用户名： 密   码：
注册 | 忘记密码？
药品详细

Clorazepate(氯氮卓)

化学结构式图
中文名
氯氮卓
英文名
Clorazepate
分子式
C16H11ClN2O3
化学名
7-chloro-2-oxo-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepine-3-carboxylic acid
分子量
Average: 314.723
Monoisotopic: 314.045819935
CAS号
23887-31-2
ATC分类
N05B 未知
药物类型
small molecule
阶段
illicit, approved
商品名
同义名
基本介绍

A water-soluble benzodiazepine derivative effective in the treatment of anxiety. It has also muscle relaxant and anticonvulsant actions. [PubChem]

生产厂家
  • Able laboratories inc
  • Alra laboratories inc
  • American therapeutics inc
  • Clonmel healthcare ltd
  • Gd searle llc
  • Lederle laboratories div american cyanamid co
  • Lundbeck inc
  • Mylan pharmaceuticals inc
  • Purepac pharmaceutical co
  • Quantum pharmics ltd
  • Ranbaxy laboratories ltd
  • Sandoz inc
  • Taro pharmaceuticals usa inc
  • Usl pharma inc
  • Warner chilcott div warner lambert co
  • Watson laboratories inc
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. : Systematic review of the benzodiazepines. Guidelines for data sheets on diazepam, chlordiazepoxide, medazepam, clorazepate, lorazepam, oxazepam, temazepam, triazolam, nitrazepam, and flurazepam. Committee on the Review of Medicines. Br Med J. 1980 Mar 29;280(6218):910-2. Pubmed
  2. McElhatton PR: The effects of benzodiazepine use during pregnancy and lactation. Reprod Toxicol. 1994 Nov-Dec;8(6):461-75. Pubmed
剂型
规格
化合物类型
Type small molecule
Classes
  • Benzodiazepines
  • Lactams
Substructures
  • Benzodiazepines
  • Hydroxy Compounds
  • Acetates
  • Keto-Acids
  • Amino Ketones
  • Benzene and Derivatives
  • Aryl Halides
  • Carboxylic Acids and Derivatives
  • Halobenzenes
  • Heterocyclic compounds
  • Aromatic compounds
  • Carboxamides and Derivatives
  • Diazepines
  • Lactams
  • Imines
  • Anilines
适应症
药理
Indication For the management of anxiety disorders or for the short-term relief of the symptoms of anxiety. Also used as adjunctive therapy in the management of partial seizures and for the symptomatic relief of acute alcohol withdrawal.
Pharmacodynamics Clorazepate is a member of the group of drugs called benzodiazepines. Pharmacologically, clorazepate has the characteristics of the benzodiazepines. It has depressant effects on the central nervous system. The primary metabolite, nordiazepam, quickly appears in the blood stream. Studies in healthy men have shown that clorazenate has depressant effects on the central nervous system. Since orally administered clorazepate dipotassium is rapidly decarboxylated to form nordiazepam, there is essentially no circulating parent drug.
Mechanism of action Benzodiazepines bind nonspecifically to benzodiazepine receptors BNZ1, which mediates sleep, and BNZ2, which affects affects muscle relaxation, anticonvulsant activity, motor coordination, and memory. As benzodiazepine receptors are thought to be coupled to gamma-aminobutyric acid-A (GABAA) receptors, this enhances the effects of GABA by increasing GABA affinity for the GABA receptor. Binding of the inhibitory neurotransmitter GABA to the site opens the chloride channel, resulting in a hyperpolarized cell membrane that prevents further excitation of the cell.
Absorption Rapidly absorbed following oral administration (bioavailability is 91%).
Volume of distribution Not Available
Protein binding The protein binding of nordiazepam in plasma is high (97-98%).
Metabolism
The drug is metabolized in the liver and excreted primarily in the urine. The primary metabolite, nordiazepam, is further metabolized by hydroxylation. The major urinary metabolite is conjugated oxazepam (3-hydroxynordiazepam), and smaller amounts of conjugated p-hydroxynordiazepam and nordiazepam are also found in the urine.

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

Substrate Enzymes Product
Clorazepate
N-desmethyldiazepam Details
Clorazepate
    		Oxazepam Details
    Clorazepate
      		3-hydroxynordiazepam Details
      Clorazepate
        		Nordiazepam Details
        Clorazepate
          		p-Hydroxynordiazepam Details
          Route of elimination The drug is metabolized in the liver and excreted primarily in the urine.
          Half life The serum half-life is about 2 days. Nordiazepam, the primary metabolite, quickly appears in the blood and is eliminated from the plasma with an apparent half-life of about 40 to 50 hours.
          Clearance Not Available
          Toxicity Oral LD50 in rats is 1320 mg/kg. In monkeys, oral LD50 exceed 1600 mg/kg. Symptoms of overdose include confusion, coma, impaired coordination, sleepiness, and slowed reaction time.
          Affected organisms
          • Humans and other mammals
          Pathways Not Available
          理化性质
          Properties
          State solid
          Experimental Properties
          Property Value Source
          water solubility Very soluble Not Available
          logP 3 Not Available
          Predicted Properties
          Property Value Source
          water solubility 2.48e-02 g/l ALOGPS
          logP 2.68 ALOGPS
          logP 3.21 ChemAxon
          logS -4.1 ALOGPS
          pKa (strongest acidic) 3.32 ChemAxon
          pKa (strongest basic) -0.64 ChemAxon
          physiological charge -1 ChemAxon
          hydrogen acceptor count 4 ChemAxon
          hydrogen donor count 2 ChemAxon
          polar surface area 78.76 ChemAxon
          rotatable bond count 2 ChemAxon
          refractivity 82.68 ChemAxon
          polarizability 30.63 ChemAxon
          药物相互作用
          Drug Interaction
          Amprenavir Amprenavir may increase the effect and toxicity of the benzodiazepine, clorazepate.
          Cimetidine Cimetidine may increase the effect of the benzodiazepine, clorazepate.
          Clozapine Increased risk of toxicity
          Ethotoin Ethotoin may increase the metabolism of clorazepate via CYP3A4.
          Fluconazole Fluconazole may increase the effect of the benzodiazepine, clorazepate.
          Fosamprenavir Fosamprenavir may increase the effect and toxicity of the benzodiazepine, clorazepate.
          Fosphenytoin Fosphenytoin may increase the metabolism of clorazepate via CYP3A4.
          Indinavir The protease inhibitor, indinavir, may increase the effect of the benzodiazepine, clorazepate.
          Itraconazole Itraconazole may increase the effect of the benzodiazepine, clorazepate.
          Kava Kava may increase the effect of the benzodiazepine, clorazepate.
          Ketoconazole Ketoconazole may increase the effect of the benzodiazepine, clorazepate.
          Mephenytoin Mephenytoin may increase the metabolism of clorazepate via CYP3A4.
          Nelfinavir The protease inhibitor, nelfinavir, may increase the effect of the benzodiazepine, clorazepate.
          Omeprazole Omeprazole may increase the effect of the benzodiazepine, clorazepate.
          Phenytoin Phenytoin may increase the metabolism of clorazepate via CYP3A4.
          Ritonavir The protease inhibitor, ritonavir, may increase the effect of the benzodiazepine, clorazepate.
          Saquinavir The protease inhibitor, saquinavir, may increase the effect of the benzodiazepine, clorazepate.
          Telithromycin Telithromycin may reduce clearance of Clorazepate. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Clorazepate if Telithromycin is initiated, discontinued or dose changed.
          Tipranavir Tipranavir may decrease the metabolism and clearance of Clorazepate. Consider alternate therapy or monitor for Clorazepate toxic effects if Tipranavir is initiated or dose increased.
          Triprolidine The CNS depressants, Triprolidine and Clorazepate, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
          Voriconazole Voriconazole may increase the serum concentration of clorazepate by decreasing its metabolism. Monitor for clorazepate toxicity if voriconazole is initiated or dose increased.
          食物相互作用
          • Avoid alcohol.
          • Take without regard to meals.

          返回 | 收藏