Tìm theo
Rufinamide
Các tên gọi khác (3) :
  • Banzel
  • RUF 331
  • Xilep
Thuốc Gốc
Small Molecule
CAS: 106308-44-5
ATC: N03AF03
CTHH: C10H8F2N4O
PTK: 238.1935
Rufinamide is a triazole derivative and an anticonvulsant medication to treat seizure disorders like Lennox-Gastuat syndrome, a form of childhood epilepsy. Clinical trials suggest its efficacy in the treatment of partial seizures.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C10H8F2N4O
Phân tử khối
238.1935
Monoisotopic mass
238.066617308
InChI
InChI=1S/C10H8F2N4O/c11-7-2-1-3-8(12)6(7)4-16-5-9(10(13)17)14-15-16/h1-3,5H,4H2,(H2,13,17)
InChI Key
InChIKey=POGQSBRIGCQNEG-UHFFFAOYSA-N
IUPAC Name
1-[(2,6-difluorophenyl)methyl]-1H-1,2,3-triazole-4-carboxamide
Traditional IUPAC Name
rufinamide
SMILES
NC(=O)C1=CN(CC2=C(F)C=CC=C2F)N=N1
Độ hòa tan
Insoluble
logP
0.835
logS
-2.6
pKa (strongest acidic)
12.69
pKa (Strongest Basic)
-1.1
PSA
73.8 Å2
Refractivity
67.07 m3·mol-1
Polarizability
20.42 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
3
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
2
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : At high concentrations will inhibit action of mGluR5 subtype receptors thus preventing the production of glutamate.
Cơ Chế Tác Dụng : Rufinamide is a triazole derivative and an anticonvulsant medication to treat seizure disorders like Lennox-Gastuat syndrome, a form of childhood epilepsy. Clinical trials suggest its efficacy in the treatment of partial seizures. Rufinamide is a triazole derivative antiepileptic that prolongs the inactive state of voltage gated sodium channels thus stabilizing membranes, ultimately blocking the spread of partial seizure activity.
Dược Động Học :
▧ Absorption :
The oral suspension and tablet are bioequivalent on a mg per mg basis. Rufinamide is well absorbed but the rate is slow and the extent of absorption decreases as dose is increases. Based on urinary excretion, the extent of absorption was at least 85% following oral administration of a single dose of 600 mg rufinamide tablet under fed conditions. Bioavailability= 70%-85% (decreases with increasing doses); Tmax, fed and fasted states= 4-6 hours; Cmax, 10 mg/kg/day= 4.01 µL/mL; Cmax, 30mg/kg/day= 8.68 µL/mL; AUC (0h-12h), 10mg/kg/day= 37.8±47 µg·h/mL; AUC (0h-12h), 30mg/kg/day= 89.3±59 µg·h/mL.
▧ Volume of Distribution :
Rufinamide was evenly distributed between erythrocytes and plasma. The apparent volume of distribution is dependent upon dose and varies with body surface area. The apparent volume of distribution was about 50 L at 3200 mg/day. Volume of distribution is similar between adults and children and is non-linear.
▧ Protein binding :
26.3% - 34.8% with 90% binding to albumin (27%).
▧ Metabolism :
Rufinamide is extensively metabolized but has no active metabolites. Metabolism by carboxyesterases into inactive metabolite CGP 47292, a carboxylic acid derivative, via hydrolysis is the primary biotransformation pathway. A few minor additional metabolites were detected in urine, which appeared to be acyl-glucuronides of CGP 47292. The cytochrome P450 enzyme system or glutathiones are not involved with the metabolism of rufinamide. Rufinamide is a weak inhibitor of CYP 2E1. Rufinamide is a weak inducer of CYP 3A4 enzymes.
▧ Route of Elimination :
Renally (91%; 66% as CGP 47292, 2% as unchanged drug) and fecally (9%) eliminated.
▧ Half Life :
Elimination half-life, healthy subjects and patients with epilepsy = 6-10 hours.
Độc Tính : The most commonly observed adverse reactions (≥10% and greater than placebo) were headache, dizziness, fatigue, somnolence, and nausea.
Chỉ Định : Adjunct therapy for treatment of seizures associated with Lennox-Gastaut syndrome.
Tương Tác Thuốc :
  • Carbamazepine Decrease concentration of rufinamide thus monitor therapy
  • Ethinyl Estradiol Rufinamide decreases plasma concentrations of ethinyl estradiol, thus consider therapy modification
  • Norethindrone Rufinamide decreases plasma concentrations of norethindrone, thus consider therapy modification
  • Phenobarbital Increases clearance of rufinamide thus decreasing plasma concentration of rufinamide.
  • Phenytoin Increases clearance of rufinamide thus decreasing plasma concentration of rufinamide.
  • Primidone Increases clearance of rufinamide thus decreasing plasma concentration of rufinamide.
  • Valproic Acid Valproic acid may increase the therapeutic/toxic effects of Rufinamide. Consider alternate therapy or monitor for changes in Rufinamide serum concentrations, therapeutic and adverse effects if Valproic acid is initiated, discontinued or dose changed. Decreases clearance of rufinamide and is a selective inhibitor of human carboxylesterase thus increasing serum concentrations.
Liều Lượng & Cách Dùng : Suspension - Oral - 40 mg/mL
Tablet - Oral - 100 mg, 200 mg, 400 mg
Dữ Kiện Thương Mại
Nhà Sản Xuất
  • Công ty : Eisai Inc.
    Sản phẩm biệt dược : Banzel
  • Công ty : Eisai Inc.
    Sản phẩm biệt dược : Inovelon
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB06201
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=129228
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=12014051
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D05775
ChemSpider
http://www.chemspider.com/Chemical-Structure.114471.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/62856-582-52
Wikipedia
http://en.wikipedia.org/wiki/Rufinamide
RxList
http://www.rxlist.com/banzel-drug.htm
Drugs.com
http://www.drugs.com/cdi/rufinamide.html
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