物质信息
ID:476
名称和标识
商标名
SuximalZaraondanZarondanAsamidEthymalPiknolepsinPemalinPetnidanSuxilepSuxinThetamidZarontinZarodanAtysmalEpileo Petit MalMesentolEmesideEtomalPentinimidPetinimidSimatinSuxinutinSuccimalSuccimitinThilopemalZartalinCapitusPemalPeptinimidPyknolepsinumRonton
IUPAC传统名
2-ethyl-2-methylsuccinimide
别名
EthosuccimideEthosuxideEtosuximidaEthosuccinimideEthosuximideAethosuximide
IUPAC标准名
3-ethyl-3-methylpyrrolidine-2,5-dione
化合物性质
理化性质
疏水性(logP)
0.1
溶解度
39.2 g/L
描述信息
Drug Groups
approved
Description
An anticonvulsant especially useful in the treatment of absence seizures unaccompanied by other types of seizures. [PubChem]
Indication
For the treatment of petit mal epilepsy.
Pharmacology
Used in the treatment of epilepsy. Ethosuximide suppresses the paroxysmal three cycle per second spike and wave activity associated with lapses of consciousness which is common in absence (petit mal) seizures. The frequency of epileptiform attacks is reduced, apparently by depression of the motor cortex and elevation of the threshold of the central nervous system to convulsive stimuli.
Toxicity
Acute overdoses may produce nausea, vomiting, and CNS depression including coma with respiratory depression.
Affected Organisms
Humans and other mammals
Biotransformation
Hepatic, via CYP3A4 and CYP2E1.
Absorption
Bioavailability following oral administration is 93%.
Half Life
53 hours
References
•
Patsalos PN: Properties of antiepileptic drugs in the treatment of idiopathic generalized epilepsies. Epilepsia. 2005;46 Suppl 9:140-8.
[Pubmed]
•
Coulter DA, Huguenard JR, Prince DA: Specific petit mal anticonvulsants reduce calcium currents in thalamic neurons. Neurosci Lett. 1989 Mar 13;98(1):74-8.
[Pubmed]
•
Coulter DA, Huguenard JR, Prince DA: Characterization of ethosuximide reduction of low-threshold calcium current in thalamic neurons. Ann Neurol. 1989 Jun;25(6):582-93.
[Pubmed]
•
Coulter DA, Huguenard JR, Prince DA: Differential effects of petit mal anticonvulsants and convulsants on thalamic neurones: calcium current reduction. Br J Pharmacol. 1990 Aug;100(4):800-6.
[Pubmed]
•
Kostyuk PG, Molokanova EA, Pronchuk NF, Savchenko AN, Verkhratsky AN: Different action of ethosuximide on low- and high-threshold calcium currents in rat sensory neurons. Neuroscience. 1992 Dec;51(4):755-8.
[Pubmed]
External Links
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参考文献
• Kostyuk PG, Molokanova EA, Pronchuk NF, Savchenko AN, Verkhratsky AN: Different action of ethosuximide on low- and high-threshold calcium currents in rat sensory neurons. Neuroscience. 1992 Dec;51(4):755-8. Pubmed
• Coulter DA, Huguenard JR, Prince DA: Specific petit mal anticonvulsants reduce calcium currents in thalamic neurons. Neurosci Lett. 1989 Mar 13;98(1):74-8. Pubmed
• Coulter DA, Huguenard JR, Prince DA: Differential effects of petit mal anticonvulsants and convulsants on thalamic neurones: calcium current reduction. Br J Pharmacol. 1990 Aug;100(4):800-6. Pubmed
• Patsalos PN: Properties of antiepileptic drugs in the treatment of idiopathic generalized epilepsies. Epilepsia. 2005;46 Suppl 9:140-8. Pubmed
• Coulter DA, Huguenard JR, Prince DA: Characterization of ethosuximide reduction of low-threshold calcium current in thalamic neurons. Ann Neurol. 1989 Jun;25(6):582-93. Pubmed