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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 ]
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.
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.
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.
Atipamezole, sold under the brand name Antisedan among others, is a synthetic α 2 adrenergic receptor antagonist used for the reversal of the sedative and analgesic effects of dexmedetomidine and medetomidine in dogs. Its reversal effect works by competing with the sedative for α 2-adrenergic receptors and displacing them.
It has several general functions in common with the α 1-adrenergic receptor, but also has specific effects of its own. Agonists (activators) of the α 2-adrenergic receptor are frequently used in anaesthesia where they affect sedation, muscle relaxation and analgesia through effects on the central nervous system (CNS). [5]
Detomidine is a sedative with analgesic properties. [3] α2-adrenergic agonists produce dose-dependent sedative and analgesic effects, mediated by activation of α2 catecholamine receptors, thus inducing a negative feedback response, reducing production of excitatory neurotransmitters.
Bekker's work on expanding uses of dexmedetomidine, a new agent introduced in 1999 for sedation of critically ill patients, led to FDA approval of this drug for procedural sedation. Bekker demonstrated that this drug mitigates the harmful effect of perioperative stress on cognition and improves postoperative recovery.