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Fomepizole

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Chemical Structure| 7554-65-6 同义名 : 4-甲基吡唑 ;4-Methylpyrazole;Antizol;Fomepizolum;Antizol-Vet
CAS号 : 7554-65-6
货号 : A195940
分子式 : C4H6N2
纯度 : 98%
分子量 : 82.104
MDL号 : MFCD00005245
存储条件：

粉末 Keep in dark place,Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(1278.87 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 100 mg/mL(1217.97 mM)，配合低频超声助溶
动物实验配方：
生物活性
靶点

  • Dehydrogenase
描述 Fomepizole, 4-methylpyrazole (4-MP), is a competitive antagonist of alcohol dehydrogenase with a binding affinity >8000 times that of ethanol. Fomepizole's wide therapeutic dose range and safety profile confer several advantages over standard ethanol therapy for the treatment of toxic alcohol exposures, including the lack of ethanol-associated side effects[3]. Fomepizole is a safe and effective antidote in the treatment of ethylene glycol poisoning[4]. Male and pregnant Sprague-Dawley rats, which were obtained at 19 days gestation, were administered fomepizole 15 mg/kg intraperitoneally. Elevated concentrations of fomepizole were detected in the fetus following maternal administration. Fetal fomepizole concentrations were fivefold higher than maternal serum concentrations. The zero order elimination rate of fomepizole from maternal serum was 7.6 mol/L/h, which was slightly slower than the elimination rate in male rats (12.9 mol/L/h) [5]. 1 dose of fomepizole for severe DERs with hypotension unresponsive to fluid resuscitation or for angioedema unresponsive to antihistamines be administered[6]. Fomepizole may precipitate bradycardia and/or hypotension during hemodialysis. Monitor vital signs closely during and immediately after infusion[7].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

12.18mL

2.44mL

1.22mL

60.90mL

12.18mL

6.09mL

121.80mL

24.36mL

12.18mL
参考文献

[1]Lepik KJ, Levy AR, et al. Adverse drug events associated with the antidotes for methanol and ethylene glycol poisoning: a comparison of ethanol and fomepizole. Ann Emerg Med. 2009 Apr;53(4):439-450.e10.

[2]Casavant MJ. Fomepizole in the treatment of poisoning. Pediatrics. 2001 Jan;107(1):170.

[3]Bestic M, Blackford M, Reed M. Fomepizole: a critical assessment of current dosing recommendations. J Clin Pharmacol. 2009 Feb;49(2):130-7

[4]Battistella M. Fomepizole as an antidote for ethylene glycol poisoning. Ann Pharmacother. 2002 Jun;36(6):1085-9

[5]Gracia R, Latimer B, McMartin KE. Kinetics of fomepizole in pregnant rats. Clin Toxicol (Phila). 2012 Sep;50(8):743-8

[6]Sande M, Thompson D, Monte AA. Fomepizole for severe disulfiram-ethanol reactions. Am J Emerg Med. 2012 Jan;30(1):262.e3-5

[7]Lepik KJ, Brubacher JR, DeWitt CR, Lam GS, Lawson EJ, Erhardt GD, Purssell RA, Kennedy JR, Brignall JL. Bradycardia and hypotension associated with fomepizole infusion during hemodialysis. Clin Toxicol (Phila). 2008 Jul;46(6):570-3