Fomepizole

From Anvita Health Wiki

Contents 1 Indications 2 Contraindications 3 Dosage 4 Pharmacokinetics 5 Monitor 6 Adverse-effects 7 Mechanism-of-action 8 More General Terms 9 Internet Database 10 References

Indications

• suspected or confirmed ethylene glycol or methanol poisoning

Contraindications

• Pregnancy Category C:

Dosage

• loading dose of 15 mg/kg should be administered, followed by doses of 10 mg/kg every 12 hours for 4 doses, then 15 mg/kg every 12 hours thereafter until ethylene glycol or methanol concentrations are undetectable or have been reduced below 20 mg/dL, and the patient is asymptomatic with normal pH
• all doses should be administered as a slow IV infusion over 30 minutes

• Supplied in packages of four vials
• Each vial contains 1.5 mL (1 g/ mL) of fomepizole

Pharmacokinetics

• volume of distribution 0.6-1.02 L/kg
• therapeutic concentration is from 8.2-24.6 mg/L (100-300 uM)

• 1/2life varies with dose

• hepatic via cyt P450 system
• primary metabolite is 4-carboxypyrazole (~80-85%)
• fomepizole rapidly induces its own metabolism
• 1-3.5% excreted unchanged in the urine
• metabolites excreted in the urine
• fomepizole is removed by hemodialysis

Monitor

• appropriate workup & therapy for metabolic acidosis

Adverse-effects

• minor allergic reactions (mild rash, eosinophilia)
• nausea, dizziness, vertigo with overdose

Mechanism-of-action

• alcohol dehydrogenase inhibitor

More General Terms

• antidote

Internet Database

PubChem: 3406
PubChem: 11957593

References

1. RxList [1]

fomepizole (Antizole, 4-methylpyrazole)