药品详细

Prazepam(普拉西)

基本信息
剂型规格
适应症
药理
临床
理化性质
相互作用
文档
专利
Pathway
文献
序列

化学结构式图

中文名

普拉西

英文名

Prazepam

分子式

C₁₉H₁₇ClN₂O

化学名

7-chloro-1-(cyclopropylmethyl)-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one

分子量

Average: 324.804
Monoisotopic: 324.102940883

CAS号

2955-38-6

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

Prazepam is a benzodiazepine that is used in the treatment of anxiety disorders. It is a schedule IV drug in the U.S.

生产厂家

Parke davis div warner lambert co
Usl pharma inc

封装厂家

Physicians Total Care Inc.

参考

Synthesis Reference	Not Available
General Reference	Not Available

剂型

规格

化合物类型

Type	small molecule

Classes

Benzodiazepines
Lactams

Substructures

Benzodiazepines
Amino Ketones
Cyclopropane and Derivatives
Benzene and Derivatives
Aliphatic and Aryl Amines
Aryl Halides
Halobenzenes
Heterocyclic compounds
Aromatic compounds
Carboxamides and Derivatives
Diazepines
Lactams
Imines
Anilines

适应症

药理

Indication	For the treatment of anxiety disorders.
Pharmacodynamics	Prazepam is a benzodiazepine derivative drug. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. Benzodiazepines may be habit-forming (causing mental or physical dependence), especially when taken for a long time or in high doses.
Mechanism of action	Prazepam is believed to stimulate GABA receptors in the ascending reticular activating system. Since GABA is inhibitory, receptor stimulation increases inhibition and blocks both cortical and limbic arousal following stimulation of the brain stem reticular formation.
Absorption	Not Available
Volume of distribution	Not Available
Protein binding	Not Available
Metabolism	Hepatic.
Route of elimination	Not Available
Half life	36-200 hours
Clearance	Not Available
Toxicity	Symptoms of overdose include somnolence, confusion, coma, and diminished reflexes. Respiration, pulse and blood pressure should be monitored.
Affected organisms	Humans and other mammals
Pathways	Not Available

理化性质

Properties

State

solid

Experimental Properties

Property	Value	Source
melting point	145-146 °C	PhysProp
logP	3.73	HANSCH,C ET AL. (1995)

Predicted Properties

Property	Value	Source
water solubility	3.99e-03 g/l	ALOGPS
logP	3.68	ALOGPS
logP	3.86	ChemAxon
logS	-4.9	ALOGPS
pKa (strongest basic)	3.06	ChemAxon
physiological charge	0	ChemAxon
hydrogen acceptor count	2	ChemAxon
hydrogen donor count	0	ChemAxon
polar surface area	32.67	ChemAxon
rotatable bond count	3	ChemAxon
refractivity	91.75	ChemAxon
polarizability	34.77	ChemAxon

药物相互作用

Drug	Interaction
Cimetidine	Cimetidine may increase the effect of the benzodiazepine, prazepam.
Clozapine	Increased risk of toxicity
Indinavir	The protease inhibitor, indinavir, may increase the effect of the benzodiazepine, prazepam.
Nelfinavir	The protease inhibitor, nelfinavir, may increase the effect of the benzodiazepine, prazepam.
Omeprazole	Omeprazole may increase the effect of the benzodiazepine, prazepam.
Tipranavir	Tipranavir may decrease the metabolism and clearance of Prazepam. Consider alternate therapy or monitor for Prazepam toxic effects if Tipranavir is initiated or dose increased.
Triprolidine	The CNS depressants, Triprolidine and Prazepam, 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 prazepam by decreasing its metabolism. Monitor for prazepam toxicity if voriconazole is initiated or dose increased.

食物相互作用

Avoid alcohol.
Avoid excessive quantities of coffee or tea (Caffeine).
Avoid taking with grapefruit juice.
Take with food.

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