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Active ingredient: Metaxalone - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

  • Muscle Relaxants, skeletal muscle
  • Analgesics
  • Hypnotics and Sedatives

Dosage Forms

  • Tablets (400 mg round, pale rose tablet and an 800 mg oval, pink scored tablet)

Brands / Synonyms

Metassalone [Dcit]; Metaxalon; Metaxalona [Inn-Spanish]; Metaxalona [Spanish]; Metaxalone [Usan:Ban:Inn]; Metaxalonum [Inn-Latin]; Metaxalonum [Latin]; Metazalone; Metazolone; Methaxalonum; Methoxolone; Skelaxin; Zorane

Indications

For the treatment of painful musculoskeletal conditions

Pharmacology

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.

Mechanism of Action

The mechanism of action of metaxalone in humans has not been established, but may be due to general central nervous system depression.

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.

Biotrnasformation / Drug Metabolism

Probably hepatic.

Contraindications

Known hypersensitivity to any components of this product.
Known tendency to drug induced, hemolytic, or other anemias.
Significantly impaired renal or hepatic function.

Drug Interactions

SKELAXIN may enhance the effects of alcohol, barbiturates and other CNS depressants.

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