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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 ]
The usual dose of 350 mg is unlikely to engender prominent side effects other than somnolence, and mild to significant euphoria or dysphoria, but the euphoria is generally short-lived due to the fast metabolism of carisoprodol into meprobamate and other metabolites; the euphoria derived is, according to new research, [11] most likely due to carisoprodol's inherent, potent anxiolytic effects ...
Carisoprodol is similar to meprobamate as they both belong to the carbamate drug class and meprobamate is a clinically significant active metabolite of carisoprodol, although carisoprodol itself possesses additional antispasmodic properties which are distinct from its metabolites.
[5] [25] 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 ...
Arbaclofen placarbil (/ ɑːr ˈ b æ k l oʊ f ɛ n p l ə ˈ k ɑːr b ɪ l / ar-BAK-loh-fen plə-KAR-bil, also known as XP19986) is a prodrug of R-baclofen.Arbaclofen placarbil possesses more favorable pharmacokinetic profile than baclofen, with less fluctuations in plasma drug levels.
However, food has been found to substantially delay the absorption of pregabalin and to significantly reduce peak levels without affecting the bioavailability of the drug; T max values for pregabalin of 0.6 hours in a fasted state and 3.2 hours in a fed state (5-fold difference), and the C max is reduced by 25–31% in a fed versus fasted state ...
[25] [26] Phenibut and baclofen, two structurally related compounds, are exceptions, as they mainly act on the GABA B receptor. [27] [28] Gabapentin, but not pregabalin, has been found to activate voltage-gated potassium channels , which might potentiate its depressant qualities.
Tolperisone is indicated for use in the treatment of pathologically increased tone of the skeletal muscle caused by neurological diseases (damage of the pyramidal tract, multiple sclerosis, myelopathy, encephalomyelitis) and of spastic paralysis and other encephalopathies manifested with muscular dystonia.