Samiksha Jaiswal (Editor)

Metaxalone

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Trade names
  
Skelaxin

MedlinePlus
  
a682010

ATC code
  
none

CAS ID
  
1665-48-1

AHFS/Drugs.com
  
Monograph

Routes of administration
  
Oral

Molar mass
  
221.252 g/mol

Metaxalone

Pregnancy category
  
US: C (Risk not ruled out)

How to pronounce metaxalone skelaxin memorizing pharmacology flashcard


Metaxalone (marketed by King Pharmaceuticals under the brand name Skelaxin) is a muscle relaxant used to relax muscles and relieve pain caused by strains, sprains, and other musculoskeletal conditions. Its exact mechanism of action is not known, but it may be due to general central nervous system depression. It is considered to be a moderately strong muscle relaxant, with relatively low incidence of side effects. Skelaxin is available in an 800 mg scored tablet. Possible side effects include nausea, vomiting, drowsiness and CNS side effects, such as dizziness, headache, and irritability.

Contents

The metabolism of metaxalone involves the liver cytochrome P450 system. Based on the information in the labeling, patients receiving metaxalone therapy and physicians prescribing metaxalone are directed to take precaution when coadministering it with other medications involving the P450 system.

Because of potential for side effects, this drug is considered high risk in the elderly. As of 2015 the cost for a typical month of medication in the United States is 100 to 200 USD.

Skelaxin metaxalone pain relief


Pharmacokinetics

Metaxalone exhibits increased bioavailability when taken with food. Specifically, in one study, compared to fasted conditions, the presence of food at the time of drug administration increased Cmax by 77.5%, AUC0-t by 23.5%, and AUC0-∞ by 15.4%. Thus, based on the information in the labeling, patients receiving metaxalone therapy are directed to take metaxalone with food, and are informed that taking metaxalone with food results in an increase in the oral bioavailability of metaxalone compared to taking metaxalone without food.

Assay

A literature survey reveals very few methods are reported for the determination of metaxalone to date. Nirogi et al. reported a liquid chromatographic method coupled to tandem mass spectrometry for the quantification of metaxalone in human plasma. A stability-indicating HPLC method was introduced by P.K. Sahu et al. Metaxalone has been used as an internal standard for few analytical methods

References

Metaxalone Wikipedia