Metaxalone

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Metaxalone

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Catalog Number	PR1665481
CAS	1665-48-1
Structure
Description	Metaxalone is a moderate to strong muscle relaxant used in the symptomatic treatment of musculoskeletal pain caused by strains, sprains, and other musculoskeletal conditions.
Synonyms	Skelaxin; Zorane; Methaxalonum; Metaxalon; Methoxolone
IUPAC Name	5-[(3,5-dimethylphenoxy)methyl]-1,3-oxazolidin-2-one
Molecular Weight	221.25
Molecular Formula	C12H15NO3
InChI	IMWZZHHPURKASS-UHFFFAOYSA-N
InChI Key	InChI=1S/C12H15NO3/c1-8-3-9(2)5-10(4-8)15-7-11-6-13-12(14)16-11/h3-5,11H,6-7H2,1-2H3,(H,13,14)
Documentation/Certification	DMF
Drug Categories	Central Nervous System Depressants; Centrally-mediated Muscle Relaxation; Drugs that are Mainly Renally Excreted; Muscle Relaxants; Muscle Relaxants, Centrally Acting Agents; Oxazoles; Peripheral Nervous System Agents; Serotonergic Drugs Shown to Increase Risk of Serotonin Syndrome
Drug Interactions	1,2-Benzodiazepine-The risk or severity of CNS depression can be increased when Metaxalone is combined with 1,2-Benzodiazepine. Abacavir-Metaxalone may decrease the excretion rate of Abacavir which could result in a higher serum level. Aceclofenac-Aceclofenac may decrease the excretion rate of Metaxalone which could result in a higher serum level. Acemetacin-Acemetacin may decrease the excretion rate of Metaxalone which could result in a higher serum level. Acetaminophen-Acetaminophen may decrease the excretion rate of Metaxalone which could result in a higher serum level.
Half-Life	9.2 (+/- 4.8) hours
Isomeric SMILES	CC1=CC(=CC(=C1)OCC2CNC(=O)O2)C
Standard	USP
Type	Small Molecule
Therapeutic Category	Muscle Relaxant

Pharmacology

Indications

Metaxalone is prescribed primarily for the management of painful peripheral musculoskeletal conditions and for addressing spasticity resulting from upper motor neuron syndromes. This medication is utilized as part of a comprehensive therapeutic approach, which may include rest and physical therapy, to alleviate discomfort associated with acute musculoskeletal injuries.

Pharmacodynamics

As a skeletal muscle relaxant, Metaxalone functions as an adjunct therapy to support the relief of discomfort arising from acute, painful musculoskeletal conditions. While the exact mechanism of action for Metaxalone remains undetermined, it is hypothesized that its efficacy may be attributed to its sedative properties. Importantly, it should be noted that Metaxalone does not exert a direct relaxing effect on tense skeletal muscles in humans.

Absorption

Currently, the absolute bioavailability of Metaxalone when administered in the form of Skelaxin tablets remains unknown. Further research may be required to elucidate the absorption characteristics of this pharmaceutical product in the human body.

Metabolism

Metaxalone is believed to be metabolized primarily by the liver. The hepatic metabolism of this medication underscores the importance of considering liver function when prescribing and administering Metaxalone for effective and safe therapeutic outcomes.

Mechanism of Action

The precise mechanism by which metaxalone operates in humans remains unidentified. However, it is hypothesized that its effects may be attributed to a general depression of the central nervous system.

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