Peringatan Keamanan

In vitro, the complex of bicisate and technetium Tc-99m has been shown to cause unscheduled DNA synthesis and caused an increased frequency of chromatid exchange. Bicisate as a unique compound increased the apparent rate of gene mutation but it did not demonstrate clastogenic activity. Studies related to clastogenic potential or effects in fertility have not been performed.L2034

Bicisate

DB11164

small molecule approved investigational

Deskripsi

Bicisate, also known as ethyl cysteinate dimer (ECD), is a N,N'-1,2-ethylene-di-yl-bis-L-cysteinate diethyl ester. It is used in conjunction with technetium Tc99m as a tracer to measure cerebral blood flow with single-photon emission computed tomography (SPECT).A32374 The complex of bicisate and technetium Tc99m as a kit was developed by Lantheus Medcl and FDA-approved on November 23, 1994.L2029

Struktur Molekul 2D

Berat 324.45
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The stability of bicisate is superior when compared to other brain radiopharmaceuticals.[T152] Thus, the reported half-life of bicisate is of 6.02 hours.[L2032] When broadly studied in clinical trials, the pharmacokinetic profile fits a three-compartment model with half-lives of 43 seconds, 49.5 minutes and 533 minutes.[A32390]
Volume Distribusi After intravenous administration of bicisate, the distribution volume was 0.74 L.[A32395]
Klirens (Clearance) The clearance of bicisate from 1 to 24 hours, studied as a loss of hydrophilic tracer, is of approximate 3.5% per hour.[A32390]

Absorpsi

After intravenous administration, bicisate presents a very large brain extraction.A32374 About 5% of the administered dose remains in the blood one hour after administration. The highest concentration of radioactivity in blood was attained 0.5 minutes after intravenous injection and it represented 13.9% of the injected dose.L2034 After intravenous administration of bicisate, the permeability surface area was 0.48 ml.g/min.A32395

Metabolisme

Bicisate is metabolized to form mono- and di-acids by the action of esterases. The exact metabolic transformation has not been elucidated.L2034, T154

Rute Eliminasi

Bicisate is primarily excreted by the kidneys. It has been reported that 50% of the dose is excreted in urine two hours after initial administration and even 74% of the administered dose is excreted in urine after 24 hours. Fecal excretion just accounts for 12.5% of the administered dose 48 hours after initial administration.L2034

Interaksi Obat

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

Referensi & Sumber

Artikel (PubMed)
  • PMID: 9430465
    Dormehl IC, Oliver DW, Langen KJ, Hugo N, Croft SA: Technetium-99m-HMPAO, technetium-99m-ECD and iodine-123-IMP cerebral blood flow measurements with pharmacological interventions in primates. J Nucl Med. 1997 Dec;38(12):1897-901.
  • PMID: 8263067
    Friberg L, Andersen AR, Lassen NA, Holm S, Dam M: Retention of 99mTc-bicisate in the human brain after intracarotid injection. J Cereb Blood Flow Metab. 1994 Jan;14 Suppl 1:S19-27.
  • PMID: 8263066
    Knudsen GM, Andersen AR, Somnier FE, Videbaek C, Hasselbalch S, Paulson OB: Brain extraction and distribution of 99mTc-bicisate in humans and in rats. J Cereb Blood Flow Metab. 1994 Jan;14 Suppl 1:S12-8.
Textbook
  • International Atomic Energy Agency (2008). Technetium-99m radiopharmaceuticals: Manufacture of kits. IAEA.
  • Kowalsky R. (2006). Technetium radiopharmaceutical chemistry. University of New Mexico Health Sciences Center.
  • Grunwald F., Kasper S., Biersack J. and Moller J. (1995). Brain SPECT Imaging in psychiatry. Walter de Gruyter.

Contoh Produk & Brand

Produk: 2 • International brands: 0
Produk
  • Bicisate
    Injection, powder, lyophilized, for solution • 1.35 mg/1 • Intravenous • US
  • Neurolite
    Injection; Kit • 0.9 mg/1 • Intravenous • US • Approved

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