antizol- fomepizole injection, solution

Land: Vereinigte Staaten

Sprache: Englisch

Quelle: NLM (National Library of Medicine)

Wirkstoff:

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

INN (Internationale Bezeichnung):

fomepizole

Darreichungsform:

INJECTION, SOLUTION

Zusammensetzung:

1 g in 1 mL

Verabreichungsweg:

INTRAVENOUS

Verschreibungstyp:

PRESCRIPTION DRUG

Anwendungsgebiete:

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

Produktbesonderheiten:

Antizol is supplied as a sterile, preservative-free solution for intravenous use as: Supplied in packages of four vials. Each vial contains 1.5 mL (1 g/mL) of fomepizole. NDC 68727-200-02 Store at controlled room temperature, 20° to 25° C (68° to 77° F) Distributed by: Jazz Pharmaceuticals, Inc. Palo Alto, CA 94304 For questions of a medical nature, call 1-888-867-7426. Part No. ANT PI-8511 Revision Date: April 2006

Fachinformation

ANTIZOL- FOMEPIZOLE INJECTION, SOLUTION
----------
ANTIZOL (FOMEPIZOLE) INJECTION
STERILE
RX ONLY
_CAUTION: MUST BE DILUTED PRIOR TO USE._
DESCRIPTION
Antizol
(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
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.
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.
®
®
4
6
2
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