Peringatan Keamanan

Ceftriaxone overdose may increase the risk of urolithiasis and subsequent post-renal acute renal failure (PARF).A215637 Other symptoms of overdose unavailable in the literature. However, they are likely similar to the adverse effects of the medication. If overdose of ceftriaxone occurs, treat with symptomatic and supportive treatment, as ceftriaxone levels will not be reduced by dialysis.L15082

Ceftriaxone

DB01212

small molecule approved

Deskripsi

Ceftriaxone is a broad-spectrum third-generation cephalosporin antibiotic.A215582 It has a very long half-life compared to other cephalosporins and is high penetrable into the meningesA215582, eyesA215647, and inner earA215627. Ceftriaxone has broader and stronger gram-negative coverage then first or second-generation cephalosporins, but worse activity against methicillin-susceptible S.aureus. Ceftriaxone is a commonly used antimicrobial due to its good activity against multi-drug resistant Enterobacteriaceae, its relatively safe adverse effect profile, and its long half-life which allows for the convenience of daily or twice-daily dosing.A215582

Struktur Molekul 2D

Berat 554.58
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half-life of ceftriaxone is 5.8-8.7 hours.[L15082] The half-life of ceftriaxone in the middle ear fluid has been estimated to be 25 hours.[L15082,A215627]
Volume Distribusi The apparent volume of distribution of an intravenous or intramuscular dose in healthy patients is 5.78 to 13.5 L.[L15082] The volume of distribution of an intravenous or intramuscular dose in septic patients is 6.48 to 35.2 L.[A215617] Ceftriaxone has good enough CSF penetration to be used as an effective treatment of bacterial meningitis.[A215622]
Klirens (Clearance) The plasma clearance of ceftriaxone in healthy adults receiving a 0.15-3g dose is 0.58 to 1.45 L/hour.[L15082] The renal clearance of ceftriaxone is 0.32 to 0.73 L/hour.[L15082] In intensive care unit patients, ceftriaxone's total drug clearance was 0.96L/h (0.55-1.28 L/h), and unbound drug clearance was 1.91 L/h (1.46-6.20 L/h).[A215632]

Absorpsi

Ceftriaxone is only given as an injection, either intramuscularly or intravenously.L15082 Ceftriaxone is less than 1% bioavailable if given orally.A215607

Metabolisme

Metabolism of ceftriaxone is negligible.

Rute Eliminasi

Ceftriaxone is primarily eliminated in the urine (33-67%).L15082 The remainder is eliminated through secretion in the bile and removed from the body via the feces.

Interaksi Obat

892 Data
Calcium acetate The risk or severity of adverse effects can be increased when Calcium acetate is combined with Ceftriaxone.
Calcium glucoheptonate The risk or severity of adverse effects can be increased when Calcium glucoheptonate is combined with Ceftriaxone.
Calcium gluconate The risk or severity of adverse effects can be increased when Calcium gluconate is combined with Ceftriaxone.
Calcium glubionate anhydrous The risk or severity of adverse effects can be increased when Calcium glubionate anhydrous is combined with Ceftriaxone.
Calcium pangamate The risk or severity of adverse effects can be increased when Calcium pangamate is combined with Ceftriaxone.
Calcium levulinate The risk or severity of adverse effects can be increased when Calcium levulinate is combined with Ceftriaxone.
Calcium cation The risk or severity of adverse effects can be increased when Calcium cation is combined with Ceftriaxone.
Calcium The risk or severity of adverse effects can be increased when Calcium is combined with Ceftriaxone.
Probenecid The serum concentration of Ceftriaxone can be increased when it is combined with Probenecid.
Foscarnet The risk or severity of nephrotoxicity can be increased when Ceftriaxone is combined with Foscarnet.
Mannitol The risk or severity of nephrotoxicity can be increased when Mannitol is combined with Ceftriaxone.
Tenofovir disoproxil Ceftriaxone may increase the nephrotoxic activities of Tenofovir disoproxil.
Tenofovir alafenamide The serum concentration of Tenofovir alafenamide can be increased when it is combined with Ceftriaxone.
Tenofovir Ceftriaxone may increase the nephrotoxic activities of Tenofovir.
Succinic acid The excretion of Succinic acid can be decreased when combined with Ceftriaxone.
Citrulline The excretion of Citrulline can be decreased when combined with Ceftriaxone.
Aminohippuric acid The excretion of Aminohippuric acid can be decreased when combined with Ceftriaxone.
Cefdinir The excretion of Cefdinir can be decreased when combined with Ceftriaxone.
Leucovorin The excretion of Leucovorin can be decreased when combined with Ceftriaxone.
Fluorescein The excretion of Fluorescein can be decreased when combined with Ceftriaxone.
Quinapril The excretion of Quinapril can be decreased when combined with Ceftriaxone.
Dinoprostone The excretion of Dinoprostone can be decreased when combined with Ceftriaxone.
Famotidine The excretion of Famotidine can be decreased when combined with Ceftriaxone.
Benzylpenicillin The excretion of Benzylpenicillin can be decreased when combined with Ceftriaxone.
Rosuvastatin The excretion of Rosuvastatin can be decreased when combined with Ceftriaxone.
Captopril The excretion of Captopril can be decreased when combined with Ceftriaxone.
Tazobactam The excretion of Tazobactam can be decreased when combined with Ceftriaxone.
Cyclic adenosine monophosphate The excretion of Cyclic adenosine monophosphate can be decreased when combined with Ceftriaxone.
Cholic Acid The excretion of Cholic Acid can be decreased when combined with Ceftriaxone.
Glutaric Acid The excretion of Glutaric Acid can be decreased when combined with Ceftriaxone.
Oxalic Acid The excretion of Oxalic Acid can be decreased when combined with Ceftriaxone.
Ellagic acid The excretion of Ellagic acid can be decreased when combined with Ceftriaxone.
Avibactam The excretion of Avibactam can be decreased when combined with Ceftriaxone.
Eluxadoline The excretion of Eluxadoline can be decreased when combined with Ceftriaxone.
Silibinin The excretion of Silibinin can be decreased when combined with Ceftriaxone.
Relebactam The excretion of Relebactam can be decreased when combined with Ceftriaxone.
Cefotiam The excretion of Cefotiam can be decreased when combined with Ceftriaxone.
Cephalexin The excretion of Cephalexin can be decreased when combined with Ceftriaxone.
Valaciclovir The excretion of Valaciclovir can be decreased when combined with Ceftriaxone.
Acyclovir The excretion of Acyclovir can be decreased when combined with Ceftriaxone.
Cefaclor The excretion of Cefaclor can be decreased when combined with Ceftriaxone.
Bumetanide The excretion of Bumetanide can be decreased when combined with Ceftriaxone.
Oseltamivir The excretion of Oseltamivir can be decreased when combined with Ceftriaxone.
Piperacillin The excretion of Piperacillin can be decreased when combined with Ceftriaxone.
Trifluridine The excretion of Trifluridine can be decreased when combined with Ceftriaxone.
Allopurinol The excretion of Allopurinol can be decreased when combined with Ceftriaxone.
Levocarnitine The excretion of Levocarnitine can be decreased when combined with Ceftriaxone.
Ceftibuten The excretion of Ceftibuten can be decreased when combined with Ceftriaxone.
Doripenem The excretion of Doripenem can be decreased when combined with Ceftriaxone.
Saxagliptin The excretion of Saxagliptin can be decreased when combined with Ceftriaxone.
Cefazolin The excretion of Cefazolin can be decreased when combined with Ceftriaxone.
Ceftizoxime The excretion of Ceftizoxime can be decreased when combined with Ceftriaxone.
Cefacetrile The excretion of Cefacetrile can be decreased when combined with Ceftriaxone.
Cefaloridine The excretion of Cefaloridine can be decreased when combined with Ceftriaxone.
Conjugated estrogens The excretion of Conjugated estrogens can be decreased when combined with Ceftriaxone.
Indomethacin The excretion of Indomethacin can be decreased when combined with Ceftriaxone.
Zidovudine The excretion of Zidovudine can be decreased when combined with Ceftriaxone.
Cimetidine The excretion of Cimetidine can be decreased when combined with Ceftriaxone.
Methotrexate The excretion of Methotrexate can be decreased when combined with Ceftriaxone.
Hydrocortisone The excretion of Hydrocortisone can be decreased when combined with Ceftriaxone.
Tetracycline The excretion of Tetracycline can be decreased when combined with Ceftriaxone.
Estradiol The excretion of Estradiol can be decreased when combined with Ceftriaxone.
Ranitidine The excretion of Ranitidine can be decreased when combined with Ceftriaxone.
Dexamethasone The excretion of Dexamethasone can be decreased when combined with Ceftriaxone.
Pravastatin The excretion of Pravastatin can be decreased when combined with Ceftriaxone.
Fexofenadine The excretion of Fexofenadine can be decreased when combined with Ceftriaxone.
Sitagliptin The excretion of Sitagliptin can be decreased when combined with Ceftriaxone.
Taurocholic acid The excretion of Taurocholic acid can be decreased when combined with Ceftriaxone.
Baricitinib The serum concentration of Baricitinib can be increased when it is combined with Ceftriaxone.
Oxytetracycline The excretion of Oxytetracycline can be decreased when combined with Ceftriaxone.
Prednisolone phosphate The excretion of Prednisolone phosphate can be decreased when combined with Ceftriaxone.
Dexamethasone acetate The excretion of Dexamethasone acetate can be decreased when combined with Ceftriaxone.
Acamprosate The excretion of Acamprosate can be decreased when combined with Ceftriaxone.
Triamterene The risk or severity of nephrotoxicity can be increased when Triamterene is combined with Ceftriaxone.
Etacrynic acid The risk or severity of nephrotoxicity can be increased when Etacrynic acid is combined with Ceftriaxone.
Hydrochlorothiazide The excretion of Hydrochlorothiazide can be decreased when combined with Ceftriaxone.
Icosapent The risk or severity of nephrotoxicity can be increased when Icosapent is combined with Ceftriaxone.
Mesalazine The risk or severity of nephrotoxicity can be increased when Mesalazine is combined with Ceftriaxone.
Cefmenoxime The risk or severity of nephrotoxicity can be increased when Cefmenoxime is combined with Ceftriaxone.
Cefmetazole The risk or severity of nephrotoxicity can be increased when Cefmetazole is combined with Ceftriaxone.
Cidofovir The risk or severity of nephrotoxicity can be increased when Cidofovir is combined with Ceftriaxone.
Cefpiramide The risk or severity of nephrotoxicity can be increased when Cefpiramide is combined with Ceftriaxone.
Ceftazidime The risk or severity of nephrotoxicity can be increased when Ceftazidime is combined with Ceftriaxone.
Loracarbef The risk or severity of nephrotoxicity can be increased when Loracarbef is combined with Ceftriaxone.
Cefalotin The risk or severity of nephrotoxicity can be increased when Cefalotin is combined with Ceftriaxone.
Nabumetone The risk or severity of nephrotoxicity can be increased when Nabumetone is combined with Ceftriaxone.
Ketorolac The risk or severity of nephrotoxicity can be increased when Ketorolac is combined with Ceftriaxone.
Tenoxicam The risk or severity of nephrotoxicity can be increased when Tenoxicam is combined with Ceftriaxone.
Celecoxib The risk or severity of nephrotoxicity can be increased when Celecoxib is combined with Ceftriaxone.
Cefotaxime The risk or severity of nephrotoxicity can be increased when Cefotaxime is combined with Ceftriaxone.
Tolmetin The risk or severity of nephrotoxicity can be increased when Tolmetin is combined with Ceftriaxone.
Rofecoxib The risk or severity of nephrotoxicity can be increased when Rofecoxib is combined with Ceftriaxone.
Piroxicam The risk or severity of nephrotoxicity can be increased when Piroxicam is combined with Ceftriaxone.
Fenoprofen The risk or severity of nephrotoxicity can be increased when Fenoprofen is combined with Ceftriaxone.
Valdecoxib The risk or severity of nephrotoxicity can be increased when Valdecoxib is combined with Ceftriaxone.
Diclofenac The risk or severity of nephrotoxicity can be increased when Diclofenac is combined with Ceftriaxone.
Sulindac The risk or severity of nephrotoxicity can be increased when Sulindac is combined with Ceftriaxone.
Bacitracin The risk or severity of nephrotoxicity can be increased when Bacitracin is combined with Ceftriaxone.
Amphotericin B The risk or severity of nephrotoxicity can be increased when Amphotericin B is combined with Ceftriaxone.
Cephaloglycin The risk or severity of nephrotoxicity can be increased when Cephaloglycin is combined with Ceftriaxone.

Target Protein

Penicillin-binding protein 2B penA
Solute carrier family 22 member 11 SLC22A11
Solute carrier family 22 member 6 SLC22A6
Organic anion transporter 3 SLC22A8
Solute carrier family 15 member 1 SLC15A1

Referensi & Sumber

Synthesis reference: Monguzzi Riccardo, Menaspace Silvano, Anzaghi Piergiorgio, "Process for the preparation of ceftriaxone." U.S. Patent US5026843, issued November, 1984.
Artikel (PubMed)
  • PMID: 6329638
    Richards DM, Heel RC, Brogden RN, Speight TM, Avery GS: Ceftriaxone. A review of its antibacterial activity, pharmacological properties and therapeutic use. Drugs. 1984 Jun;27(6):469-527. doi: 10.2165/00003495-198427060-00001.
  • PMID: 2019372
    Park HZ, Lee SP, Schy AL: Ceftriaxone-associated gallbladder sludge. Identification of calcium-ceftriaxone salt as a major component of gallbladder precipitate. Gastroenterology. 1991 Jun;100(6):1665-70. doi: 10.1016/0016-5085(91)90667-a.
  • PMID: 16641464
    Lee S, Kim SK, Lee DY, Chae SY, Byun Y: Pharmacokinetics of a new, orally available ceftriaxone formulation in physical complexation with a cationic analogue of bile acid in rats. Antimicrob Agents Chemother. 2006 May;50(5):1869-71. doi: 10.1128/AAC.50.5.1869-1871.2006.
  • PMID: 21545483
    Garot D, Respaud R, Lanotte P, Simon N, Mercier E, Ehrmann S, Perrotin D, Dequin PF, Le Guellec C: Population pharmacokinetics of ceftriaxone in critically ill septic patients: a reappraisal. Br J Clin Pharmacol. 2011 Nov;72(5):758-67. doi: 10.1111/j.1365-2125.2011.04005.x.
  • PMID: 8586029
    Rockowitz J, Tunkel AR: Bacterial meningitis. Practical guidelines for management. Drugs. 1995 Nov;50(5):838-53. doi: 10.2165/00003495-199550050-00005.
  • PMID: 9535262
    Gudnason T, Gudbrandsson F, Barsanti F, Kristinsson KG: Penetration of ceftriaxone into the middle ear fluid of children. Pediatr Infect Dis J. 1998 Mar;17(3):258-60. doi: 10.1097/00006454-199803000-00022.
  • PMID: 25808018
    Schleibinger M, Steinbach CL, Topper C, Kratzer A, Liebchen U, Kees F, Salzberger B, Kees MG: Protein binding characteristics and pharmacokinetics of ceftriaxone in intensive care unit patients. Br J Clin Pharmacol. 2015 Sep;80(3):525-33. doi: 10.1111/bcp.12636. Epub 2015 Jun 11.
  • PMID: 26913690
    Shen-Hua W, Fan-Yi M, Qing-Ling Z, Li-Na Z, Li-Jun M: Ceftriaxone-associated renal toxicity in adults: a case report and recommendations for the management of such cases. J Clin Pharm Ther. 2016 Jun;41(3):348-350. doi: 10.1111/jcpt.12358. Epub 2016 Feb 23.
Menampilkan 8 dari 9 artikel.
Textbook
  • Sivapalasingam S., Steigbigel N. (2015). Mandell, Douglas and Bennett's Principles and practice of infectious diseases (8th ed.). Elsevier.

Contoh Produk & Brand

Produk: 257 • International brands: 3
Produk
  • Ceftriaxone
    Injection, powder, for solution • 10 g/1 • Intravenous • US • Generic • Approved
  • Ceftriaxone
    Injection, powder, for solution • 250 mg/1 • Intramuscular; Intravenous • US • Generic • Approved
  • Ceftriaxone
    Injection, powder, for solution • 500 mg/1 • Intramuscular; Intravenous • US • Generic • Approved
  • Ceftriaxone
    Injection, powder, for solution • 250 mg/1 • Intramuscular; Intravenous • US • Generic • Approved
  • Ceftriaxone
    Injection, powder, for solution • 500 mg/1 • Intramuscular; Intravenous • US • Generic • Approved
  • Ceftriaxone
    Injection, powder, for solution • 1 g/1 • Intramuscular; Intravenous • US • Generic • Approved
  • Ceftriaxone
    Injection, powder, for solution • 2 g/1 • Intramuscular; Intravenous • US • Generic • Approved
  • Ceftriaxone
    Injection, powder, for solution • 250 mg/1 • Intramuscular; Intravenous • US • Generic • Approved
Menampilkan 8 dari 257 produk.
International Brands
  • Acantex — Roche
  • Biotrakson — Bioton
  • Rocephine — Roche

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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