Chlorzoxazone
/api/v1/drug/chlorzoxazoneMechanism of action
Sourced from openFDAMechanism-of-action class: Unknown Cellular or Molecular Interaction.
Indications
Sourced from openFDA- 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.
Contraindications
Sourced from openFDA- Chlorzoxazone is contraindicated in patients with known intolerance to the drug.contraindicated
Dosage & administration
Sourced from openFDAUsual Adult Dosage One tablet three or four times daily. If adequate response is not obtained with this dose, it may be increased to one and one-half tablets (750 mg) three or four times daily. As improvement occurs dosage can usually be reduced.
Warnings & precautions
Sourced from openFDASerious (including fatal) hepatocellular toxicity has been reported rarely in patients receiving chlorzoxazone. The mechanism is unknown but appears to be idiosyncratic and unpredictable. Factors predisposing patients to this rare event are not known. Patients should be instructed to report early signs and/or symptoms of hepatotoxicity such as fever, rash, anorexia, nausea, vomiting, fatigue, right upper quadrant pain, dark urine, or jaundice. Chlorzoxazone should be discontinued immediately and a physician consulted if any of these signs or symptoms develop. Chlorzoxazone use should also be discontinued if a patient develops abnormal liver enzymes (e.g., AST, ALT, alkaline phosphatase and bilirubin.) The concomitant use of alcohol or other central nervous system depressants may have an additive effect. Usage in Pregnancy The safe use of chlorzoxazone has not been established with respect to the possible adverse effects upon fetal development. Therefore, it should be used in women of childbearing potential only when, in the judgment of the physician, the potential benefits outweigh the possible risks.
Adverse reactions
Sourced from openFDAChlorzoxazone containing products are usually well tolerated. It is possible in rare instances that chlorzoxazone may have been associated with gastrointestinal bleeding. Drowsiness, dizziness, lightheadedness, malaise, or over-stimulation may be noted by an occasional patient. Rarely, allergic type skin rashes, petechiae, or ecchymoses may develop during treatment. Angioneurotic edema or anaphylactic reactions are extremely rare. There is no evidence that the drug will cause renal damage. Rarely, a patient may note discoloration of the urine resulting from a phenolic metabolite of chlorzoxazone. This finding is of no known clinical significance. To report SUSPECTED ADVERSE EVENTS, contact Aurobindo Pharma USA, Inc. at 1-866-850-2876 or FDA at 1-800- FDA-1088 or http://www.fda.gov/ for voluntary reporting of adverse reactions.
Overdosage
Sourced from openFDASymptoms Initially, gastrointestinal disturbances such as nausea, vomiting, or diarrhea together with drowsiness, dizziness, lightheadedness or headache may occur. Early in the course there may be malaise or sluggishness followed by marked loss of muscle tone, making voluntary movement impossible. The deep tendon reflexes may be decreased or absent. The sensorium remains intact, and there is no peripheral loss of sensation. Respiratory depression may occur with rapid, irregular respiration and intercostal and substernal retraction. The blood pressure is lowered, but shock has not been observed. Treatment Gastric lavage or induction of emesis should be carried out, followed by administration of activated charcoal. Thereafter, treatment is entirely supportive. If respirations are depressed, oxygen and artificial respiration should be employed and a patent airway assured by use of an oropharyngeal airway or endotracheal tube. Hypotension may be counteracted by use of dextran, plasma, concentrated albumin or a vasopressor agent such as norepinephrine. Cholinergic drugs or analeptic drugs are of no value and should not be used.
Approval history
Sourced from openFDA- May 4, 1988ANDAANDA089853Aurobindo Pharma Ltd
- May 4, 1988ANDAANDA089859Watson Labs
- Jun 24, 2016ANDAANDA207483Anda Repository
- Sep 12, 2019ANDAANDA212254Novitium Pharma
- Jul 21, 2020ANDAANDA211849Dr Reddys Labs Sa
- Nov 2, 2020ANDAANDA212743Ph Health
- Jul 29, 2021ANDAANDA215158Senores Pharms
- Apr 5, 2022ANDAANDA213126Rising
FAERS reports
- 1Nausea987.7%
- 2Dizziness957.4%
- 3Fatigue937.3%
- 4Pain927.2%
- 5Drug Ineffective826.4%
- 6Headache765.9%
- 7Anxiety665.2%
- 8Diarrhoea584.5%
- 9Chronic Kidney Disease564.4%
- 10Dyspnoea514.0%
- 11Somnolence514.0%
- 12Weight Decreased473.7%
- 13Back Pain463.6%
- 14Fall463.6%
- 15Completed Suicide433.4%
Literature
Recent PubMed references pinned to Chlorzoxazone as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.
- Drug Metabolism by Engineered Toluene o-Xylene Monooxygenases of Pseudomonas sp. OX1.Biotechnology and bioengineering · 2026 · Younan N, Dacpano FA, Frazer E, et al.PMID 41328664DOI 10.1002/bit.70117
- Feasible salting-out assisted extraction integrated with green TLC approach for concurrent chlorzoxazone and ibuprofen determination in human plasma.Journal of chromatography. A · 2025 · Derayea SM, Abdulrazik SG, Attia TZ, et al.PMID 40848494DOI 10.1016/j.chroma.2025.466299
- Lignin as a Bioactive Additive in Chlorzoxazone-Loaded Pharmaceutical Tablets.Molecules (Basel, Switzerland) · 2025 · Creteanu A, Lisa G, Vasile C, et al.PMID 40286006DOI 10.3390/molecules30071426
- Effect of muscle relaxant drug chlorzoxazone on the conformational stability and activity of bovine serum albumin: a spectroscopic and computational study.Journal of biomolecular structure & dynamics · 2025 · Patel R, Singh B, Siddiquee MA, et al.PMID 40135823DOI 10.1080/07391102.2025.2480260
- A Simple and Rapid HPLC Method Development for Quantification of Sodium Benzoate Content in Chlorzoxazone Oral Solid Dosage Forms.Biomedical chromatography : BMC · 2025 · Lankalapalli PK, Kamireddy T, Sambu P, et al.PMID 39562514DOI 10.1002/bmc.6048
- Novel Pharmaceutical Cocrystal Consisting of Chlorzoxazone and Nicotinamide: A New Promising Carrier for Solubility Augmentation.Assay and drug development technologies · 2024 · Sekhani A, Jha R, Shah PJ, et al.PMID 39512129DOI 10.1089/adt.2024.051
- Development, evaluation of critical method variables and stability assessment using a Box-Behnken design for the determination of organic impurities in a pharmaceutical dosage form of a centrally acting muscle relaxant drug chlorzoxazone.Biomedical chromatography : BMC · 2024 · Ettaboina SK, Nannapaneni S, Jeedimalla N, et al.PMID 39233497DOI 10.1002/bmc.6001
- Therapeutic efficacy of the BKCa channel opener chlorzoxazone in a mouse model of Fragile X syndrome.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2024 · Ferraguto C, Piquemal-Lagoueillat M, Lemaire V, et al.PMID 39223257DOI 10.1038/s41386-024-01956-6
Clinical trials
The 10 most recently updated of 10 ClinicalTrials.gov registrations naming Chlorzoxazone as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.
- Effectiveness of Chlorzoxazone Versus Orphenadrine Citrate in Alleviating Bruxism PainRecruiting · Phase 4 · Interventional · 60 enrolled · University of BaghdadNCT07109882updated 2025-08-07
- Pharmacokinetic and Bioequivalence Comparison of Baclofen and Chlorzoxazone Administered Individually or ConcurrentlyCompleted · Phase 1 · Interventional · 19 enrolled · University of Texas Southwestern Medical CenterNCT05257447updated 2023-03-31
- Placebo-Controlled Cross Over Trial of Chlorzoxazone IntakeCompleted · Phase 4 · Interventional · 48 enrolled · University of California, San FranciscoNCT01342341updated 2020-11-20
- Effect of Ethanol and Genetic Polymorphisms on Bupropion MetabolismWithdrawn · Interventional · 0 enrolled · Tufts UniversityNCT00330434updated 2020-11-10
- Chlorzoxazone in Hip and Knee ArthroplastyCompleted · Phase 4 · Interventional · 400 enrolled · Northern Orthopaedic Division, DenmarkNCT02405104updated 2019-09-09
- Evaluation of CYP450 Activities in Diabetic Patients vs. Non-diabetic SubjectsCompleted · Phase 4 · Interventional · 73 enrolled · Centre hospitalier de l'Université de Montréal (CHUM)NCT02291666updated 2019-07-23
- Effects of LRYGB on Pharmacokinetics of Nine CYP Probe DrugsCompleted · Interventional · 13 enrolled · University of Eastern FinlandNCT03563287updated 2018-06-21
- A Study to Investigate the Potential Influence of Nitisinone on the Metabolism and the Transport of Other Drugs in Healthy VolunteersCompleted · Phase 1 · Interventional · 36 enrolled · Swedish Orphan BiovitrumNCT03103568updated 2017-08-10
- The Effect of Chlorzoxazone on Moderate to Severe Postoperative Pain After Spine SurgeryCompleted · Phase 4 · Interventional · 110 enrolled · Rigshospitalet, DenmarkNCT01933542updated 2015-09-17
- Pharmacokinetic Study to Investigate Low-dose Combinations of a Cocktail of Seven Drugs for Simultaneous Phenotyping of CytochromesCompleted · Phase 1 · Interventional · 16 enrolled · University Hospital, Basel, SwitzerlandNCT01187862updated 2015-04-17
Frequently asked questions
- How does Chlorzoxazone work?
- Mechanism-of-action class: Unknown Cellular or Molecular Interaction.
- What is Chlorzoxazone used for?
- According to FDA labeling, Chlorzoxazone carries indications including: 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.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
- What class of drug is Chlorzoxazone?
- Chlorzoxazone is classified as Oxazol, thiazine, and triazine derivatives, Muscle Relaxant, Unknown Cellular or Molecular Interaction, Centrally-mediated Muscle Relaxation, Decreased Central Nervous System Organized Electrical Activity, Striated Muscle Metabolic Alteration.
- What are the brand names for Chlorzoxazone?
- Chlorzoxazone is marketed under brand names including Lorzone.
- What are the contraindications for Chlorzoxazone?
- Chlorzoxazone labeling lists contraindications including: Chlorzoxazone is contraindicated in patients with known intolerance to the drug.. Always consult the full prescribing information and a clinician.
chlorzoxazone is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.