Drug reference

Flumazenil

Antidote · Reversal Agent for Benzodiazepine Effects

AntidoteReversal Agent for Benzodiazepine Effects

CDSCO approvedSchedule H

EXCRETION

—

not curated

INTERACTIONS

10 major

SEVERE in our sources

PREGNANCY

Not known to be harmful; manufacturer

FDA category + note

Top interactionssee all 10 →

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Mechanism

Flumazenil is a benzodiazepine antagonist that reverses the central sedative effects of benzodiazepines.

Indications

Reversal of the central sedative effects of benzodiazepines after anaesthetic and similar proceduresPrevention of the need for ventilation in benzodiazepine poisoning (unlicensed indication)Management of suspected benzodiazepine overdoseReversal of sedative effects produced by benzodiazepines administered during general anesthesia and diagnostic or therapeutic proceduresAntidote in the treatment of benzodiazepine overdoseReversing the postsurgical effects of long-acting benzodiazepines used as anestheticsreverse BZD anaesthesiaBZD overdosedifferential diagnosis of mixed CNS depressant poisoning

Dosing

Adult: a further, smaller dose may be required before surgery. Alternatively, the ﬁrst dose may be given on the day of the procedure. Benzodiazepines Benzodiazepines possess useful properties for premedication including relief of anxiety, sedation, and amnesia; shortacting benzodiazepines taken by mouth are the most common premedicants.…

Pharmacokinetics

Onset

Starts in seconds (i.v.)

Duration

Lasts for 1–2 hours. Resedation generally occurs within 1 hour.

Half-life

about 1 h

Bioavailability

~16% (oral, not used orally)

Metabolism

Eliminated almost entirely by hepatic metabolism to inactive products

Contraindications

Hazardous in mixed overdoses involving tricyclic antidepressants
Hazardous in benzodiazepine-dependent patients
Patients poisoned with tricyclic antidepressants

Side effects

Common

Headache (oral doses)Dizziness (oral doses)agitationdiscomforttearfulnessanxietycoldness

Serious

Convulsions (particularly in mixed overdoses involving tricyclic antidepressants or in benzodiazepine-dependent patients)
May precipitate seizures or other withdrawal signs in patients taking benzodiazepines for protracted periods and in whom tolerance or dependence may have developed
May be associated with the onset of seizures, especially in patients poisoned with tricyclic antidepressants
withdrawal seizures (occasional)
incomplete reversal of respiratory depression