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药品详细

Paramethadione(Paramethadione)

化学结构式图
中文名
Paramethadione
英文名
Paramethadione
分子式
C7H11NO3
化学名
5-ethyl-3,5-dimethyl-1,3-oxazolidine-2,4-dione
分子量
Average: 157.1671
Monoisotopic: 157.073893223
CAS号
115-67-3
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

Paramethadione is an anticonvulsant in the oxazolidinedione class. It is associated with fetal trimethadione syndrome, which is also known as paramethadione syndrome.

生产厂家
  • Abbott laboratories pharmaceutical products div
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Hoffman DJ, Chun AH: Paramethadione and metabolite serum levels in humans after a single oral paramethadione dose. J Pharm Sci. 1975 Oct;64(10):1702-3. Pubmed
  2. Feldman GL, Weaver DD, Lovrien EW: The fetal trimethadione syndrome: report of an additional family and further delineation of this syndrome. Am J Dis Child. 1977 Dec;131(12):1389-92. Pubmed
剂型
规格
化合物类型
Type small molecule
Classes
  • Carbamates and Derivatives
  • Oxazolidinones
Substructures
  • Carbamates and Derivatives
  • Amino Ketones
  • Ethers
  • Oxazolidinones
  • Heterocyclic compounds
  • Carboxamides and Derivatives
  • Carboxylic Acids and Derivatives
适应症
药理
Indication Used for the control of absence (petit mal) seizures that are refractory to treatment with other medications.
Pharmacodynamics Paramethadione is an oxazolidinedione anticonvulsant similar to trimethadione that acts on the central nervous system (CNS) to reduce the number of absence seizures (often seen in epileptics). Absence seizures involve an interruption to consciousness where the person experiencing the seizure seems to become vacant and unresponsive for a short period of time (usually up to 30 seconds). Paramethadione acts on thalamic neurons in the thalamic reticular nucleus (which studies have shown to be associated with absence seizures, von Krosigk et al., 1993).
Mechanism of action Dione anticonvulsants such as paramethadione reduce T-type calcium currents in thalamic neurons (including thalamic relay neurons). This inhibits corticothalamic transmission and raises the threshold for repetitive activity in the thalamus. This results in a dampening of the abnormal thalamocortical rhythmicity proposed to underlie the 3-Hz spike-and-wave discharge seen on electroencephalogram (EEG) during absence seizures.
Absorption Rapid via the digestive tract.
Volume of distribution Not Available
Protein binding Not significant
Metabolism
Primarily hepatic (mainly via cytochrome P450 isozyme 2C9), paramethadione is completely demethylated to 5-ethyl-5-methyl-2,4-oxazolidinedione, the active metabolite.

Important The metabolism module of DrugBank is currently in beta. Questions or suggestions? Please contact us.

Substrate Enzymes Product
Paramethadione
5-ethyl-5-methyl-2,4-oxazolidinedione Details
Route of elimination Not Available
Half life 12 to 24 hours (however the half-life for the active metabolite is not known)
Clearance Not Available
Toxicity Symptoms of overdose include clumsiness or unsteadiness, coma, severe dizziness, severe drowsiness, severe nausea, and problems with vision.
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State liquid
Experimental Properties
Property Value Source
boiling point 101.5 °C Not Available
water solubility 8.4 mg/mL Not Available
logP 0.3 Not Available
Predicted Properties
Property Value Source
water solubility 1.35e+02 g/l ALOGPS
logP 0.9 ALOGPS
logP 1.03 ChemAxon
logS -0.07 ALOGPS
physiological charge 0 ChemAxon
hydrogen acceptor count 2 ChemAxon
hydrogen donor count 0 ChemAxon
polar surface area 46.61 ChemAxon
rotatable bond count 1 ChemAxon
refractivity 37.72 ChemAxon
polarizability 15.39 ChemAxon
药物相互作用
食物相互作用
Not Available

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