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

Brands, Medical Use, Clinical Data

Drug Category

  • Muscle Relaxants, Central

Dosage Forms

  • Tablet (500 mg)

Brands / Synonyms

Biomioran; Chloroxazone; Chlorzoxane; Chlorzoxazon; Chlorzoxazone; Escoflex; EZE-DS; Flexazone; Mioran; Miotran; Myoflexin; Myoflexine; Neoflex; Paraflex; Parafon Forte Dsc; Pathorysin; Relaxazone; Remular; Remular-S; Solaxin; Strifon Forte Dsc; Usaf Ma-10

Indications

For the relief of discomfort associated with acute painful musculoskeletal conditions.

Pharmacology

Chlorzoxazone, a synthetic compound, inhibits antigen-induced bronchospasms and, hence, is used to treat asthma and allergic rhinitis. Chlorzoxazone is used as an ophthalmic solution to treat conjunctivitis and is taken orally to treat systemic mastocytosis and ulcerative colitis. Chlorzoxazone is also a centrally-acting agent for painful musculoskeletal conditions. Data available from animal experiments as well as human study indicate that chlorzoxazone acts primarily at the level of the spinal cord and subcortical areas of the brain where it inhibits multisynaptic reflex a.c. involved in producing and maintaining skeletal muscle spasm of varied etiology. The clinical result is a reduction of the skeletal muscle spasm with relief of pain and increased mobility of the involved muscles.

Mechanism of Action

Chlorzoxazone inhibits degranulation of mast cells, subsequently preventing the release of histamine and slow-reacting substance of anaphylaxis (SRS-A), mediators of type I allergic reactions. Chlorzoxazone also may reduce the release of inflammatory leukotrienes. Chlorzoxazone may act by inhibiting calcium influx.

Absorption

Not Available

Toxicity

Oral, mouse: LD50 = 440 mg/kg; Oral, rat: LD50 = 763 mg/kg; Symptoms of overdose include diarrhea, dizziness, drowsiness, headache, light-headedness, nausea, and vomiting.

Biotrnasformation / Drug Metabolism

Chlorzoxazone is rapidly metabolized in the liver and is excreted in the urine, primarily in a conjugated form as the glucuronide.

Contraindications

PARAFON FORTE DSC chlorzoxazone is contraindicated in patients with known intolerance to the drug.

Drug Interactions

The concomitant use of alcohol or other central nervous system depressants may have an additive effect.

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