Tìm theo
Methsuximide
Các tên gọi khác (16 ) :
  • (RS)-1,3-Dimethyl-3-phenyl-2,5-pyrrolidindion
  • 1,3-Dimethyl-3-phenyl-2,5-dioxopyrrolidine
  • 1,3-Dimethyl-3-phenyl-2,5-pyrrolidinedione
  • 1,3-Dimethyl-3-phenyl-pyrrolidin-2,5-dione
  • 1,3-Dimethyl-3-phenylsuccinimide
  • Alpha-methyl-alpha-phenyl n-methyl succinimide
  • Alpha-methylphensuximide
  • Celontin
  • Mesuximida
  • Mesuximide
  • Mesuximidum
  • Methsuximid
  • Metosuccimmide
  • Metsuccimide
  • N-methyl-alpha-methyl-alpha-phenylsuccinimide
  • N,2-Dimethyl-2-phenylsuccinimide
Thuốc chống co giật, chống động kinh
Thuốc Gốc
Small Molecule
CAS: 77-41-8
ATC: N03AD03
ĐG : Farmea
CTHH: C12H13NO2
PTK: 203.2371
Mesuximide (or methsuximide) is an anticonvulsant medication. It is sold by Pfizer under the name Petinutin. [Wikipedia]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C12H13NO2
Phân tử khối
203.2371
Monoisotopic mass
203.094628665
InChI
InChI=1S/C12H13NO2/c1-12(9-6-4-3-5-7-9)8-10(14)13(2)11(12)15/h3-7H,8H2,1-2H3
InChI Key
InChIKey=AJXPJJZHWIXJCJ-UHFFFAOYSA-N
IUPAC Name
1,3-dimethyl-3-phenylpyrrolidine-2,5-dione
Traditional IUPAC Name
methsuximide
SMILES
CN1C(=O)CC(C)(C1=O)C1=CC=CC=C1
Độ tan chảy
52.5 °C
Độ sôi
121.5 °C at 1.00E-01 mm Hg
Độ hòa tan
2.13e+00 g/l
logP
1.46
logS
-2
pKa (strongest acidic)
19.03
pKa (Strongest Basic)
-7.2
PSA
37.38 Å2
Refractivity
56.35 m3·mol-1
Polarizability
21.4 Å3
Rotatable Bond Count
1
H Bond Acceptor Count
2
H Bond Donor Count
0
Physiological Charge
0
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Used in the treatment of epilepsy. Methsuximide 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.
Cơ Chế Tác Dụng : Mesuximide (or methsuximide) is an anticonvulsant medication. It is sold by Pfizer under the name Petinutin. [Wikipedia] Binds to T-type voltage sensitive calcium channels. Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hormone or neurotransmitter release, gene expression, cell motility, cell division and cell death. The isoform alpha-1G gives rise to T-type calcium currents. T-type calcium channels belong to the "low-voltage activated (LVA)" group and are strongly blocked by mibefradil. A particularity of this type of channels is an opening at quite negative potentials and a voltage-dependent inactivation. T-type channels serve pacemaking functions in both central neurons and cardiac nodal cells and support calcium signaling in secretory cells and vascular smooth muscle. They may also be involved in the modulation of firing patterns of neurons which is important for information processing as well as in cell growth processes.
Dược Động Học :

▧ Half Life :
1.4-2.6 hours for mesuximide and 28-38 hours for the active metabolite.
Độc Tính : Acute overdoses may produce nausea, vomiting, and CNS depression including coma with respiratory depression. Levels greater than 40 µg/mL have caused toxicity and coma has been seen at levels of 150 µg/mL.
Chỉ Định : For the control of absence (petit mal) seizures that are refractory to other drugs.
Tương Tác Thuốc :
  • Lamotrigine Methsuximide decreases the effect of lamotrigine
  • Ticlopidine Ticlopidine may decrease the metabolism and clearance of Methsuximide. Consider alternate therapy or monitor for adverse/toxic effects of Methsuximide if Ticlopidine is initiated, discontinued or dose changed.
  • Triprolidine The CNS depressants, Triprolidine and Methsuximide, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
Liều Lượng & Cách Dùng : Capsule - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Celontin
  • Công ty :
    Sản phẩm biệt dược : Petinutin
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB05246
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=6476
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505339
ChemSpider
http://www.chemspider.com/Chemical-Structure.6231.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0071-0525-24
PharmGKB
http://www.pharmgkb.org/drug/PA164743145
Wikipedia
http://en.wikipedia.org/wiki/Methsuximide
RxList
http://www.rxlist.com/cgi/generic/methsuximide.htm
Drugs.com
http://www.drugs.com/cdi/methsuximide.html
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