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Baclofen, sold under the brand name Lioresal among others, is a medication used to treat muscle spasticity, such as from a spinal cord injury or multiple sclerosis. [8] [9] It may also be used for hiccups and muscle spasms near the end of life [9], and off-label to treat alcohol use disorder [10] [11] or opioid withdrawal symptoms. [12]
Baclofen also inhibits neural function presynaptically, by reducing calcium ion influx, and thereby reducing the release of excitatory neurotransmitters in both the brain and spinal cord. It may also reduce pain in patients by inhibiting the release of substance P in the spinal cord, as well. [5] [25]
There is evidence, albeit limited, of the clinical effectiveness of baclofen, [168] dantrolene, [169] diazepam, [170] and tizanidine. [171] [172] [173] In the most complicated cases intrathecal injections of baclofen can be used. [174] There are also palliative measures like castings, splints or customized seatings. [93]
Baclofen does not have relevant actions at α 2 δ receptors and so it is not regarded as a gabapentinoid. Pregabalin has demonstrated significantly greater potency (about 2.5-fold) than gabapentin in clinical studies [ 21 ] and mirogabalin is even more potent in vivo.
Quinazolinone's structure is very similar to that of some antibiotics. Quinazolinone's main mechanism of action is binding to the GABA A receptor. [163] It does not bind to the ethanol, barbiturate, neurosteroid, or benzodiazepine site. [163] Instead, it binds on a site directly between the GABRB2 (β2) and (α1) GABRA1 proteins on the GABA A ...
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Effectiveness appears similar to baclofen or diazepam. [4] It is taken by mouth. [5] Common side effects of tizanidine include dry mouth, sleepiness, weakness, and dizziness. [5] Serious side effects may include low blood pressure, liver problems, psychosis, and QT prolongation. [5] It is unclear if use in pregnancy and breastfeeding is safe. [6]
This drug article relating to the nervous system is a stub. You can help Wikipedia by expanding it.
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related to: baclofen site of action- 109 S High St #100, Columbus, OH · Directions · (614) 224-4261
"Your pet's prescription needs met at a price you can afford." - Patch