Chlorzoxazone
Chlorzoxazone Uses, Dosage, Side Effects, Food Interaction and all others data.
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)
Chlorzoxazone is 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.
Trade Name | Chlorzoxazone |
Availability | Prescription only |
Generic | Chlorzoxazone |
Chlorzoxazone Other Names | 5-chlorobenzoxazolidone, Chlorzoxane, Chlorzoxazon, Chlorzoxazona, Chlorzoxazone, Chlorzoxazonum, Clorzoxazona, Clorzoxazone |
Related Drugs | cyclobenzaprine, tizanidine, diazepam, methocarbamol, Flexeril, Soma |
Weight | 250mg, 375mg, 500mg, 750mg |
Type | Oral tablet |
Formula | C7H4ClNO2 |
Weight | Average: 169.565 Monoisotopic: 168.993056084 |
Protein binding | 13-18% |
Groups | Approved |
Therapeutic Class | |
Manufacturer | |
Available Country | United States |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Chlorzoxazone is a drug with muscle relaxant properties that is used as an adjunct to physical therapy and analgesics to treat stiffness and pain caused by a variety of musculoskeletal conditions.
For the relief of discomfort associated with acute painful musculoskeletal conditions.
Chlorzoxazone is also used to associated treatment for these conditions: Pain, Moderate Muscle Spasm, Severe Muscle Spasm
How Chlorzoxazone works
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 and potassium influx which would lead to neuronal inhibition and muscle relaxation. 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 arcs involved in producing and maintaining skeletal muscle spasm
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.
Food Interaction
- Avoid alcohol.
- Take with or without food. The absorption is unaffected by food.
[Moderate] GENERALLY AVOID: Alcohol may potentiate some of the pharmacologic effects of CNS-active agents such as chlorzoxazone.
Use in combination may result in additive central nervous system depression and In addition, in one small study, watercress was reported to increase chlorzoxazone peak concentrations, AUC, and half-life. The proposed mechanism is inhibition of CYP450 2E1 metabolism. The clinical significance is unknown. Ambulatory patients should be counseled to avoid hazardous activities requiring complete mental alertness and motor coordination until they know how chlorzoxazone affects them, and to notify their physician if they experience excessive or prolonged CNS effects that interfere with their normal activities. Watercress should be avoided if an interaction is suspected; e.g., excess sedation, nausea, or headache occurs.
MANAGEMENT: Patients receiving chlorzoxazone should be advised to avoid or limit consumption of alcohol.
Chlorzoxazone Drug Interaction
Major: acetaminophen / hydrocodone, acetaminophen / hydrocodoneModerate: diphenhydramine, diphenhydramine, duloxetine, duloxetine, pregabalin, pregabalin, alprazolam, alprazolam, cetirizine, cetirizineUnknown: aspirin, aspirin, esomeprazole, esomeprazole, cyanocobalamin, cyanocobalamin, cholecalciferol, cholecalciferol
Chlorzoxazone Disease Interaction
Elimination Route
Chlorzoxazone is rapidly metabolized and is excreted in the urine, primarily in a conjugated form as the glucuronide.
Innovators Monograph
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