Metaxalone

Absorption

The absolute bioavailability of metaxalone from Skelaxin tablets is not known.

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. Some adverse events associated with the drug include nausea, vomiting, drowsiness and CNS side effects such as dizziness, headache, and irritability.

Chemical properties

White Crystalline Solid

Originator

Skelaxin,Robins,US,1962

The Uses of Metaxalone

Metaxalone is a skeletal muscle relaxant that has applications in reducing muscle spasm, limitations in normal motion, and pain caused by musculoskeletal conditions. It is commonly used in combination with analgesics to address low back pain. The molecular or cellular actions of metaxalone is not known.[Cayman Chemical]

The Uses of Metaxalone

It is a muscle relaxant used to relax muscles and relieve pain

The Uses of Metaxalone

muscle relaxant (skeletal)

The Uses of Metaxalone

For the treatment of painful peripheral musculoskeletal conditions and spasticity from upper motor neuron syndromes.

Background

Metaxalone is a moderate to strong muscle relaxant used in the symptomatic treatment of musculoskeletal pain caused by strains, sprains, and other musculoskeletal conditions. It is marketed by King Pharmaceuticals under the brand name Skelaxin?. Its main mechanism of action is thought to involve general central nervous system depression. Metaxalone is associated with few side effects and is available as a 800 mg scored tablet.

Indications

For the treatment of painful peripheral musculoskeletal conditions and spasticity from upper motor neuron syndromes.

What are the applications of Application

Metaxalone is which may act as a general central nervous system depressant

Definition

ChEBI: Metaxalone is an aromatic ether.

Manufacturing Process

Urea (118 g, 1.96 mols) was added to 192 g (0.98 mol) of 3-(3',5'- dimethylphenoxy)-1,2-propane-diol which had previously been heated to 150°C. The reaction mixture was then heated rapidly to 195° to 200°C and maintained at this temperature for 5 hours with constant stirring. The resulting mixture was partitioned between water and ethyl acetate and the ethyl acetate layer was dried over sodium sulfate and concentrated. The residue was distilled in vacuo and the fraction boiling at 220° to 225°C/1.5 mm was collected. Yield, 172 g (79%). The distillate was crystallized from dry ethyl acetate; MP, 121.5° to 123°C.

Therapeutic Function

Muscle relaxant

Pharmacokinetics

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.

Metabolism

Probably hepatic.