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药品详细

Phenacemide(苯乙酰)

化学结构式图
中文名
苯乙酰
英文名
Phenacemide
分子式
C9H10N2O2
化学名
(2-phenylacetyl)urea
分子量
Average: 178.1879
Monoisotopic: 178.074227574
CAS号
63-98-9
ATC分类
N03A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍

Phenacemide is used to control certain seizures in the treatment of epilepsy. This medicine acts on the central nervous system (CNS) to reduce the number and severity of seizures.

生产厂家
  • Abbott laboratories pharmaceutical products div
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Coker SB: The use of phenacemide for intractable partial complex epilepsy in children. Pediatr Neurol. 1986 Jul-Aug;2(4):230-2. Pubmed
  2. Coker SB, Holmes EW, Egel RT: Phenacemide therapy of complex partial epilepsy in children: determination of plasma drug concentrations. Neurology. 1987 Dec;37(12):1861-6. Pubmed
剂型
规格
化合物类型
Type small molecule
Classes
  • Phenethylamines
Substructures
  • Carboxylic Acids and Derivatives
  • Amino Ketones
  • Benzene and Derivatives
  • Ureas and Derivatives
  • Carbamates and Derivatives
  • Phenethylamines
  • Aromatic compounds
  • Carboxamides and Derivatives
适应症
药理
Indication Used to control certain seizures in the treatment of epilepsy.
Pharmacodynamics Phenacemide is a ureal anticonvulsant indicated for control of severe epilepsy, particularly mixed forms of complex partial (psychomotor or temporal lobe) seizures, refractory to other anticonvulsants. Phenacemide elevates the threshold for minimal electroshock convulsions and abolishes the tonic phase of maximal electroshock seizures. It also prevents or modifies seizures induced by pentylenetetrazol or other convulsants.
Mechanism of action Phenacemide binds to and blocks neuronal sodium channels or voltage sensitive calcium channels. This blocks or suppresses neuronal depolarization and hypersynchronization. Hypersynchronization is what often causes seizures.
Absorption Almost completely absorbed.
Volume of distribution Not Available
Protein binding Not Available
Metabolism
Metabolized in the liver by hepatic microsomal enzymes, where it is inactivated by p-hydroxylation.
Route of elimination Not Available
Half life 22-25 hours.
Clearance Not Available
Toxicity Oral, mouse: LD50 = 987 mg/kg; Oral, rabbit: LD50 = 2500 mg/kg; Oral, rat: LD50 = 1600 mg/kg
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
melting point 215 °C PhysProp
water solubility 10.2 g/L Not Available
logP 0.87 HANSCH,C ET AL. (1995)
Predicted Properties
Property Value Source
water solubility 1.06e+00 g/l ALOGPS
logP 0.81 ALOGPS
logP 0.46 ChemAxon
logS -2.2 ALOGPS
pKa (strongest acidic) 11.75 ChemAxon
pKa (strongest basic) -7.8 ChemAxon
physiological charge 0 ChemAxon
hydrogen acceptor count 2 ChemAxon
hydrogen donor count 2 ChemAxon
polar surface area 72.19 ChemAxon
rotatable bond count 2 ChemAxon
refractivity 47.43 ChemAxon
polarizability 17.49 ChemAxon
药物相互作用
食物相互作用
  • May be taken with food if stomach upset occurs.

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