Detomidine

Detomidine produce dose-dependent sedative and analgesic effects, is a nonnarcotic, synthetic α2-adrenergic agonist

Pharmacokinetics of detomidine following intravenous or oral-transmucosal administration and sedative effects of the oral-transmucosal treatment in dogs.[Pubmed:27027842]

Am J Vet Res. 2016 Apr;77(4):413-20.

OBJECTIVE: To determine the pharmacokinetics of Detomidine hydrochloride administered IV (as an injectable formulation) or by the oral-transmucosal (OTM) route (as a gel) and assess sedative effects of the OTM treatment in healthy dogs. ANIMALS: 12 healthy adult dogs. PROCEDURES: In phase 1, Detomidine was administered by IV (0.5 mg/m(2)) or OTM (1 mg/m(2)) routes to 6 dogs. After a 24-hour washout period, each dog received the alternate treatment. Blood samples were collected for quantification via liquid chromatography with mass spectrometry and pharmacokinetic analysis. In phase 2, 6 dogs received dexmeDetomidine IV (0.125 mg/m(2)) or Detomidine gel by OTM administration (0.5 mg/m(2)), and sedation was measured by a blinded observer using 2 standardized sedation scales while dogs underwent jugular catheter placement. After a l-week washout period, each dog received the alternate treatment. RESULTS: Median maximum concentration, time to maximum concentration, and bioavailability for Detomidine gel following OTM administration were 7.03 ng/mL, 1.00 hour, and 34.52%, respectively; harmonic mean elimination half-life was 0.63 hours. All dogs were sedated and became laterally recumbent with phase 1 treatments. In phase 2, median global sedation score following OTM administration of Detomidine gel was significantly lower (indicating a lesser degree of sedation) than that following IV dexmeDetomidine treatment; however, total sedation score during jugular vein catheterization did not differ between treatments. The gel was subjectively easy to administer, and systemic absorption was sufficient for sedation. CONCLUSIONS AND CLINICAL RELEVANCE: Detomidine gel administered by the OTM route provided sedation suitable for a short, minimally invasive procedure in healthy dogs.

Sedation and mechanical hypoalgesia after sublingual administration of detomidine hydrochloride gel to donkeys.[Pubmed:27308886]

J Am Vet Med Assoc. 2016 Jul 1;249(1):83-9.

OBJECTIVE To compare sedative and mechanical hypoalgesic effects of sublingual administration of 2 doses of Detomidine gel to donkeys. DESIGN Randomized blinded controlled trial. ANIMALS 6 healthy castrated male donkeys. PROCEDURES In a crossover study design, donkeys received each of the following sublingual treatments 1 week apart in a randomly assigned order: 1 mL of molasses (D0) or Detomidine hydrochloride gel at 20 mug/kg (9 mug/lb; D20) or 40 mug/kg (18 mug/lb; D40). Sedation score (SS), head height above the ground (HHAG), and mechanical nociceptive threshold (MNT) were assessed before and for 180 minutes after treatment. Areas under the effect change-versus-time curves (AUCs) from 0 to 30, 30 to 60, 60 to 120, and 120 to 180 minutes after administration were computed for SS, HHAG, and MNT and compared among treatments. RESULTS D20 and D40 resulted in greater SS AUCs from 60 to 120 minutes and smaller HHAG AUCs from 30 through 180 minutes than did D0. The D40 resulted in smaller HHAG AUCs from 60 to 120 minutes than did D20. Compared with D0 values, MNT AUCs from 60 to 120 minutes were higher for D20, whereas MNT AUCs from 30 through 180 minutes were higher for D40. CONCLUSIONS AND CLINICAL RELEVANCE D20 and D40 induced sedation and mechanical hypoalgesia in donkeys by > 30 minutes after administration, but only sedation was dose dependent. Sublingual administration of Detomidine gel at 40 mug/kg may be useful for sedation of standing donkeys prior to potentially painful minor procedures.

Effect of the alpha2 -receptor agonists medetomidine, detomidine, xylazine, and romifidine on the ketamine metabolism in equines assessed with enantioselective capillary electrophoresis.[Pubmed:28251651]

Electrophoresis. 2017 Aug;38(15):1895-1904.

The combination of ketamine and an alpha2 -receptor agonist is often used in veterinary medicine. Four different alpha2 -receptor agonists, meDetomidine, Detomidine, xylazine, and romifidine, which differ in their chemical structure and thus in selectivity for the alpha2 -receptor and in the sedative and analgesic potency, are typically employed during surgery of equines. Recovery following anesthesia with ketamine and an alpha2 -receptor agonist is dependent on the alpha2 -receptor agonist. This prompted us to investigate (i) the inhibition characteristics for the N-demethylation of ketamine to norketamine and (ii) the formation of the ketamine metabolites norketamine, 6-hydroxynorketamine (6HNK), and 5,6-dehydronorketamine (DHNK) in presence of the four alpha2 -receptor agonists and equine liver microsomes. Samples were analyzed with enantioselective capillary electrophoresis using highly sulfated gamma-cyclodextrin as chiral selector. All four alpha2 -receptor agonists have an impact on the ketamine metabolism. MeDetomidine was found to be the strongest inhibitor, followed by Detomidine, whereas xylazine and romifidine showed almost no effect on the ketamine N-demethylation in the inhibition studies with a short-incubation period of the reaction mixture. After prolonged incubation, inhibition with xylazine and romifidine was also observed. The formation of 6HNK and DHNK is affected by all selected alpha2 -receptor agonists. With meDetomidine, levels of these metabolites are reduced compared to the case without an alpha2 -receptor agonist. For Detomidine, xylazine, and romifidine, the opposite was found.

Detomidine produce dose-dependent sedative and analgesic effects, is a nonnarcotic, synthetic α2-adrenergic agonist Target: α2-adrenergic agonist Detomidine is an imidazole derivative and α2-adrenergic agonist, used as a large animal sedative, primarily used in horses.

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