New Release: Alpha testing version has been released.

Chlorzoxazone

M03B - Muscle relaxants, centrally acting agents ATC M03BB03 Small molecule approved 1958 Oral Natural product

JFDA label: Relaxon Forte™ Tablets

Mechanism of Action

Opener of Intermediate conductance calcium-activated potassium channel protein 4 — Intermediate conductance calcium-activated potassium channel protein 4 opener

TargetActionGene / class
Intermediate conductance calcium-activated potassium channel protein 4 efficacy OPENER KCNN4

Indications

Approved

  • Musculoskeletal conditions

Contraindications

Source: Lexicomp

  • Hypersensitivity to chlorzoxazone or any component of the formulation Absolute

Adverse Reactions

Very Common >10%Common 1–10%Uncommon 0.1–1% Rare 0.01–0.1%Very Rare <0.01%Not Known

Nervous system disorders (4)

Not Known Dizziness · drowsiness · malaise · paradoxical central nervous system stimulation

Renal and urinary disorders (1)

Not Known Urine discoloration

Dosing

Source: Lexicomp

Musculoskeletal conditions: Oral: 250 to 500 mg 3 or 4 times daily, may increase to 750 mg 3 or 4 times daily; for painful musculoskeletal conditions, start with 500 mg 3 or 4 times daily. Consider dose reductions as symptoms improve.
Refer to adult dosing.
There are no dosage adjustments provided in the manufacturer’s labeling.
There are no dosage adjustments provided in the manufacturer’s labeling.

Warnings & Precautions

Source: Lexicomp

CNS depression

May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks that require mental alertness (eg, operating machinery or driving).

Hepatotoxicity

Rare, serious (including fatal) idiosyncratic and unpredictable hepatocellular toxicity has been reported with use. Discontinue immediately if early signs/symptoms of hepatic toxicity arise (eg, fever, rash, anorexia, nausea, vomiting, fatigue, right upper quadrant pain, dark urine, jaundice). Also discontinue if elevated liver enzymes (eg, AST, ALT, alkaline phosphatase, bilirubin) develop.

Hypersensitivity reaction

Use caution in patients with known allergies or a history of allergic reactions to drugs; if sensitivity (itching, redness, urticaria) occurs, discontinue therapy. Concurrent drug therapy issues:

Drug-drug interactions

Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information. Dosage form specific issues:

Benzyl alcohol and derivatives

Some dosage forms may contain sodium benzoate/benzoic acid; benzoic acid (benzoate) is a metabolite of benzyl alcohol; large amounts of benzyl alcohol (≥99 mg/kg/day) have been associated with a potentially fatal toxicity ("gasping syndrome") in neonates; the "gasping syndrome" consists of metabolic acidosis, respiratory distress, gasping respirations, CNS dysfunction (including convulsions, intracranial hemorrhage), hypotension and cardiovascular collapse (AAP 1997; CDC 1982); some data suggests that benzoate displaces bilirubin from protein binding sites (Ahlfors 2001); avoid or use dosage forms containing benzyl alcohol derivative with caution in neonates. See manufacturer's labeling.

Pregnancy & Lactation

Pregnancy

Animal reproduction studies have not been conducted.

Monitoring

Clinical pearlLiver functions tests (periodic); signs/symptoms of hepatotoxicity

Chemistry & Properties

2D structure
FormulaC7H4ClNO2
Molecular weight169.57 g/mol
IUPAC name5-chloro-3H-1,3-benzoxazol-2-one
CAS95-25-0
PubChem CID2733
InChIKeyTZFWDZFKRBELIQ-UHFFFAOYSA-N
logP1.77 (XLogP 1.8)
Polar surface area46.0 Ų
H-bond acceptors / donors2 / 1
Drug-likeness (QED)0.65
Lipinski violations0
SMILESO=c1[nH]c2cc(Cl)ccc2o1

Biology & Pharmacokinetics

Pharmacokinetics

BBB penetrantYes

Enzyme interactions

EnzymeRoleDetail
CYP1A2Inhibitor
CYP1A2Substrate
CYP2C8Inhibitor
CYP3A4Substrate

Transporters

BCRP (Inhibitor)BCRP (Inhibitor)BSEP (Inhibitor)BSEP (Inhibitor)MDR1 (Inhibitor)MRP1 (Inhibitor)MRP2 (Inhibitor)MRP4 (Inhibitor)OAT3 (Inhibitor)OATP1B1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)OATP1B3 (Inhibitor)OATP2B1 (Inhibitor)OCT1 (Inhibitor)P-gp (Inhibitor)P-gp (Substrate)

Drug–drug interactions (55, DDInter)

Interacting drugSeverityManagement
Codeine major
Hydrocodone major
Leflunomide major
Morphine major
Morphine (liposomal) major
Teriflunomide major
Aldesleukin moderate
Alimemazine moderate
Asparaginase Escherichia coli moderate
Azatadine moderate
Brentuximab vedotin moderate
Brimonidine (ophthalmic) moderate
Brimonidine (topical) moderate
Brompheniramine moderate
Carbinoxamine moderate
Ceritinib moderate
Cetirizine moderate
Chlorpheniramine moderate
Clemastine moderate
Clofarabine moderate
Clofedanol moderate
Cyclizine moderate
Cyproheptadine moderate
Dexbrompheniramine moderate
Dextromethorphan moderate
Diphenhydramine moderate
Disulfiram moderate
Doxepin moderate
Doxepin (topical) moderate
Doxylamine moderate
Dronabinol moderate
Ethanol moderate
Idelalisib moderate
Ifosfamide moderate
Interferon beta-1a moderate
Interferon beta-1b moderate
Levocetirizine moderate
Mepyramine moderate
Methotrexate moderate
Metoclopramide moderate

Showing 40 of 55.

Registered Products (2)

BrandForm / strengthPackAgentCitizen (JOD)
Relaxon Forte™ Tablets Tablet 500 mg 30 tab Land Of Medicine Drug Store 2.720
Relaxon Tablet 300 mg, 250 mg 30 tab شركة مستودع ادوية الايمان 2.970