5.28%)4.05%
Observational1 (0.31%)0.25%
Other205 (63.66%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]