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药品详细

Nitrazepam(硝西泮)

化学结构式图
中文名
硝西泮
英文名
Nitrazepam
分子式
C15H11N3O3
化学名
7-nitro-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-2-one
分子量
Average: 281.2661
Monoisotopic: 281.080041233
CAS号
146-22-5
ATC分类
N05C 未知;N05C 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

A benzodiazepine derivative used as an anticonvulsant and hypnotic.

生产厂家
    封装厂家
    参考
    Synthesis Reference Not Available
    General Reference
    1. Rickels K: The clinical use of hypnotics: indications for use and the need for a variety of hypnotics. Acta Psychiatr Scand Suppl. 1986;332:132-41. Pubmed
    2. Robertson MD, Drummer OH: Postmortem drug metabolism by bacteria. J Forensic Sci. 1995 May;40(3):382-6. Pubmed
    3. Oelschlager H: [Chemical and pharmacologic aspects of benzodiazepines] Schweiz Rundsch Med Prax. 1989 Jul 4;78(27-28):766-72. Pubmed
    4. Podhorna J, Krsiak M: Behavioural effects of a benzodiazepine receptor partial agonist, Ro 19-8022, in the social conflict test in mice. Behav Pharmacol. 2000 Apr;11(2):143-51. Pubmed
    5. Nowakowska E, Chodera A: Studies on the involvement of opioid mechanism in the locomotor effects of benzodiazepines in rats. Pharmacol Biochem Behav. 1991 Feb;38(2):265-6. Pubmed
    剂型
    规格
    化合物类型
    Type small molecule
    Classes
    • Benzodiazepines
    • Lactams
    Substructures
    • Benzodiazepines
    • Nitrobenzenes
    • Oxoazaniums
    • Amino Ketones
    • Benzene and Derivatives
    • Carboxylic Acids and Derivatives
    • Nitro compounds
    • Heterocyclic compounds
    • Aromatic compounds
    • Carboxamides and Derivatives
    • Diazepines
    • Lactams
    • Imines
    • Anilines
    适应症
    药理
    Indication Used to treat short-term sleeping problems (insomnia), such as difficulty falling asleep, frequent awakenings during the night, and early-morning awakening.
    Pharmacodynamics Nitrazepam is a type of benzodiazepine drug. It is a powerful hypnotic drug which possesses strong sedative, anxiolytic, amnestic, anticonvulsant, and skeletal muscle relaxant properties. Nitrazepam shortens the time required to fall asleep and lengthens the duration of sleep. It is also useful for the management of myoclonic seizures.
    Mechanism of action Nitrazepam belongs to a group of medicines called benzodiazepines. It acts on benzodiazepine receptors in the brain which are associated with the GABA receptors causing an enhanced binding of GABA (gamma amino butyric acid) to GABAA receptors. GABA is a major inhibitory neurotransmitter in the brain, involved in inducing sleepiness, muscular relaxation and control of anxiety and fits, and slows down the central nervous system. The anticonvulsant properties of nitrazepam and other benzodiazepines may be in part or entirely due to binding to voltage-dependent sodium channels rather than benzodiazepine receptors. Sustained repetitive firing seems to be limited by benzodiazepines effect of slowing recovery of sodium channels from inactivation.
    Absorption Bioavailability is 53-94% following oral administration.
    Volume of distribution Not Available
    Protein binding Not Available
    Metabolism
    Not Available
    Route of elimination Not Available
    Half life 15-38 hours (mean elimination half life 26 hours).
    Clearance Not Available
    Toxicity Nitrazepam is a drug which is very frequently involved in drug intoxication, including overdose. Nitrazepam overdose may result in stereotypical symptoms of benzodiazepine overdose including intoxication, impaired balance, slurred speech. In cases of severe overdose this may progress to a comatose state with the possibility of death.
    Affected organisms
    • Humans and other mammals
    Pathways Not Available
    理化性质
    Properties
    State solid
    Experimental Properties
    Property Value Source
    melting point 225 °C PhysProp
    logP 2.25 HANSCH,C ET AL. (1995)
    logS -3.8 ADME Research, USCD
    Predicted Properties
    Property Value Source
    water solubility 2.99e-02 g/l ALOGPS
    logP 1.95 ALOGPS
    logP 2.55 ChemAxon
    logS -4 ALOGPS
    pKa (strongest acidic) 11.9 ChemAxon
    pKa (strongest basic) 2.61 ChemAxon
    physiological charge 0 ChemAxon
    hydrogen acceptor count 4 ChemAxon
    hydrogen donor count 1 ChemAxon
    polar surface area 87.28 ChemAxon
    rotatable bond count 2 ChemAxon
    refractivity 79.22 ChemAxon
    polarizability 27.59 ChemAxon
    药物相互作用
    Drug Interaction
    Clozapine Increased risk of toxicity
    食物相互作用
    • Avoid alcohol.
    • Avoid excessive quantities of coffee or tea (Caffeine).
    • Take with food.

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