Overview
| Generic Names: | Chloroxazone; Chlorzoxane; Chlorzoxazon |
|---|---|
| Trade Names: | Biomioran; EZE-DS; Escoflex; Flexazone; Mioran; Miotran; Myoflexin; Myoflexine; Neoflex; Paraflex; Parafon Forte Dsc; Pathorysin; Relaxazone; Remular; Remular-S; Solaxin; Strifon Forte Dsc; Usaf Ma-10 |
| Brand Mixtures: | Acetazone Forte (Acetaminophen + Chlorzoxazone); Acetazone Forte C8 (Acetaminophen + Chlorzoxazone + Codeine Phosphate); Back-Aid Forte - Tab (Acetaminophen + Chlorzoxazone); Extra Strength Tylenol Aches and Strains (Acetaminophen + Chlorzoxazone); Gin Pain Pills - Tab (Acetaminophen + Chlorzoxazone); Gin Pain Pills- Chlorzoxazone & Acetamin.Tab (Acetaminophen + Chlorzoxazone); Parafon Forte (Acetaminophen + Chlorzoxazone); Parafon Forte C8 W Codeine Tab (Acetaminophen + Chlorzoxazone + Codeine Phosphate); Parafon Forte Tablets (Acetaminophen + Chlorzoxazone) |
| PharmGKB Accession Id: | PA448971 |
Description
A centrally acting central muscle relaxant with sedative properties. It is claimed to inhibit muscle spasm by exerting an effect primarily at the level of the spinal cord and subcortical areas of the brain. (From Martindale, The Extra Pharmacopoea, 30th ed, p1202) (source: Drug Bank)
Indication
For the relief of discomfort associated with acute painful musculoskeletal conditions. (source: Drug Bank)
ATC Therapeutic Category
- M03BB:Oxazol, thiazine, and triazine derivatives
Pharmacology, Interactions, and Contraindications
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. (source: Drug Bank)
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. (source: Drug Bank)
Food Interactions
Avoid alcohol.
Take without regard to meals.
(source:
Drug Bank)
Absorption, Distribution, Metabolism, Elimination & Toxicity
Biotransformation
Chlorzoxazone is rapidly metabolized in the liver and is excreted in the urine, primarily in a conjugated form as the glucuronide. (source: Drug Bank)
Protein Binding
13-18% (source: Drug Bank)
Toxicity
Oral, mouse: LD<sub>50</sub> = 440 mg/kg; Oral, rat: LD<sub>50</sub> = 763 mg/kg; Symptoms of overdose include diarrhea, dizziness, drowsiness, headache, light-headedness, nausea, and vomiting. (source: Drug Bank)
Isomeric SMILES Code:
c1cc2c(cc1Cl)nc(o2)O (source: Drug Bank)
The following genes are in curated knowledge about this drug.
| Gene | Relationship | Evidence | |
|---|---|---|---|
|
|
CYP2E1 |
|
Publications |
A list of non-curated publications that mention this drug along with other genes is available.
Drug Targets
| Gene | Description | |
|---|---|---|
| KCNMA1 |
|
(source: Drug Bank) |
A list of non-curated publications that mention this drug along with other drugs is available.
Drug Interactions
| Drug | Description | |
|---|---|---|
| disulfiram |
|
Disulfiram increases chlorzoxazone levels (source: Drug Bank) |
Non-Curated Information
A list of non-curated publications that mention this drug along with other diseases is available.
Additional Datasets
These datasets are minimally curated and are sorted alphabetically by title.
LinkOuts
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Non-Curated Publications
A list of non-curated publications that mention this drug is available.
