Flumazenil

Benzodiazepine Antagonist — VARIOUS

Key facts

Flumazenil is an ofp drug in the Benzodiazepine Antagonist class catalogued in DrugCentral. It was first approved by the FDA in 1991. DrugCentral lists 16 molecular targets, including GABRA1|GABRB1|GABRA2|GABRA3|GABRA4|GABRG2, Gabrg2|Gabra1|Gabrb2 and GABRA5. Recorded indications include Benzodiazepine Induced Sedation, Benzodiazepine Maintained Anesthesia and Benzodiazepine Toxicity.

• Approval status: ofp (first approved 1991 by the FDA).
• Drug class: Benzodiazepine Antagonist.
• Molecular targets: GABRA1|GABRB1|GABRA2|GABRA3|GABRA4|GABRG2, Gabrg2|Gabra1|Gabrb2, GABRA5 and GABRG2|GABRB3|GABRA5 (16 listed in DrugCentral).
• Indications: Benzodiazepine Induced Sedation, Benzodiazepine Maintained Anesthesia and Benzodiazepine Toxicity.
• ATC code: V03AB25 (Antidotes).
• Molecular formula: C15H14FN3O3; molecular weight 303.29 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (3)

• Benzodiazepine Induced Sedation
• Benzodiazepine Maintained Anesthesia
• Benzodiazepine Toxicity

Contraindications (9)

• Anxiety
• Benzodiazepine dependence
• Disease of liver
• Epilepsy
• Heart disease
• Injury of head
• Neuromuscular block, function
• Panic disorder
• Tricyclic Antidepressant Toxicity

Mechanism & targets

• Established pharmacologic class: Benzodiazepine Antagonist

Molecular targets (16)

Target	Gene	Action	Activity
GABA-A receptor; anion channel	GABRA1|GABRB1|GABRA2|GABRA3|GABRA4|GABRG2	unknown	Ki 10.05
GABA-A receptor; alpha-1/beta-2/gamma-2	Gabrg2|Gabra1|Gabrb2	unknown	Ki 9.30
Gamma-aminobutyric acid receptor subunit alpha-5	GABRA5	unknown	Kd 9.30
GABA-A receptor alpha-5/beta-3/gamma-2	GABRG2|GABRB3|GABRA5	other	Ki 9.22
GABA A receptor alpha-3/beta-2/gamma-2	Gabrg2|Gabra3|Gabrb2	unknown	Ki 9.22
GABA-A receptor; anion channel	Gabrp|Gabrb1|Gabrd|Gabrg2|Gabra5|Gabra3|Gabrg1|Gabra2|Gabra4|Gabrg3|Gabra6|Gabra1|Gabrb3|Gabrb2|Gabrq|Gabre	unknown	Ki 9.10
GABA-A receptor alpha-1/beta-3/gamma-2	GABRA1|GABRG2|GABRB3	other	Ki 9.10
GABA-A receptor; anion channel	GABRP|GABRD|GABRA1|GABRB1|GABRG2|GABRB3|GABRA5|GABRA3|GABRA2|GABRB2|GABRA4|GABRE|GABRA6|GABRG1|GABRG3|GABRQ	unknown	Ki 9.05
GABA-A receptor alpha-2/beta-3/gamma-2	GABRG2|GABRB3|GABRA2	other	Ki 9.05
GABA-A receptor alpha-3/beta-3/gamma-2	GABRG2|GABRB3|GABRA3	other	Ki 8.98
Gamma-aminobutyric acid receptor subunit alpha-1	GABRA1	unknown	Kd 8.70
Gamma-aminobutyric acid receptor subunit alpha-4	GABRA4	other	Ki 8.70
Gamma-aminobutyric acid receptor subunit alpha-2	GABRA2	unknown	Ki 8.24
Gamma-aminobutyric acid receptor subunit alpha-3	GABRA3	unknown	Ki 8.09
GABA A receptor alpha-6/beta-2/gamma-2	Gabrg2|Gabra6|Gabrb2	unknown	Ki 7.82
GABA-A receptor alpha-6/beta-3/gamma-2	GABRG2|GABRB3|GABRA6	other	Ki 6.83

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
1991-12-20	FDA	—	—

ATC classification

ATC code	Therapeutic hierarchy
V03AB25	VARIOUS › ALL OTHER THERAPEUTIC PRODUCTS › ALL OTHER THERAPEUTIC PRODUCTS › Antidotes

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Intentional overdose	283.8
Drug withdrawal convulsions	246.2
Seizure	142.5
Coma	135.3
Intentional product misuse	127.3
Drug dependence	127.0
Depressed level of consciousness	121.6
Psychogenic seizure	81.3
Toxicity to various agents	76.0
Suicide attempt	67.9
Product use issue	64.5
Unresponsive to stimuli	57.2

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Flumazenil is on its molecule page.

• Molecular formula: C₁₅H₁₄FN₃O₃
• Molecular weight: 303.29 g/mol
• CAS number: 78755-81-4
• InChIKey: OFBIFZUFASYYRE-UHFFFAOYSA-N
• PubChem CID: 3373

CCOC(=O)C1=C2CN(C)C(=O)C3=CC(F)=CC=C3N2C=N1

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Flumazenil used for?

DrugCentral lists the following indications for Flumazenil: Benzodiazepine Induced Sedation, Benzodiazepine Maintained Anesthesia and Benzodiazepine Toxicity.

How does Flumazenil work?

Its molecular targets in DrugCentral include GABRA1|GABRB1|GABRA2|GABRA3|GABRA4|GABRG2, Gabrg2|Gabra1|Gabrb2, GABRA5 and GABRG2|GABRB3|GABRA5.

When was Flumazenil first approved?

Flumazenil was first approved by the FDA in 1991.

What drug class does Flumazenil belong to?

Flumazenil is in the Benzodiazepine Antagonist class.

What is the chemical formula of Flumazenil?

Flumazenil has the molecular formula C15H14FN3O3 and a molecular weight of 303.29 g/mol.

Sources

• DrugCentral drug card 1195 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL407 — compound record and bioactivity
• PubChem CID 3373 — chemical identifiers
• DrugBank DB01205 — drug record
• FDA UNII 40P7XK9392 — substance identity
• DailyMed: FDA labels for Flumazenil — current prescribing information (label search)
• UniProt P31644 (GABRA5) — target protein
• UniProt P14867 (GABRA1) — target protein
• UniProt P48169 (GABRA4) — target protein
• UniProt P47869 (GABRA2) — target protein
• UniProt P34903 (GABRA3) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.