Do I need a prescription for Flumazenil 500micrograms/5ml solution for injection ampoules?

Flumazenil 500micrograms/5ml solution for injection ampoules is classified as a Valid as a prescribable product in the UK. However, always consult a pharmacist or doctor before use. (Source: NHS dm+d)

What are the brand names for Flumazenil 500micrograms/5ml solution for injection ampoules?

Flumazenil 500micrograms/5ml solution for injection ampoules is the generic name. It is available under brand names including: Anexate 500micrograms/5ml solution for injection ampoules, Flumazenil 500micrograms/5ml solution for injection ampoules, Flumazenil 500micrograms/5ml solution for injection ampoules, Flumazenil 500micrograms/5ml solution for injection ampoules, Flumazenil 500micrograms/5ml solution for injection ampoules and 2 more. (Source: NHS dm+d — Actual Medicinal Products)

Flumazenil 500micrograms/5ml solution for injection ampoules

Prescription only

Requires a prescription from a doctor or prescriber

Injection

5ml

Parenteral

Oral liquids

Active ingredients:

Flumazenil

ATC classificationBrowse ATC index

International classification by the WHO, grouping medicines by the organ system they act on

ATC V03AB25

Chemical classBrowse classes

Classification based on the molecule's chemical structure and properties

Check interactions for Flumazenil

No active safety alerts

Official documents, adverse reaction reporting, and safety monitoring

Report a side effect

Submit a Yellow Card report to the MHRA

Official medicine documents

Yellow Card

Report side effects (MHRA)

Drug safety updates

MHRA alerts for Flumazenil

Source: MHRA Products DatabaseOGL 3.0

Updated 16 Jan 2026

Safety monitoring data

Yellow Card reports

MHRA

The MHRA Yellow Card scheme collects reports of suspected side effects from healthcare professionals and patients. View the Drug Analysis Profile (iDAP) for real-world adverse reaction data.

View Drug Analysis Profile

Suspected adverse reactions reported for Flumazenil

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Report a side effect

Submit a Yellow Card report to the MHRA

Data from the MHRA Yellow Card scheme. A reported reaction does not necessarily mean the medicine caused it. Contains public sector information licensed under the Open Government Licence v3.0.

EudraVigilance

EMA

The European Medicines Agency (EMA) collects suspected adverse reaction reports from across the EU/EEA through the EudraVigilance system. Search for safety data on this medicine.

View EudraVigilance report

Suspected adverse reactions reported for Flumazenil

About EudraVigilance

Learn about EU pharmacovigilance and safety monitoring

EudraVigilance data is published by the European Medicines Agency (EMA). A suspected adverse reaction is not necessarily caused by the medicine.

7 branded products available

7 products

Possibly available on the UK marketDiscontinuedAvailability per NHS dm+d

MHRA licensed products

View all licensed products for Flumazenil on the MHRA register

Flumazenil 500micrograms/5ml solution for injection ampoules

hameln pharma Ltd

Flumazenil 500micrograms/5ml solution for injection ampoules

A A H Pharmaceuticals Ltd

Flumazenil 500micrograms/5ml solution for injection ampoules

Hikma Pharmaceuticals International Ltd

Anexate 500micrograms/5ml solution for injection ampoules

Roche Products Ltd

Discontinued

Flumazenil 500micrograms/5ml solution for injection ampoules

Teva UK Ltd

Discontinued

Flumazenil 500micrograms/5ml solution for injection ampoules

Actavis UK Ltd

Discontinued

Flumazenil 500micrograms/5ml solution for injection ampoules

Kent Pharma (UK) Ltd

Discontinued

Source: NHS dm+dOGL 3.0

Updated 1 Mar 2026

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Similarity is based on WHO Anatomical Therapeutic Chemical (ATC) classification and on a factual NHS dm+d therapeutic-grouping code prefix. Source data: NHS dm+d via TRUD (OGL v3.0), WHO ATC/DDD Index.

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Codes for healthcare professionals and prescribing systems

These codes are used by healthcare IT systems and prescribers to identify this medicine.

NHS UK identifiers

SNOMED CT

36067711000001104

dm+d ID

36067711000001104

VTM (Virtual Therapeutic Moiety)

775985005

VMP (Virtual Medicinal Product)

36067711000001104

International identifiers

ATC code — Anatomical Therapeutic Chemical (WHO)

V03AB25

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SNOMED CT and dm+d codes from NHS TRUD (Technology Reference data Update Distribution), licensed under the Open Government Licence v3.0. ATC codes from the WHO Collaborating Centre for Drug Statistics Methodology (whocc.no).

Active and completed clinical studies from ClinicalTrials.gov

Searching UK clinical trials...

Source: ClinicalTrials.gov, a database of the U.S. National Library of Medicine (NLM), National Institutes of Health (NIH). Data accessed via ClinicalTrials.gov API v2. Trial information is provided for research purposes and does not constitute medical advice.

Academic studies and reviews for this medicine's active substance

Showing the 50 most relevant studies.

Reviews & meta-analyses: 22 · Randomised trials: 14 · 1988–2026

Sort

Flumazenil vs. placebo in hepatic encephalopathy in patients with cirrhosis: a meta‐analysis

C. Goulenok, B. Bernard, J. Cadranel, et al.

Alimentary Pharmacology & Therapeutics, 2002

Meta-analysis

Cited by 106

Clinical enigma: Case-based systematic review of flumazenil in the management of paradoxical reactions to midazolam - A quarter-century perspective.

Utami NP, Rachmadhianto R, Wiyono MR, et al.

2025

Systematic review

Open access

Cited by 1

Background and aimsThe mechanism of paradoxical reaction is still a big question for the medical world, but several theoretical approaches have arisen. Midazolam, a high-potency benzodiazepine, carries a higher risk of paradoxical reaction. Paradoxical reactions associated with midazolam are often misunderstood and mismanaged, with clinicians frequently attributing them to factors like inadequate dosing or low sedation levels. This leads to the common practice of escalating midazolam dosage or exploring alternative sedatives, despite flumazenil offering a safer solution theoretically. Flumazenil emerges as a viable antidote as it swiftly and effectively reverses paradoxical reactions, proving to be a safer alternative to dose escalation strategies.Material and methodsIn this systematic review, we conducted a search regarding the use of flumazenil in midazolam-induced paradoxical reactions over a quarter-century period (1998-2023) in three databases. We include 10 case reports presenting a total of 14 cases, which adhered to the specified inclusion criteria.ResultWe selected 10 case reports published from 1998 to 2023 with a total of 14 cases. Study characteristics, patient demographics, midazolam dose and administration route, incident of paradoxical effect, flumazenil dose and administration route, and outcome of flumazenil administration.ConclusionsAll the cases showed the prosperous effectiveness of flumazenil in reducing paradoxical reaction symptoms with no adverse effect on hemodynamics. Ongoing research and study in this field are essential to refine protocols and enhance patient outcomes.

Abstract licence: CC BY-NC-SA

Flumazenil reversal of remimazolam-induced sedation: a narrative review of safety, pharmacokinetics, and clinical considerations.

Zhou Y, Wu W, Zhang Y, et al.

2026

Systematic review

Could Flumazenil Be Used Pre-hospital by Intramuscular Injection for Coma due to Mixed Drug Overdose Not Responding to Naloxone?: A Systematic Review of the Evidence.

Farcas I, Schölin L, Eddleston M

2025

Systematic review

Coma
Flumazenil
Antidotes

Flumazenil in cirrhotic patients in hepatic coma: A randomized double‐blind placebo‐controlled crossover trial

G. Pomier-Layrargues, J. Giguère, J. Lavoie, et al.

Hepatology, 1994

Randomised trial

Cited by 128

Adverse Events Associated with Flumazenil Treatment for the Management of Suspected Benzodiazepine Intoxication--A Systematic Review with Meta-Analyses of Randomised Trials.

E. Penninga, N. Graudal, M. Ladekarl, et al.

Basic & clinical pharmacology & toxicology, 2016

Review

Cited by 134

Remimazolam-based anesthesia with flumazenil allows faster emergence than propofol-based anesthesia in older patients undergoing spinal surgery: A randomized controlled trial

Yukari Toyota, T. Kondo, Kyoko Oshita, et al.

Medicine, 2023

Randomised trial

Cited by 13

Comparison of remimazolam-flumazenil versus propofol on delayed emergence from anaesthesia in major spine surgery: protocol for a multicentre, single-blinded, randomised controlled trial.

Sun J, Luo W, Wen L, et al.

2025

Randomised trial

Cited by 1

Spine
Propofol
Benzodiazepines

Effects of Remimazolam-Propofol with Flumazenil Reversal on the Emergence Time and Hemodynamics of Patients Undergoing Laparoscopic Partial Hepatectomy: A Prospective Randomized Controlled Trial.

Feng Y, Jia JM, Cheng YX, et al.

2025

Randomised trial

Open access

Cited by 1

Propofol
Benzodiazepines
Flumazenil

BackgroundLaparoscopic partial hepatectomy, characterized by significant surgical trauma, profound stress responses, prolonged duration, and high anesthetic requirements, may lead to delayed recovery or emergence agitation. Whether remimazolam and propofol combined with flumazenil reversal can accelerate the recovery and enhance hemodynamic stability remains controversial.MethodsFifty patients aged 18-70 years with American Society of Anesthesiologists (ASA) class I-III and Child-Pugh classification A or B undergoing elective laparoscopic partial hepatectomy were enrolled. Participants were randomly assigned to either the remimazolam combined with propofol group (RP group) or the propofol group (P group). Both groups received intravenous sufentanil and cisatracurium for induction, followed by either remimazolam-propofol with flumazenil reversal or propofol alone. Emergence parameters, including time to obey verbal commands, BIS over 80, and tracheal tube removal were recorded. The Sedation-Agitation Scale (SAS) and Visual Analog Scale (VAS) scores at predefined intervals, hemodynamics, and adverse events were recorded.ResultsThe time to obey verbal commands (p), BIS over 80 (p =0.0011), and tracheal tube removal (p=0.0002) were all significantly shorter in the RP group than in the P group. The SAS score after 30 min (p=0.0488) in the PACU was significantly higher, but the VAS score after 15 min (p=0.0086) and 30 min (p=0.0084) in the PACU, were significantly lower in the RP group than in the P group. MAP at T1 (p=0.0470) was significantly lower in the P group than in the RP group. In addition, the RP group demonstrated reduced post-induction hypotension, required no postoperative rescue analgesia, and reported no emergence agitation.ConclusionCompared to propofol alone, remimazolam-propofol with flumazenil reversal provides faster and more complete recovery, superior hemodynamic stability perioperatively, and reduced analgesic requirements in laparoscopic partial hepatectomy patients.

Abstract licence: CC BY-NC

Effect of flumazenil on recovery of memory following recovery of consciousness from general anesthesia with remimazolam: a randomized, open-label, single-center controlled trial

Keiko Nobukuni, Kazuhiro Shirozu, Masako Asada, et al.

JA Clinical Reports, 2025

Randomised trial

Sources: aggregated from Europe PMC (EMBL-EBI), OpenAlex, Crossref, PubMed and other open scholarly databases. Retracted articles are excluded. Study information is provided for research purposes and does not constitute medical advice.

Pharmacology and chemical data from DrugBank

go.drugbank.com

Key facts

Drug status

Approved

Major interactions

None known

Half-life

4 to 11 minutes

Mechanism

Flumazenil, an imidazobenzodiazepine derivative, is a benzodiazepine antagonist.

Food interactions

1 warning

Human targets

8 targets

Data: DrugBank · CC BY-NC 4.0

Pharmacokinetics at a glance

Half-life

4 to 11 minutes

Initial distribution half-life is 4 to 11 minutes and the terminal half-life is 40 to 80 minutes.…

Protein binding

50%

Protein binding is approximately 50%, mostly (66%) to albumin. Protein binding is reduced in patients with hepatic cirrhosis.

Volume of distribution

0.9 to 1.1 L/kg

* 0.9 to 1.1 L/kg

Metabolism

99%

Hepatic. Flumazenil is completely (99%) metabolized. The major metabolites of flumazenil identified in urine are the de-ethylated free acid and its glucuronide conjugate.…

Elimination

99%

Flumazenil is completely (99%) metabolized. Elimination of radiolabeled drug is essentially complete within 72 hours, with 90% to 95% of the…

Clearance

1 L/h

* 1 L/hr/kg [healthy volunteers receiving a 5-minute infusion of a total of 1 mg]

Pharmacokinetic data: DrugBank · CC BY-NC 4.0

Status:

Approved

Investigational

Small molecule

About this compound

Fumazenil is an imidazobenzodiazepine derivative and a potent benzodiazepine receptor antagonist that competitively inhibits the activity at the benzodiazepine recognition site on the GABA/benzodiazepine receptor complex, thereby reversing the effects of benzodiazepine on the central nervous system.

Properties:

solid

Avg. mass: 303.29 Da

View FDA drug label

DrugBank indication

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, and where sedation has been produced with benzodiazepines for diagnostic and therapeutic procedures. Also for the management of benzodiazepine overdose as an adjunct for appropriate supportive and symptomatic measures.

Also known as(54)

Flumazenil

Flumazenilo

Flumazenilum

Flumazepil

GABA(A) receptor subunit gamma-2

GABAAR subunit gamma-2

GABA(A) receptor subunit alpha-5

GABAAR subunit alpha-5

Molecular properties(18)

Drug interactions(743)

Known interactions with other medicines. Always consult a healthcare professional.

Lorazepam

Moderate

DB00186

Flumazenil may decrease the sedative activities of Lorazepam.

Check this interaction

Temazepam

Moderate

DB00231

Flumazenil may decrease the sedative activities of Temazepam.

Check this interaction

Eszopiclone

Moderate

DB00402

Flumazenil may decrease the sedative activities of Eszopiclone.

Check this interaction

Zolpidem

Moderate

DB00425

Flumazenil may decrease the sedative activities of Zolpidem.

Check this interaction

Midazolam

Moderate

DB00683

Flumazenil may decrease the sedative activities of Midazolam.

Check this interaction

Diazepam

Moderate

DB00829

Flumazenil may decrease the sedative activities of Diazepam.

Check this interaction

Oxazepam

Moderate

DB00842

Flumazenil may decrease the sedative activities of Oxazepam.

Check this interaction

Triazolam

Moderate

DB00897

Flumazenil may decrease the sedative activities of Triazolam.

Check this interaction

Zaleplon

Moderate

DB00962

Flumazenil may decrease the sedative activities of Zaleplon.

Check this interaction

Zopiclone

Moderate

DB01198

Flumazenil may decrease the sedative activities of Zopiclone.

Check this interaction

Estazolam

Moderate

DB01215

Flumazenil may decrease the sedative activities of Estazolam.

Check this interaction

Flunitrazepam

Moderate

DB01544

Flumazenil may decrease the sedative activities of Flunitrazepam.

Check this interaction

Bromazepam

Moderate

DB01558

Flumazenil may decrease the sedative activities of Bromazepam.

Check this interaction

Quazepam

Moderate

DB01589

Flumazenil may decrease the sedative activities of Quazepam.

Check this interaction

Cinolazepam

Moderate

DB01594

Flumazenil may decrease the sedative activities of Cinolazepam.

Check this interaction

Nitrazepam

Moderate

DB01595

Flumazenil may decrease the sedative activities of Nitrazepam.

Check this interaction

Brotizolam

Moderate

DB09017

Flumazenil may decrease the sedative activities of Brotizolam.

Check this interaction

Etizolam

Moderate

DB09166

Flumazenil may decrease the sedative activities of Etizolam.

Check this interaction

Medazepam

Moderate

DB13437

Flumazenil may decrease the sedative activities of Medazepam.

Check this interaction

Loprazolam

Moderate

DB13643

Flumazenil may decrease the sedative activities of Loprazolam.

Check this interaction

Remimazolam

Moderate

DB12404

Flumazenil may decrease the sedative activities of Remimazolam.

Check this interaction

Cyclosporine

Moderate

DB00091

Cyclosporine may decrease the excretion rate of Flumazenil which could result in a higher serum level.

Check this interaction

Icosapent

Moderate

DB00159

Icosapent may decrease the excretion rate of Flumazenil which could result in a higher serum level.

Check this interaction

Cefotiam

Moderate

DB00229

Cefotiam may decrease the excretion rate of Flumazenil which could result in a higher serum level.

Check this interaction

Mesalazine

Moderate

DB00244

Mesalazine may decrease the excretion rate of Flumazenil which could result in a higher serum level.

Check this interaction

Cefmenoxime

Moderate

DB00267

Cefmenoxime may decrease the excretion rate of Flumazenil which could result in a higher serum level.

Check this interaction

Cefmetazole

Moderate

DB00274

Cefmetazole may decrease the excretion rate of Flumazenil which could result in a higher serum level.

Check this interaction

Pamidronic acid

Moderate

DB00282

Pamidronic acid may decrease the excretion rate of Flumazenil which could result in a higher serum level.

Check this interaction

Tenofovir disoproxil

Moderate

DB00300

Tenofovir disoproxil may decrease the excretion rate of Flumazenil which could result in a higher serum level.

Check this interaction

Indomethacin

Moderate

DB00328

Indomethacin may decrease the excretion rate of Flumazenil which could result in a higher serum level.

Check this interaction

Cidofovir

Moderate

DB00369

Cidofovir may decrease the excretion rate of Flumazenil which could result in a higher serum level.

Check this interaction

Cefpiramide

Moderate

DB00430

Cefpiramide may decrease the excretion rate of Flumazenil which could result in a higher serum level.

Check this interaction

Ceftazidime

Moderate

DB00438

Ceftazidime may decrease the excretion rate of Flumazenil which could result in a higher serum level.

Check this interaction

Loracarbef

Moderate

DB00447

Loracarbef may decrease the excretion rate of Flumazenil which could result in a higher serum level.

Check this interaction

Cefalotin

Moderate

DB00456

Cefalotin may decrease the excretion rate of Flumazenil which could result in a higher serum level.

Check this interaction

Nabumetone

Moderate

DB00461

Nabumetone may decrease the excretion rate of Flumazenil which could result in a higher serum level.

Check this interaction

Ketorolac

Moderate

DB00465

Ketorolac may decrease the excretion rate of Flumazenil which could result in a higher serum level.

Check this interaction

Tenoxicam

Moderate

DB00469

Tenoxicam may decrease the excretion rate of Flumazenil which could result in a higher serum level.

Check this interaction

Celecoxib

Moderate

DB00482

Celecoxib may decrease the excretion rate of Flumazenil which could result in a higher serum level.

Check this interaction

Cefotaxime

Moderate

DB00493

Cefotaxime may decrease the excretion rate of Flumazenil which could result in a higher serum level.

Check this interaction

Tolmetin

Moderate

DB00500

Tolmetin may decrease the excretion rate of Flumazenil which could result in a higher serum level.

Check this interaction

Foscarnet

Moderate

DB00529

Foscarnet may decrease the excretion rate of Flumazenil which could result in a higher serum level.

Check this interaction

Rofecoxib

Moderate

DB00533

Rofecoxib may decrease the excretion rate of Flumazenil which could result in a higher serum level.

Check this interaction

Piroxicam

Moderate

DB00554

Piroxicam may decrease the excretion rate of Flumazenil which could result in a higher serum level.

Check this interaction

Methotrexate

Moderate

DB00563

Methotrexate may decrease the excretion rate of Flumazenil which could result in a higher serum level.

Check this interaction

Cephalexin

Moderate

DB00567

Cephalexin may decrease the excretion rate of Flumazenil which could result in a higher serum level.

Check this interaction

Fenoprofen

Moderate

DB00573

Fenoprofen may decrease the excretion rate of Flumazenil which could result in a higher serum level.

Check this interaction

Valaciclovir

Moderate

DB00577

Valaciclovir may decrease the excretion rate of Flumazenil which could result in a higher serum level.

Check this interaction

Valdecoxib

Moderate

DB00580

Valdecoxib may decrease the excretion rate of Flumazenil which could result in a higher serum level.

Check this interaction

Diclofenac

Moderate

DB00586

Diclofenac may decrease the excretion rate of Flumazenil which could result in a higher serum level.

Check this interaction

Showing 50 of 743 interactions

Food & lifestyle interactions

Advice

Take separate from meals. Eating during an intravenous infusion of flumazenil increases the elimination of flumazenil, potentially through elevated hepatic blood flow.

Toxicity & overdose

In clinical studies, most adverse reactions to flumazenil were an extension of the pharmacologic effects of the drug in reversing benzodiazepine effects.

How it works

Mechanism of action

Flumazenil, an imidazobenzodiazepine derivative, is a benzodiazepine antagonist. It competitively inhibits the benzodiazepine binding 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.

Pharmacodynamics

Flumazenil antagonizes the CNS effects produced by benzodiazepines, but 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.

Pharmacokinetics

How the body processes this drug — absorption, distribution, metabolism, and elimination

Half-life

Initial distribution half-life is 4 to 11 minutes and the terminal half-life is 40 to 80 minutes. Prolongation of the half-life to 1.3 hours in patients with moderate hepatic impairment and 2.4 hours in severely impaired patients. Compared to adults, the elimination half-life in pediatric patients was more variable, averaging 40 minutes (range: 20 to 75 minutes).

Protein binding

Protein binding is approximately 50%, mostly (66%) to albumin. Protein binding is reduced in patients with hepatic cirrhosis.

Volume of distribution

* 0.9 to 1.1 L/kg

Metabolism

Hepatic. Flumazenil is completely (99%) metabolized. The major metabolites of flumazenil identified in urine are the de-ethylated free acid and its glucuronide conjugate.

Route of elimination

Flumazenil is completely (99%) metabolized. Elimination of radiolabeled drug is essentially complete within 72 hours, with 90% to 95% of the radioactivity appearing in urine and 5% to 10% in the feces.

Clearance

* 1 L/hr/kg [healthy volunteers receiving a 5-minute infusion of a total of 1 mg]

Drug targets(8)

Proteins and enzymes this drug interacts with in the body

Gamma-aminobutyric acid receptor subunit gamma-2

BE0003592

GABRG2

antagonist

Specific functionbenzodiazepine receptor activity

Cellular location

Postsynaptic cell membrane

General function & pharmacology

Gamma subunit of the heteropentameric ligand-gated chloride channel gated by gamma-aminobutyric acid (GABA), a major inhibitory neurotransmitter in the brain .
PMID:14993607 PMID:16412217 PMID:23909897 PMID:2538761 PMID:25489750 PMID:27864268 PMID:29950725 PMID:30602789

GABA-gated chloride channels, also named GABA(A) receptors (GABAAR), consist of five subunits arranged around a central pore and contain GABA active binding site(s) located at the alpha and beta subunit interface(s) .
PMID:29950725 PMID:30602789
When activated by GABA, GABAARs selectively allow the flow of chloride anions across the cell membrane down their electrochemical gradient .
PMID:14993607 PMID:16412217 PMID:2538761 PMID:27864268 PMID:29950725 PMID:30602789

Gamma-2/GABRG2-containing GABAARs are found at both synaptic and extrasynaptic sites (By similarity). Chloride influx into the postsynaptic neuron following GABAAR opening decreases the neuron ability to generate a new action potential, thereby reducing nerve transmission (By similarity). GABAARs containing alpha-1 and beta-2 or -3 subunits exhibit synaptogenic activity; the gamma-2 subunit being necessary but not sufficient to induce rapid synaptic contacts formation .
PMID:23909897 PMID:25489750
Extrasynaptic gamma-2-containing receptors contribute to the tonic GABAergic inhibition (By similarity).

GABAARs function also as histamine receptor where histamine binds at the interface of two neighboring beta subunits and potentiates GABA response in a gamma-2 subunit-controlled manner (By similarity)

Gamma-aminobutyric acid receptor subunit alpha-5

BE0000471

GABRA5

antagonist

Specific functionGABA receptor binding

Cellular location

Postsynaptic cell membrane

General function & pharmacology

Alpha subunit of the heteropentameric ligand-gated chloride channel gated by gamma-aminobutyric acid (GABA), a major inhibitory neurotransmitter in the brain .
PMID:14993607 PMID:29961870 PMID:30140029 PMID:31056671

GABA-gated chloride channels, also named GABA(A) receptors (GABAAR), consist of five subunits arranged around a central pore and contain GABA active binding site(s) located at the alpha and beta subunit interface(s) .
PMID:30140029
When activated by GABA, GABAARs selectively allow the flow of chloride anions across the cell membrane down their electrochemical gradient .
PMID:14993607 PMID:30140029
GABAARs containing alpha-5/GABRA5 subunits are mainly extrasynaptic and contribute to the tonic GABAergic inhibition in the hippocampus (By similarity). Extrasynaptic alpha-5-containing GABAARs in CA1 pyramidal neurons play a role in learning and memory processes (By similarity)

Gamma-aminobutyric acid receptor subunit theta

BE0004797

GABRQ

positive allosteric modulator

Specific functionGABA-A receptor activity

Cellular location

Postsynaptic cell membrane

General function & pharmacology

Theta subunit of the heteropentameric ligand-gated chloride channel gated by gamma-aminobutyric acid (GABA), a major inhibitory neurotransmitter in the brain .
PMID:10449790 PMID:16412217
GABA-gated chloride channels, also named GABA(A) receptors (GABAAR), consist of five subunits arranged around a central pore and contain GABA active binding site(s) located at the alpha and beta subunit interfaces (By similarity). When activated by GABA, GABAARs selectively allow the flow of chloride anions across the cell membrane down their electrochemical gradient PMID:10449790 PMID:16412217

Gamma-aminobutyric acid receptor subunit alpha-1

BE0000795

GABRA1

antagonist

Specific functionGABA-A receptor activity

Cellular location

Postsynaptic cell membrane

General function & pharmacology

Alpha subunit of the heteropentameric ligand-gated chloride channel gated by Gamma-aminobutyric acid (GABA), a major inhibitory neurotransmitter in the brain .
PMID:23909897 PMID:25489750 PMID:29950725 PMID:30602789

GABA-gated chloride channels, also named GABA(A) receptors (GABAAR), consist of five subunits arranged around a central pore and contain GABA active binding site(s) located at the alpha and beta subunit interface(s) .
PMID:29950725 PMID:30602789
When activated by GABA, GABAARs selectively allow the flow of chloride anions across the cell membrane down their electrochemical gradient .
PMID:23909897 PMID:29950725 PMID:30602789

Alpha-1/GABRA1-containing GABAARs are largely synaptic (By similarity). Chloride influx into the postsynaptic neuron following GABAAR opening decreases the neuron ability to generate a new action potential, thereby reducing nerve transmission (By similarity). GABAARs containing alpha-1 and beta-2 or -3 subunits exhibit synaptogenic activity; the gamma-2 subunit being necessary but not sufficient to induce rapid synaptic contacts formation .
PMID:23909897 PMID:25489750
GABAARs function also as histamine receptor where histamine binds at the interface of two neighboring beta subunits and potentiates GABA response (By similarity).

GABAARs containing alpha, beta and epsilon subunits also permit spontaneous chloride channel activity while preserving the structural information required for GABA-gated openings (By similarity). Alpha-1-mediated plasticity in the orbitofrontal cortex regulates context-dependent action selection (By similarity). Together with rho subunits, may also control neuronal and glial GABAergic transmission in the cerebellum (By similarity)

Gamma-aminobutyric acid receptor subunit gamma-3

BE0003594

GABRG3

allosteric modulator

Specific functionGABA-A receptor activity

Cellular location

Postsynaptic cell membrane

General function & pharmacology

Gamma subunit of the heteropentameric ligand-gated chloride channel gated by gamma-aminobutyric acid (GABA), a major inhibitory neurotransmitter in the brain (By similarity). GABA-gated chloride channels, also named GABA(A) receptors (GABAAR), consist of five subunits arranged around a central pore and contain GABA active binding site(s) located at the alpha and beta subunit interface(s) (By similarity). When activated by GABA, GABAARs selectively allow the flow of chloride across the cell membrane down their electrochemical gradient (By similarity)

Scientific references(3)

Ngo A.S., Anthony C.R., Samuel M., Wong E., Ponampalam R.

Should a benzodiazepine antagonist be used in unconscious patients presenting to the emergency department?.

Resuscitation

200774(1):27-37. doi: 10.1016/j.resuscitation.2006.11.010

PMID: 17306436 DOI: 10.1016/j.resuscitation.2006.11.010

Olkkola K.T., Ahonen J.

Midazolam and other benzodiazepines.

Handb Experimental Pharmacology

2008(182):335-60. doi: 10.1007/978-3-540-74806-9_16

PMID: 18175099 DOI: 10.1007/978-3-540-74806-9_16

Maeda S., Miyawaki T., Higuchi H., Shimada M.

Effect of flumazenil on disturbance of equilibrium function induced by midazolam.

Anesth Prog

2008 Fall55(3):73-7. doi: 10.2344/0003-3006-55.3.73

PMID: 18788841 DOI: 10.2344/0003-3006-55.3.73

ATC classification(1 code)

ATC V03AB25

Affected organisms(1)

Humans and other mammals

Experimental properties(3)

External resources(2)

RxList Drugs.com

Protein Data Bank entries(4)

Chemical identifiers

CAS, UNII, InChI Key and database cross-references

Show

Linked compound data from DrugBank Open Data (CC BY-NC 4.0)

Flumazenil

DB01205

CAS number

78755-81-4

UNII (FDA)

40P7XK9392

InChI Key (molecular fingerprint)

OFBIFZUFASYYRE-UHFFFAOYSA-N

Additional database identifiers

Drugs Product Database (DPD)

1227

ChEBI

5103

PubChem Compound

3373

PubChem Substance

46507438

KEGG Compound

C07825

KEGG Drug

D00697

ChemSpider

3256

BindingDB

26263

PharmGKB

PA449659

PDB

FYP

Therapeutic Targets Database

DAP000685

Wikipedia

Flumazenil

ChEMBL

CHEMBL407

ZINC

ZINC000000001464

RxCUI

4457

HUGO Gene Nomenclature Committee (HGNC)

HGNC:4087

GeneCards

GABRG2

GenBank Gene Database

X15376

GenBank Protein Database

31637

UniProtKB

P18507

UniProt Accession

GBRG2_HUMAN

HUGO Gene Nomenclature Committee (HGNC)

HGNC:4079

GenAtlas

GABRA5

GeneCards

GABRA5

GenBank Gene Database

L08485

GenBank Protein Database

182916

IUPHAR

408

Guide to Pharmacology

408

UniProtKB

P31644

UniProt Accession

GBRA5_HUMAN

HUGO Gene Nomenclature Committee (HGNC)

HGNC:4075

GenAtlas

GABRA1

GeneCards

GABRA1

GenBank Gene Database

X13584

GenBank Protein Database

31631

IUPHAR

404

Guide to Pharmacology

404

UniProtKB

P14867

UniProt Accession

GBRA1_HUMAN

HUGO Gene Nomenclature Committee (HGNC)

HGNC:4076

GenAtlas

GABRA2

GeneCards

GABRA2

GenBank Gene Database

S62907

GenBank Protein Database

386422

IUPHAR

405

Guide to Pharmacology

405

UniProtKB

P47869

UniProt Accession

GBRA2_HUMAN

HUGO Gene Nomenclature Committee (HGNC)

HGNC:4077

GenAtlas

GABRA3

GeneCards

GABRA3

GenBank Gene Database

S62908

GenBank Protein Database

386424

IUPHAR

406

Guide to Pharmacology

406

UniProtKB

P34903

UniProt Accession

GBRA3_HUMAN

HUGO Gene Nomenclature Committee (HGNC)

HGNC:4078

GenAtlas

GABRA4

GeneCards

GABRA4

GenBank Gene Database

U30461

GenBank Protein Database

905393

IUPHAR

407

Guide to Pharmacology

407

UniProtKB

P48169

UniProt Accession

GBRA4_HUMAN

HUGO Gene Nomenclature Committee (HGNC)

HGNC:4079

GenAtlas

GABRA5

GeneCards

GABRA5

GenBank Gene Database

L08485

GenBank Protein Database

182916

IUPHAR

408

Guide to Pharmacology

408

UniProtKB

P31644

UniProt Accession

GBRA5_HUMAN

HUGO Gene Nomenclature Committee (HGNC)

HGNC:4080

GenAtlas

GABRA6

GeneCards

GABRA6

GenBank Gene Database

S81944

GenBank Protein Database

1470364

IUPHAR

409

Guide to Pharmacology

409

UniProtKB

Q16445

UniProt Accession

GBRA6_HUMAN

HUGO Gene Nomenclature Committee (HGNC)

HGNC:4081

GenAtlas

GABRB1

GeneCards

GABRB1

GenBank Gene Database

X14767

GenBank Protein Database

31635

IUPHAR

410

UniProtKB

P18505

UniProt Accession

GBRB1_HUMAN

HUGO Gene Nomenclature Committee (HGNC)

HGNC:4082

GenAtlas

GABRB2

GeneCards

GABRB2

GenBank Gene Database

S67368

GenBank Protein Database

455946

IUPHAR

411

UniProtKB

P47870

UniProt Accession

GBRB2_HUMAN

HUGO Gene Nomenclature Committee (HGNC)

HGNC:4083

GenAtlas

GABRB3

GeneCards

GABRB3

GenBank Gene Database

M82919

GenBank Protein Database

182925

IUPHAR

412

Guide to Pharmacology

412

UniProtKB

P28472

UniProt Accession

GBRB3_HUMAN

HUGO Gene Nomenclature Committee (HGNC)

HGNC:4084

GeneCards

GABRD

GenBank Gene Database

AF016917

GenBank Protein Database

2388693

UniProtKB

O14764

UniProt Accession

GBRD_HUMAN

HUGO Gene Nomenclature Committee (HGNC)

HGNC:4085

GeneCards

GABRE

GenBank Gene Database

U66661

GenBank Protein Database

1857126

UniProtKB

P78334

UniProt Accession

GBRE_HUMAN

HUGO Gene Nomenclature Committee (HGNC)

HGNC:4086

GeneCards

GABRG1

GenBank Gene Database

AK122845

GenBank Protein Database

193783776

UniProtKB

Q8N1C3

UniProt Accession

GBRG1_HUMAN

HUGO Gene Nomenclature Committee (HGNC)

HGNC:4087

GeneCards

GABRG2

GenBank Gene Database

X15376

GenBank Protein Database

31637

UniProtKB

P18507

UniProt Accession

GBRG2_HUMAN

HUGO Gene Nomenclature Committee (HGNC)

HGNC:4088

GeneCards

GABRG3

GenBank Gene Database

S82769

GenBank Protein Database

1754749

UniProtKB

Q99928

UniProt Accession

GBRG3_HUMAN

HUGO Gene Nomenclature Committee (HGNC)

HGNC:4089

GeneCards

GABRP

GenBank Gene Database

U95367

GenBank Protein Database

2197001

UniProtKB

O00591

UniProt Accession

GBRP_HUMAN

HUGO Gene Nomenclature Committee (HGNC)

HGNC:14454

GeneCards

GABRQ

GenBank Gene Database

AF189259

GenBank Protein Database

7861736

UniProtKB

Q9UN88

UniProt Accession

GBRT_HUMAN

HUGO Gene Nomenclature Committee (HGNC)

HGNC:4075

GenAtlas

GABRA1

GeneCards

GABRA1

GenBank Gene Database

X13584

GenBank Protein Database

31631

IUPHAR

404

Guide to Pharmacology

404

UniProtKB

P14867

UniProt Accession

GBRA1_HUMAN

HUGO Gene Nomenclature Committee (HGNC)

HGNC:4088

GeneCards

GABRG3

GenBank Gene Database

S82769

GenBank Protein Database

1754749

UniProtKB

Q99928

UniProt Accession

GBRG3_HUMAN

HUGO Gene Nomenclature Committee (HGNC)

HGNC:4076

GenAtlas

GABRA2

GeneCards

GABRA2

GenBank Gene Database

S62907

GenBank Protein Database

386422

IUPHAR

405

Guide to Pharmacology

405

UniProtKB

P47869

UniProt Accession

GBRA2_HUMAN

HUGO Gene Nomenclature Committee (HGNC)

HGNC:4077

GenAtlas

GABRA3

GeneCards

GABRA3

GenBank Gene Database

S62908

GenBank Protein Database

386424

IUPHAR

406

Guide to Pharmacology

406

UniProtKB

P34903

UniProt Accession

GBRA3_HUMAN

HUGO Gene Nomenclature Committee (HGNC)

HGNC:1158

GenAtlas

TSPO

GeneCards

TSPO

GenBank Gene Database

M36035

GenBank Protein Database

306883

Guide to Pharmacology

2879

UniProtKB

P30536

UniProt Accession

TSPO_HUMAN

DrugBank citations

If you use DrugBank data in your research, please cite:

DrugBank 6.02024Recommended citation
Knox C., Wilson M., Klinger C.M., et al
DrugBank 6.
0: the DrugBank Knowledgebase for 2024
Nucleic Acids Res. 2024 Jan 552(D1):D1265-D1275
PMID: 37953279
DrugBank 5.02018
Wishart D.S., Feunang Y.D., Guo A.C., et al
DrugBank 5.
0: a major update to the DrugBank database for 2018
Nucleic Acids Res. 2017 Nov 846(D1):D1074-D1082
PMID: 29126136
DrugBank 4.02014
Law V., Knox C., Djoumbou Y., et al
DrugBank 4.
0: shedding new light on drug metabolism
Nucleic Acids Res. 2014 Jan 142(1):D1091-7
PMID: 24203711
DrugBank 3.02011
Knox C., Law V., Jewison T., et al
DrugBank 3.
0: a comprehensive resource for 'omics' research on drugs
Nucleic Acids Res. 2011 Jan39(Database issue):D1035-41
PMID: 21059682
DrugBank 2.02008
Wishart D.S., Knox C., Guo A.C., et al
DrugBank: a knowledgebase for drugs, drug actions and drug targets.
Nucleic Acids Research
2008 Jan36(Database issue):D901-6
PMID: 18048412
DrugBank 1.02006
Wishart D.S., Knox C., Guo A.C., et al
DrugBank: a comprehensive resource for in silico drug discovery and exploration.
Nucleic Acids Research
2006 Jan 134(Database issue):D668-72
PMID: 16381955

Source: go.drugbank.comCC BY-NC 4.0

Updated 8 Mar 2026

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