Substance

ID:500

Names and Identifiers
Brand Name
Parametadiona [INN-Spanish]ParametadioneParamethadionum [INN-Latin]Paramethadione [BAN:INN]Parametadione [DCIT]IsoethadioneParadioneParadione (TN)
IUPAC name
5-ethyl-3,5-dimethyl-1,3-oxazolidine-2,4-dione
IUPAC Traditional name
@paramethadione
Synonyms
Paramethadione
Registration numbers
PubChem CID
PubChem SID
CAS Number
Properties
Physical Property
Hydrophobicity(logP)
0.3
Solubility
8.4 mg/mL
Molecule Details
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
Molecular Spectra
No Data Available
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References
• 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