Tìm theo
Flumazenil
Các tên gọi khác (5 ) :
  • Anexate
  • Flumazenilo
  • Flumazenilum
  • Flumazepil
  • Lanexat
Thuốc cấp cứu & giải độc
Thuốc Gốc
Small Molecule
CAS: 78755-81-4
ATC: V03AB25
ĐG : Akorn Inc. , http://www.akorn.com
CTHH: C15H14FN3O3
PTK: 303.2884
Fumazenil is an imidazobenzodiazepine derivative and a potent benzodiazepine receptor antagonist that competitively inhibits the activity at the benzodiazepine recognition site on the GABA/benzodiazepine receptor complex, thereby reversing the effects of benzodiazepine on the central nervous system.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C15H14FN3O3
Phân tử khối
303.2884
Monoisotopic mass
303.101919534
InChI
InChI=1S/C15H14FN3O3/c1-3-22-15(21)13-12-7-18(2)14(20)10-6-9(16)4-5-11(10)19(12)8-17-13/h4-6,8H,3,7H2,1-2H3
InChI Key
InChIKey=OFBIFZUFASYYRE-UHFFFAOYSA-N
IUPAC Name
ethyl 12-fluoro-8-methyl-9-oxo-2,4,8-triazatricyclo[8.4.0.0^{2,6}]tetradeca-1(10),3,5,11,13-pentaene-5-carboxylate
Traditional IUPAC Name
flumazenil
SMILES
CCOC(=O)C1=C2CN(C)C(=O)C3=C(C=CC(F)=C3)N2C=N1
Độ tan chảy
201-203 °C
Độ hòa tan
128 mg/L
logP
1.00
logS
-2.5
pKa (Strongest Basic)
3.27
PSA
64.43 Å2
Refractivity
87.93 m3·mol-1
Polarizability
29.97 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
3
H Bond Donor Count
0
Physiological Charge
0
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Flumazenil antagonizes the CNS effects produced by benzodiazepines, but does not antagonize the central nervous system effects of drugs affecting GABA-ergic neurons by means other than the benzodiazepine receptor (including ethanol, barbiturates, or general anesthetics) and does not reverse the effects of opioids.
Cơ Chế Tác Dụng : Fumazenil is an imidazobenzodiazepine derivative and a potent benzodiazepine receptor antagonist that competitively inhibits the activity at the benzodiazepine recognition site on the GABA/benzodiazepine receptor complex, thereby reversing the effects of benzodiazepine on the central nervous system. Flumazenil, an imidazobenzodiazepine derivative, antagonizes the actions of benzodiazepines on the central nervous system. Flumazenil competitively inhibits the activity at the benzodiazepine recognition site on the GABA/benzodiazepine receptor complex. Flumazenil is a weak partial agonist in some animal models of activity, but has little or no agonist activity in man.
Dược Động Học :

▧ Volume of Distribution :
* 0.9 to 1.1 L/kg
▧ Protein binding :
Protein binding is approximately 50%, mostly (66%) to albumin. Protein binding is reduced in patients with hepatic cirrhosis.
▧ Metabolism :
Hepatic. Flumazenil is completely (99%) metabolized. The major metabolites of flumazenil identified in urine are the de-ethylated free acid and its glucuronide conjugate.
▧ Route of Elimination :
Flumazenil is completely (99%) metabolized. Elimination of radiolabeled drug is essentially complete within 72 hours, with 90% to 95% of the radioactivity appearing in urine and 5% to 10% in the feces.
▧ Half Life :
Initial distribution half-life is 4 to 11 minutes and the terminal half-life is 40 to 80 minutes. Prolongation of the half-life to 1.3 hours in patients with moderate hepatic impairment and 2.4 hours in severely impaired patients. Compared to adults, the elimination half-life in pediatric patients was more variable, averaging 40 minutes (range: 20 to 75 minutes).
▧ Clearance :
* 1 L/hr/kg [healthy volunteers receiving a 5-minute infusion of a total of 1 mg]
Độc Tính : In clinical studies, most adverse reactions to flumazenil were an extension of the pharmacologic effects of the drug in reversing benzodiazepine effects.
Chỉ Định : For the complete or partial reversal of the sedative effects of benzodiazepines in cases where general anesthesia has been induced and/or maintained with benzodiazepines, and where sedation has been produced with benzodiazepines for diagnostic and therapeutic procedures. Also for the management of benzodiazepine overdose as an adjunct for appropriate supportive and symptomatic measures.
Liều Lượng & Cách Dùng : Solution - Intravenous
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Sản phẩm biệt dược : Anexate
  • Công ty :
    Sản phẩm biệt dược : Lanexat
  • Công ty :
    Sản phẩm biệt dược : Mazicon
  • Công ty :
    Sản phẩm biệt dược : Romazicon
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01205
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3373
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507438
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07825
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00697
ChemSpider
http://www.chemspider.com/Chemical-Structure.3256.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=26263
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0004-6911-06
PharmGKB
http://www.pharmgkb.org/drug/PA449659
Wikipedia
http://en.wikipedia.org/wiki/Flumazenil
RxList
http://www.rxlist.com/cgi/generic3/flumazenil.htm
Drugs.com
http://www.drugs.com/cdi/flumazenil.html
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