Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Monoisotopic mass
143.058243159
InChI
InChI=1S/C6H9NO3/c1-6(2)4(8)7(3)5(9)10-6/h1-3H3
InChI Key
InChIKey=IRYJRGCIQBGHIV-UHFFFAOYSA-N
IUPAC Name
trimethyl-1,3-oxazolidine-2,4-dione
Traditional IUPAC Name
trimethadione
SMILES
CN1C(=O)OC(C)(C)C1=O
Refractivity
33.2 m3·mol-1
Dược Lực Học :
Paramethadione and trimethadione are anticonvulsants indicated in the control of absence (petit mal) seizures that are refractory to treatment with other medications. Dione anticonvulsants are used in the treatment of epilepsy. They act on the central nervous system (CNS) to reduce the number of seizures.
Cơ Chế Tác Dụng :
An anticonvulsant effective in absence seizures, but generally reserved for refractory cases because of its toxicity. (From AMA Drug Evaluations Annual, 1994, p378)
Dione anticonvulsants reduce T-type calcium currents in thalamic neurons, including thalamic relay neurons. It does so via the inhibition of voltage dependent T-type calcium channels. This raises the threshold for repetitive activity in the thalamus, and inhibits corticothalamic transmission. Thus, the abnormal thalamocortical rhythmicity, which is thought to underlie the 3-Hz spike-and-wave discharge seen on electroencephalogram(EEG) with absence seizures, is dampened.
Dược Động Học :
▧ Protein binding :
90%
Độc Tính :
Symptoms of overdose include clumsiness or unsteadiness, coma, dizziness (severe), drowsiness (severe), nausea (severe), and problems with vision.
Chỉ Định :
Used in the control of absence (petit mal) seizures that are refractory to treatment with other medications.
Tương Tác Thuốc :
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Disulfiram
Disulfiram, a strong CYP2E1 inhibitor, may decrease the metabolism and clearance of Trimethadione, a CYP2E1 substrate. Consider alternate therapy or monitor for changes in Trimethadione therapeutic and adverse effects if Disulfiram is initiated, discontinued or dose changed.
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Triprolidine
The CNS depressants, Triprolidine and Trimethadione, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.