Country: United States
Language: English
Source: NLM (National Library of Medicine)
FLUMAZENIL (UNII: 40P7XK9392) (FLUMAZENIL - UNII:40P7XK9392)
Cardinal Health
FLUMAZENIL
FLUMAZENIL 0.1 mg in 1 mL
INTRAVENOUS
PRESCRIPTION DRUG
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, USP is indicated for the reversal of conscious sedation induced with benzodiazepines (see PRECAUTIONS: Pediatric Use ). Flumazenil is contraindicated: Flumazenil acts as a benzodiazepine antagonist, blocks the effect 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.
5 mL multiple dose vial containing 0.1 mg/mL flumazenil overbagged with 1 vial per bag, (NDC 55154-7474-8)
Abbreviated New Drug Application
FLUMAZENIL- FLUMAZENIL INJECTION, SOLUTION CARDINAL HEALTH ---------- 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 injection 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% sodium chloride, 0.01% edetate disodium, and 0.01% acetic acid; the pH is adjusted to approximately 4 with hydrochloric acid and/or, if necessary, sodium hydroxide. 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 in Read the complete document