Peringatan Keamanan

Avycaz is contraindicated in patients with known serious hypersensitivity to avibactam-containing products, ceftazidime or other members of the cephalosporin class.

Avibactam

DB09060

small molecule approved

Deskripsi

Avibactam is a non-?-lactam ?-lactamase inhibitor that is available in combination with ceftazidime (Avycaz). This combination was approved by the FDA on February 25, 2015 for the treatment of complicated intra-abdominal infections in combination with metronidazole, and the treatment of complicated urinary tract infections, including pyelonephritis caused by antibiotic resistant-pathogens, including those caused by multi-drug resistant gram-negative bacterial pathogens. As there is limited clinical safety and efficacy data, Avycaz should be reserved for patients over 18 years old who have limited or not alternative treatment options.

Struktur Molekul 2D

Berat 265.24
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Ceftazidime-avibactam has a half life of ~2.7-3.0 hours.
Volume Distribusi The steady state volumes of distribution of avibactam and ceftazidime is 22.2L and 17L respectively.
Klirens (Clearance) Avibactam and ceftazidime has a clearance of ~12L/h and ~7L/h respectively.

Absorpsi

Data absorpsi tidak tersedia.

Metabolisme

No metabolism of avibactam was observed in human liver preparations. Unchanged avibactam is the major drug-related component in human plasma and urine. 80-90% of ceftazidime is eliminated as unchanged .

Rute Eliminasi

Avibactam and ceftazidime are excreted mainly by the kidneys.

Interaksi Obat

88 Data
Aspartame The excretion of Avibactam can be decreased when combined with Aspartame.
Pravastatin The excretion of Avibactam can be decreased when combined with Pravastatin.
Pantoprazole The excretion of Avibactam can be decreased when combined with Pantoprazole.
Cefotiam The excretion of Avibactam can be decreased when combined with Cefotiam.
Liothyronine The excretion of Avibactam can be decreased when combined with Liothyronine.
Conjugated estrogens The excretion of Avibactam can be decreased when combined with Conjugated estrogens.
Valproic acid The excretion of Avibactam can be decreased when combined with Valproic acid.
Indomethacin The excretion of Avibactam can be decreased when combined with Indomethacin.
Aminohippuric acid The excretion of Avibactam can be decreased when combined with Aminohippuric acid.
Lansoprazole The excretion of Avibactam can be decreased when combined with Lansoprazole.
Cefalotin The excretion of Avibactam can be decreased when combined with Cefalotin.
Tenoxicam The excretion of Avibactam can be decreased when combined with Tenoxicam.
Cefotaxime The excretion of Avibactam can be decreased when combined with Cefotaxime.
Zidovudine The excretion of Avibactam can be decreased when combined with Zidovudine.
Cimetidine The excretion of Avibactam can be decreased when combined with Cimetidine.
Guanidine The excretion of Avibactam can be decreased when combined with Guanidine.
Piroxicam The excretion of Avibactam can be decreased when combined with Piroxicam.
Methotrexate The excretion of Avibactam can be decreased when combined with Methotrexate.
Cephalexin The excretion of Avibactam can be decreased when combined with Cephalexin.
Enalapril The excretion of Avibactam can be decreased when combined with Enalapril.
Diclofenac The excretion of Avibactam can be decreased when combined with Diclofenac.
Oxytetracycline The excretion of Avibactam can be decreased when combined with Oxytetracycline.
Leucovorin The excretion of Avibactam can be decreased when combined with Leucovorin.
Furosemide The excretion of Avibactam can be decreased when combined with Furosemide.
Esomeprazole The excretion of Avibactam can be decreased when combined with Esomeprazole.
Tetracycline The excretion of Avibactam can be decreased when combined with Tetracycline.
Acyclovir The excretion of Avibactam can be decreased when combined with Acyclovir.
Phenylbutazone The excretion of Avibactam can be decreased when combined with Phenylbutazone.
Cefaclor The excretion of Avibactam can be decreased when combined with Cefaclor.
Bumetanide The excretion of Avibactam can be decreased when combined with Bumetanide.
Quinidine The excretion of Avibactam can be decreased when combined with Quinidine.
Dinoprostone The excretion of Avibactam can be decreased when combined with Dinoprostone.
Famotidine The excretion of Avibactam can be decreased when combined with Famotidine.
Salicylic acid The excretion of Avibactam can be decreased when combined with Salicylic acid.
Acetylsalicylic acid The excretion of Avibactam can be decreased when combined with Acetylsalicylic acid.
Ganciclovir The excretion of Avibactam can be decreased when combined with Ganciclovir.
Ketoprofen The excretion of Avibactam can be decreased when combined with Ketoprofen.
Minocycline The excretion of Avibactam can be decreased when combined with Minocycline.
Probenecid The excretion of Avibactam can be decreased when combined with Probenecid.
Mercaptopurine The excretion of Avibactam can be decreased when combined with Mercaptopurine.
Ibuprofen The excretion of Avibactam can be decreased when combined with Ibuprofen.
Novobiocin The excretion of Avibactam can be decreased when combined with Novobiocin.
Benzylpenicillin The excretion of Avibactam can be decreased when combined with Benzylpenicillin.
Melatonin The excretion of Avibactam can be decreased when combined with Melatonin.
Ouabain The excretion of Avibactam can be decreased when combined with Ouabain.
Rosuvastatin The excretion of Avibactam can be decreased when combined with Rosuvastatin.
Cefadroxil The excretion of Avibactam can be decreased when combined with Cefadroxil.
Ceftriaxone The excretion of Avibactam can be decreased when combined with Ceftriaxone.
Cefamandole The excretion of Avibactam can be decreased when combined with Cefamandole.
Cefazolin The excretion of Avibactam can be decreased when combined with Cefazolin.
Cefoperazone The excretion of Avibactam can be decreased when combined with Cefoperazone.
Ceftizoxime The excretion of Avibactam can be decreased when combined with Ceftizoxime.
Cefacetrile The excretion of Avibactam can be decreased when combined with Cefacetrile.
Ceftibuten The excretion of Avibactam can be decreased when combined with Ceftibuten.
Liotrix The excretion of Avibactam can be decreased when combined with Liotrix.
Cilastatin The excretion of Avibactam can be decreased when combined with Cilastatin.
Tazobactam The excretion of Avibactam can be decreased when combined with Tazobactam.
trans-2-hydroxycinnamic acid The excretion of Avibactam can be decreased when combined with trans-2-hydroxycinnamic acid.
Topiroxostat The excretion of Avibactam can be decreased when combined with Topiroxostat.
Cholic Acid The excretion of Avibactam can be decreased when combined with Cholic Acid.
Glutaric Acid The excretion of Avibactam can be decreased when combined with Glutaric Acid.
Benzoic acid The excretion of Avibactam can be decreased when combined with Benzoic acid.
Taurocholic acid The excretion of Avibactam can be decreased when combined with Taurocholic acid.
Caprylic acid The excretion of Avibactam can be decreased when combined with Caprylic acid.
Ataluren The excretion of Avibactam can be decreased when combined with Ataluren.
Teriflunomide The excretion of Avibactam can be decreased when combined with Teriflunomide.
Dabrafenib The excretion of Avibactam can be decreased when combined with Dabrafenib.
Dolutegravir The excretion of Avibactam can be decreased when combined with Dolutegravir.
Cefaloridine The excretion of Avibactam can be decreased when combined with Cefaloridine.
Lenvatinib The excretion of Avibactam can be decreased when combined with Lenvatinib.
Cabotegravir The excretion of Avibactam can be decreased when combined with Cabotegravir.
Apalutamide The excretion of Avibactam can be decreased when combined with Apalutamide.
Pradigastat The excretion of Avibactam can be decreased when combined with Pradigastat.
Enasidenib The excretion of Avibactam can be decreased when combined with Enasidenib.
Gemfibrozil The excretion of Avibactam can be decreased when combined with Gemfibrozil.
Dronedarone The excretion of Avibactam can be decreased when combined with Dronedarone.
Favipiravir The excretion of Avibactam can be decreased when combined with Favipiravir.
Tafamidis The excretion of Avibactam can be decreased when combined with Tafamidis.
Linezolid The excretion of Avibactam can be decreased when combined with Linezolid.
Testosterone The excretion of Avibactam can be increased when combined with Testosterone.
Methyltestosterone The excretion of Avibactam can be increased when combined with Methyltestosterone.
Testosterone cypionate The excretion of Avibactam can be increased when combined with Testosterone cypionate.
Testosterone enanthate The excretion of Avibactam can be increased when combined with Testosterone enanthate.
Fexinidazole The excretion of Avibactam can be decreased when combined with Fexinidazole.
Pretomanid The serum concentration of Avibactam can be increased when it is combined with Pretomanid.
Vadadustat The serum concentration of Avibactam can be increased when it is combined with Vadadustat.
Capivasertib The excretion of Avibactam can be decreased when combined with Capivasertib.
Encorafenib The excretion of Avibactam can be decreased when combined with Encorafenib.

Target Protein

Beta-lactamase TEM bla
Beta-lactamase CTX-M
Beta-lactamase ampC
Beta-lactamase SHV-1 bla
Beta-lactamase SHV-2 bla
Beta-lactamase SHV-1 bla
Class D OXA-48 carbapenemase OXA-48
Carbapenem-hydrolyzing beta-lactamase KPC bla
Beta-lactamase UOE-1 blaUOE-1
Extended-spectrum beta-lactamase PER-1 per1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 19493866
    Stachyra T, Levasseur P, Pechereau MC, Girard AM, Claudon M, Miossec C, Black MT: In vitro activity of the {beta}-lactamase inhibitor NXL104 against KPC-2 carbapenemase and Enterobacteriaceae expressing KPC carbapenemases. J Antimicrob Chemother. 2009 Aug;64(2):326-9. doi: 10.1093/jac/dkp197. Epub 2009 Jun 2.
  • PMID: 26516584
    Das S, Li J, Armstrong J, Learoyd M, Edeki T: Randomized pharmacokinetic and drug-drug interaction studies of ceftazidime, avibactam, and metronidazole in healthy subjects. Pharmacol Res Perspect. 2015 Oct;3(5):e00172. doi: 10.1002/prp2.172. Epub 2015 Aug 25.
  • PMID: 25223999
    MacVane SH, Crandon JL, Nichols WW, Nicolau DP: In vivo efficacy of humanized exposures of Ceftazidime-Avibactam in comparison with Ceftazidime against contemporary Enterobacteriaceae isolates. Antimicrob Agents Chemother. 2014 Nov;58(11):6913-9. doi: 10.1128/AAC.03267-14. Epub 2014 Sep 15.
  • PMID: 26666933
    Pages JM, Peslier S, Keating TA, Lavigne JP, Nichols WW: Role of the Outer Membrane and Porins in Susceptibility of beta-Lactamase-Producing Enterobacteriaceae to Ceftazidime-Avibactam. Antimicrob Agents Chemother. 2015 Dec 14;60(3):1349-59. doi: 10.1128/AAC.01585-15.
  • PMID: 22753474
    Ehmann DE, Jahic H, Ross PL, Gu RF, Hu J, Kern G, Walkup GK, Fisher SL: Avibactam is a covalent, reversible, non-beta-lactam beta-lactamase inhibitor. Proc Natl Acad Sci U S A. 2012 Jul 17;109(29):11663-8. doi: 10.1073/pnas.1205073109. Epub 2012 Jul 2.
  • PMID: 23913691
    Ehmann DE, Jahic H, Ross PL, Gu RF, Hu J, Durand-Reville TF, Lahiri S, Thresher J, Livchak S, Gao N, Palmer T, Walkup GK, Fisher SL: Kinetics of avibactam inhibition against Class A, C, and D beta-lactamases. J Biol Chem. 2013 Sep 27;288(39):27960-71. doi: 10.1074/jbc.M113.485979. Epub 2013 Aug 2.
  • PMID: 22041508
    Aktas Z, Kayacan C, Oncul O: In vitro activity of avibactam (NXL104) in combination with beta-lactams against Gram-negative bacteria, including OXA-48 beta-lactamase-producing Klebsiella pneumoniae. Int J Antimicrob Agents. 2012 Jan;39(1):86-9. doi: 10.1016/j.ijantimicag.2011.09.012. Epub 2011 Oct 29.

Contoh Produk & Brand

Produk: 3 • International brands: 0
Produk
  • Avycaz
    Powder, for solution • - • Intravenous • US • Approved
  • Emblaveo
    Injection, powder, for solution • - • Intravenous • EU • Approved
  • Zavicefta
    Injection, powder, for solution • - • Intravenous • EU • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul