Antizol (Fomepizole): A Critical Antidote In Toxicology
Antizol, the brand name for fomepizole, is an essential antidote used in the treatment of ethylene glycol and methanol poisoning.
These toxic alcohols are commonly found in antifreeze, solvents, and various household products. Without prompt and effective treatment, ingestion can lead to severe metabolic acidosis, renal failure, blindness, and even death.
Antizol Mechanism Of Action
Fomepizole functions as a competitive inhibitor of the enzyme alcohol dehydrogenase (ADH). By inhibiting ADH, fomepizole prevents the metabolism of ethylene glycol and methanol into their toxic metabolites—glycolic acid and oxalic acid from ethylene glycol, and formic acid from methanol.
This inhibition halts the progression of toxicity, allowing the body to eliminate the parent compounds safely.
Clinical Use And Administration
Approved by the U.S. Food and Drug Administration (FDA) in 1997, Antizol is administered intravenously. The standard dosing regimen begins with a loading dose of 15 mg/kg, followed by 10 mg/kg every 12 hours for four doses.
Subsequent doses are increased to 15 mg/kg every 12 hours to account for autoinduction of metabolism. In severe cases, fomepizole is used in conjunction with hemodialysis to expedite the removal of toxins.
Advantages Over Traditional Therapies
Historically, ethanol was used as an antidote for toxic alcohol poisoning due to its ability to inhibit ADH. However, ethanol therapy presents challenges, including central nervous system depression, hypoglycemia, and the need for intensive monitoring. Fomepizole offers several advantages:
- Predictable pharmacokinetics
- Fewer side effects
- No need for blood level monitoring
- Simplified administration
These benefits make fomepizole the preferred treatment in many clinical settings.
Veterinary Use And Market Withdrawal
A veterinary formulation, Antizol-Vet, was previously available for treating ethylene glycol poisoning in animals. However, due to low demand and high production costs, Paladin Labs ceased manufacturing Antizol-Vet by October 1, 2014.
The FDA approved the withdrawal of the drug’s approval in April 2015. Veterinarians have since relied on compounded versions of fomepizole or alternative treatments such as ethanol administration.
Emerging Research
Recent studies have explored the potential use of fomepizole as an adjunctive treatment in acetaminophen (paracetamol) toxicity.
Fomepizole’s inhibition of the CYP2E1 enzyme may reduce the formation of N-acetyl-p-benzoquinone imine (NAPQI), a toxic metabolite responsible for liver damage in acetaminophen overdose.
While N-acetylcysteine remains the primary antidote, fomepizole may offer additional hepatoprotective benefits in severe cases.
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