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Dexmedetomidine, sold under the brand name Precedex among others, is a medication used for sedation. [4] Veterinarians use dexmedetomidine for similar purposes in treating cats, dogs, and horses. [ 10 ] [ 11 ] It is also used in humans to treat acute agitation associated with schizophrenia or bipolar disorder . [ 5 ]
MDCalc is a free online medical reference for healthcare professionals that provides point-of-care clinical decision-support tools, including medical calculators, scoring systems, and algorithms. [1]
Medetomidine is a racemic mixture of two optical or stereoisomers, levomedetomidine and dexmedetomidine. [4] The latter causes the alpha 2- adrenergic agonist effects. [5] It is often used as the hydrochloride salt, medetomidine hydrochloride, a crystalline white solid that can be administered as an intravenous drug solution with sterile water.
Atipamezole is a competitive antagonist at ɑ 2-adrenergic receptors that competes with dexmedetomidine, an ɑ 2-adrenergic receptors agonist. It does not directly interact with dexmedetomidine; [34] rather, their structural similarity allows atipamezole to easily compete for receptor binding sites. [12]
Detomidine is a sedative with analgesic properties. [3] α 2-adrenergic receptor agonists produce dose-dependent sedative and analgesic effects, mediated by activation of α 2 catecholamine receptors, thus inducing a negative feedback response, reducing production of excitatory neurotransmitters.
Medications such as clonidine and dexmedetomidine target pre-synaptic auto receptors, therefore leading to an overall decrease in norepinephrine which clinically can cause effects such as sedation, analgesia, lowering of blood pressure and bradycardia. There is also low quality evidence that they can reduce shivering post operatively.
They are mainly used in research, having found limited clinical application in human medicine. They are extensively used in veterinary medicine to reverse the effects of alpha-2 agonist drugs used as sedatives, like xylazine, medetomidine and dexmedetomidine. Alpha-2 blockers increase noradrenaline release.
Other nonselective agonists include dexmedetomidine, lofexidine (another antihypertensive), TDIQ (partial agonist), tizanidine (in spasms, cramping) and xylazine. Xylazine has veterinary use. In the European Union, dexmedetomidine received a marketing authorization from the European Medicines Agency (EMA) on August 10, 2012, under the brand ...