Peringatan Keamanan

Dosage adjustment is necessary in patients with moderate and severe renal impairment.

Doripenem's FDA label includes a warning against use in ventilator-associated bacterial pneumonia, as a clinical trial for that indication resulted in increased mortality with doripenem (23% vs. 16.7% recieving imipenem) as well as lower clinical response rates.

Seizures have been reported with doripenem treatment; patients at greater risk of developing seizures we found to have pre-existing central nervous system (CNS) conditions, compromised renal function, or patients receiving higher doses than 500 mg every 8 hours. Doripenem also reduces plasma levels of valproic acid when administered concomitantly; therefore patients with pre-existing seizure disorders on valproic acid are at even higher risk of breakthrough seizures if receiving both drugs at the same time.

Doripenem is considered pregnancy category B as it was not found to be teratogenic or produce effects on ossification, developmental delays, or fetal weight in rat and rabbit studies. There are no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed. It is not known whether doripenem is excreted into breast milk, therefore caution should be exercised with doripenem administration to nursing women.

Doripenem

DB06211

small molecule approved investigational

Deskripsi

Doripenem is a broad-spectrum, carbapenem antibiotic marketed under the brand name Doribax by Janssen. Doripenem injection was approved by the FDA in 2007 to treat complicated urinary tract and intra-abdominal infections. In a clinical trial of doripenem treatment in ventilator associated pneumonia (vs. imipenem and cilastatin), it was found that doripenem carried an increased risk of death and lower clinical cure rates, resulting in a premature termination of the trial. The FDA revised the doripenem label in 2014 to include a warning against use in ventilator-associated pneumonia and to reiterate its safety and efficacy for its approved indications.

Struktur Molekul 2D

Berat 420.504
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 1 hour, in healthy non-elderly adults.
Volume Distribusi The average Vd is 16.8 L (8.09-55.5 L) at steady-state in healthy subjects. Doripenem penetrates into many tissues and fluids, including potential sites of approved indication infections.
Klirens (Clearance) 10.3 L/hour.

Absorpsi

Doripenem is administered intravenously as an infusion. There was no accumulation of doripenem following mulitiple infusions of either 500mg or 1g administered every 8 hours for 7-10 days in subjects with normal renal function.

Metabolisme

Metabolism of doripenem is via dehydropeptidase-I (also called dipeptidase-1) into a microbiologically inactive ring-opened metabolite, doripenem-M1. Doripenem does not appear to be a substrate of the hepatic CYP450 enzymes.

Rute Eliminasi

Doripenem is primarily eliminated unchanged by the kidneys and undergoes glomerular filtration and active tubular secretion. A mean of 71% and 15% of the dose was recovered in urine as unchanged drug and the ring-opened metabolite, respectively, within 48 hours of 500 mg dose in healthy adults. Following the administration of a single 500 mg dose of radiolabeled doripenem to healthy adults, less than 1% of the total radioactivity was recovered in feces after one week.

Interaksi Obat

821 Data
Aspartame The excretion of Doripenem can be decreased when combined with Aspartame.
Pravastatin The excretion of Doripenem can be decreased when combined with Pravastatin.
Aminohippuric acid The excretion of Doripenem can be decreased when combined with Aminohippuric acid.
Lansoprazole The excretion of Doripenem can be decreased when combined with Lansoprazole.
Zidovudine The excretion of Doripenem can be decreased when combined with Zidovudine.
Guanidine The excretion of Doripenem can be decreased when combined with Guanidine.
Enalapril The excretion of Doripenem can be decreased when combined with Enalapril.
Oxytetracycline The excretion of Doripenem can be decreased when combined with Oxytetracycline.
Leucovorin The excretion of Doripenem can be decreased when combined with Leucovorin.
Esomeprazole The excretion of Doripenem can be decreased when combined with Esomeprazole.
Dinoprostone The excretion of Doripenem can be decreased when combined with Dinoprostone.
Famotidine The excretion of Doripenem can be decreased when combined with Famotidine.
Minocycline The excretion of Doripenem can be decreased when combined with Minocycline.
Mercaptopurine The excretion of Doripenem can be decreased when combined with Mercaptopurine.
Novobiocin The excretion of Doripenem can be decreased when combined with Novobiocin.
Benzylpenicillin The excretion of Doripenem can be decreased when combined with Benzylpenicillin.
Melatonin The excretion of Doripenem can be decreased when combined with Melatonin.
Ouabain The excretion of Doripenem can be decreased when combined with Ouabain.
Rosuvastatin The excretion of Doripenem can be decreased when combined with Rosuvastatin.
Liotrix The excretion of Doripenem can be decreased when combined with Liotrix.
Cilastatin The excretion of Doripenem can be decreased when combined with Cilastatin.
Tazobactam The excretion of Doripenem can be decreased when combined with Tazobactam.
trans-2-hydroxycinnamic acid The excretion of Doripenem can be decreased when combined with trans-2-hydroxycinnamic acid.
Cholic Acid The excretion of Doripenem can be decreased when combined with Cholic Acid.
Glutaric Acid The excretion of Doripenem can be decreased when combined with Glutaric Acid.
Benzoic acid The excretion of Doripenem can be decreased when combined with Benzoic acid.
Taurocholic acid The excretion of Doripenem can be decreased when combined with Taurocholic acid.
Caprylic acid The excretion of Doripenem can be decreased when combined with Caprylic acid.
Ataluren The excretion of Doripenem can be decreased when combined with Ataluren.
Teriflunomide The excretion of Doripenem can be decreased when combined with Teriflunomide.
Dabrafenib The excretion of Doripenem can be decreased when combined with Dabrafenib.
Dolutegravir The excretion of Doripenem can be decreased when combined with Dolutegravir.
Lenvatinib The excretion of Doripenem can be decreased when combined with Lenvatinib.
Cabotegravir The excretion of Doripenem can be decreased when combined with Cabotegravir.
Pradigastat The excretion of Doripenem can be decreased when combined with Pradigastat.
Enasidenib The excretion of Doripenem can be decreased when combined with Enasidenib.
Cefotiam The excretion of Doripenem can be decreased when combined with Cefotiam.
Indomethacin The excretion of Doripenem can be decreased when combined with Indomethacin.
Cefalotin The excretion of Doripenem can be decreased when combined with Cefalotin.
Tenoxicam The excretion of Doripenem can be decreased when combined with Tenoxicam.
Cefotaxime The excretion of Doripenem can be decreased when combined with Cefotaxime.
Piroxicam The excretion of Doripenem can be decreased when combined with Piroxicam.
Methotrexate The excretion of Doripenem can be decreased when combined with Methotrexate.
Cephalexin The excretion of Doripenem can be decreased when combined with Cephalexin.
Diclofenac The excretion of Doripenem can be decreased when combined with Diclofenac.
Acyclovir The excretion of Doripenem can be decreased when combined with Acyclovir.
Phenylbutazone The excretion of Doripenem can be decreased when combined with Phenylbutazone.
Cefaclor The excretion of Doripenem can be decreased when combined with Cefaclor.
Salicylic acid The excretion of Doripenem can be decreased when combined with Salicylic acid.
Acetylsalicylic acid The excretion of Doripenem can be decreased when combined with Acetylsalicylic acid.
Ketoprofen The excretion of Doripenem can be decreased when combined with Ketoprofen.
Ibuprofen The excretion of Doripenem can be decreased when combined with Ibuprofen.
Cefadroxil The excretion of Doripenem can be decreased when combined with Cefadroxil.
Ceftriaxone The excretion of Doripenem can be decreased when combined with Ceftriaxone.
Cefamandole The excretion of Doripenem can be decreased when combined with Cefamandole.
Cefazolin The excretion of Doripenem can be decreased when combined with Cefazolin.
Cefoperazone The excretion of Doripenem can be decreased when combined with Cefoperazone.
Ceftizoxime The excretion of Doripenem can be decreased when combined with Ceftizoxime.
Cefacetrile The excretion of Doripenem can be decreased when combined with Cefacetrile.
Ceftibuten The excretion of Doripenem can be decreased when combined with Ceftibuten.
Cefaloridine The excretion of Doripenem can be decreased when combined with Cefaloridine.
Pantoprazole The excretion of Doripenem can be decreased when combined with Pantoprazole.
Liothyronine The excretion of Doripenem can be decreased when combined with Liothyronine.
Conjugated estrogens The excretion of Doripenem can be decreased when combined with Conjugated estrogens.
Cimetidine The excretion of Doripenem can be decreased when combined with Cimetidine.
Tetracycline The excretion of Doripenem can be decreased when combined with Tetracycline.
Ganciclovir The excretion of Doripenem can be decreased when combined with Ganciclovir.
Probenecid The excretion of Doripenem can be decreased when combined with Probenecid.
Gemfibrozil The excretion of Doripenem can be decreased when combined with Gemfibrozil.
Topiroxostat The excretion of Doripenem can be decreased when combined with Topiroxostat.
Baricitinib Doripenem may decrease the excretion rate of Baricitinib which could result in a higher serum level.
Apalutamide The excretion of Doripenem can be decreased when combined with Apalutamide.
Dronedarone The excretion of Doripenem can be decreased when combined with Dronedarone.
Favipiravir The excretion of Doripenem can be decreased when combined with Favipiravir.
Tafamidis The excretion of Doripenem can be decreased when combined with Tafamidis.
Linezolid The excretion of Doripenem can be decreased when combined with Linezolid.
Valproic acid The serum concentration of Valproic acid can be decreased when it is combined with Doripenem.
BCG vaccine The therapeutic efficacy of BCG vaccine can be decreased when used in combination with Doripenem.
Typhoid vaccine The therapeutic efficacy of Typhoid vaccine can be decreased when used in combination with Doripenem.
Cyclosporine Cyclosporine may decrease the excretion rate of Doripenem which could result in a higher serum level.
Icosapent Icosapent may decrease the excretion rate of Doripenem which could result in a higher serum level.
Mesalazine Mesalazine may decrease the excretion rate of Doripenem which could result in a higher serum level.
Cefmenoxime Cefmenoxime may decrease the excretion rate of Doripenem which could result in a higher serum level.
Cefmetazole Cefmetazole may decrease the excretion rate of Doripenem which could result in a higher serum level.
Pamidronic acid Pamidronic acid may decrease the excretion rate of Doripenem which could result in a higher serum level.
Tenofovir disoproxil Tenofovir disoproxil may decrease the excretion rate of Doripenem which could result in a higher serum level.
Cidofovir Cidofovir may decrease the excretion rate of Doripenem which could result in a higher serum level.
Cefpiramide Cefpiramide may decrease the excretion rate of Doripenem which could result in a higher serum level.
Ceftazidime Ceftazidime may decrease the excretion rate of Doripenem which could result in a higher serum level.
Loracarbef Loracarbef may decrease the excretion rate of Doripenem which could result in a higher serum level.
Nabumetone Nabumetone may decrease the excretion rate of Doripenem which could result in a higher serum level.
Ketorolac Ketorolac may decrease the excretion rate of Doripenem which could result in a higher serum level.
Celecoxib Celecoxib may decrease the excretion rate of Doripenem which could result in a higher serum level.
Tolmetin Tolmetin may decrease the excretion rate of Doripenem which could result in a higher serum level.
Foscarnet Foscarnet may decrease the excretion rate of Doripenem which could result in a higher serum level.
Rofecoxib Rofecoxib may decrease the excretion rate of Doripenem which could result in a higher serum level.
Fenoprofen Fenoprofen may decrease the excretion rate of Doripenem which could result in a higher serum level.
Valaciclovir Valaciclovir may decrease the excretion rate of Doripenem which could result in a higher serum level.
Valdecoxib Valdecoxib may decrease the excretion rate of Doripenem which could result in a higher serum level.
Sulindac Sulindac may decrease the excretion rate of Doripenem which could result in a higher serum level.

Target Protein

Dihydropteroate synthase folP
Penicillin-binding protein 1A mrcA
Penicillin-binding protein 1B mrcB
Penicillin-binding protein 2 mrdA
Cell division protein pbpB
Penicillin-binding protein 4 pbp4

Referensi & Sumber

Artikel (PubMed)
  • PMID: 15273134
    Jones RN, Huynh HK, Biedenbach DJ: Activities of doripenem (S-4661) against drug-resistant clinical pathogens. Antimicrob Agents Chemother. 2004 Aug;48(8):3136-40.
  • PMID: 21098373
    Chahine EB, Ferrill MJ, Poulakos MN: Doripenem: a new carbapenem antibiotic. Am J Health Syst Pharm. 2010 Dec 1;67(23):2015-24. doi: 10.2146/ajhp090672.
  • PMID: 19485791
    Dedhia HV, McKnight R: Doripenem: position in clinical practice. Expert Rev Anti Infect Ther. 2009 Jun;7(5):507-14. doi: 10.1586/eri.09.37.
  • PMID: 19243706
    Matthews SJ, Lancaster JW: Doripenem monohydrate, a broad-spectrum carbapenem antibiotic. Clin Ther. 2009 Jan;31(1):42-63. doi: 10.1016/j.clinthera.2009.01.013.

Contoh Produk & Brand

Produk: 10 • International brands: 1
Produk
  • Doribax
    Powder, for solution • 500 mg/10mL • Intravenous • US • Approved
  • Doribax
    Powder, for solution • 500 mg/10mL • Intravenous • US • Approved
  • Doribax
    Powder, for solution • 250 mg/10mL • Intravenous • US • Approved
  • Doribax
    Powder, for solution • 500 mg/10mL • Intravenous • US • Approved
  • Doribax
    Powder, for solution • 250 mg/10mL • Intravenous • US • Approved
  • Doribax
    Powder, for solution • 500 mg / vial • Intravenous • Canada • Approved
  • Doribax
    Injection, powder, for solution • 500 mg • Intravenous • EU
  • Doribax
    Injection, powder, for solution • 250 mg • Intravenous • EU
Menampilkan 8 dari 10 produk.
International Brands
  • Finibax — Shionogi Co.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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