Comparative Pharmacology
Head-to-head clinical analysis: ACETADOTE versus FOMEPIZOLE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ACETADOTE versus FOMEPIZOLE.
ACETADOTE vs FOMEPIZOLE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Acetylcysteine serves as a precursor to glutathione, replenishing hepatic glutathione stores and enhancing the detoxification of the toxic metabolite N-acetyl-p-benzoquinoneimine (NAPQI) in acetaminophen overdose.
Fomepizole is a competitive inhibitor of alcohol dehydrogenase, the enzyme that catalyzes the first step in the metabolism of ethylene glycol and methanol to their toxic metabolites. By inhibiting alcohol dehydrogenase, fomepizole prevents the formation of toxic metabolites such as glycolic acid, glyoxylic acid, and oxalic acid from ethylene glycol, and formic acid from methanol.
Intravenous loading dose of 150 mg/kg over 60 minutes, then 50 mg/kg over 4 hours, then 100 mg/kg over 16 hours (total 300 mg/kg over 21 hours). Oral: 140 mg/kg loading dose, then 70 mg/kg every 4 hours for 17 doses.
Loading dose of 15 mg/kg intravenously over 15 minutes, followed by 10 mg/kg every 12 hours for 4 doses, then 15 mg/kg every 12 hours if ethanol co-ingestion is present; otherwise 10 mg/kg every 12 hours until ethylene glycol or methanol levels <20 mg/dL.
None Documented
None Documented
Clinical Note
moderateFomepizole + Artesunate
"The serum concentration of the active metabolites of Artesunate can be reduced when Artesunate is used in combination with Fomepizole resulting in a loss in efficacy."
Terminal elimination half-life: 5.6 hours (range 4.1-7.6). In acetaminophen overdose, half-life may be prolonged (up to 20 hours) due to saturation of metabolic pathways.
Terminal: 5-7 hours in healthy adults; prolonged to 8-14 hours in patients with ethanol co-ingestion due to competitive inhibition; no significant change in severe renal impairment.
Renal: 60-80% as unchanged drug and metabolites (sulfate, glucuronide, cysteine, N-acetylcysteine conjugates). Fecal: minor (less than 3%).
Renal: 70-90% as unchanged drug and metabolites (4-carboxypyrazole, 4-hydroxymethylpyrazole); biliary/fecal: minor (<5% total).
Category C
Category C
Antidote
Antidote