Kinetics and metabolism of fomepizole in healthy humans

References

• Jacobsen D, McMartin KE. Methanol and ethylene glycol poisonings: Mechanism of toxicity, clinical course, diagnosis and treatment. Med Toxicol 1986; 1:309–334.
   PubMedGoogle Scholar
• Brent J, McMartin KE, Phillips S, Burkhart KK, Donovan JW, Wells M, Kulig K. Fomepizole for the treatment of ethylene glycol poisoning. N Engl J Med 1999; 340:832–838.
   PubMed Web of Science ®Google Scholar
• Brent J, McMartin KE, Phillips S, Aaron C, Kulig K. Fomepizole for the treatment of methanol poisoning. New Engl J Med 2001; 444: 424–429.
   Web of Science ®Google Scholar
• Besenhofer LM, Adegboyega PA, Bartels M, Filary MJ, Perala AW, McLaren MC, McMartin KE. Inhibition of metabolism of diethylene glycol prevents target organ toxicity in rats. Toxicol Sci 2010; 117: 25–35.
   PubMed Web of Science ®Google Scholar
• Lindros KO, Stowell A, Pikkarainen P, Salaspuro M. The disulfiram (antabuse)-alcohol reaction in male alcoholics: its efficient management by 4-methylpyrazole. Alcoholism Clin Exp Res 1981; 5: 528–530.
   PubMed Web of Science ®Google Scholar
• Brent J. Fomepizole for ethylene glycol and methanol poisoning. New Engl J Med 2009; 360:2216–2223.
   PubMed Web of Science ®Google Scholar
• McMartin KE. Antidotes for alcohol and glycol toxicity – translating mechanisms to treatments. Clin Pharmacol Therap 2010; 88: 400–404.
   PubMed Web of Science ®Google Scholar
• Hovda KE, Julsrud J, Ovrebo S, Brors O, Jacobsen D. Studies on ethylene glycol poisoning: one patient – 154 admissions. Clin Toxicol 2011; 49:478–484.
   PubMed Web of Science ®Google Scholar
• Jacobsen D, Barron SK, Sebastian CS, Blomstrand R, McMartin KE. Non-linear kinetics of 4-methylpyrazole in healthy human subjects. Eur J Clin Pharmacol 1989; 37:599–604.
   PubMed Web of Science ®Google Scholar
• Jacobsen D, Østensen J, Bredesen L, Ullstein E, McMartin KE. 4-Methylpyrazole (4-MP) is effectively removed by haemodialysis in the pig model. Human Exp Toxicol 1996; 15:494–496.
   PubMed Web of Science ®Google Scholar
• Jobard E, Harry P, Turcant A, Roy PM, Allain P. 4-Methylpyrazole and hemodialysis in ethylene glycol poisoning. Clin Toxicol 1996; 34:373–377.
   Web of Science ®Google Scholar
• McMartin KE, Hedstrom KG, Tolf BR, Ostling-Wintzell H, Blomstrand R. Studies on the metabolic interactions between 4-methylpyrazole and methanol using the monkey as an animal model. Arch Biochem Biophys 1980; 199:606–614.
   PubMed Web of Science ®Google Scholar
• Mayersohn MI, Owens SM, Anaya AL, Bliss M, Achari R. 4-methylpyrazole disposition in the dog: Evidence for saturable elimination. J Pharmac Sci 1985; 74:895–896.
   PubMed Web of Science ®Google Scholar
• McMartin KE, Collins TD. Distribution of 4-methylpyrazole in the rat: inhibition of elimination by ethanol. J Toxicol Clin Toxicol 1988; 26:451–466.
   PubMed Web of Science ®Google Scholar
• Murphy RC, Watkins WD. Pharmacology of pyrazoles I. Structure elucidation of metabolites of 4-methylpyrazole. Biochem Biophys Res Commun 1972; 49:283–291.
   PubMed Web of Science ®Google Scholar
• Blomstrand R, Ohman G. Studies on the metabolites of the ADH inhibitor 4-methylpyrazole in the rat. Life Sci 1973; 13:107–112.
   PubMed Web of Science ®Google Scholar
• Bestic M, Blackford M, Reed M. Fomepizole: a critical assessment of current dosing recommendations. J Clin Pharmacol 2009; 49: 130–137.
   PubMed Web of Science ®Google Scholar
• Marraffa JM, Forrest A, Grant W, Stork C, McMartin KE, Howland MA. Oral administration of fomepizole produces similar blood levels as identical intravenous dose. Clin Toxicol 2007; 46:181–186.
   Web of Science ®Google Scholar
• Wallemacq PE, Vanbinst R, Haufroid V, Di Fazio V, Konig J, Detaille T, Hantson P. Plasma and tissue determination of 4-methylpyrazole for pharmacokinetic analysis in acute adult and pediatric methanol/ethylene glycol poisoning. Ther Drug Monit 2004; 26:258–262.
   PubMed Web of Science ®Google Scholar
• McMartin KE, Collins TD, Hewlett TP. High pressure liquid chromatographic assay of 4-methylpyrazole. Measurements of plasma and urine levels. J Toxicol Clin Toxicol 1984; 22:133–148.
   PubMed Web of Science ®Google Scholar
• Vu BD, Crouzier C, Hubert I, Galliot M, Baud FJ, Bourdon R. Etude analytique et pharmacocinetique du 4-methylpyrazole, nouvel antidote pour le traitement de l'intoxication a l'ethylene glycol. Ann Fais Exp Chim 1992; 85:99–110.
   Google Scholar
• Jacobsen D, Sebastian CS, Barron SK, Carriere EW, McMartin KE. Effects of 4methylpyrazole, methanol/ethylene glycol antidote, in healthy humans. J Emerg Med 1990; 8:455–461.
   PubMedGoogle Scholar
• Feiermann DE, Cederbaum AI. Increased content of cytochrome P-450 and 4-methylpyrazole binding spectra after 4-methylpyrazole treatment. Biochem Biophys Res Commun 1985; 126:1076–1081.
   PubMed Web of Science ®Google Scholar
• Mailman RB, Hodgson E. The cytochrome P-450 substrate optical difference spectra of pesticides with mouse hepatic microsomes. Bull Environm Contam Toxicol 1972; 8:186–192.
   PubMed Web of Science ®Google Scholar
• Feiermann DE, Cederbaum AI. Interaction of pyrazole and 4-methylpyrazole with hepatic microsomes: effect on cytochrome P-450 content, microsomal oxidation of alcohols and binding spectra. Alcoholism Clin Exp Res 1985; 9:421–428.
   PubMed Web of Science ®Google Scholar
• Krikun G, Feierman DE, Cederbaum AI. Rat liver microsomal induction of the oxidation of drugs and alcohols, and sodium dodecyl sufate-gel profiles after in vivo treatment with pyrazole or 4-methylpyrazole. J Pharmacol Exp Therap 1986; 237:1012–1019.
   PubMed Web of Science ®Google Scholar
• Winters DK, Cederbaum AI. Time course characterization of the induction of cytochrome P-450 2E1 by pyrazole and 4-methylpyrazole. Biochem Biophys Acta 1992; 1117:15–24.
   PubMed Web of Science ®Google Scholar
• Baud FJ, Bismuth C, Garnier R, Galliot M, Astier A, Maistre G, Soffer M. 4-Methylpyrazole may be an alternative to ethanol therapy for ethylene glycol intoxication in man. J Toxicol Clin Toxicol 1986–1987; 24:463–483.
   PubMed Web of Science ®Google Scholar
• Hantson P, Wallemacq P, Brau M, Vanbinst R, Haufroid V, Mahieu P. Two cases of acute methanol poisoning partially treated by oral 4-methylpyrazole. Intensive Care Med 1999; 25:528–531.
   PubMed Web of Science ®Google Scholar
• Megarbane B, Houze P, Baud FJ. Oral fomepizole administration to treat ethylene glycol and methanol poisonings: advantages and limitations. Clin Toxicol 2008; 46:1097.
   Web of Science ®Google Scholar
• Marraffa JM, Grant WD, Howland MA. Authors’ reply. Clin Toxicol 2008; 46:1097–1098.
   Web of Science ®Google Scholar
• Jacobsen D, Sebastian S, Blomstrand R, McMartin KE. 4-methylpyrazole: a controlled study of safety in healthy human subjects after single, ascending doses. Alcohol Clin Exp Res 1988; 12: 516–522.
   PubMed Web of Science ®Google Scholar