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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 ]
Carisoprodol, sold under the brand name Soma among others, is a medication used for musculoskeletal pain. [6] Effects generally begin within half an hour and last for up to six hours. [ 6 ] It is taken orally ( by mouth ).
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]
Patients taking carisoprodol for a prolonged time have reported dependence, withdrawal and abuse, although most of these cases were reported by patients with addiction history. These effects were also reported by patients who took it in combination with other drugs with abuse potential, and in fewer cases, reports of carisoprodol-associated ...
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.
Physical and psychological dependence does happen with long-term use of carbamates, particularly carisoprodol. Today, carisoprodol is only used in the short term for muscle pain, particularly back pain. Discontinuation after long-term use could be very intense and even possibly fatal.
In one study, the affinity (K i) values of gabapentinoids for the α 2 δ subunit expressed in rat brain were found to be 0.05 μM for gabapentin, 23 μM for (R)-phenibut, 39 μM for (S)-phenibut, and 156 μM for baclofen. [9] Their affinities (K i) for the GABA B receptor were >1 mM for gabapentin, 92 μM for (R)-phenibut, >1 mM for (S)-phenibut.
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]