Peringatan Keamanan

Oral, mouse: LD50 = 300 mg/kg; Oral, rabbit: LD50 = 3200 mg/kg; Oral, rat: LD50 = 980 mg/kg.

Flupirtine

DB06623

small molecule investigational

Deskripsi

Flupirtine is a pyridine derivative that is in clinical use as a nonopioid analgesic. It was approved for the treatment of pain in 1984 in Europe. It is not approved for use in the U.S. or Canada, but is currently in phase II trials for the treatment of fibromyalgia.

Struktur Molekul 2D

Berat 304.3195
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 6.5 hrs (average), 11.2-16.8 hrs (average 14 hrs) (elderly), 8.7-10.9 hrs (average 9.8 hrs) (in those with moderate-level renal impairment).
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Bioavailability: 90% (oral), 70% (rectal)

Metabolisme

Hepatic to 2-amino-3-acetylamino-6-(para-fluorobenzylamino) pyridine (which has 20-30% the analgesic potential of its parent compound) and Para-fluorohippuric acid.

Rute Eliminasi

72% of flupirtine and its metabolites appear in urine and 18% appear in faeces.

Interaksi Obat

727 Data
Cyclosporine Cyclosporine may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Icosapent Icosapent may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Cefotiam Cefotiam may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Mesalazine Mesalazine may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Cefmenoxime Cefmenoxime may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Cefmetazole Cefmetazole may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Pamidronic acid Pamidronic acid may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Tenofovir disoproxil Tenofovir disoproxil may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Indomethacin Indomethacin may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Cidofovir Cidofovir may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Cefpiramide Cefpiramide may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Ceftazidime Ceftazidime may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Loracarbef Loracarbef may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Cefalotin Cefalotin may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Nabumetone Nabumetone may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Ketorolac Ketorolac may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Tenoxicam Tenoxicam may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Celecoxib Celecoxib may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Cefotaxime Cefotaxime may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Tolmetin Tolmetin may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Foscarnet Foscarnet may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Rofecoxib Rofecoxib may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Piroxicam Piroxicam may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Methotrexate Methotrexate may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Cephalexin Cephalexin may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Fenoprofen Fenoprofen may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Valaciclovir Valaciclovir may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Valdecoxib Valdecoxib may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Diclofenac Diclofenac may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Sulindac Sulindac may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Bacitracin Bacitracin may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Amphotericin B Amphotericin B may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Cephaloglycin Cephaloglycin may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Flurbiprofen Flurbiprofen may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Adefovir dipivoxil Adefovir dipivoxil may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Pentamidine Pentamidine may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Etodolac Etodolac may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Mefenamic acid Mefenamic acid may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Acyclovir Acyclovir may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Naproxen Naproxen may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Sulfasalazine Sulfasalazine may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Phenylbutazone Phenylbutazone may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Meloxicam Meloxicam may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Carprofen Carprofen may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Cefaclor Cefaclor may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Diflunisal Diflunisal may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Tacrolimus Tacrolimus may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Ceforanide Ceforanide may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Salicylic acid Salicylic acid may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Meclofenamic acid Meclofenamic acid may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Acetylsalicylic acid Acetylsalicylic acid may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Carboplatin Carboplatin may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Oxaprozin Oxaprozin may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Ketoprofen Ketoprofen may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Balsalazide Balsalazide may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Ibuprofen Ibuprofen may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Cefditoren Cefditoren may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Atazanavir Atazanavir may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Colistimethate Colistimethate may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Cefuroxime Cefuroxime may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Cefapirin Cefapirin may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Cefadroxil Cefadroxil may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Cefprozil Cefprozil may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Ceftriaxone Ceftriaxone may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Olsalazine Olsalazine may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Lumiracoxib Lumiracoxib may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Cefamandole Cefamandole may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Cefazolin Cefazolin may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Cefonicid Cefonicid may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Cefoperazone Cefoperazone may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Cefotetan Cefotetan may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Cefoxitin Cefoxitin may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Ceftizoxime Ceftizoxime may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Cefradine Cefradine may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Magnesium salicylate Magnesium salicylate may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Salsalate Salsalate may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Choline magnesium trisalicylate Choline magnesium trisalicylate may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Cefepime Cefepime may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Cefacetrile Cefacetrile may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Ceftibuten Ceftibuten may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Cefpodoxime Cefpodoxime may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Antrafenine Antrafenine may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Aminophenazone Aminophenazone may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Antipyrine Antipyrine may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Tiaprofenic acid Tiaprofenic acid may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Lopinavir Lopinavir may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Etoricoxib Etoricoxib may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Hydrolyzed Cephalothin Hydrolyzed Cephalothin may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Cephalothin Group Cephalothin Group may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Oxyphenbutazone Oxyphenbutazone may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Latamoxef Latamoxef may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Nimesulide Nimesulide may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Benoxaprofen Benoxaprofen may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Metamizole Metamizole may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Zomepirac Zomepirac may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Ceftobiprole Ceftobiprole may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Cimicoxib Cimicoxib may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Ceftaroline fosamil Ceftaroline fosamil may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Lornoxicam Lornoxicam may decrease the excretion rate of Flupirtine which could result in a higher serum level.
Aceclofenac Aceclofenac may decrease the excretion rate of Flupirtine which could result in a higher serum level.

Target Protein

Alpha-2A adrenergic receptor ADRA2A

Referensi & Sumber

Artikel (PubMed)
  • PMID: 10996019
    Muller WE, Laplanche JL, Ushijima H, Schroder HC: Novel approaches in diagnosis and therapy of Creutzfeldt-Jakob disease. Mech Ageing Dev. 2000 Jul 31;116(2-3):193-218.
  • PMID: 11921051
    Dhar S, Bitting RL, Rylova SN, Jansen PJ, Lockhart E, Koeberl DD, Amalfitano A, Boustany RM: Flupirtine blocks apoptosis in batten patient lymphoblasts and in human postmitotic CLN3- and CLN2-deficient neurons. Ann Neurol. 2002 Apr;51(4):448-66.
  • PMID: 2901483
    Swedberg MD, Shannon HE, Nickel B, Goldberg SR: Pharmacological mechanisms of action of flupirtine: a novel, centrally acting, nonopioid analgesic evaluated by its discriminative effects in the rat. J Pharmacol Exp Ther. 1988 Sep;246(3):1067-74.
  • PMID: 3200777
    Abrams SM, Baker LR, Crome P, White AS, Johnston A, Ankier SI, Warrington SJ, Turner P, Niebch G: Pharmacokinetics of flupirtine in elderly volunteers and in patients with moderate renal impairment. Postgrad Med J. 1988 May;64(751):361-3.
  • PMID: 6707137
    Narang PK, Tourville JF, Chatterji DC, Gallelli JF: Quantitation of flupirtine and its active acetylated metabolite by reversed-phase high-performance liquid chromatography using fluorometric detection. J Chromatogr. 1984 Jan 13;305(1):135-43.

Contoh Produk & Brand

Produk: 0 • International brands: 6
International Brands
  • Awegal
  • Effirma
  • Efiret
  • Katadolon
  • Metanor
  • Trancolong

Sekuens Gen/Protein (FASTA)

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