FLUMAZENIL injection

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

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

Available from:

Baxter Healthcare Corporation

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: Flumazenil acts as a benzodiazepine antagonist, blocks the effects of benzodiazepines in animals and man, antagonizes benzodiazepine reinforcement in animal models, produces dysphoria in normal subjects, and has had no reported abuse in foreign marketing. Although flumazenil has a benzodiazepine-like structure it does not act as a benzodiazepine agonist in man and is not a controlled substance.

Product summary:

Flumazenil Injection, USP, for Intravenous use is supplied in: For Intravenous Multiple-Dose Use: AIN00213 NDC 36000-148-10 , 0.1 mg/mL, 5 mL vial; Pack of 10 Vials For Intravenous Multiple-Dose Use: AIN00212 NDC 36000-149-10 , 0.1 mg/mL, 10 mL vial; Pack of 10 Vials Sterile, Nonpyrogenic. The container closure is not made with natural rubber latex. Storage Store at 20° to 25°C (68° to 77°F). [See USP Controlled Room Temperature.] PROTECT FROM LIGHT. DO NOT FREEZE. Manufactured for: Baxter Healthcare Corporation Deerfield, IL 60015 USA Manufactured by: Baxter Pharmaceuticals India Private Ltd Ahmedabad 382213, India 1400006464 2018/08/09

Authorization status:

Abbreviated New Drug Application

Summary of Product characteristics

FLUMAZENIL- FLUMAZENIL INJECTION
BAXTER HEALTHCARE CORPORATION
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FLUMAZENIL INJECTION, USP
RX ONLY
DESCRIPTION
Flumazenil Injection, USP 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:
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 is
available as a sterile parenteral dosage form for intravenous
administration. Each mL contains 0.1 mg of
Flumazenil compounded with 1.8 mg of Methylparaben , 0.2 mg of
Propylparaben , 0.9% mg Sodium
Chloride , 0.01% Edetate Disodium Dihydrate , and 0.1 mg Glacial
Acetic Acid ; the pH is adjusted to
3.4 to 4.6 with Hydrochloric Acid and/or, if necessary, Sodium
Hydroxide and Water for Injection q.s.
to 1 mL.
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 ve