Fomepizole

Fomepizole Uses, Dosage, Side Effects, Food Interaction and all others data.

Fomepizole is used as an antidote in confirmed or suspected methanol or ethylene glycol poisoning. Fomepizole is a competitive inhibitor of alcohol dehydrogenase, the enzyme that catalyzes the initial steps in the metabolism of ethylene glycol and methanol to their toxic metabolites.

Fomepizole is a competitive inhibitor of alcohol dehydrogenase, the enzyme that catalyzes the initial steps in the metabolism of ethylene glycol and methanol to their toxic metabolites. Ethylene glycol is first metabolized to glycoaldehyde which then undergoes further oxidation to glycolate, glyoxylate, and oxalate. Glycolate and oxalate are primarily responsible for metabolic acidosis and renal damage seen in ethylene glycol toxicity. {01}{03} Methanol is first metabolized to formaldehyde and then undergoes subsequent oxidation via formaldehyde dehydrogenase to become formic acid. It is formic acid that is primarily responsible for the metabolic acidosis and visual disturbances that are associated with methanol poisoning.

Trade Name Fomepizole
Availability Prescription only
Generic Fomepizole
Fomepizole Other Names 4-methylpyrazol, 4-methylpyrazole, Fomepizol, Fomepizole, Fomepizolum
Weight 1g/ml
Type Intravenous solution
Formula C4H6N2
Weight Average: 82.1038
Monoisotopic: 82.053098202
Groups Approved, Vet approved
Therapeutic Class
Manufacturer
Available Country United States
Last Updated: September 19, 2023 at 7:00 am
Fomepizole
Fomepizole

Uses

Fomepizole is an inhibitor of alcohol dehydrogenase used as an antidote in confirmed or suspected methanol or ethylene glycol poisoning.

Antizol is indicated as an antidote for ethylene glycol (such as antifreeze) or methanol poisoning, or for use in suspected ethylene glycol or methanol ingestion, either alone or in combination with hemodialysis

Fomepizole is also used to associated treatment for these conditions: Ethylene glycol poisoning, Methanol poisoning

How Fomepizole works

Antizol (fomepizole) is a competitive inhibitor of alcohol dehydrogenase. Alcohol dehydrogenase catalyzes the oxidation of ethanol to acetaldehyde. Alcohol dehydrogenase also catalyzes the initial steps in the metabolism of ethylene glycol and methanol to their toxic metabolites.

Toxicity

Headache, nausea, dizziness

Food Interaction

  • Avoid alcohol. Fomepizole reduces the metabolism of alcohol by alcohol dehydrogenase, and alcohol also reduces fomepizole metabolism and elimination.

Fomepizole Alcohol interaction

[Major] GENERALLY AVOID:

The manufacturer reports that oral doses of fomepizole (10 to 20 mg/kg) will significantly reduce the rate of elimination of moderate doses of ethanol by approximately 40% when given to healthy volunteers.

The mechanism is via alcohol dehydrogenase inhibition.

By a similar mechanism, ethanol will decrease the rate of elimination of fomepizole.



In general, ethanol and fomepizole should not be coadministered in the treatment of ethylene glycol poisoning.

Fomepizole Disease Interaction

Moderate: hepatic/renal dysfunction

Volume of Distribution

  • 0.6 to 1.02 L/kg

Elimination Route

Rapid and complete

Half Life

The plasma half-life of Antizol varies with dose, even in patients with normal renal function, and has not been calculated.

Elimination Route

In healthy volunteers, only 1-3.5% of the administered dose of AntizolĀ® (7-20 mg/kg oral and IV) was excreted unchanged in the urine, indicating that metabolism is the major route of elimination. In humans, the primary metabolite of AntizolĀ® is 4-carboxypyrazole (approximately 80-85% of administered dose), which is excreted in the urine. The metabolites of AntizolĀ® are excreted renally.

Innovators Monograph

You find simplified version here Fomepizole

http://classyfire.wishartlab.com/tax_nodes/C0000000
http://classyfire.wishartlab.com/tax_nodes/C0000002
http://classyfire.wishartlab.com/tax_nodes/C0000436
http://classyfire.wishartlab.com/tax_nodes/C0000087
http://classyfire.wishartlab.com/tax_nodes/C0000087
http://classyfire.wishartlab.com/tax_nodes/C0004144
http://classyfire.wishartlab.com/tax_nodes/C0004139
http://classyfire.wishartlab.com/tax_nodes/C0004557
http://classyfire.wishartlab.com/tax_nodes/C0000278
http://classyfire.wishartlab.com/tax_nodes/C0004150
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:5141
http://metacyc.org/META/new-image?type=COMPOUND&object=CPD0-1652
http://www.hmdb.ca/metabolites/HMDB0015344
http://www.genome.jp/dbget-bin/www_bget?drug:D00707
http://www.genome.jp/dbget-bin/www_bget?cpd:C07837
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=3406
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46508566
https://www.chemspider.com/Chemical-Structure.3289.html
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50226186
https://mor.nlm.nih.gov/RxNav/search?searchBy=RXCUI&searchTerm=15226
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=5141
https://www.ebi.ac.uk/chembldb/index.php/compound/inspect/CHEMBL1308
https://zinc.docking.org/substances/ZINC000000897288
http://bidd.nus.edu.sg/group/cjttd/ZFTTDDRUG.asp?ID=DAP000568
http://www.pharmgkb.org/drug/PA449697
https://www.ebi.ac.uk/pdbe-srv/pdbechem/chemicalCompound/show/4PZ
http://www.rxlist.com/cgi/generic/antizol.htm
https://www.drugs.com/mtm/fomepizole.html
https://en.wikipedia.org/wiki/Fomepizole
*** Taking medicines without doctor's advice can cause long-term problems.
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