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药品详细

Chlordiazepoxide(利眠宁)

化学结构式图
中文名
利眠宁
英文名
Chlordiazepoxide
分子式
C16H14ClN3O
化学名
7-chloro-2-(methylamino)-5-phenyl-3H-1,4$l^{5}-benzodiazepin-4-one
分子量
Average: 299.755
Monoisotopic: 299.082539792
CAS号
58-25-3
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

An anxiolytic benzodiazepine derivative with anticonvulsant, sedative, and amnesic properties. It has also been used in the symptomatic treatment of alcohol withdrawal. [PubChem]

生产厂家
  • Abbott laboratories pharmaceutical products div
  • Alra laboratories inc
  • Ascot hosp pharmaceuticals inc div travenol laboratories inc
  • Barr laboratories inc
  • Halsey drug co inc
  • Impax laboratories inc
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • John j ferrante
  • Lederle laboratories div american cyanamid co
  • Mm mast and co
  • Mylan pharmaceuticals inc
  • Parke davis div warner lambert co
  • Pioneer pharmaceuticals inc
  • Purepac pharmaceutical co
  • Rachelle laboratories inc
  • Roxane laboratories inc
  • Sandoz inc
  • Superpharm corp
  • Teva pharmaceuticals usa inc
  • Usl pharma inc
  • Valeant pharmaceuticals international
  • Vangard laboratories inc div midway medical co
  • Watson laboratories inc
  • West ward pharmaceutical corp
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Skerritt JH, Johnston GA: Enhancement of GABA binding by benzodiazepines and related anxiolytics. Eur J Pharmacol. 1983 May 6;89(3-4):193-8. Pubmed
  2. Oishi R, Nishibori M, Itoh Y, Saeki K: Diazepam-induced decrease in histamine turnover in mouse brain. Eur J Pharmacol. 1986 May 27;124(3):337-42. Pubmed
  3. Earley JV, Fryer RI, Ning RY: Quinazolines and 1,4-benzodiazepines. LXXXIX: Haptens useful in benzodiazepine immunoassay development. J Pharm Sci. 1979 Jul;68(7):845-50. Pubmed
  4. Olive G, Dreux C: [Pharmacologic bases of use of benzodiazepines in pereinatal medicine] Arch Fr Pediatr. 1977 Jan;34(1):74-89. Pubmed
  5. Vozeh S: [Pharmacokinetic of benzodiazepines in old age] Schweiz Med Wochenschr. 1981 Nov 21;111(47):1789-93. Pubmed
剂型
规格
化合物类型
Type small molecule
Classes Not Available
Substructures Not Available
适应症
药理
Indication For the management of anxiety disorders or for the short-term relief of symptoms of anxiety, withdrawal symptoms of acute alcoholism, and preoperative apprehension and anxiety.
Pharmacodynamics Chlordiazepoxide has antianxiety, sedative, appetite-stimulating and weak analgesic actions. The drug seems to block EEG arousal from stimulation in the brain stem reticular formation. The drug has been studied extensively in many species of animals and these studies are suggestive of action on the limbic system of the brain, which recent evidence indicates is involved in emotional responses. Hostile monkeys were made tame by oral drug doses which did not cause sedation. Chlordiazepoxide revealed a "taming" action with the elimination of fear and aggression. The taming effect of chlordiazepoxide was further demonstrated in rats made vicious by lesions in the septal area of the brain. The drug dosage which effectively blocked the vicious reaction was well below the dose which caused sedation in these animals.
Mechanism of action Chlordiazepoxide binds to stereospecific benzodiazepine (BZD) binding sites on GABA (A) receptor complexes at several sites within the central nervous system, including the limbic system and reticular formation. This results in an increased binding of the inhibitory neurotransmitter GABA to the GABA(A) receptor.BZDs, therefore, enhance GABA-mediated chloride influx through GABA receptor channels, causing membrane hyperpolarization. The net neuro-inhibitory effects result in the observed sedative, hypnotic, anxiolytic, and muscle relaxant properties.
Absorption Not Available
Volume of distribution Not Available
Protein binding Not Available
Metabolism
Hepatic.
Route of elimination Chlordiazepoxide is excreted in the urine, with 1% to 2% unchanged and 3% to 6% as conjugate.
Half life 24-48 hours
Clearance Not Available
Toxicity LD50=537 mg/kg (Orally in rats). Signs of overdose include respiratory depression, muscle weakness, somnolence (general depressed activity).
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
melting point 236.2 °C PhysProp
water solubility 2000 mg/L YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP 2.44 HANSCH,C ET AL. (1995)
pKa 4.8 MERCK INDEX (1996)
Predicted Properties
Property Value Source
water solubility 1.99e-02 g/l ALOGPS
logP 2.01 ALOGPS
logP 3.05 ChemAxon
logS -4.2 ALOGPS
pKa (strongest acidic) 18.52 ChemAxon
pKa (strongest basic) 6.43 ChemAxon
physiological charge 0 ChemAxon
hydrogen acceptor count 3 ChemAxon
hydrogen donor count 1 ChemAxon
polar surface area 53.14 ChemAxon
rotatable bond count 1 ChemAxon
refractivity 87.34 ChemAxon
polarizability 30.97 ChemAxon
药物相互作用
Drug Interaction
Cimetidine Cimetidine may increase the effect of the benzodiazepine, chlordiazepoxide.
Clozapine Increased risk of toxicity
Ethotoin Ethotoin may increase the metabolism of chlordiazepoxide via CYP3A4.
Fluconazole Fluconazole may increase the effect of the benzodiazepine, chlordiazepoxide.
Fosphenytoin Fosphenytoin may increase the metabolism of chlordiazepoxide via CYP3A4.
Indinavir The protease inhibitor, indinavir, may increase the effect of the benzodiazepine, chlordiazepoxide.
Itraconazole Itraconazole may increase the effect of the benzodiazepine, chlordiazepoxide.
Kava Kava may increase the effect of the benzodiazepine, chlordiazepoxide.
Ketoconazole Ketoconazole may increase the effect of the benzodiazepine, chlordiazepoxide.
Mephenytoin Mephenytoin may increase the metabolism of chlordiazepoxide via CYP3A4.
Nelfinavir The protease inhibitor, nelfinavir, may increase the effect of the benzodiazepine, chlordiazepoxide.
Omeprazole Omeprazole may increase the effect of the benzodiazepine, chlordiazepoxide.
Phenytoin Phenytoin may increase the metabolism of chlordiazepoxide via CYP3A4.
Ritonavir The protease inhibitor, ritonavir, may increase the effect of the benzodiazepine, chlordiazepoxide.
Saquinavir The protease inhibitor, saquinavir, may increase the effect of the benzodiazepine, chlordiazepoxide.
Telithromycin Telithromycin may reduce clearance of Chlordiazepoxide. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Chlordiazepoxide if Telithromycin is initiated, discontinued or dose changed.
Tipranavir Tipranavir may decrease the metabolism and clearance of Chlordiazepoxide. Consider alternate therapy or monitor for Alprazolam toxic effects if Tipranavir is initiated or dose increased.
Triprolidine The CNS depressants, Triprolidine and Chlordiazepoxide, 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 chlordiazepoxide by decreasing its metabolism. Monitor for chlordiazepoxide toxicity if voriconazole is initiated or dose increased.
食物相互作用
  • Avoid alcohol.
  • Take without regard to meals.

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