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Chlorzoxazone (Chlorzoxazone) - Summary



Chlorzoxazone USP is a centrally acting skeletal muscle relaxant.

Chlorzoxazone is indicated as an adjunct to rest, physical therapy, and other measures for the relief of discomfort 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. Chlorzoxazone does not directly relax tense skeletal muscles in man.
See all Chlorzoxazone indications & dosage >>


Media Articles Related to Chlorzoxazone

Muscle Spasms
Source: MedicineNet Amyotrophic Lateral Sclerosis Specialty [2015.01.28]
Title: Muscle Spasms
Category: Diseases and Conditions
Created: 6/16/2009 12:00:00 AM
Last Editorial Review: 1/28/2015 12:00:00 AM

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Published Studies Related to Chlorzoxazone

Effect of high-dose aspirin on CYP2E1 activity in healthy subjects measured using chlorzoxazone as a probe. [2006.01]
The authors evaluated the effect of high-dose aspirin at a therapeutic dose, using chlorzoxazone as a probe for CYP2E1 enzyme activity. In a randomized, open-label, 2-way crossover study, 10 healthy men were treated 3 times daily for 6 days with 1 g aspirin or placebo...

An interaction between the cytochrome P450 probe substrates chlorzoxazone (CYP2E1) and midazolam (CYP3A). [2001.11]
AIMS: The use of multiple probe substrates to evaluate the activity of drug metabolizing enzymes requires that there are no inter-substrate interactions. As part of a series of studies to develop a clinically useful collection of probe substrates that could be given alone or in any combination, we observed an interaction between midazolam (MDZ) and another component of the six-drug cocktail. Published data indicated that the interacting component was likely to be chlorzoxazone. This was investigated as part of a second study. The data relating to the interaction from both studies are reported here... CONCLUSIONS: Chlorzoxazone appears to significantly influence the pharmacokinetics of oral MDZ, probably through inhibition of first pass metabolism by CYP3A in the GI tract. Data from these studies and literature evidence showing a further interaction between chlorzoxazone and CYP1A2 substrates and questions concerning the specificity of chlorzoxazone as a probe substrate for CYP2E1, indicate that the use of chlorzoxazone in multisubstrate probe cocktails should be avoided.

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Clinical Trials Related to Chlorzoxazone

Placebo-Controlled Cross Over Trial of Chlorzoxazone Intake [Recruiting]
The overall goals of this study are to (1) expand knowledge about interactions of chlorzoxazone with alcohol by assessing the effects of chlorzoxazone compared to placebo in moderate and heavy social alcohol users and (2) to compare the effects of chlorzoxazone on visual cue induced alcohol craving to placebo in moderate to heavy social alcohol users.

The Effect of Chlorzoxazone on Moderate to Severe Postoperative Pain After Spine Surgery [Recruiting]

Effect of Ethanol and Genetic Polymorphisms on Bupropion Metabolism [Completed]
The two purposes of this study are

1. to determine what effect the chronic and moderate/heavy drinking of alcoholic beverages has

1. on the blood level of bupropion and chlorzoxazone and their major breakdown products in the blood and

2. on the stimulant effect of bupropion and

2. to determine what effect a normal and common (25% frequency) genetic variation of a specific liver enzyme (that breaks down bupropion) has

1. on the blood levels of bupropion and its major breakdown products in the blood and

2. on the stimulant effect of bupropion.

Two groups of volunteers will be recruited for this study:

1. volunteers who drink moderate to heavy amounts of alcohol frequently and

2. volunteers who usually do not drink alcohol.

Volunteers will NOT be asked to change their drinking (or nondrinking) habits during the study.

Pharmacokinetic Study to Investigate Low-dose Combinations of a Cocktail of Seven Drugs for Simultaneous Phenotyping of Cytochromes [Recruiting]
The purpose of this study is to assess whether a cocktail of seven approved drugs (so-called "Basel cocktail") can be used for simultaneous phenotyping of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, CYP2E1 and CYP3A4.

Evaluation of CYP450 Activities in Diabetic Patients vs. Non-diabetic Subjects [Not yet recruiting]
Type 2 diabetes (T2D) could modulate CYP450 activities involved in drug-metabolism and cardiovascular homeostasis. We propose to carry out, for the first time, a comprehensive characterization of the effects of T2D on the expression and activity of major CYP450s. In our studies, patients with T2D will be studied since hyperglycaemia and/or hyperinsulinemia are believed to modulate CYP450s. This vicious cycle puts patients at risk of micro- and macro-vascular complications and inadequately controlled T2D due to high intersubject variability in drug disposition and action. Characterization of the effects of T2D on drug metabolism capacity will be performed using a cocktail of CYP450 probe drugs. CYP450 phenotype will be determined in 3 groups of patients (n=126 patients): 1) 42 T2D patients with good glycemic control; 2) 42 T2D patients with poor glycemic control; and 3) 42 non-T2D healthy subjects following a single oral administration of a cocktail of CYP450 probe drugs. Subjects will receive the CRCHUM-MT cocktail consisting of caffeine (CYP1A2), bupropion (CYP2B6), tolbutamide (CYP2C9), omeprazole (CYP2C19), dextromethorphan (CYP2D6), midazolam (CYP3A4/5) and chlorxozaxone (which will be administered separately) (CYP2E1). Serial blood samples will be drawn and urine collected. Metabolic ratios will be calculated and compared between three groups of subjects. Other co-variables to be studied include T2D biomarkers at baseline (glucose, insulin, HbA1c), medications, genetic polymorphisms and inflammatory markers. Our cocktail probe drug approach should allow us to demonstrate the effects of T2D on the activity of major CYP450s. Moreover, this project will indicate to us whether glycemic control should be considered as a covariate of intersubject variability in drug metabolism capacity.

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Reports of Suspected Chlorzoxazone Side Effects

Completed Suicide (12)Poisoning (2)Toxicity TO Various Agents (2)Hepatic Enzyme Increased (2)Feeling Abnormal (2)Confusional State (1)Drug Ineffective (1)Pain (1)Somnolence (1)Abdominal Pain Upper (1)more >>

Page last updated: 2015-01-28

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