Tìm theo
Paramethadione
Các tên gọi khác (5 ) :
  • Paradione
  • Parametadiona
  • Parametadione
  • Paramethadione
  • Paramethadionum
Thuốc Gốc
Small Molecule
CAS: 115-67-3
ATC: N03AC01
CTHH: C7H11NO3
PTK: 157.1671
Paramethadione is an anticonvulsant in the oxazolidinedione class. It is associated with fetal trimethadione syndrome, which is also known as paramethadione syndrome.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C7H11NO3
Phân tử khối
157.1671
Monoisotopic mass
157.073893223
InChI
InChI=1S/C7H11NO3/c1-4-7(2)5(9)8(3)6(10)11-7/h4H2,1-3H3
InChI Key
InChIKey=VQASKUSHBVDKGU-UHFFFAOYSA-N
IUPAC Name
5-ethyl-3,5-dimethyl-1,3-oxazolidine-2,4-dione
Traditional IUPAC Name
paramethadione
SMILES
CCC1(C)OC(=O)N(C)C1=O
Độ sôi
101.5 °C
Độ hòa tan
8.4 mg/mL
logP
0.3
logS
-0.07
PSA
46.61 Å2
Refractivity
37.72 m3·mol-1
Polarizability
15.39 Å3
Rotatable Bond Count
1
H Bond Acceptor Count
2
H Bond Donor Count
0
Physiological Charge
0
Number of Rings
1
Bioavailability
1
Rule of Five
true
Dược Lực Học : 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).
Cơ Chế Tác Dụng : Paramethadione is an anticonvulsant in the oxazolidinedione class. It is associated with fetal trimethadione syndrome, which is also known as paramethadione syndrome. 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.
Dược Động Học :
▧ Absorption :
Rapid via the digestive tract.
▧ 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.
▧ Half Life :
12 to 24 hours (however the half-life for the active metabolite is not known)
Độc Tính : Symptoms of overdose include clumsiness or unsteadiness, coma, severe dizziness, severe drowsiness, severe nausea, and problems with vision.
Chỉ Định : Used for the control of absence (petit mal) seizures that are refractory to treatment with other medications.
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00617
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=8280
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46509173
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07411
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00495
ChemSpider
http://www.chemspider.com/Chemical-Structure.7979.html
PharmGKB
http://www.pharmgkb.org/drug/PA164748880
Wikipedia
http://en.wikipedia.org/wiki/Paramethadione
Drugs.com
http://www.drugs.com/mtm/paramethadione.html
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