Tìm theo
Ethosuximide
Các tên gọi khác (20 ) :
  • (+-)-2-Ethyl-2-methylsuccinimide
  • (±)-2-ethyl-2-methylsuccinimide
  • 2-ethyl-2-methylsuccinimide
  • 2-Methyl-2-ethylsuccinimide
  • 3-ethyl-3-methyl-2,5-pyrrolidinedione
  • 3-Ethyl-3-methylsuccinimide
  • 3-Methyl-3-ethylpyrrolidine-2,5-dione
  • 3-Methyl-3-ethylsuccinimide
  • Aethosuximide
  • alpha-Ethyl-alpha-methylsuccinimide
  • alpha-Methyl-alpha-ethylsuccinimide
  • Atysmal
  • Ethosuximid
  • Ethosuximide
  • Ethosuximidum
  • Etosuximida
  • gamma-Ethyl-gamma-methyl-succinimide
  • gamma-Methyl-gamma-ethyl-succinimide
  • Thilopemal
  • γ-ethyl-γ-methyl-succinimide
Thuốc chống co giật, chống động kinh
Thuốc Gốc
Small Molecule
CAS: 77-67-8
ATC: N03AD01
ĐG : Barr Pharmaceuticals
CTHH: C7H11NO2
PTK: 141.1677
An anticonvulsant especially useful in the treatment of absence seizures unaccompanied by other types of seizures. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C7H11NO2
Phân tử khối
141.1677
Monoisotopic mass
141.078978601
InChI
InChI=1S/C7H11NO2/c1-3-7(2)4-5(9)8-6(7)10/h3-4H2,1-2H3,(H,8,9,10)
InChI Key
InChIKey=HAPOVYFOVVWLRS-UHFFFAOYSA-N
IUPAC Name
3-ethyl-3-methylpyrrolidine-2,5-dione
Traditional IUPAC Name
ethosuximide
SMILES
CCC1(C)CC(=O)NC1=O
Độ tan chảy
64.5 °C
Độ hòa tan
39.2 g/L
logP
0.38
logS
-0.15
pKa (strongest acidic)
10.73
pKa (Strongest Basic)
-6.6
PSA
46.17 Å2
Refractivity
35.96 m3·mol-1
Polarizability
14.45 Å3
Rotatable Bond Count
1
H Bond Acceptor Count
2
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
1
Bioavailability
1
Rule of Five
true
Dược Lực Học : Used in the treatment of epilepsy. Ethosuximide 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 : An anticonvulsant especially useful in the treatment of absence seizures unaccompanied by other types of seizures. [PubChem] 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 :
▧ Absorption :
Bioavailability following oral administration is 93%.
▧ Metabolism :
Hepatic, via CYP3A4 and CYP2E1.
▧ Half Life :
53 hours
Độc Tính : Acute overdoses may produce nausea, vomiting, and CNS depression including coma with respiratory depression.
Chỉ Định : For the treatment of petit mal epilepsy.
Tương Tác Thuốc :
  • Telithromycin Telithromycin may reduce clearance of Ethosuximide. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Ethosuximide if Telithromycin is initiated, discontinued or dose changed.
  • Triprolidine The CNS depressants, Triprolidine and Ethosuximide, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
  • Voriconazole Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of ethosuximide by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of ambrisentan if voriconazole is initiated, discontinued or dose changed.
Liều Lượng & Cách Dùng : Capsule - Oral
Syrup - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Chemidex
    Sản phẩm biệt dược : Emeside
  • Công ty : Apotex Europe
    Sản phẩm biệt dược : Ethymal
  • Công ty : Apsen
    Sản phẩm biệt dược : Etoxin
  • Công ty : Osel
    Sản phẩm biệt dược : Petimid
  • Công ty : Gerot
    Sản phẩm biệt dược : Petinimid
  • Công ty : Desitin
    Sản phẩm biệt dược : Petnidan
  • Công ty : Jenapharm
    Sản phẩm biệt dược : Suxilep
  • Công ty : McNeil
    Sản phẩm biệt dược : Suxinutin
  • Công ty : Pfizer
    Sản phẩm biệt dược : Zarondan
  • Công ty : Pfizer
    Sản phẩm biệt dược : Zarontin
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00593
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3291
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507617
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07505
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00539
ChemSpider
http://www.chemspider.com/Chemical-Structure.3175.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50240424
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0071-0237-24
PharmGKB
http://www.pharmgkb.org/drug/PA449533
Wikipedia
http://en.wikipedia.org/wiki/Ethosuximide
RxList
http://www.rxlist.com/cgi/generic/ethosuximide.htm
Drugs.com
http://www.drugs.com/cdi/ethosuximide.html
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