FOMEPIZOLE injection, solution

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

FOMEPIZOLE (UNII: 83LCM6L2BY) (FOMEPIZOLE - UNII:83LCM6L2BY)

Available from:

Zydus Pharmaceuticals USA Inc.

Administration route:

INTRAVENOUS

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Fomepizole 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 (see DOSAGE AND ADMINISTRATION ). Fomepizole should not be administered to patients with a documented serious hypersensitivity reaction to fomepizole or other pyrazoles.

Product summary:

Fomepizole Injection is available as a sterile, preservative-free solution for intravenous use, in vials containing1.5mL (1 g/mL) of fomepizole. Fomepizole injection is supplied in cartons of one single use vial (NDC 70710-1478-1) Store at controlled room temperature, 20° to 25°C (68° to 77°F). Distributed by: Zydus Pharmaceuticals USA Inc. Pennington, NJ 08534 Revised: 02/2023 30270718 R2

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

FOMEPIZOLE - FOMEPIZOLE INJECTION, SOLUTION
ZYDUS PHARMACEUTICALS USA INC.
----------
RX ONLY
STERILE
CAUTION : MUST BE DILUTED PRIOR TO USE. DO NOT USE POLYCARBONATE
SYRINGES OR
POLYCARBONATE-CONTAINING NEEDLES (INCLUDING POLYCARBONATE FILTER
NEEDLES)
WITH FOMEPIZOLE INJECTION.
DESCRIPTION
Fomepizole Injection is a competitive inhibitor of alcohol
dehydrogenase. The chemical
name of fomepizole is 4-methylpyrazole. It has the molecular formula C
H N and a
molecular weight of 82.1. The structural formula is:
It is a clear to yellow liquid at room temperature. Its melting point
is 25°C(77°F) and it
may present as solid form at room temperature. Fomepizole is soluble
in water and very
soluble in ethanol, diethyl ether, and chloroform. Each vial contains
1.5 mL (1 g/mL) of
fomepizole.
CLINICAL PHARMACOLOGY
MECHANISM OF ACTION:
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.
Ethylene glycol, the main component of most antifreezes and coolants,
is metabolized to
glycoaldehyde, which undergoes subsequent sequential oxidations to
yield glycolate,
glyoxylate, and oxalate. Glycolate and oxalate are the metabolic
byproducts primarily
responsible for the metabolic acidosis and renal damage seen in
ethylene glycol
toxicosis. The lethal dose of ethylene glycol in humans is
approximately 1.4mL/kg.
Methanol, the main component of windshield wiper fluid, is slowly
metabolized via alcohol
4
6
2
dehydrogenase to formaldehyde with subsequent oxidation via
formaldehyde
dehydrogenase to yield formic acid. Formic acid is primarily
responsible for the metabolic
acidosis and visual disturbances (e.g., decreased visual acuity and
potential blindness)
associated with methanol poisoning. A lethal dose of methanol in
humans is
approximately 1 to 2mL/kg.
Fomepizole has been shown in vitro to block alcohol dehydrogenase
en