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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]
Clonidine was initially developed as a treatment for high blood pressure. Low doses in evenings and/or afternoons are sometimes used in conjunction with stimulants to help with sleep and because clonidine sometimes helps moderate impulsive and oppositional behavior and may reduce tics. [96] It may be more useful for comorbid Tourette syndrome.
ATC code C02 Antihypertensives is a therapeutic subgroup of the Anatomical Therapeutic Chemical Classification System, a system of alphanumeric codes developed by the World Health Organization (WHO) for the classification of drugs and other medical products.
Imidazoline receptors are the primary receptors on which clonidine and other imidazolines act. [1] [2] [3] There are three main classes of imidazoline receptor: I 1 is involved in inhibition of the sympathetic nervous system to lower blood pressure, [4] I 2 has as yet uncertain functions but is implicated in several psychiatric conditions, [5] [6] and I 3 regulates insulin secretion.
Xylazine is a structural analog of clonidine and an α 2-adrenergic receptor agonist, [1] sold under many trade names worldwide, most notably the Bayer brand name Rompun, [2] as well as Anased, Sedazine and Chanazine.
Clonidine and other imidazoline compounds have also been shown to reduce muscle spasms by their central nervous system activity. Tizanidine is perhaps the most thoroughly studied clonidine analog, and is an agonist at α 2-adrenergic receptors, but reduces spasticity at doses that result in significantly less hypotension than clonidine. [26]
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]
However, there are exceptions: clonidine is an adrenergic agonist at the α2 receptor; since this receptor is located presynaptically, agonism at this receptor inhibits the presynaptic release of adrenaline and noradrenaline, preventing postsynaptic adrenergic receptor activation and downstream signaling.
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