Peringatan Keamanan

If overdose with the combination product which includes relebactam, imipenem and cilastatin occurs, the drug should be stopped immediately and the patient should be provided with supportive care.label Relebactam, imipenem, and cilastatin may be removed via hemodialysis; however, the use of hemodialysis to manage cases of overdose has not been studied.label

Relebactam

DB12377

small molecule approved investigational

Deskripsi

Relebactam is a diazabicyclooctane beta-lactamase inhibitor, similar in structure to avibactam.A181195,A181207 It includes a piperidine ring which reduces export from bacterial cells by producing a positive charge.A181207 It is currently available in a combination product which includes imipenem and cilastatin to treat complicated urinary tract infections (UTIs), pyelonephritis, and complicated intra-abdominal infections in adults.label It is considered to be a last-line treatment option and gained FDA approval as part of the combination product Recarbrio? in July 2019.L7568

Struktur Molekul 2D

Berat 348.37
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) Relebactam has a half-life of 1.2 hours as per official FDA labeling.[label] Values reported in pharmacokinetic studies vary from 1.35-1.8 hours.[A181117,A181120]
Volume Distribusi Relebactam has a volume of distribution of approximately 19 L with both single and steady state dosing.[label,A181117,A181120]
Klirens (Clearance) Relebactam has a reported total clearance of approximately 130-150 mL/min (8 L/h).[label,A181117,A181120] About 30% of the total drug clearance can be attributed to active tubular secretion.[label]

Absorpsi

Currently, relebactam is only available as an intravenous product; therefore, there is no relevant absorption data in the literature.

Metabolisme

Relebactam does not undergo significant metabolism and can be found mostly unchanged in human plasma.label

Rute Eliminasi

Approximately 90-100% of relebactam is renally eliminated.label,A181117,A181120

Interaksi Obat

126 Data
Aspartame The excretion of Relebactam can be decreased when combined with Aspartame.
Pravastatin The excretion of Relebactam can be decreased when combined with Pravastatin.
Pantoprazole The excretion of Relebactam can be decreased when combined with Pantoprazole.
Cefotiam The excretion of Relebactam can be decreased when combined with Cefotiam.
Liothyronine The excretion of Relebactam can be decreased when combined with Liothyronine.
Conjugated estrogens The excretion of Relebactam can be decreased when combined with Conjugated estrogens.
Valproic acid The excretion of Relebactam can be decreased when combined with Valproic acid.
Indomethacin The excretion of Relebactam can be decreased when combined with Indomethacin.
Aminohippuric acid The excretion of Relebactam can be decreased when combined with Aminohippuric acid.
Lansoprazole The excretion of Relebactam can be decreased when combined with Lansoprazole.
Cefalotin The excretion of Relebactam can be decreased when combined with Cefalotin.
Tenoxicam The excretion of Relebactam can be decreased when combined with Tenoxicam.
Cefotaxime The excretion of Relebactam can be decreased when combined with Cefotaxime.
Zidovudine The excretion of Relebactam can be decreased when combined with Zidovudine.
Cimetidine The excretion of Relebactam can be decreased when combined with Cimetidine.
Piroxicam The excretion of Relebactam can be decreased when combined with Piroxicam.
Methotrexate The excretion of Relebactam can be decreased when combined with Methotrexate.
Cephalexin The excretion of Relebactam can be decreased when combined with Cephalexin.
Enalapril The excretion of Relebactam can be decreased when combined with Enalapril.
Diclofenac The excretion of Relebactam can be decreased when combined with Diclofenac.
Oxytetracycline The excretion of Relebactam can be decreased when combined with Oxytetracycline.
Leucovorin The excretion of Relebactam can be decreased when combined with Leucovorin.
Furosemide The excretion of Relebactam can be decreased when combined with Furosemide.
Esomeprazole The excretion of Relebactam can be decreased when combined with Esomeprazole.
Tetracycline The excretion of Relebactam can be decreased when combined with Tetracycline.
Acyclovir The excretion of Relebactam can be decreased when combined with Acyclovir.
Phenylbutazone The excretion of Relebactam can be decreased when combined with Phenylbutazone.
Cefaclor The excretion of Relebactam can be decreased when combined with Cefaclor.
Bumetanide The excretion of Relebactam can be decreased when combined with Bumetanide.
Quinidine The excretion of Relebactam can be decreased when combined with Quinidine.
Dinoprostone The excretion of Relebactam can be decreased when combined with Dinoprostone.
Famotidine The excretion of Relebactam can be decreased when combined with Famotidine.
Salicylic acid The excretion of Relebactam can be decreased when combined with Salicylic acid.
Acetylsalicylic acid The excretion of Relebactam can be decreased when combined with Acetylsalicylic acid.
Ganciclovir The excretion of Relebactam can be decreased when combined with Ganciclovir.
Ketoprofen The excretion of Relebactam can be decreased when combined with Ketoprofen.
Minocycline The excretion of Relebactam can be decreased when combined with Minocycline.
Probenecid The excretion of Relebactam can be decreased when combined with Probenecid.
Mercaptopurine The excretion of Relebactam can be decreased when combined with Mercaptopurine.
Ibuprofen The excretion of Relebactam can be decreased when combined with Ibuprofen.
Novobiocin The excretion of Relebactam can be decreased when combined with Novobiocin.
Benzylpenicillin The excretion of Relebactam can be decreased when combined with Benzylpenicillin.
Melatonin The excretion of Relebactam can be decreased when combined with Melatonin.
Ouabain The excretion of Relebactam can be decreased when combined with Ouabain.
Rosuvastatin The excretion of Relebactam can be decreased when combined with Rosuvastatin.
Cefadroxil The excretion of Relebactam can be decreased when combined with Cefadroxil.
Ceftriaxone The excretion of Relebactam can be decreased when combined with Ceftriaxone.
Cefamandole The excretion of Relebactam can be decreased when combined with Cefamandole.
Cefazolin The excretion of Relebactam can be decreased when combined with Cefazolin.
Cefoperazone The excretion of Relebactam can be decreased when combined with Cefoperazone.
Ceftizoxime The excretion of Relebactam can be decreased when combined with Ceftizoxime.
Cefacetrile The excretion of Relebactam can be decreased when combined with Cefacetrile.
Ceftibuten The excretion of Relebactam can be decreased when combined with Ceftibuten.
Liotrix The excretion of Relebactam can be decreased when combined with Liotrix.
Tazobactam The excretion of Relebactam can be decreased when combined with Tazobactam.
trans-2-hydroxycinnamic acid The excretion of Relebactam can be decreased when combined with trans-2-hydroxycinnamic acid.
Topiroxostat The excretion of Relebactam can be decreased when combined with Topiroxostat.
Cholic Acid The excretion of Relebactam can be decreased when combined with Cholic Acid.
Glutaric Acid The excretion of Relebactam can be decreased when combined with Glutaric Acid.
Benzoic acid The excretion of Relebactam can be decreased when combined with Benzoic acid.
Taurocholic acid The excretion of Relebactam can be decreased when combined with Taurocholic acid.
Caprylic acid The excretion of Relebactam can be decreased when combined with Caprylic acid.
Ataluren The excretion of Relebactam can be decreased when combined with Ataluren.
Teriflunomide The excretion of Relebactam can be decreased when combined with Teriflunomide.
Dabrafenib The excretion of Relebactam can be decreased when combined with Dabrafenib.
Dolutegravir The excretion of Relebactam can be decreased when combined with Dolutegravir.
Cefaloridine The excretion of Relebactam can be decreased when combined with Cefaloridine.
Lenvatinib The excretion of Relebactam can be decreased when combined with Lenvatinib.
Cabotegravir The excretion of Relebactam can be decreased when combined with Cabotegravir.
Apalutamide The excretion of Relebactam can be decreased when combined with Apalutamide.
Pradigastat The excretion of Relebactam can be decreased when combined with Pradigastat.
Enasidenib The excretion of Relebactam can be decreased when combined with Enasidenib.
Gemfibrozil The excretion of Relebactam can be decreased when combined with Gemfibrozil.
Dronedarone The excretion of Relebactam can be decreased when combined with Dronedarone.
Favipiravir The excretion of Relebactam can be decreased when combined with Favipiravir.
Guanidine The excretion of Relebactam can be decreased when combined with Guanidine.
Tafamidis The excretion of Relebactam can be decreased when combined with Tafamidis.
Linezolid The excretion of Relebactam can be decreased when combined with Linezolid.
Testosterone The excretion of Relebactam can be increased when combined with Testosterone.
Methyltestosterone The excretion of Relebactam can be increased when combined with Methyltestosterone.
Testosterone cypionate The excretion of Relebactam can be increased when combined with Testosterone cypionate.
Testosterone enanthate The excretion of Relebactam can be increased when combined with Testosterone enanthate.
Metformin The excretion of Relebactam can be decreased when combined with Metformin.
Ciprofloxacin The excretion of Relebactam can be decreased when combined with Ciprofloxacin.
Levofloxacin The excretion of Relebactam can be decreased when combined with Levofloxacin.
Cefradine The excretion of Relebactam can be decreased when combined with Cefradine.
Estrone sulfate The excretion of Relebactam can be decreased when combined with Estrone sulfate.
N-methylnicotinamide The excretion of Relebactam can be decreased when combined with N-methylnicotinamide.
Solriamfetol The excretion of Solriamfetol can be decreased when combined with Relebactam.
Nadolol The excretion of Relebactam can be decreased when combined with Nadolol.
Flecainide The excretion of Relebactam can be decreased when combined with Flecainide.
Emtricitabine The excretion of Relebactam can be decreased when combined with Emtricitabine.
Topotecan The excretion of Topotecan can be decreased when combined with Relebactam.
Procainamide The excretion of Procainamide can be decreased when combined with Relebactam.
Abemaciclib The excretion of Abemaciclib can be decreased when combined with Relebactam.
Baricitinib The excretion of Relebactam can be decreased when combined with Baricitinib.
Pyrimethamine The excretion of Relebactam can be decreased when combined with Pyrimethamine.
Lofexidine The excretion of Relebactam can be decreased when combined with Lofexidine.
Tafenoquine The excretion of Relebactam can be decreased when combined with Tafenoquine.
Bictegravir The excretion of Relebactam can be decreased when combined with Bictegravir.

Target Protein

Beta-lactamase blaZ
Beta-lactamase TEM bla
Beta-lactamase SHV-1 bla
Beta-lactamase CTX-M
Beta-lactamase KPC-2
Beta-lactamase ampC

Referensi & Sumber

Artikel (PubMed)
  • PMID: 29914955
    Rhee EG, Rizk ML, Calder N, Nefliu M, Warrington SJ, Schwartz MS, Mangin E, Boundy K, Bhagunde P, Colon-Gonzalez F, Jumes P, Liu Y, Butterton JR: Pharmacokinetics, Safety, and Tolerability of Single and Multiple Doses of Relebactam, a beta-Lactamase Inhibitor, in Combination with Imipenem and Cilastatin in Healthy Participants. Antimicrob Agents Chemother. 2018 Aug 27;62(9). pii: AAC.00280-18. doi: 10.1128/AAC.00280-18. Print 2018 Sep.
  • PMID: 30589457
    Crass RL, Pai MP: Pharmacokinetics and Pharmacodynamics of beta-Lactamase Inhibitors. Pharmacotherapy. 2019 Feb;39(2):182-195. doi: 10.1002/phar.2210. Epub 2019 Jan 20.
  • PMID: 29610205
    Papp-Wallace KM, Barnes MD, Alsop J, Taracila MA, Bethel CR, Becka SA, van Duin D, Kreiswirth BN, Kaye KS, Bonomo RA: Relebactam Is a Potent Inhibitor of the KPC-2 beta-Lactamase and Restores Imipenem Susceptibility in KPC-Producing Enterobacteriaceae. Antimicrob Agents Chemother. 2018 May 25;62(6). pii: AAC.00174-18. doi: 10.1128/AAC.00174-18. Print 2018 Jun.
  • PMID: 29530851
    Barnes MD, Bethel CR, Alsop J, Becka SA, Rutter JD, Papp-Wallace KM, Bonomo RA: Inactivation of the Pseudomonas-Derived Cephalosporinase-3 (PDC-3) by Relebactam. Antimicrob Agents Chemother. 2018 Apr 26;62(5). pii: AAC.02406-17. doi: 10.1128/AAC.02406-17. Print 2018 May.
  • PMID: 29230684
    Zhanel GG, Lawrence CK, Adam H, Schweizer F, Zelenitsky S, Zhanel M, Lagace-Wiens PRS, Walkty A, Denisuik A, Golden A, Gin AS, Hoban DJ, Lynch JP 3rd, Karlowsky JA: Imipenem-Relebactam and Meropenem-Vaborbactam: Two Novel Carbapenem-beta-Lactamase Inhibitor Combinations. Drugs. 2018 Jan;78(1):65-98. doi: 10.1007/s40265-017-0851-9.
  • PMID: 27642504
    Jones JA, Virga KG, Gumina G, Hevener KE: Recent Advances in the Rational Design and Optimization of Antibacterial Agents. Medchemcomm. 2016 Sep 1;7(9):1694-1715. doi: 10.1039/C6MD00232C. Epub 2016 Jul 7.
  • PMID: 28303449
    Wong D, van Duin D: Novel Beta-Lactamase Inhibitors: Unlocking Their Potential in Therapy. Drugs. 2017 Apr;77(6):615-628. doi: 10.1007/s40265-017-0725-1.
  • PMID: 29311084
    Rizk ML, Rhee EG, Jumes PA, Gotfried MH, Zhao T, Mangin E, Bi S, Chavez-Eng CM, Zhang Z, Butterton JR: Intrapulmonary Pharmacokinetics of Relebactam, a Novel beta-Lactamase Inhibitor, Dosed in Combination with Imipenem-Cilastatin in Healthy Subjects. Antimicrob Agents Chemother. 2018 Feb 23;62(3). pii: AAC.01411-17. doi: 10.1128/AAC.01411-17. Print 2018 Mar.

Contoh Produk & Brand

Produk: 2 • International brands: 0
Produk
  • Recarbrio
    Injection, powder, for solution • - • Intravenous • EU • Approved
  • Recarbrio
    Injection, powder, for solution • - • Intravenous • US • Approved

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