Peringatan Keamanan

The oral median lethal dose (LD50) in mouse is >500 mg/kg.L44436

Intravenous administration of ertapenem at a dose of 2 g over 30 min or 3 g over 1-2 hours in healthy adults resulted in increased incidence of nausea. In clinical trials in adults, inadvertent administration of three 1 g doses of ertapenem in a 24 hour period resulted in diarrhea and transient dizziness in one patient. As there is no known antidote for ertapenem overdose, the drug should be discontinued with the initiation of general supportive treatment until renal elimination takes place. Ertapenem can be removed by hemodialysis to some extent: the plasma clearance of the total fraction of ertapenem was increased by 30% in subjects with end-stage renal disease when hemodialysis was performed immediately following administration. However, no information is available on the use of hemodialysis to treat ertapenem overdosage.L14339

Ertapenem

DB00303

small molecule approved investigational

Deskripsi

Ertapenem is a 1-? methyl-carbapenem that is structurally related to beta-lactam antibiotics.L14339 It was first authorized for use in the US in November 2001 and in Europe in April 2002.A447 Shown to be effective against a wide range of Gram-positive and Gram-negative aerobic and anaerobic bacteria, ertapenem is used to treat various bacterial infections.

Struktur Molekul 2D

Berat 475.515
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The mean plasma half-life was approximately four hours in healthy young adults and adolescents and approximately 2.5 hours in children three to 12 years of age.[L14339] The long half-life of ertapenem can be explained by its high protein binding.[A10372]
Volume Distribusi The apparent volume of distribution at steady state (V<sub>ss</sub>) of ertapenem is approximately 0.12 L/kg in adults, 0.2 L/kg in children three months to 12 years of age, and 0.16 L/kg in adolescents 13 to 17 years of age. Ertapenem does not accumulate.[L14339]
Klirens (Clearance) The mean plasma clearance in healthy young adults was approximately 1.8 L/hour.[L14339] The mean renal clearance of intact ertapenem was 12.8 mL/min compared with a total clearance of 28.4 mL/min.[A447]

Absorpsi

Ertapenem is almost completely absorbed following intramuscular administration, with a mean bioavailability of approximately 90%.L14339 Plasma concentrations of ertapenem are similar whether given intramuscularly or intravenously; however, the peak concentrations are lower when given via the intramuscular route. The time to reach the Cmax (Tmax) is slightly longer when given via the intramuscular route.A447 Following daily intramuscular administration of one gram of ertapenem, the Tmax was approximately 2.3 hours.L14339 In healthy young adults who received a single 30-minute intravenous infusion of one gram of ertapenem, the Cmax was 155 µG/mL at 0.5 hours postdose.L44416

Metabolisme

In healthy young adults, unchanged ertapenem accounted for most plasma radioactivity.L14339 The major metabolite of ertapenem is the ring-opened derivative formed by dehydropeptidase I-mediated hydrolysis of the beta-lactam ring.A255572,L44416 This metabolite is pharmacologically inactive.L14339 Dehydropeptidase I (DHP-I) is found predominantly in the kidneys.A447 Hepatic metabolism is negligible.A255567

Rute Eliminasi

Ertapenem predominantly undergoes renal elimination, where it undergoes glomerular filtration and net tubular secretion.A447 In healthy young adults who received one gram of IV radiolabeled ertapenem, approximately 80% of the radioactivity was recovered in urine and 10% of the radioactivity was recovered in feces. The mean percentage of the administered dose excreted in urine was 17.4% during 0-2 hours postdose, 5.4% during 4-6 hours postdose, and 2.4% during 12-24 hours postdose.L14339 Of the 80% radioactivity in urine, about 38% accounted for unchanged ertapenem and 37% accounted for its ring-opened metabolite.L14339

Interaksi Obat

776 Data
Probenecid Probenecid may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Ertapenem.
Valproic acid The serum concentration of Valproic acid can be decreased when it is combined with Ertapenem.
BCG vaccine The therapeutic efficacy of BCG vaccine can be decreased when used in combination with Ertapenem.
Typhoid vaccine The therapeutic efficacy of Typhoid vaccine can be decreased when used in combination with Ertapenem.
Cyclosporine Cyclosporine may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Icosapent Icosapent may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Cefotiam Cefotiam may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Mesalazine Mesalazine may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Cefmenoxime Cefmenoxime may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Cefmetazole Cefmetazole may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Pamidronic acid Pamidronic acid may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Tenofovir disoproxil Tenofovir disoproxil may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Indomethacin Indomethacin may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Cidofovir Cidofovir may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Cefpiramide Cefpiramide may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Ceftazidime Ceftazidime may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Loracarbef Loracarbef may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Cefalotin Cefalotin may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Nabumetone Nabumetone may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Ketorolac Ketorolac may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Tenoxicam Tenoxicam may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Celecoxib Celecoxib may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Cefotaxime Cefotaxime may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Tolmetin Tolmetin may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Foscarnet Foscarnet may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Rofecoxib Rofecoxib may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Piroxicam Piroxicam may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Methotrexate Methotrexate may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Cephalexin Cephalexin may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Fenoprofen Fenoprofen may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Valaciclovir Valaciclovir may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Valdecoxib Valdecoxib may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Diclofenac Diclofenac may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Sulindac Sulindac may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Bacitracin Bacitracin may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Amphotericin B Amphotericin B may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Cephaloglycin Cephaloglycin may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Flurbiprofen Flurbiprofen may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Adefovir dipivoxil Adefovir dipivoxil may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Pentamidine Pentamidine may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Etodolac Etodolac may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Mefenamic acid Mefenamic acid may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Acyclovir Acyclovir may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Naproxen Naproxen may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Sulfasalazine Sulfasalazine may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Phenylbutazone Phenylbutazone may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Meloxicam The risk or severity of methemoglobinemia can be increased when Ertapenem is combined with Meloxicam.
Carprofen Carprofen may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Cefaclor Cefaclor may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Diflunisal Diflunisal may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Ceforanide Ceforanide may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Salicylic acid Salicylic acid may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Meclofenamic acid Meclofenamic acid may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Acetylsalicylic acid Acetylsalicylic acid may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Carboplatin Carboplatin may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Oxaprozin Oxaprozin may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Ketoprofen Ketoprofen may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Balsalazide Balsalazide may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Ibuprofen Ibuprofen may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Cefditoren Cefditoren may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Atazanavir Atazanavir may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Colistimethate Colistimethate may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Cefuroxime Cefuroxime may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Cefapirin Cefapirin may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Cefadroxil Cefadroxil may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Cefprozil Cefprozil may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Ceftriaxone Ceftriaxone may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Olsalazine Olsalazine may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Lumiracoxib Lumiracoxib may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Cefamandole Cefamandole may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Cefazolin Cefazolin may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Cefonicid Cefonicid may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Cefoperazone Cefoperazone may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Cefotetan Cefotetan may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Cefoxitin Cefoxitin may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Ceftizoxime Ceftizoxime may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Cefradine Cefradine may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Magnesium salicylate Magnesium salicylate may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Salsalate Salsalate may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Choline magnesium trisalicylate Choline magnesium trisalicylate may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Cefepime Cefepime may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Cefacetrile Cefacetrile may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Ceftibuten Ceftibuten may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Cefpodoxime Cefpodoxime may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Antrafenine Antrafenine may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Aminophenazone Aminophenazone may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Antipyrine Antipyrine may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Tiaprofenic acid Tiaprofenic acid may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Lopinavir Lopinavir may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Etoricoxib Etoricoxib may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Hydrolyzed Cephalothin Hydrolyzed Cephalothin may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Cephalothin Group Cephalothin Group may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Oxyphenbutazone Oxyphenbutazone may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Latamoxef Latamoxef may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Nimesulide Nimesulide may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Benoxaprofen Benoxaprofen may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Metamizole Metamizole may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Zomepirac Zomepirac may decrease the excretion rate of Ertapenem which could result in a higher serum level.
Ceftobiprole Ceftobiprole may decrease the excretion rate of Ertapenem which could result in a higher serum level.

Target Protein

Penicillin-binding protein 1A mrcA
Penicillin-binding protein 1B mrcB
Penicillin-binding protein 2 mrdA
Penicillin-binding protein 2 mrdA
Peptidoglycan synthase FtsI ftsI
Peptidoglycan synthase FtsI ftsI
D-alanyl-D-alanine carboxypeptidase DacB dacB
D-alanyl-D-alanine carboxypeptidase DacC dacC

Referensi & Sumber

Synthesis reference: Ying Shi, Kun Li, Zan Xie, Xuebin Zhao, Jian Lv, Xiuqin Yu, "INTERMEDIATE OF ERTAPENEM, A COMPOSITION COMPRISING THE SAME AND PREPARATION METHODS THEREOF." U.S. Patent US20120095209, issued April 19, 2012.
Artikel (PubMed)
  • PMID: 15150180
    Nix DE, Majumdar AK, DiNubile MJ: Pharmacokinetics and pharmacodynamics of ertapenem: an overview for clinicians. J Antimicrob Chemother. 2004 Jun;53 Suppl 2:ii23-8.
  • PMID: 11772242
    Odenholt I: Ertapenem: a new carbapenem. Expert Opin Investig Drugs. 2001 Jun;10(6):1157-66.
  • PMID: 20163277
    Congeni BL: Ertapenem. Expert Opin Pharmacother. 2010 Mar;11(4):669-72. doi: 10.1517/14656561003631397.
  • PMID: 12921489
    Curran M, Simpson D, Perry C: Ertapenem: a review of its use in the management of bacterial infections. Drugs. 2003;63(17):1855-78. doi: 10.2165/00003495-200363170-00006.

Contoh Produk & Brand

Produk: 30 • International brands: 0
Produk
  • Ertapenem
    Injection • 1 g/1 • Intramuscular; Intravenous • US • Generic • Approved
  • Ertapenem
    Injection • 1 g/20mL • Intramuscular; Intravenous • US • Generic • Approved
  • Ertapenem
    Injection • 1 g/20mL • Intramuscular; Intravenous • US • Generic • Approved
  • Ertapenem
    Injection, powder, lyophilized, for solution • 1 g/1 • Intramuscular; Intravenous • US • Generic • Approved
  • Ertapenem
    Injection • 1 g/20mL • Intramuscular; Intravenous • US • Generic • Approved
  • Ertapenem
    Injection, powder, lyophilized, for solution • 1 g/1 • Intramuscular; Intravenous • US • Generic • Approved
  • Ertapenem
    Injection, powder, lyophilized, for solution • 1 g/1 • Intramuscular; Intravenous • US • Approved
  • Ertapenem
    Injection, powder, lyophilized, for solution • 1 g/1 • Intramuscular; Intravenous • US • Generic • Approved
Menampilkan 8 dari 30 produk.

Sekuens Gen/Protein (FASTA)

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