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Methocarbamol is a central muscle relaxant used to treat skeletal muscle spasms. Under the trade name Robaxin, it is marketed by Actient Pharmaceuticals in the United States and Pfizer in Canada. The mechanism of action of methocarbamol is currently unknown, but may involve the inhibition of carbonic anhydrase.
1.1 Abuse potential
4 See also
Potential side-effects include: drowsiness, dizziness, clumsiness ( ataxia ), upset stomach, flushing, blurred vision, and fever. Both tachycardia (fast heart rate) and bradycardia (slow heart rate) have been reported;
Methocarbamol has a high therapeutic index, i.e., a wide range of safe and effective dosages. Consumer (OTC) doses are in the range 3–6 g per day,
Because of the potential for side-effects, this drug is considered to be a high-risk medication for the elderly.
Unlike other carbamates such as meprobamate and its prodrug carisoprodol, methocarbamol has greatly reduced abuse potential. Studies comparing it to the benzodiazepine lorazepam and the antihistamine diphenhydramine, along with placebo, find that methocarbamol produces increased “liking” responses and some sedative-like effects, however, at higher doses dysphoria is reported. It is considered to have an abuse profile similar to, but weaker than, lorazepam.
Methocarbamol is the carbamate of guaifenesin, but does not produce guaifenesin as a metabolite, because the carbamate bond is not hydrolyzed metabolically; metabolism is by Phase I ring hydroxylation and O -demethylation, followed by Phase II conjugation. All the major metabolites are unhydrolyzed carbamates.
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Methocarbamol without other ingredients is sold under the brand name Robaxin in the U.K., U.S. and Canada; it is marketed as Lumirelax in France, Ortoton in Germany and many other names world-wide. However, in Spain the tradename Robaxisal is used for the Paracetamol combination instead of Robaxacet. These combinations are also available from independent manufacturers under generic names.
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