Tìm theo
Fomepizole
Các tên gọi khác (6 ) :
  • 4-Methylpyrazol
  • 4-methylpyrazole
  • Antizol
  • Fomepizol
  • Fomepizole
  • Fomepizolum
antidotes
Thuốc Gốc
Small Molecule
CAS: 7554-65-6
ATC: V03AB34
ĐG : Alliance Medical Products , http://www.amp-us.com
CTHH: C4H6N2
PTK: 82.1038
Fomepizole is used as an antidote in confirmed or suspected methanol or ethylene glycol poisoning. Fomepizole is a competitive inhibitor of alcohol dehydrogenase, the enzyme that catalyzes the initial steps in the metabolism of ethylene glycol and methanol to their toxic metabolites.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C4H6N2
Phân tử khối
82.1038
Monoisotopic mass
82.053098202
InChI
InChI=1S/C4H6N2/c1-4-2-5-6-3-4/h2-3H,1H3,(H,5,6)
InChI Key
InChIKey=RIKMMFOAQPJVMX-UHFFFAOYSA-N
IUPAC Name
4-methyl-1H-pyrazole
Traditional IUPAC Name
fomepizole
SMILES
CC1=CNN=C1
Độ tan chảy
25 °C
Độ hòa tan
5.59e+02 g/l
logP
0.9
logS
0.83
pKa (strongest acidic)
15.82
pKa (Strongest Basic)
2.13
PSA
28.68 Å2
Refractivity
24.79 m3·mol-1
Polarizability
8.58 Å3
Rotatable Bond Count
0
H Bond Acceptor Count
1
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
1
Bioavailability
1
Rule of Five
true
Dược Lực Học : Fomepizole is a competitive inhibitor of alcohol dehydrogenase, the enzyme that catalyzes the initial steps in the metabolism of ethylene glycol and methanol to their toxic metabolites. Ethylene glycol is first metabolized to glycoaldehyde which then undergoes further oxidation to glycolate, glyoxylate, and oxalate. It is glycolate and oxalate that are primarily responsible for the metabolic acidosis and renal damage that are seen in ethylene glycol poisoning. {01}{03} Methanol is first metabolized to formaldehyde and then undergoes subsequent oxidation via formaldehyde dehydrogenase to become formic acid. It is formic acid that is primarily responsible for the metabolic acidosis and visual disturbances that are associated with methanol poisoning.
Cơ Chế Tác Dụng : Fomepizole is used as an antidote in confirmed or suspected methanol or ethylene glycol poisoning. Fomepizole is a competitive inhibitor of alcohol dehydrogenase, the enzyme that catalyzes the initial steps in the metabolism of ethylene glycol and methanol to their toxic metabolites. Antizol (fomepizole) is a competitive inhibitor of alcohol dehydrogenase. Alcohol dehydrogenase catalyzes the oxidation of ethanol to acetaldehyde. Alcohol dehydrogenase also catalyzes the initial steps in the metabolism of ethylene glycol and methanol to their toxic metabolites.
Dược Động Học :
▧ Absorption :
Rapid and complete
▧ Volume of Distribution :
* 0.6 to 1.02 L/kg
▧ Metabolism :
Primarily hepaticm the primary metabolite is 4-carboxypyrazole (approximately 80 to 85% of an administered dose). Other metabolites include 4-hydroxymethylpyrazole and the N -glucuronide conjugates of 4-carboxypyrazole and 4-hydroxymethylpyrazole.
▧ Route of Elimination :
In healthy volunteers, only 1-3.5% of the administered dose of Antizol® (7-20 mg/kg oral and IV) was excreted unchanged in the urine, indicating that metabolism is the major route of elimination. In humans, the primary metabolite of Antizol® is 4-carboxypyrazole (approximately 80-85% of administered dose), which is excreted in the urine. The metabolites of Antizol® are excreted renally.
▧ Half Life :
The plasma half-life of Antizol varies with dose, even in patients with normal renal function, and has not been calculated.
Độc Tính : Headache, nausea, dizziness
Chỉ Định : Antizol is indicated as an antidote for ethylene glycol (such as antifreeze) or methanol poisoning, or for use in suspected ethylene glycol or methanol ingestion, either alone or in combination with hemodialysis
Liều Lượng & Cách Dùng : Liquid - Intravenous
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Antizol
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01213
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3406
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508566
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07837
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00707
ChemSpider
http://www.chemspider.com/Chemical-Structure.3289.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/46129-200-02
PharmGKB
http://www.pharmgkb.org/drug/PA449697
Wikipedia
http://en.wikipedia.org/wiki/Fomepizole
RxList
http://www.rxlist.com/cgi/generic/antizol.htm
Drugs.com
http://www.drugs.com/mtm/fomepizole.html
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