FLUMAZENIL- flumazenil injection

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

FLUMAZENIL (UNII: 40P7XK9392) (FLUMAZENIL - UNII:40P7XK9392)

Available from:

Sandoz Inc

INN (International Name):

FLUMAZENIL

Composition:

FLUMAZENIL 0.1 mg in 1 mL

Administration route:

INTRAVENOUS

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Flumazenil injection is indicated for the complete or partial reversal of the sedative effects of benzodiazepines in cases where general anesthesia has been induced and/or maintained with benzodiazepines, where sedation has been produced with benzodiazepines for diagnostic and therapeutic procedures, and for the management of benzodiazepine overdose. Flumazenil injection is indicated for the reversal of conscious sedation induced with benzodiazepines (see PRECAUTIONS: Pediatric Use ). Flumazenil injection is contraindicated: - in patients with a known hypersensitivity to flumazenil or benzodiazepines. - in patients who have been given a benzodiazepine for control of a potentially life-threatening condition (eg, control of intracranial pressure or status epilepticus). - in patients who are showing signs of serious cyclic antidepressant overdose (see WARNINGS ). Flumazenil acts as a benzodiazepine antagonist, blocks the effects of benzodiazepines in animals and man, antagonizes benzodiazepine reinforcement in a

Product summary:

Flumazenil injection contains 0.1 mg of flumazenil per mL and is supplied as follows: NDC 0781-3003-92 multiple-dose vials of 5 mL in boxes of 10. NDC 0781-3003-95 multiple-dose vials of 10 mL in boxes of 10. Store at 20°-25°C (68°-77°F) (see USP Controlled Room Temperature). 07-2009M D1006819 Manufactured in Canada by Sandoz Canada Inc. for Sandoz Inc. Princeton, NJ 08540

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

FLUMAZENIL- FLUMAZENIL INJECTION
SANDOZ INC
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FLUMAZENIL INJECTION
DESCRIPTION
Flumazenil injection is a benzodiazepine receptor antagonist.
Chemically, flumazenil is ethyl 8-fluoro-
5,6-dihydro-5-methyl-6-oxo-4H-imidazo[1,5-a](1,4)
benzodiazepine-3-carboxylate. Flumazenil has an
imidazobenzodiazepine structure, a calculated molecular weight of
303.3 and the following structural
formula:
C H FN O
Flumazenil is a white to off-white crystalline compound with an
octanol:buffer partition coefficient of
14 to 1 at pH 7.4. It is insoluble in water but slightly soluble in
acidic aqueous solutions. Flumazenil
injection is available as a sterile parenteral dosage form for
intravenous administration. Each mL
contains flumazenil 0.1 mg. In addition, the following inactive
ingredients are included: methylparaben
1.8 mg, propylparaben 0.2 mg, sodium chloride 0.9 %, edetate disodium
0.01%, acetic acid 0.01%,
hydrochloric acid and/or sodium hydroxide to adjust pH to 3.5 to 4.5,
and water for injection.
CLINICAL PHARMACOLOGY
Flumazenil, an imidazobenzodiazepine derivative, antagonizes the
actions of benzodiazepines on the
central nervous system. Flumazenil competitively inhibits the activity
at the benzodiazepine recognition
site on the GABA/benzodiazepine receptor complex. Flumazenil is a weak
partial agonist in some animal
models of activity, but has little or no agonist activity in man.
Flumazenil does not antagonize the central nervous system effects of
drugs affecting GABA-ergic
neurons by means other than the benzodiazepine receptor (including
ethanol, barbiturates, or general
anesthetics) and does not reverse the effects of opioids.
In animals pretreated with high doses of benzodiazepines over several
weeks, flumazenil elicited
symptoms of benzodiazepine withdrawal, including seizures. A similar
effect was seen in adult human
subjects.
PHARMACODYNAMICS
Intravenous flumazenil has been shown to antagonize sedation,
impairment of recall, psychomotor
impairment and ventilatory depression produced by benzodiazepines i