|Elimination half-life||1.14–1.24 hours|
|Chemical and physical data|
|Molar mass||241.241 g/mol|
|3D model (JSmol)|
|(what is this?)|
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. The muscle relaxant effects of methocarbamol are largely attributed to central depressant effects; however, peripheral effects of methocarbamol to prolong muscle refractory period have also been reported.
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; these can be serious. Other serious side-effects include the development of a severe skin rash or itching, fainting, jaundice, persistent nausea/vomiting, stomach/abdominal pain, mental/mood changes, trouble urinating, and signs of infection. If taken in large amounts at once or more than directed or as prescribed, dysphoria or suicidal thoughts may occur. In addition, methocarbamol may cause urine to turn black, blue, or green. However, this effect is harmless.
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, while clinical doses can be as high as 24 g per day for severe conditions such as tetanus.
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.
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. In combination with other active ingredients it is sold under other names: with acetaminophen (Paracetamol), under trade names Robaxacet and Tylenol Body Pain Night; with ibuprofen as Robax Platinum; with acetylsalicylic acid as Robaxisal in the U.S. and Canada. 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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