Peringatan Keamanan

There are no data regarding overdosage with ceftobiprole medocaril. In cases of suspected overdose, discontinue therapy and institute general symptomatic and supportive treatment. Ceftobiprole can be removed from the circulation via hemodialysis, however no information is available on the use of hemodialysis to treat ceftobiprole overdose.L50442

Ceftobiprole

DB04918

small molecule approved investigational

Deskripsi

Ceftobiprole is a fifth-generation semisynthetic cephalosporin antibacterial which is available commercially as the prodrug ceftobiprole medocaril. Ceftobiprole is a broad-spectrum agent with demonstrated activity against both Gram-positive and Gram-negative bacteria, including antibiotic-resistant strains of Staphylcoccus aureus (methicillin-resistant Staphylococcus aureus; MRSA).

The EMA's Committee for Medicinal Products for Human Use (CHMP) adopted a negative opinion of ceftobiprole medocaril in February 2010, recommending the refusal of its marketing authorization in the European Union primarily due to data quality issues in pivotal clinical studies.L50467 It received its first approval in Canada in October 2017 for use in certain patients with bacterial pneumonia,L50472 and was subsequently approved in the United States with additional indications for skin and skin structure infections and bacteremia in April 2024.L50442,L50457

Struktur Molekul 2D

Berat 534.57
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half-life of active [ceftobiprole] following multiple-dose administration is approximately 3.3 hours.[L50442,L50472]
Volume Distribusi The steady-state volume of distribution of active [ceftobiprole] is 15.5-18.0 L, which approximates extracellular fluid volume in humans.[L50442,L50472]
Klirens (Clearance) The mean clearance of active [ceftobiprole] following multiple-dose administration is 4.98 L/h.[L50442,L50472]

Absorpsi

Because ceftobiprole medocaril is administered intravenously, its bioavailability is 100%.L50472 The mean Cmax and AUC0-8h of ceftobiprole after multiple-dose administration are 33.0 µg/mL and 102 µg*h/mL, respectively.L50472

Metabolisme

Conversion of prodrug ceftobiprole medocaril to the active moiety ceftobiprole occurs rapidly and is mediated by non-specific plasma esterases.L50472 Ceftobiprole itself is minimally metabolized to a microbiologically inactive open-ring metabolite, which accounts for approximately 4% of the parent exposure in subject with a normal renal function.L50472

Rute Eliminasi

Active ceftobiprole is eliminated primarily unchanged by renal excretion.L50472 Approximately 89% of the administered dose is recovered in the urine as active ceftobiprole (83%), the open-ring metabolite (5%) and ceftobiprole medocaril (<1%).L50472

Interaksi Obat

849 Data
Probenecid The serum concentration of Ceftobiprole can be increased when it is combined with Probenecid.
Foscarnet The risk or severity of nephrotoxicity can be increased when Ceftobiprole is combined with Foscarnet.
Mannitol The risk or severity of nephrotoxicity can be increased when Mannitol is combined with Ceftobiprole.
Tenofovir disoproxil Ceftobiprole may increase the nephrotoxic activities of Tenofovir disoproxil.
Tenofovir alafenamide Ceftobiprole may increase the nephrotoxic activities of Tenofovir alafenamide.
Tenofovir Ceftobiprole may increase the nephrotoxic activities of Tenofovir.
Cyclosporine The risk or severity of nephrotoxicity can be increased when Cyclosporine is combined with Ceftobiprole.
Icosapent The risk or severity of nephrotoxicity can be increased when Icosapent is combined with Ceftobiprole.
Cefotiam The risk or severity of nephrotoxicity can be increased when Cefotiam is combined with Ceftobiprole.
Mesalazine The risk or severity of nephrotoxicity can be increased when Mesalazine is combined with Ceftobiprole.
Cefmenoxime The risk or severity of nephrotoxicity can be increased when Cefmenoxime is combined with Ceftobiprole.
Cefmetazole The risk or severity of nephrotoxicity can be increased when Cefmetazole is combined with Ceftobiprole.
Indomethacin The risk or severity of nephrotoxicity can be increased when Indomethacin is combined with Ceftobiprole.
Triamterene The risk or severity of nephrotoxicity can be increased when Triamterene is combined with Ceftobiprole.
Cefpiramide The risk or severity of nephrotoxicity can be increased when Cefpiramide is combined with Ceftobiprole.
Loracarbef The risk or severity of nephrotoxicity can be increased when Loracarbef is combined with Ceftobiprole.
Cefalotin The risk or severity of nephrotoxicity can be increased when Cefalotin is combined with Ceftobiprole.
Nabumetone The risk or severity of nephrotoxicity can be increased when Nabumetone is combined with Ceftobiprole.
Ketorolac The risk or severity of nephrotoxicity can be increased when Ketorolac is combined with Ceftobiprole.
Tenoxicam The risk or severity of nephrotoxicity can be increased when Tenoxicam is combined with Ceftobiprole.
Celecoxib The risk or severity of nephrotoxicity can be increased when Celecoxib is combined with Ceftobiprole.
Cefotaxime The risk or severity of nephrotoxicity can be increased when Cefotaxime is combined with Ceftobiprole.
Tolmetin The risk or severity of nephrotoxicity can be increased when Tolmetin is combined with Ceftobiprole.
Rofecoxib The risk or severity of nephrotoxicity can be increased when Rofecoxib is combined with Ceftobiprole.
Fenoprofen The risk or severity of nephrotoxicity can be increased when Fenoprofen is combined with Ceftobiprole.
Valdecoxib The risk or severity of nephrotoxicity can be increased when Valdecoxib is combined with Ceftobiprole.
Diclofenac The risk or severity of nephrotoxicity can be increased when Diclofenac is combined with Ceftobiprole.
Sulindac The risk or severity of nephrotoxicity can be increased when Sulindac is combined with Ceftobiprole.
Bacitracin The risk or severity of nephrotoxicity can be increased when Bacitracin is combined with Ceftobiprole.
Amphotericin B The risk or severity of nephrotoxicity can be increased when Amphotericin B is combined with Ceftobiprole.
Cephaloglycin The risk or severity of nephrotoxicity can be increased when Cephaloglycin is combined with Ceftobiprole.
Adefovir dipivoxil The risk or severity of nephrotoxicity can be increased when Adefovir dipivoxil is combined with Ceftobiprole.
Pentamidine The risk or severity of nephrotoxicity can be increased when Pentamidine is combined with Ceftobiprole.
Mefenamic acid The risk or severity of nephrotoxicity can be increased when Mefenamic acid is combined with Ceftobiprole.
Naproxen The risk or severity of nephrotoxicity can be increased when Naproxen is combined with Ceftobiprole.
Sulfasalazine The risk or severity of nephrotoxicity can be increased when Sulfasalazine is combined with Ceftobiprole.
Phenylbutazone The risk or severity of nephrotoxicity can be increased when Phenylbutazone is combined with Ceftobiprole.
Meloxicam The risk or severity of methemoglobinemia can be increased when Ceftobiprole is combined with Meloxicam.
Carprofen The risk or severity of nephrotoxicity can be increased when Carprofen is combined with Ceftobiprole.
Tacrolimus The risk or severity of nephrotoxicity can be increased when Tacrolimus is combined with Ceftobiprole.
Etacrynic acid The risk or severity of nephrotoxicity can be increased when Etacrynic acid is combined with Ceftobiprole.
Ceforanide The risk or severity of nephrotoxicity can be increased when Ceforanide is combined with Ceftobiprole.
Salicylic acid The risk or severity of nephrotoxicity can be increased when Salicylic acid is combined with Ceftobiprole.
Acetylsalicylic acid The risk or severity of nephrotoxicity can be increased when Acetylsalicylic acid is combined with Ceftobiprole.
Hydrochlorothiazide The risk or severity of nephrotoxicity can be increased when Hydrochlorothiazide is combined with Ceftobiprole.
Balsalazide The risk or severity of nephrotoxicity can be increased when Balsalazide is combined with Ceftobiprole.
Cefditoren The risk or severity of nephrotoxicity can be increased when Cefditoren is combined with Ceftobiprole.
Atazanavir The risk or severity of nephrotoxicity can be increased when Atazanavir is combined with Ceftobiprole.
Colistimethate The risk or severity of nephrotoxicity can be increased when Colistimethate is combined with Ceftobiprole.
Cefuroxime The risk or severity of nephrotoxicity can be increased when Cefuroxime is combined with Ceftobiprole.
Cefapirin The risk or severity of nephrotoxicity can be increased when Cefapirin is combined with Ceftobiprole.
Cefprozil The risk or severity of nephrotoxicity can be increased when Cefprozil is combined with Ceftobiprole.
Olsalazine The risk or severity of nephrotoxicity can be increased when Ceftobiprole is combined with Olsalazine.
Lumiracoxib The risk or severity of nephrotoxicity can be increased when Lumiracoxib is combined with Ceftobiprole.
Cefamandole The risk or severity of nephrotoxicity can be increased when Cefamandole is combined with Ceftobiprole.
Cefazolin The risk or severity of nephrotoxicity can be increased when Cefazolin is combined with Ceftobiprole.
Cefonicid The risk or severity of nephrotoxicity can be increased when Cefonicid is combined with Ceftobiprole.
Cefoperazone The risk or severity of nephrotoxicity can be increased when Cefoperazone is combined with Ceftobiprole.
Cefoxitin The risk or severity of nephrotoxicity can be increased when Cefoxitin is combined with Ceftobiprole.
Ceftizoxime The risk or severity of nephrotoxicity can be increased when Ceftizoxime is combined with Ceftobiprole.
Magnesium salicylate The risk or severity of nephrotoxicity can be increased when Magnesium salicylate is combined with Ceftobiprole.
Salsalate The risk or severity of nephrotoxicity can be increased when Salsalate is combined with Ceftobiprole.
Choline magnesium trisalicylate The risk or severity of nephrotoxicity can be increased when Choline magnesium trisalicylate is combined with Ceftobiprole.
Cefepime The risk or severity of nephrotoxicity can be increased when Cefepime is combined with Ceftobiprole.
Cefacetrile The risk or severity of nephrotoxicity can be increased when Cefacetrile is combined with Ceftobiprole.
Cefpodoxime The risk or severity of nephrotoxicity can be increased when Cefpodoxime is combined with Ceftobiprole.
Antrafenine The risk or severity of nephrotoxicity can be increased when Antrafenine is combined with Ceftobiprole.
Aminophenazone The risk or severity of nephrotoxicity can be increased when Aminophenazone is combined with Ceftobiprole.
Antipyrine The risk or severity of nephrotoxicity can be increased when Antipyrine is combined with Ceftobiprole.
Tiaprofenic acid The risk or severity of nephrotoxicity can be increased when Tiaprofenic acid is combined with Ceftobiprole.
Lopinavir The risk or severity of nephrotoxicity can be increased when Lopinavir is combined with Ceftobiprole.
Etoricoxib The risk or severity of nephrotoxicity can be increased when Etoricoxib is combined with Ceftobiprole.
Hydrolyzed Cephalothin The risk or severity of nephrotoxicity can be increased when Hydrolyzed Cephalothin is combined with Ceftobiprole.
Cephalothin Group The risk or severity of nephrotoxicity can be increased when Cephalothin Group is combined with Ceftobiprole.
Oxyphenbutazone The risk or severity of nephrotoxicity can be increased when Oxyphenbutazone is combined with Ceftobiprole.
Latamoxef The risk or severity of nephrotoxicity can be increased when Latamoxef is combined with Ceftobiprole.
Nimesulide The risk or severity of nephrotoxicity can be increased when Nimesulide is combined with Ceftobiprole.
Benoxaprofen The risk or severity of nephrotoxicity can be increased when Benoxaprofen is combined with Ceftobiprole.
Metamizole The risk or severity of nephrotoxicity can be increased when Metamizole is combined with Ceftobiprole.
Zomepirac The risk or severity of nephrotoxicity can be increased when Zomepirac is combined with Ceftobiprole.
Cimicoxib The risk or severity of nephrotoxicity can be increased when Ceftobiprole is combined with Cimicoxib.
Ceftaroline fosamil The risk or severity of nephrotoxicity can be increased when Ceftobiprole is combined with Ceftaroline fosamil.
Lornoxicam The risk or severity of nephrotoxicity can be increased when Ceftobiprole is combined with Lornoxicam.
Zaltoprofen The risk or severity of nephrotoxicity can be increased when Ceftobiprole is combined with Zaltoprofen.
Azapropazone The risk or severity of nephrotoxicity can be increased when Ceftobiprole is combined with Azapropazone.
Parecoxib The risk or severity of nephrotoxicity can be increased when Ceftobiprole is combined with Parecoxib.
Salicylamide The risk or severity of nephrotoxicity can be increased when Ceftobiprole is combined with Salicylamide.
Kebuzone The risk or severity of nephrotoxicity can be increased when Ceftobiprole is combined with Kebuzone.
Isoxicam The risk or severity of nephrotoxicity can be increased when Ceftobiprole is combined with Isoxicam.
Indoprofen The risk or severity of nephrotoxicity can be increased when Ceftobiprole is combined with Indoprofen.
Ibuproxam The risk or severity of nephrotoxicity can be increased when Ceftobiprole is combined with Ibuproxam.
Floctafenine The risk or severity of nephrotoxicity can be increased when Ceftobiprole is combined with Floctafenine.
Fenbufen The risk or severity of nephrotoxicity can be increased when Ceftobiprole is combined with Fenbufen.
Etofenamate The risk or severity of nephrotoxicity can be increased when Ceftobiprole is combined with Etofenamate.
Epirizole The risk or severity of nephrotoxicity can be increased when Ceftobiprole is combined with Epirizole.
Cefaloridine The risk or severity of nephrotoxicity can be increased when Ceftobiprole is combined with Cefaloridine.
Cefminox The risk or severity of nephrotoxicity can be increased when Ceftobiprole is combined with Cefminox.
Dexibuprofen The risk or severity of nephrotoxicity can be increased when Ceftobiprole is combined with Dexibuprofen.
Droxicam The risk or severity of nephrotoxicity can be increased when Ceftobiprole is combined with Droxicam.
Tolfenamic acid The risk or severity of nephrotoxicity can be increased when Ceftobiprole is combined with Tolfenamic acid.

Target Protein

MecA mecA
Penicillin-binding protein 2x pbpX
Penicillin-binding protein 2B penA
Penicillin-binding protein 2X pbpX
Peptidoglycan synthase FtsI ftsI

Referensi & Sumber

Artikel (PubMed)
  • PMID: 17470659
    Davies TA, Page MG, Shang W, Andrew T, Kania M, Bush K: Binding of ceftobiprole and comparators to the penicillin-binding proteins of Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, and Streptococcus pneumoniae. Antimicrob Agents Chemother. 2007 Jul;51(7):2621-4. Epub 2007 Apr 30.
  • PMID: 17488373
    Noel GJ: Clinical profile of ceftobiprole, a novel beta-lactam antibiotic. Clin Microbiol Infect. 2007 Jun;13 Suppl 2:25-9.
  • PMID: 17911001
    Yun HC, Ellis MW, Jorgensen JH: Activity of ceftobiprole against community-associated methicillin-resistant Staphylococcus aureus isolates recently recovered from US military trainees. Diagn Microbiol Infect Dis. 2007 Dec;59(4):463-6. Epub 2007 Oct 29.
  • PMID: 17997257
    Lin G, Appelbaum PC: Activity of ceftobiprole compared with those of other agents against Staphylococcus aureus strains with different resistotypes by time-kill analysis. Diagn Microbiol Infect Dis. 2008 Feb;60(2):233-5. Epub 2007 Nov 7.
  • PMID: 17954698
    Noel GJ, Strauss RS, Amsler K, Heep M, Pypstra R, Solomkin JS: Results of a double-blind, randomized trial of ceftobiprole treatment of complicated skin and skin structure infections caused by gram-positive bacteria. Antimicrob Agents Chemother. 2008 Jan;52(1):37-44. Epub 2007 Oct 22.

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