In the setting of musculoskeletal pain, numerous pathological processes are at work, including altered biomechanics, destructive arthritic processes, and inflammation to neural structures. When a practitioner considers using an antispasmodic agent, the first decision to be made is whether the use is for a musculoskeletal disorder or spasticity from central origin. Diazepam is a sedative hypnotic from the class of benzodiazepines, and promotes the release of GABA from GABA-A neurons, resulting in presynaptic inhibition across the central neural axis. It is an effective treatment for spasticity, but is also used to treat anxiety and epilepsy. Antispasmodics for musculoskeletal pain are centrally acting and reserved to two classes such as benzodiazepines (e.g. diazepam, lorazepam), and nonbenzodiazepines. Non-benzodiazepine agents are amongst the more commonly used antispasmodics for musculoskeletal pain, and include cyclobenzaprine, methocarbamol, metaxalone, and carisoprodol.