Chlorzoxazone

Chlorzoxazone (INN) is a centrally acting muscle relaxant used to treat muscle spasm and the resulting pain or discomfort. It can also be administered for acute pain in general and for tension headache (muscle contraction headache). It acts on the spinal cord by depressing reflexes. It is sold under the brand names Lorzone, Paraflex and Muscol and in combination form as Parafon Forte, a combination of chlorzoxazone and acetaminophen (paracetamol). Possible side effects include dizziness, lightheadedness, malaise, nausea, vomiting, and liver dysfunction. Used with acetaminophen it has added risk of hepatotoxicity,.

Chlorzoxazone
Clinical data
Trade namesLorzone, Paraflex ,Muscol
AHFS/Drugs.comMonograph
MedlinePlusa682577
License data
Routes of
administration		By mouth
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailabilitywell absorbed
Protein binding13–18%
Metabolismhepatic
Elimination half-life1.1 hr Duration of action 3-4 hrs.
Excretionurine (<1%)
Identifiers
IUPAC name
  • 5-chloro-3H-benzooxazol-2-one
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.002.186
Chemical and physical data
FormulaC7H4ClNO2
Molar mass169.56 g·mol−1
3D model (JSmol)
SMILES
  • Clc2cc1c(OC(=O)N1)cc2
InChI
  • InChI=1S/C7H4ClNO2/c8-4-1-2-6-5(3-4)9-7(10)11-6/h1-3H,(H,9,10) Y
  • Key:TZFWDZFKRBELIQ-UHFFFAOYSA-N Y
  (verify)

Like metaxalone, its mechanism of action is still in question. It is believed that metaxalone works by altering serotonin levels and acting as a mild MAO inhibitor. The mechanism of action of chlorzoaxazone is thought to act on Gaba-A & B receptors and voltage-gated calcium channels to a degree. General central nervous system depression is the only currently accepted aspect to its medical benefits. Elucidation of the exact mechanism of action is ongoing but there is limited study due to the existence of more effective, safe muscle relaxants (ex. diazepam, cyclobenzaprine, tizanidine), greatly limiting the potential benefit of identifying novel compounds which share chlorzoxazone's mechanism of action.

See also

References
  1. "Parafon DSC- chlorzoxazone tablet". DailyMed. 9 February 2010. Retrieved 5 November 2020.
  2. "Lorzone- chlorzoxazone tablet". DailyMed. 21 June 2019. Retrieved 5 November 2020.

Further reading


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