Abstract: Methocarbamol is classified as a centrally acting muscle relaxant. Pharmacological studies demonstrated its main locus of action to be at the internuncial neurons of the spinal cord. It is used to treat articular muscle sprain, lumbar muscle spain and Sciatica, etc. It is also used for the treatment of hypertrophic spondylitis and rheumatoid arthritis. It can also be used for cosmetic surgery to control postoperative pain, severe muscle spasm and neurological disorders. Methocarbamol is a useful adjunct in improving patient recovery. In this article, we summarized its pharmacokinetics, synthesis, pharmacological effect, clinical use and safety.