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GABA-A Antagonist·Toxicology & Antidotes
Reversal of conscious sedation (iatrogenic), pure benzodiazepine overdose in non-habituated patients
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Max Dose
2 mg (STAT)
Caution: Half-life
40–80 mins
High risk: Seizure Risk
CRITICAL
Caution: Resedation
HIGH RISK
Avoid / Cautions
Known seizure disorder, chronic benzodiazepine use, mixed overdose with proconvulsant drugs (TCAs, Bupropion, Venlafaxine). Pregnancy Category B3.
Overview
Competitive benzodiazepine receptor antagonist. Rapidly reverses benzodiazepine-induced sedation and respiratory depression.
Clinical Focus
Do NOT use in mixed overdoses or chronic benzo users. Stripping benzos off the receptor in a dependent patient will trigger uncontrollable, fatal status epilepticus.
Bottom Line
Flumazenil is the specific benzodiazepine antagonist for reversal of BZD sedation and overdose, but can precipitate seizures in chronic benzodiazepine users and has a shorter half-life than most BZDs.
Brand Names
Anexate
Parenteral
Ampoules (500 mcg/5 mL) for IV use only.
Prescribing & PBS
Hospital supply. Restricted.
Primary
Reversal of conscious sedation (iatrogenic), pure benzodiazepine overdose in non-habituated patients.
Clinical Place
Highly restricted in ED toxicology. Mostly used by anesthetists to wake patients up post-endoscopy.
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