Metaxalone

CAS No:
1665-48-1 Category:
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Product Details:

  • CAS No: 1665-48-1
  • AHFC code:
  • Synonyms: Metassalone [Dcit] Metaxalon Metaxalona [INN-Spanish] Metaxalonum [INN-Latin] Metaxalonum [Latin] Metazalone Metazolone Methaxalonum Methoxolone
  • ATC Code:
  • Chemical Formula: C10H13NO4
  • Molecular Weight: 221.2524
  • Assay/Purity: Typically NLT 98%
  • DrugBank: DB00660 (APRD00514)
  • SMILES: CC1=CC(OCC2CNC(=O)O2)=CC(C)=C1
  • InChl: IMWZZHHPURKASS-UHFFFAOYSA-N
  • PubChem: 15459
  • IUPAC: 5-(3,5-dimethylphenoxymethyl)-1,3-oxazolidin-2-one

Additional Details

Indication:
For the treatment of painful peripheral musculoskeletal conditions and spasticity from upper motor neuron syndromes.
Pharmacodynamics:
Metaxalone is a skeletal muscle relaxant indicated as an adjunct to rest, physical therapy, and other measures for the relief of discomforts associated with acute, painful musculoskeletal conditions. The mode of action of this drug has not been clearly identified, but may be related to its sedative properties. Metaxalone does not directly relax tense skeletal muscles in man.
Mode of Action:
The mechanism of action of metaxalone in humans has not been established, but may be due to general central nervous system depression.
Metabolism:
Probably hepatic.
Toxicity:
LD50=775mg/kg (Rat, oral); LD50=1690 mg/kg (Mouse, oral). When determining the LD50 in rats and mice, progressive sedation, hypnosis and finally respiratoryfailure were noted as the dosage increased. In dogs, no LD50 could be determined as the higher doses produced an emetic action in 15 to 30 minutes.
General Reference:
See S, Ginzburg R: Choosing a skeletal muscle relaxant. Am Fam Physician. 2008 Aug 1;78(3):365-70. Pubmed Elenbaas JK: Centrally acting oral skeletal muscle relaxants. Am J Hosp Pharm. 1980 Oct;37(10):1313-23. Pubmed
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