FOMEPIZOLE injection, solution

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

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

Available from:

American Regent, Inc.

Administration route:

INTRAVENOUS

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Fomepizole injection 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 injection should not be administered to patients with a documented serious hypersensitivity reaction to fomepizole injection or other pyrazoles.

Product summary:

Fomepizole is supplied as a sterile, preservative-free solution for intravenous use as: Supplied in single vial cartons. Each vial contains 1.5 mL (1 g/mL) of fomepizole. NDC 0517-0710-88 Store at 20° to 25°C (68° to 77°F) [See USP Controlled Room Temperature]. Manufactured by: American Regent, Inc. Shirley, NY  11967 RQ1088-B Revised: November 2020 Novaplus is a registered trademark of Vizient, Inc.

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

FOMEPIZOLE- FOMEPIZOLE INJECTION, SOLUTION
AMERICAN REGENT, INC.
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FOMEPIZOLE INJECTION
STERILE
RX ONLY
_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 in a
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 by-products primarily
responsible for the metabolic acidosis
and renal damage seen in ethylene glycol toxicosis. The lethal dose of
ethylene glycol in humans is
approximately 1.4 mL/kg.
Methanol, the main component of windshield wiper fluid, is slowly
metabolized via alcohol
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 1-2 mL/kg.
Fomepizole has been shown in vitro to block alcohol de