用户名： 密   码：
注册 | 忘记密码？
药品详细

Amobarbital(异戊巴比妥)

化学结构式图
中文名
异戊巴比妥
英文名
Amobarbital
分子式
C11H18N2O3
化学名
5-ethyl-5-(3-methylbutyl)-1,3-diazinane-2,4,6-trione
分子量
Average: 226.2722
Monoisotopic: 226.131742452
CAS号
57-43-2
ATC分类
N05C 未知
药物类型
small molecule
阶段
illicit, approved
商品名
同义名
基本介绍

A barbiturate with hypnotic and sedative properties (but not antianxiety). Adverse effects are mainly a consequence of dose-related CNS depression and the risk of dependence with continued use is high. (From Martindale, The Extra Pharmacopoeia, 30th ed, p565)

生产厂家
    封装厂家
    参考
    Synthesis Reference Not Available
    General Reference
    1. Kim HS, Wan X, Mathers DA, Puil E: Selective GABA-receptor actions of amobarbital on thalamic neurons. Br J Pharmacol. 2004 Oct;143(4):485-94. Epub 2004 Sep 20. Pubmed
    2. Maynert EW: The alcoholic metabolites of pentobarbital and amobarbital in man. J Pharmacol Exp Ther. 1965 Oct;150(1):118-21. Pubmed
    3. Tang BK, Kalow W, Grey AA: Amobarbital metabolism in man: N-glucoside formation. Res Commun Chem Pathol Pharmacol. 1978 Jul;21(1):45-53. Pubmed
    4. Soine PJ, Soine WH: High-performance liquid chromatographic determination of the diastereomers of 1-(beta-D-glucopyranosyl)amobarbital in urine. J Chromatogr. 1987 Nov 27;422:309-14. Pubmed
    5. McCall WV: The addition of intravenous caffeine during an amobarbital interview. J Psychiatry Neurosci. 1992 Nov;17(5):195-7. Pubmed
    剂型
    规格
    化合物类型
    Type small molecule
    Classes
    • Barbiturates
    Substructures
    • Barbiturates
    • Carbonyl Compounds
    • Carboxylic Acids and Derivatives
    • Amino Ketones
    • Ureas and Derivatives
    • Pyrimidines and Derivatives
    • Heterocyclic compounds
    • Carboxamides and Derivatives
    适应症
    药理
    Indication Not Available
    Pharmacodynamics Not Available
    Mechanism of action Amobarbital (like all barbiturates) works by binding to the GABAA receptor at either the alpha or the beta sub unit. These are binding sites that are distinct from GABA itself and also distinct from the benzodiazepine binding site. Like benzodiazepines, barbiturates potentiate the effect of GABA at this receptor. This GABAA receptor binding decreases input resistance, depresses burst and tonic firing, especially in ventrobasal and intralaminar neurons, while at the same time increasing burst duration and mean conductance at individual chloride channels; this increases both the amplitude and decay time of inhibitory postsynaptic currents. In addition to this GABA-ergic effect, barbiturates also block the AMPA receptor, a subtype of glutamate receptor. Glutamate is the principal excitatory neurotransmitter in the mammalian CNS. Amobarbital also appears to bind neuronal nicotinic acetylcholine receptors.
    Absorption Not Available
    Volume of distribution Not Available
    Protein binding Not Available
    Metabolism
    Not Available
    Route of elimination Not Available
    Half life Not Available
    Clearance Not Available
    Toxicity Not Available
    Affected organisms Not Available
    Pathways Not Available
    理化性质
    Properties
    State solid
    Experimental Properties
    Property Value Source
    melting point 157 °C PhysProp
    water solubility 603 mg/L (at 25 °C) YALKOWSKY,SH & DANNENFELSER,RM (1992)
    logP 2.07 HANSCH,C ET AL. (1995)
    logS -2.57 ADME Research, USCD
    pKa 7.84 SANGSTER (1994)
    Predicted Properties
    Property Value Source
    water solubility 8.97e-01 g/l ALOGPS
    logP 1.87 ALOGPS
    logP 1.89 ChemAxon
    logS -2.4 ALOGPS
    pKa (strongest acidic) 8.48 ChemAxon
    physiological charge 0 ChemAxon
    hydrogen acceptor count 3 ChemAxon
    hydrogen donor count 2 ChemAxon
    polar surface area 75.27 ChemAxon
    rotatable bond count 4 ChemAxon
    refractivity 58 ChemAxon
    polarizability 23.45 ChemAxon
    药物相互作用
    Drug Interaction
    Aminophylline The barbiturate, amobarbital, decreases the effect of aminophylline.
    Betamethasone The barbiturate, amobarbital, may decrease the effect of the corticosteroid, betamethasone.
    Clomifene The enzyme inducer, amobarbital, decreases the effect of the hormone agent, clomifene.
    Conjugated Estrogens The enzyme inducer, amobarbital, decreases the effect of the hormone agent, conjugated estrogens.
    Cyclosporine The barbiturate, amobarbital, increases the effect of cyclosporine.
    Dexamethasone The barbiturate, amobarbital, may decrease the effect of the corticosteroid, dexamethasone.
    Diethylstilbestrol The enzyme inducer, amobarbital, decreases the effect of the hormone agent, diethylstilbestrol.
    Doxycycline The anticonvulsant, amobarbital, decreases the effect of doxycycline.
    Eltrombopag Affects hepatic CYP1A2 metabolism, will decrease effect/level of eltrombopag. Affects hepatic CYP2C9/10 metabolism, will decrease effect/level of eltrombopag.
    Estradiol The enzyme inducer, amobarbital, decreases the effect of the hormone agent, estradiol.
    Ethinyl Estradiol This product may cause a slight decrease of contraceptive effect
    Felodipine The barbiturate, amobarbital, decreases the effect of felodipine.
    Fludrocortisone The barbiturate, amobarbital, may decrease the effect of the corticosteroid, fludrocortisone.
    Folic Acid Folic acid decreases the effect of anticonvulsant, amobarbital.
    Gefitinib The CYP3A4 inducer, amobarbital, may decrease the serum concentration and therapeutic effects of gefitinib.
    Griseofulvin The barbiturate, amobarbital, decreases the effect of griseofulvin.
    Hydrocortisone The barbiturate, amobarbital, may decrease the effect of the corticosteroid, hydrocortisone.
    Levonorgestrel Phenobarbital decreases the effect of levonorgestrel
    Medroxyprogesterone The enzyme inducer, amobarbital, decreases the effect of the hormone agent, medroxyprogesterone.
    Megestrol The enzyme inducer, amobarbital, decreases the effect of the hormone agent, megestrol.
    Methadone The barbiturate, amobarbital, decreases the effect of methadone.
    Metronidazole The barbiturate, amobarbital, decreases the effect of metronidazole.
    Nifedipine The barbiturate, amobarbital, decreases the effect of the calcium channel blocker, nifedipine.
    Norethindrone This product may cause a slight decrease of contraceptive effect
    Oxtriphylline The barbiturate, amobarbital, decreases the effect of oxtriphylline.
    Prednisolone The barbiturate, amobarbital, may decrease the effect of the corticosteroid, prednisolone.
    Prednisone The barbiturate, amobarbital, may decrease the effect of the corticosteroid, prednisone.
    Quinidine The anticonvulsant, amobarbital, decreases the effect of quinidine.
    Theophylline The barbiturate, amobarbital, decreases the effect of theophylline.
    Triamcinolone The barbiturate, amobarbital, may decrease the effect of the corticosteroid, triamcinolone.
    Trimipramine The barbiturate, Amobarbital, may increase the metabolism and clearance of Trimipramine. Monitor for changes in the therapeutics and adverse effects of Trimipramine if Amobarbital is initiated, discontinued or dose changed. Dose adjustments of Trimipramine may be required.
    Triprolidine The CNS depressants, Triprolidine and Amobarbital, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
    Verapamil Amobarbital, a CYP3A4 inducer, may increase the serum concentration of Verapamil, a CYP3A4 substrate. Monitor for changes in the therapeutic/adverse effects of Verapamil if Amobarbital is initiated, discontinued or dose changed.
    Voriconazole Amobarbital may reduce serum concentrations and efficacy of voriconazole. Concomitant voriconazole and long-acting barbiturates therapy is contraindicated.
    Warfarin Amobarbital may decrease the serum concentration of warfarin by increasing its metabolism. Monitor for changes in the therapeutic and adverse effects of warfarin if amobarbital is initiated, discontinued or dose changed.
    食物相互作用
    Not Available

    返回 | 收藏