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药品详细

Chlorzoxazone(氯唑沙宗)

化学结构式图
中文名
氯唑沙宗
英文名
Chlorzoxazone
分子式
C7H4ClNO2
化学名
5-chloro-2,3-dihydro-1,3-benzoxazol-2-one
分子量
Average: 169.565
Monoisotopic: 168.993056084
CAS号
95-25-0
ATC分类
M03B 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

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)

生产厂家
  • Actavis totowa llc
  • Barr laboratories inc
  • Ferndale laboratories inc
  • Mikart inc
  • Mutual pharmaceutical co inc
  • Ohm laboratories inc
  • Ortho mcneil janssen pharmaceuticals inc
  • Ortho mcneil pharmaceutical inc
  • Par pharmaceutical inc
  • Pioneer pharmaceuticals inc
  • Sandoz inc
  • Watson laboratories inc
封装厂家
参考
Synthesis Reference Not Available
General Reference
  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
  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
  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
剂型
规格
化合物类型
Type small molecule
Classes
  • Benzoxazoles
Substructures
  • Benzene and Derivatives
  • Aryl Halides
  • Halobenzenes
  • Benzoxazoles
  • Heterocyclic compounds
  • Aromatic compounds
  • Oxazoles
适应症
药理
Indication For the relief of discomfort associated with acute painful musculoskeletal conditions.
Pharmacodynamics Chlorzoxazone, a synthetic compound, inhibits antigen-induced bronchospasms and, hence, is used to treat asthma and allergic rhinitis. Chlorzoxazone is used as an ophthalmic solution to treat conjunctivitis and is taken orally to treat systemic mastocytosis and ulcerative colitis. Chlorzoxazone is also 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.
Mechanism of action 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
Absorption Not Available
Volume of distribution Not Available
Protein binding 13-18%
Metabolism
Chlorzoxazone is rapidly metabolized in the liver and is excreted in the urine, primarily in a conjugated form as the glucuronide.

Important The metabolism module of DrugBank is currently in beta. Questions or suggestions? Please contact us.

Substrate Enzymes Product
Chlorzoxazone
6-hydroxychlorzoxazone Details
Route of elimination Chlorzoxazone is rapidly metabolized and is excreted in the urine, primarily in a conjugated form as the glucuronide.
Half life Not Available
Clearance Not Available
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.
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
melting point 191.5 °C PhysProp
water solubility 1000 mg/L Not Available
logP 1.6 Not Available
Predicted Properties
Property Value Source
water solubility 2.96e+00 g/l ALOGPS
logP 2.09 ALOGPS
logP 1.94 ChemAxon
logS -1.8 ALOGPS
pKa (strongest acidic) 9.39 ChemAxon
pKa (strongest basic) -2.2 ChemAxon
physiological charge 0 ChemAxon
hydrogen acceptor count 2 ChemAxon
hydrogen donor count 1 ChemAxon
polar surface area 38.33 ChemAxon
rotatable bond count 0 ChemAxon
refractivity 41.07 ChemAxon
polarizability 14.94 ChemAxon
药物相互作用
Drug Interaction
Disulfiram Disulfiram may increase the serum level of chlorzoxazone by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of chlorzoxazone if diltiazem is initiated, discontinued or dose changed.
Triprolidine The CNS depressants, Triprolidine and Chlorzoxazone, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
食物相互作用
  • Avoid alcohol.
  • Take without regard to meals.

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