flumazenil- Flumazenil injection

Country: United States

Language: English

Source: NLM (National Library of Medicine)

Active ingredient:

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

Available from:

Akorn-Strides, LLC

INN (International Name):

Flumazenil

Pharmaceutical form:

INJECTION

Administration route:

INTRAVENOUS

Prescription type:

PRESCRIPTION DRUG

Therapeutic indications:

Flumazenil injection, USP 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, USP 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 (e.g., 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 reinfo

Summary of Product characteristics

FLUMAZENIL- FLUMAZENIL INJECTION
AKORN-STRIDES, LLC
----------
FLUMAZENIL INJECTION, USP
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
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: ACTIVE:
Flumazenil 0.1 mg. PRESERVATIVES: Methylparaben 1.8 mg, Propylparaben
0.2 mg, INACTIVES: Acetic
Acid 0.01%, Edetate Disodium 0.01%, the pH is adjusted to
approximately 4.0 with Hydrochloric Acid
and/or, if necessary, Sodium Hydroxide, Sodium Chloride 0.9%, 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
impa