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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 ]
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.
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.
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]
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PS75 is an experimental analgesic drug which acts as a functionally selective alpha-2A adrenergic agonist, with a K i of 8.2nM and an EC 50 of 4.8nM at the α 2A receptor. In animal studies it was found to produce analgesia but without the sedation typical of older drugs acting at this target such as dexmedetomidine.
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.