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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]
Lesogaberan (AZD-3355) was [1] an experimental drug candidate developed by AstraZeneca for the treatment of gastroesophageal reflux disease (GERD). [2] As a GABA B receptor agonist, [3] it has the same mechanism of action as baclofen, but is anticipated to have fewer of the central nervous system side effects that limit the clinical use of baclofen for the treatment of GERD.
A GABA analogue is a compound which is an analogue or derivative of the neurotransmitter gamma-Aminobutyric acid (GABA) (the IUPAC of which is 4-aminobutanoic acid). Many GABA analogues are used as drugs , especially as anticonvulsants , sedatives , and anxiolytics .
Gamma-aminobutyric acid, a GABA-B receptor agonist. A GABA receptor agonist is a drug that is an agonist for one or more of the GABA receptors, producing typically sedative effects, and may also cause other effects such as anxiolytic, anticonvulsant, and muscle relaxant effects. [1] There are three receptors of the gamma-aminobutyric acid. The ...
Gabapentin, sold under the brand name Neurontin among others, is an anticonvulsant medication primarily used to treat neuropathic pain and also for partial seizures [10] [7] of epilepsy. It is a commonly used medication for the treatment of neuropathic pain caused by diabetic neuropathy , postherpetic neuralgia , and central pain . [ 11 ]
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.