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Clonidine, sold under the brand name Catapres among others, is an α 2A-adrenergic receptor agonist [12] medication used to treat high blood pressure, ADHD, drug withdrawal (e.g., alcohol, opioids, or nicotine), menopausal flushing, diarrhea, spasticity, and certain pain conditions. [13] The drug is often prescribed off-label for tics.
The alpha-adrenergic receptor has two subclasses α 1 and α 2. Alpha 2 receptors are associated with sympatholytic properties. Alpha-adrenergic agonists have the opposite function of alpha blockers. Alpha adrenoreceptor ligands mimic the action of epinephrine and norepinephrine signaling in the heart, smooth muscle and central nervous system, with
In non-human species this is an immobilizing and anesthetic drug, presumptively also mediated by α 2 adrenergic receptors because it is reversed by yohimbine, an α 2 antagonist. α 2A selective agonists include guanfacine (an antihypertensive) and brimonidine (UK 14,304). -3-nitrobiphenyline is an α 2C selective agonist as well as being a ...
Tizanidine, sold under the brand name Zanaflex among others, is an alpha-2 (α 2) adrenergic receptor agonist, [2] similar to clonidine, that is used to treat muscle spasticity due to spinal cord injury, multiple sclerosis, and spastic cerebral palsy. [3] Effectiveness appears similar to baclofen or diazepam. [4] It is taken by mouth. [5]
The alpha-2 blocker acts on alpha-2 receptors. The alpha-2 receptor is a G-protein coupled receptor as well, which exert its action by Gi function, leading to an inhibition of adenylyl cyclase and thus reducing synthesis of cAMP. [3] It lowers the amount of calcium inside the cell. [3]
This is the first class of non-opioid pain medication approved to treat moderate to severe acute pain approved by the FDA in more than 20 years. The U.S. Food and Drug Administration (FDA) on ...
Many tricyclic antidepressants, tetracyclic antidepressants, antipsychotics, ergolines, and some piperazines like buspirone, trazodone, nefazodone, etoperidone, and mepiprazole antagonize α 1-adrenergic receptors as well, which contributes to their side effects such as orthostatic hypotension.
They inhibit the release of circulating adrenergic neurotransmitters like norepinephrine, which contributes to the contraction of smooth muscles. [2] Examples of alpha 2 blockers include yohimbine and idazoxan. [2] Apart from being used as antidotes to reverse the overdose effects of alpha 2 agonists, they only have a limited number of ...