FOMEPIZOLE injection, solution

Ország: Egyesült Államok

Nyelv: angol

Forrás: NLM (National Library of Medicine)

Aktív összetevők:

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

Beszerezhető a:

EMCURE

INN (nemzetközi neve):

fomepizole

Gyógyszerészeti forma:

INJECTION, SOLUTION

Összetétel:

1 g in 1 mL

Az alkalmazás módja:

INTRAVENOUS

Recept típusa:

PRESCRIPTION DRUG

Terápiás javallatok:

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.

Termék összefoglaló:

Fomepizole Injection is available as a sterile, preservative-free solution for intravenous use, in vials containing 1.5mL (1 g/mL) of fomepizole. Fomepizole Injection is supplied in cartons of one single use vial (NDC 14593-123-01) or four individual cartons placed into one outer carton (NDC 14593-123-02). Store at controlled room temperature, 20° to 25°C (68° to 77°F) [see USP]. Date of Revision: 10/2008 Version 04

Termékjellemzők

FOMEPIZOLE- FOMEPIZOLE INJECTION, SOLUTION
EMCURE
----------
FOMEPIZOLE INJECTION
RX ONLY
STERILE
CAUTION: MUST BE DILUTED PRIOR TO USE.
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 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 1.4 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 to 2 mL/kg.
Fomepizole has been shown _in vitro_ to block alcohol dehydrogenase
enzyme activity in dog, monkey,
4
6
2
and human liver. The concentration of fomepizole at which alcohol
dehydrogenase is inhibited by 50%
_in v