FOMEPIZOLE injection solution

Land: Vereinigte Staaten

Sprache: Englisch

Quelle: NLM (National Library of Medicine)

Wirkstoff:

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

Verfügbar ab:

X-GEN Pharmaceuticals

INN (Internationale Bezeichnung):

FOMEPIZOLE

Zusammensetzung:

FOMEPIZOLE 1 g in 1 mL

Verschreibungstyp:

PRESCRIPTION DRUG

Berechtigungsstatus:

Abbreviated New Drug Application

Fachinformation

FOMEPIZOLE- FOMEPIZOLE INJECTION, SOLUTION
X-GEN PHARMACEUTICALS
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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 C4H6N2 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 dehydrogenase
enzyme activity in dog, monkey,
and human liver. The concentration of fomepizole at which alcohol
dehydrogenase is inhibited by 50%
in vitro is approximately 0.1 µmol/L.
In a study of