物质信息

ID:500

名称和标识
商标名
Parametadiona [INN-Spanish]ParametadioneParamethadionum [INN-Latin]Paramethadione [BAN:INN]Parametadione [DCIT]IsoethadioneParadioneParadione (TN)
IUPAC标准名
5-ethyl-3,5-dimethyl-1,3-oxazolidine-2,4-dione
IUPAC传统名
@paramethadione
别名
Paramethadione
数据登录号
PubChem CID
PubChem SID
CAS号
化合物性质
理化性质
疏水性(logP)
0.3
溶解度
8.4 mg/mL
描述信息
Drug Groups
approved
Description
Paramethadione is an anticonvulsant in the oxazolidinedione class. It is associated with fetal trimethadione syndrome, which is also known as paramethadione syndrome.
Indication
Used for the control of absence (petit mal) seizures that are refractory to treatment with other medications.
Pharmacology
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).
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
Biotransformation
Primarily hepatic (mainly via cytochrome P450 isozyme 2C9), paramethadione is completely demethylated to 5-ethyl-5-methyl-2,4-oxazolidinedione, the active metabolite.
Absorption
Rapid via the digestive tract.
Half Life
12 to 24 hours (however the half-life for the active metabolite is not known)
Protein Binding
Not significant
References
• 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]
• 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]
External Links
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参考文献
• 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
• 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