Tìm theo
Felbamate
Các tên gọi khác (6 ) :
  • 2-Phenyl-1,3-propanediol dicarbamate
  • Carbamic acid 2-phenyltrimethylene ester
  • Carbamic acid 3-carbamoyloxy-2-phenyl-propyl ester
  • Felbamate
  • Felbamato
  • Felbamatum
Thuốc chống co giật, chống động kinh
Thuốc Gốc
Small Molecule
CAS: 25451-15-4
ATC: N03AX10
ĐG : Aptuit Laurus Pvt Ltd. , http://www.aptuitlaurus.com
CTHH: C11H14N2O4
PTK: 238.2399
Felbamate is an anticonvulsant drug used in the treatment of epilepsy. It is used to treat partial seizures (with and without generalization) in adults and partial and generalized seizures associated with Lennox-Gastaut syndrome in children. It has a weak inhibitory effect on GABA receptor binding sites.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C11H14N2O4
Phân tử khối
238.2399
Monoisotopic mass
238.095356946
InChI
InChI=1S/C11H14N2O4/c12-10(14)16-6-9(7-17-11(13)15)8-4-2-1-3-5-8/h1-5,9H,6-7H2,(H2,12,14)(H2,13,15)
InChI Key
InChIKey=WKGXYQFOCVYPAC-UHFFFAOYSA-N
IUPAC Name
3-(carbamoyloxy)-2-phenylpropyl carbamate
Traditional IUPAC Name
felbamate
SMILES
NC(=O)OCC(COC(N)=O)C1=CC=CC=C1
Độ tan chảy
151.5 °C
Độ hòa tan
Slightly soluble in water
logP
0.3
logS
-2.5
pKa (strongest acidic)
14.98
PSA
104.64 Å2
Refractivity
59.59 m3·mol-1
Polarizability
23.52 Å3
Rotatable Bond Count
7
H Bond Acceptor Count
2
H Bond Donor Count
2
Physiological Charge
0
Number of Rings
1
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Felbamate is an antiepileptic indicated as monotherapy or as an adjunct to other anticonvulsants for the treatment of partial seizures resulting from epilepsy. Receptor-binding studies in vitro indicate that felbamate has weak inhibitory effects on GABA-receptor binding, benzodiazepine receptor binding, and is devoid of activity at the MK-801 receptor binding site of the NMDA receptor-ionophore complex. However, felbamate does interact as an antagonist at the strychnine-insensitive glycine recognition site of the NMDA receptor-ionophore complex.
Cơ Chế Tác Dụng : Felbamate is an anticonvulsant drug used in the treatment of epilepsy. It is used to treat partial seizures (with and without generalization) in adults and partial and generalized seizures associated with Lennox-Gastaut syndrome in children. It has a weak inhibitory effect on GABA receptor binding sites. The mechanism by which felbamate exerts its anticonvulsant activity is unknown, but in animal test systems designed to detect anticonvulsant activity, felbamate has properties in common with other marketed anticonvulsants. In vitro receptor binding studies suggest that felbamate may be an antagonist at the strychnine-insensitive glycine-recognition site of the N-methyl-D-aspartate (NMDA) receptor-ionophore complex. Antagonism of the NMDA receptor glycine binding site may block the effects of the excitatory amino acids and suppress seizure activity. Animal studies indicate that felbamate may increase the seizure threshold and may decrease seizure spread. It is also indicated that felbamate has weak inhibitory effects on GABA-receptor binding, benzodiazepine receptor binding.
Dược Động Học :
▧ Absorption :
>90%
▧ Volume of Distribution :
* 756±82 mL/kg
▧ Protein binding :
20-36%
▧ Metabolism :
Hepatic
▧ Half Life :
20-23 hours
▧ Clearance :
* 26 +/- 3 mL/hr/kg [single 1200 mg dose] * 30 +/- 8 mL/hr/kg [multiple daily doses of 3600 mg]
Độc Tính : LD50=5000 mg/kg (Orally in rats)
Chỉ Định : For use only in those patients who respond inadequately to alternative treatments and whose epilepsy is so severe that a substantial risk of aplastic anemia and/or liver failure is deemed acceptable in light of the benefits conferred by its use.
Tương Tác Thuốc :
  • Carbamazepine Decreased effect of both products
  • Ethotoin Increased phenytoin levels and decreased felbamate levels
  • Fosphenytoin Increased phenytoin levels and decreased felbamate levels
  • Mephenytoin Increased phenytoin levels and decreased felbamate levels
  • Phenobarbital Felbamate increases the effect and toxicity of phenobarbital/primidone
  • Phenytoin Increased phenytoin levels and decreased felbamate levels
  • Primidone Felbamate may increase the effect and toxicity of primidone.
  • Quinupristin This combination presents an increased risk of toxicity
  • Telithromycin Telithromycin may reduce clearance of Felbamate. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Felbamate if Telithromycin is initiated, discontinued or dose changed.
  • Triprolidine The CNS depressants, Triprolidine and Felbamate, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
  • Ulipristal Concomitant therapy with strong CYP3A4 inducers may decrease plasma concentrations of ulipristal and ultimately its effectiveness. Avoid combination therapy.
  • Valproic Acid Felbamate, a CYP2C19 inhibitor, may decrease the metabolism of Valproic acid, a CYP2C19 substrate. Consider alternate therapy or monitor for changes in Valproic acid therapeutic and adverse effects if Felbamate is initiated, discontinued or dose changed.
  • Voriconazole Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of felbamate by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of felbamate if voriconazole is initiated, discontinued or dose changed.
Liều Lượng & Cách Dùng : Suspension - Oral
Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Felbamyl
  • Công ty :
    Sản phẩm biệt dược : Felbatol
  • Công ty :
    Sản phẩm biệt dược : Taloxa
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00949
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3331
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506375
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07501
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00536
ChemSpider
http://www.chemspider.com/Chemical-Structure.3214.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50240678
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0037-0430-01
PharmGKB
http://www.pharmgkb.org/drug/PA449590
Wikipedia
http://en.wikipedia.org/wiki/Felbamate
RxList
http://www.rxlist.com/cgi/generic3/felbamate.htm
Drugs.com
http://www.drugs.com/cdi/felbamate.html
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