Peringatan Keamanan

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

Flumazenil

DB01205

small molecule approved

Deskripsi

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.

Struktur Molekul 2D

Berat 303.2884
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (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).
Volume Distribusi * 0.9 to 1.1 L/kg
Klirens (Clearance) * 1 L/hr/kg [healthy volunteers receiving a 5-minute infusion of a total of 1 mg]

Absorpsi

Data absorpsi tidak tersedia.

Metabolisme

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

Rute Eliminasi

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.

Interaksi Makanan

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

Interaksi Obat

738 Data
Lorazepam Flumazenil may decrease the sedative activities of Lorazepam.
Temazepam Flumazenil may decrease the sedative activities of Temazepam.
Eszopiclone Flumazenil may decrease the sedative activities of Eszopiclone.
Zolpidem Flumazenil may decrease the sedative activities of Zolpidem.
Midazolam Flumazenil may decrease the sedative activities of Midazolam.
Diazepam Flumazenil may decrease the sedative activities of Diazepam.
Oxazepam Flumazenil may decrease the sedative activities of Oxazepam.
Triazolam Flumazenil may decrease the sedative activities of Triazolam.
Zaleplon Flumazenil may decrease the sedative activities of Zaleplon.
Zopiclone Flumazenil may decrease the sedative activities of Zopiclone.
Estazolam Flumazenil may decrease the sedative activities of Estazolam.
Flunitrazepam Flumazenil may decrease the sedative activities of Flunitrazepam.
Bromazepam Flumazenil may decrease the sedative activities of Bromazepam.
Quazepam Flumazenil may decrease the sedative activities of Quazepam.
Cinolazepam Flumazenil may decrease the sedative activities of Cinolazepam.
Nitrazepam Flumazenil may decrease the sedative activities of Nitrazepam.
Brotizolam Flumazenil may decrease the sedative activities of Brotizolam.
Etizolam Flumazenil may decrease the sedative activities of Etizolam.
Medazepam Flumazenil may decrease the sedative activities of Medazepam.
Loprazolam Flumazenil may decrease the sedative activities of Loprazolam.
Remimazolam Flumazenil may decrease the sedative activities of Remimazolam.
Cyclosporine Cyclosporine may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Icosapent Icosapent may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Cefotiam Cefotiam may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Mesalazine Mesalazine may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Cefmenoxime Cefmenoxime may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Cefmetazole Cefmetazole may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Pamidronic acid Pamidronic acid may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Tenofovir disoproxil Tenofovir disoproxil may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Indomethacin Indomethacin may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Cidofovir Cidofovir may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Cefpiramide Cefpiramide may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Ceftazidime Ceftazidime may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Loracarbef Loracarbef may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Cefalotin Cefalotin may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Nabumetone Nabumetone may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Ketorolac Ketorolac may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Tenoxicam Tenoxicam may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Celecoxib Celecoxib may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Cefotaxime Cefotaxime may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Tolmetin Tolmetin may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Foscarnet Foscarnet may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Rofecoxib Rofecoxib may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Piroxicam Piroxicam may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Methotrexate Methotrexate may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Cephalexin Cephalexin may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Fenoprofen Fenoprofen may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Valaciclovir Valaciclovir may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Valdecoxib Valdecoxib may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Diclofenac Diclofenac may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Sulindac Sulindac may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Bacitracin Bacitracin may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Amphotericin B Amphotericin B may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Cephaloglycin Cephaloglycin may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Flurbiprofen Flurbiprofen may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Adefovir dipivoxil Adefovir dipivoxil may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Pentamidine Pentamidine may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Etodolac Etodolac may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Mefenamic acid Mefenamic acid may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Acyclovir Acyclovir may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Naproxen Naproxen may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Sulfasalazine Sulfasalazine may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Phenylbutazone Phenylbutazone may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Meloxicam Meloxicam may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Carprofen Carprofen may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Cefaclor Cefaclor may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Diflunisal Diflunisal may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Tacrolimus Tacrolimus may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Ceforanide Ceforanide may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Salicylic acid Salicylic acid may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Meclofenamic acid Meclofenamic acid may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Acetylsalicylic acid Acetylsalicylic acid may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Carboplatin Carboplatin may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Oxaprozin Oxaprozin may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Ketoprofen Ketoprofen may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Balsalazide Balsalazide may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Ibuprofen Ibuprofen may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Cefditoren Cefditoren may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Atazanavir Atazanavir may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Colistimethate Colistimethate may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Cefuroxime Cefuroxime may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Cefapirin Cefapirin may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Cefadroxil Cefadroxil may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Cefprozil Cefprozil may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Ceftriaxone Ceftriaxone may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Olsalazine Olsalazine may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Lumiracoxib Lumiracoxib may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Cefamandole Cefamandole may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Cefazolin Cefazolin may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Cefonicid Cefonicid may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Cefoperazone Cefoperazone may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Cefotetan Cefotetan may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Cefoxitin Cefoxitin may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Ceftizoxime Ceftizoxime may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Cefradine Cefradine may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Magnesium salicylate Magnesium salicylate may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Salsalate Salsalate may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Choline magnesium trisalicylate Choline magnesium trisalicylate may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Cefepime Cefepime may decrease the excretion rate of Flumazenil which could result in a higher serum level.
Cefacetrile Cefacetrile may decrease the excretion rate of Flumazenil which could result in a higher serum level.

Target Protein

Translocator protein TSPO
Gamma-aminobutyric acid receptor subunit gamma-2 GABRG2
Gamma-aminobutyric acid receptor subunit alpha-2 GABRA2
Gamma-aminobutyric acid receptor subunit gamma-3 GABRG3
Gamma-aminobutyric acid receptor subunit alpha-3 GABRA3
Gamma-aminobutyric acid receptor subunit alpha-5 GABRA5
GABA(A) Receptor GABRA1
Gamma-aminobutyric acid receptor subunit alpha-1 GABRA1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 17306436
    Ngo AS, Anthony CR, Samuel M, Wong E, Ponampalam R: Should a benzodiazepine antagonist be used in unconscious patients presenting to the emergency department? Resuscitation. 2007 Jul;74(1):27-37. Epub 2007 Feb 15.
  • PMID: 18175099
    Olkkola KT, Ahonen J: Midazolam and other benzodiazepines. Handb Exp Pharmacol. 2008;(182):335-60. doi: 10.1007/978-3-540-74806-9_16.
  • PMID: 18788841
    Maeda S, Miyawaki T, Higuchi H, Shimada M: Effect of flumazenil on disturbance of equilibrium function induced by midazolam. Anesth Prog. 2008 Fall;55(3):73-7. doi: 10.2344/0003-3006-55.3.73.

Contoh Produk & Brand

Produk: 59 • International brands: 3
Produk
  • Anexate Inj 0.1mg/ml
    Solution • 0.1 mg / mL • Intravenous • Canada • Approved
  • Flumazenil
    Injection • 0.1 mg/1mL • Intravenous • US • Approved
  • Flumazenil
    Injection • 0.1 mg/1mL • Intravenous • US • Generic • Approved
  • Flumazenil
    Injection • 0.1 mg/1mL • Intravenous • US • Generic • Approved
  • Flumazenil
    Injection • 0.1 mg/1mL • Intravenous • US • Generic • Approved
  • Flumazenil
    Injection • 0.1 mg/1mL • Intravenous • US • Generic • Approved
  • Flumazenil
    Injection • 0.1 mg/1mL • Intravenous • US • Generic • Approved
  • Flumazenil
    Injection • 0.1 mg/1mL • Intravenous • US • Generic • Approved
Menampilkan 8 dari 59 produk.
International Brands
  • Anexate — Hoffmann-La Roche
  • Lanexat
  • Mazicon

Sekuens Gen/Protein (FASTA)

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