Chlorzoxazone


Description

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, 3...

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Pharmacology

Indication

For the relief of discomfort associated with acute painful musculoskeletal conditions.

Pharmacodynamic

Chlorzoxazone is a centrally-acting agent for painful musculoskeletal conditions. Data available fro... Read more

Mechanism of action

Chlorzoxazone inhibits degranulation of mast cells, subsequently preventing the release of histamine... Read more

Absorption

Information currently not available.

Protein binding

13-18%

Volume of distribution

Information currently not available.

Clearance

Information currently not available.

Half life

Information currently not available.

Route of elimination

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

Toxicity

Oral, mouse: LD50 = 440 mg/kg; Oral, rat: LD50 = 763 mg/kg; Symptoms of overdo... Read more


Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Ecchymosis US
Varying Reports
Petechiae US
Varying Reports
Allergic-type skin rashes US
Varying Reports
Over-stimulation US
Varying Reports
Urine discoloration US
Varying Reports
Anaphylaxis US
Varying Reports
Angioneurotic Edema US
Varying Reports
Gastrointesinal bleeding US
Varying Reports
Drowsiness US
Varying Reports
Dizziness US
Varying Reports
Lightheadedness US
Varying Reports
Malaise US
Varying Reports

Contraindications

  • Regions: US
  • Patient Conditions:
      • Name: Drug intolerance
      • Drugbank Id: DBCOND0012019

Food Interactions

  • Avoid alcohol.
  • Take without regard to meals.

Interactions

Type in a drug name to check for interaction with Chlorzoxazone

The metabolism of (R)-warfarin can be decreased when combined with Chlorzoxazone.
The metabolism of (S)-Warfarin can be decreased when combined with Chlorzoxazone.
The risk or severity of adverse effects can be increased when Chlorzoxazone is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
The metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Chlorzoxazone.
The risk or severity of adverse effects can be increased when Chlorzoxazone is combined with 4-Bromo-2,5-dimethoxyamphetamine.
The metabolism of 4-hydroxycoumarin can be decreased when combined with Chlorzoxazone.
The risk or severity of adverse effects can be increased when Chlorzoxazone is combined with 4-Methoxyamphetamine.
The metabolism of 5-androstenedione can be decreased when combined with Chlorzoxazone.
The risk or severity of adverse effects can be increased when Chlorzoxazone is combined with 5-methoxy-N,N-dimethyltryptamine.
The metabolism of Chlorzoxazone can be decreased when combined with 6-Deoxyerythronolide B.
The metabolism of 6-O-benzylguanine can be decreased when combined with Chlorzoxazone.
The metabolism of Chlorzoxazone can be decreased when combined with 7-ethyl-10-hydroxycamptothecin.
The risk or severity of adverse effects can be increased when Chlorzoxazone is combined with 7-Nitroindazole.
The risk or severity of adverse effects can be increased when Chlorzoxazone is combined with 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline.
The metabolism of 8-azaguanine can be decreased when combined with Chlorzoxazone.
The metabolism of 8-chlorotheophylline can be decreased when combined with Chlorzoxazone.
The metabolism of 9-aminocamptothecin can be decreased when combined with Chlorzoxazone.
The metabolism of 9-Deazaguanine can be decreased when combined with Chlorzoxazone.
The metabolism of 9-Methylguanine can be decreased when combined with Chlorzoxazone.
Chlorzoxazone may decrease the excretion rate of Abacavir which could result in a higher serum level.

References

  • 1 . Dong DL, Luan Y, Feng TM, Fan CL, Yue P, Sun ZJ, Gu RM, Yang BF: Chlorzoxazone inhibits contraction of rat thoracic aorta. Eur J Pharmacol. 2006 Sep 18;545(2-3):161-6. Epub 2006 Jun 29. [PubMed: 16859676]
  • 2 . Park JY, Kim KA, Park PW, Ha JM: Effect of high-dose aspirin on CYP2E1 activity in healthy subjects measured using chlorzoxazone as a probe. J Clin Pharmacol. 2006 Jan;46(1):109-14. [PubMed: 16397290]
  • 3 . Wan J, Ernstgard L, Song BJ, Shoaf SE: Chlorzoxazone metabolism is increased in fasted Sprague-Dawley rats. J Pharm Pharmacol. 2006 Jan;58(1):51-61. [PubMed: 16393464]

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