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
Chlorzoxazone
Chlorzoxazone

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.



MANAGEMENT: Patients receiving chlorzoxazone should be advised to avoid or limit consumption of alcohol.

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.

Chlorzoxazone Disease Interaction

Major: hepatotoxicity

Elimination Route

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

Innovators Monograph

You find simplified version here Chlorzoxazone

*** Taking medicines without doctor's advice can cause long-term problems.
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