Peringatan Keamanan

In case of overdose with the combination product, including relebactam and cilastatin, it is recommended to provide supportive care.L7568 Imipenem, cilastatin, and relebactam may be removed via hemodialysis.

Imipenem

DB01598

small molecule approved

Deskripsi

Imipenem is a semisynthetic thienamycin that has a wide spectrum of antibacterial activity against gram-negative and gram-positive aerobic and anaerobic bacteria, including many multiresistant strains.label It is stable to many beta-lactamases. Similar compounds include meropenem, known for having greater activity against Gram negative bacteria, and the newer ertapenem which exhibits a longer half-life due to increased binding to plasma proteins.A15389 Imipenem is commonly used in combination with cilastatin and is now available in a triple-drug product with cilastatin and relebactam which was recently approved by the FDA. Imipenem was first approved by the FDA in November 1985 as the combination product Primaxin marketed by Merck & Co.L7628

Struktur Molekul 2D

Berat 299.346
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) When given via IV injection imipenem has a half-life of 1 h.[label,A2530,A181271] The apparent half-life of the IM injection ranges from 1.3-5.1 h, likely due to slower absorption form the injection site.
Volume Distribusi The reported volume of distribution for imipenem ranges from 0.23-0.31 L/kg.[label,A2530,A181271]
Klirens (Clearance) The total clearance of imipenem is 0.2 L/h/kg.[A181271] When used alone, the renal clearance is 0.05 L/h/kg. In combination with cilastatin the renal clearance of imipenem is 0.15 L/h/kg, likely due to the increased concentration of the parent drug.

Absorpsi

Imipenem is not effectively absorbed from the gastrointestinal tract and therefore must be administered parenterally. The bioavailability of the IM injection is 89%. A181271

Metabolisme

Imipenem is metabolized by renal dehydropeptidase.label,L7526

Rute Eliminasi

Approximately 70% of imipenem is excreted in the urine as the parent drug.label,L7526

Interaksi Obat

286 Data
Cyclosporine Cyclosporine may increase the neurotoxic activities of Imipenem.
Ganciclovir The risk or severity of generalized seizure can be increased when Ganciclovir is combined with Imipenem.
Valganciclovir The risk or severity of generalized seizure can be increased when Valganciclovir is combined with Imipenem.
Probenecid The serum concentration of Imipenem can be increased when it is combined with Probenecid.
Valproic acid The serum concentration of Valproic acid can be decreased when it is combined with Imipenem.
BCG vaccine The therapeutic efficacy of BCG vaccine can be decreased when used in combination with Imipenem.
Typhoid vaccine The therapeutic efficacy of Typhoid vaccine can be decreased when used in combination with Imipenem.
Dicoumarol The risk or severity of bleeding can be increased when Imipenem is combined with Dicoumarol.
Phenindione The risk or severity of bleeding can be increased when Imipenem is combined with Phenindione.
Warfarin The risk or severity of bleeding can be increased when Imipenem is combined with Warfarin.
Phenprocoumon The risk or severity of bleeding can be increased when Imipenem is combined with Phenprocoumon.
Acenocoumarol The risk or severity of bleeding can be increased when Imipenem is combined with Acenocoumarol.
4-hydroxycoumarin The risk or severity of bleeding can be increased when Imipenem is combined with 4-hydroxycoumarin.
Coumarin The risk or severity of bleeding can be increased when Imipenem is combined with Coumarin.
(R)-warfarin The risk or severity of bleeding can be increased when Imipenem is combined with (R)-warfarin.
Ethyl biscoumacetate The risk or severity of bleeding can be increased when Imipenem is combined with Ethyl biscoumacetate.
Fluindione The risk or severity of bleeding can be increased when Imipenem is combined with Fluindione.
Clorindione The risk or severity of bleeding can be increased when Imipenem is combined with Clorindione.
Diphenadione The risk or severity of bleeding can be increased when Imipenem is combined with Diphenadione.
Tioclomarol The risk or severity of bleeding can be increased when Imipenem is combined with Tioclomarol.
(S)-Warfarin The risk or severity of bleeding can be increased when Imipenem is combined with (S)-Warfarin.
Succinylcholine Succinylcholine may increase the neurotoxic activities of Imipenem.
Reserpine Reserpine may increase the neurotoxic activities of Imipenem.
Ziprasidone Ziprasidone may increase the neurotoxic activities of Imipenem.
Cycloserine Cycloserine may increase the neurotoxic activities of Imipenem.
Amitriptyline Amitriptyline may increase the neurotoxic activities of Imipenem.
Protriptyline Protriptyline may increase the neurotoxic activities of Imipenem.
Vinorelbine Vinorelbine may increase the neurotoxic activities of Imipenem.
Clozapine Clozapine may increase the neurotoxic activities of Imipenem.
Thiethylperazine Thiethylperazine may increase the neurotoxic activities of Imipenem.
Sulpiride Sulpiride may increase the neurotoxic activities of Imipenem.
Loxapine Loxapine may increase the neurotoxic activities of Imipenem.
Remoxipride Remoxipride may increase the neurotoxic activities of Imipenem.
Promazine Promazine may increase the neurotoxic activities of Imipenem.
Prochlorperazine Prochlorperazine may increase the neurotoxic activities of Imipenem.
Teniposide Teniposide may increase the neurotoxic activities of Imipenem.
Droperidol Droperidol may increase the neurotoxic activities of Imipenem.
Imipramine Imipramine may increase the neurotoxic activities of Imipenem.
Chlorpromazine Chlorpromazine may increase the neurotoxic activities of Imipenem.
Haloperidol Haloperidol may increase the neurotoxic activities of Imipenem.
Triflupromazine Triflupromazine may increase the neurotoxic activities of Imipenem.
Cyclophosphamide Cyclophosphamide may increase the neurotoxic activities of Imipenem.
Nortriptyline Nortriptyline may increase the neurotoxic activities of Imipenem.
Vincristine Vincristine may increase the neurotoxic activities of Imipenem.
Amoxapine Amoxapine may increase the neurotoxic activities of Imipenem.
Fluphenazine Fluphenazine may increase the neurotoxic activities of Imipenem.
Stavudine Stavudine may increase the neurotoxic activities of Imipenem.
Thioridazine Thioridazine may increase the neurotoxic activities of Imipenem.
Moricizine Moricizine may increase the neurotoxic activities of Imipenem.
Trimipramine Trimipramine may increase the neurotoxic activities of Imipenem.
Risperidone Risperidone may increase the neurotoxic activities of Imipenem.
Trifluoperazine Trifluoperazine may increase the neurotoxic activities of Imipenem.
Perphenazine Perphenazine may increase the neurotoxic activities of Imipenem.
Flupentixol Flupentixol may increase the neurotoxic activities of Imipenem.
Ethanol Ethanol may increase the neurotoxic activities of Imipenem.
Didanosine Didanosine may increase the neurotoxic activities of Imipenem.
Cyclobenzaprine Cyclobenzaprine may increase the neurotoxic activities of Imipenem.
Mesoridazine Mesoridazine may increase the neurotoxic activities of Imipenem.
Acetophenazine Acetophenazine may increase the neurotoxic activities of Imipenem.
Promethazine Promethazine may increase the neurotoxic activities of Imipenem.
Pimozide Pimozide may increase the neurotoxic activities of Imipenem.
Doxepin Doxepin may increase the neurotoxic activities of Imipenem.
Desipramine Desipramine may increase the neurotoxic activities of Imipenem.
Clindamycin Clindamycin may increase the neurotoxic activities of Imipenem.
Tubocurarine Tubocurarine may increase the neurotoxic activities of Imipenem.
Paclitaxel Paclitaxel may increase the neurotoxic activities of Imipenem.
Aripiprazole Aripiprazole may increase the neurotoxic activities of Imipenem.
Chlorprothixene Chlorprothixene may increase the neurotoxic activities of Imipenem.
Clomipramine Clomipramine may increase the neurotoxic activities of Imipenem.
Decamethonium Decamethonium may increase the neurotoxic activities of Imipenem.
Alimemazine Alimemazine may increase the neurotoxic activities of Imipenem.
Paliperidone Paliperidone may increase the neurotoxic activities of Imipenem.
Lithium cation Lithium cation may increase the neurotoxic activities of Imipenem.
Methotrimeprazine Methotrimeprazine may increase the neurotoxic activities of Imipenem.
Periciazine Imipenem may increase the neurotoxic activities of Periciazine.
Acepromazine Imipenem may increase the neurotoxic activities of Acepromazine.
Aceprometazine Imipenem may increase the neurotoxic activities of Aceprometazine.
Molindone Imipenem may increase the neurotoxic activities of Molindone.
Pipotiazine Imipenem may increase the neurotoxic activities of Pipotiazine.
Thioproperazine Imipenem may increase the neurotoxic activities of Thioproperazine.
Thiothixene Imipenem may increase the neurotoxic activities of Thiothixene.
Zuclopenthixol Imipenem may increase the neurotoxic activities of Zuclopenthixol.
Lincomycin Imipenem may increase the neurotoxic activities of Lincomycin.
Amineptine Imipenem may increase the neurotoxic activities of Amineptine.
Fluspirilene Imipenem may increase the neurotoxic activities of Fluspirilene.
Osanetant Imipenem may increase the neurotoxic activities of Osanetant.
Bifeprunox Imipenem may increase the neurotoxic activities of Bifeprunox.
Iloperidone Imipenem may increase the neurotoxic activities of Iloperidone.
Pimavanserin Imipenem may increase the neurotoxic activities of Pimavanserin.
BL-1020 Imipenem may increase the neurotoxic activities of BL-1020.
Cariprazine Imipenem may increase the neurotoxic activities of Cariprazine.
Sertindole Imipenem may increase the neurotoxic activities of Sertindole.
Asenapine Imipenem may increase the neurotoxic activities of Asenapine.
Amisulpride Imipenem may increase the neurotoxic activities of Amisulpride.
Lurasidone Imipenem may increase the neurotoxic activities of Lurasidone.
Perospirone Imipenem may increase the neurotoxic activities of Perospirone.
Amperozide Imipenem may increase the neurotoxic activities of Amperozide.
Dimetacrine Imipenem may increase the neurotoxic activities of Dimetacrine.
Cyamemazine Imipenem may increase the neurotoxic activities of Cyamemazine.
Butriptyline Imipenem may increase the neurotoxic activities of Butriptyline.

Target Protein

Penicillin-binding protein 2 mrdA
Penicillin-binding protein 1B mrcB
Penicillin-binding protein 1A mrcA
Penicillin-binding protein 3 pbpC
Penicillin-binding protein 4 pbp4
Beta-lactamase blaB

Referensi & Sumber

Synthesis reference: Maurizio Zenoni, "Imipenem production process." U.S. Patent US20020095034, issued July 18, 2002.
Artikel (PubMed)
  • PMID: 19076841
    Kattan JN, Villegas MV, Quinn JP: New developments in carbapenems. Clin Microbiol Infect. 2008 Dec;14(12):1102-11. doi: 10.1111/j.1469-0691.2008.02101.x.
  • PMID: 3530614
    Pastel DA: Imipenem-cilastatin sodium, a broad-spectrum carbapenem antibiotic combination. Clin Pharm. 1986 Sep;5(9):719-36.
  • PMID: 1382937
    Buckley MM, Brogden RN, Barradell LB, Goa KL: Imipenem/cilastatin. A reappraisal of its antibacterial activity, pharmacokinetic properties and therapeutic efficacy. Drugs. 1992 Sep;44(3):408-44.
  • PMID: 9573653
    Richerson MA, Ambrose PG, Quintiliani R, Nightingale CH: Formulary review of the carbapenems: comparison of imipenem/cilastatin and meropenem. Conn Med. 1998 Mar;62(3):165-9.
  • PMID: 3859213
    Birnbaum J, Kahan FM, Kropp H, MacDonald JS: Carbapenems, a new class of beta-lactam antibiotics. Discovery and development of imipenem/cilastatin. Am J Med. 1985 Jun 7;78(6A):3-21.
  • PMID: 1921491
    Hellinger WC, Brewer NS: Imipenem. Mayo Clin Proc. 1991 Oct;66(10):1074-81.
  • PMID: 6365872
    Kahan FM, Kropp H, Sundelof JG, Birnbaum J: Thienamycin: development of imipenen-cilastatin. J Antimicrob Chemother. 1983 Dec;12 Suppl D:1-35.
  • PMID: 8741235
    Balfour JA, Bryson HM, Brogden RN: Imipenem/cilastatin: an update of its antibacterial activity, pharmacokinetics and therapeutic efficacy in the treatment of serious infections. Drugs. 1996 Jan;51(1):99-136. doi: 10.2165/00003495-199651010-00008.
Menampilkan 8 dari 10 artikel.
Textbook
  • ISBN: 978-1-25-958473-2
    Brunton LL, Hilal-Dandan R, Knollmann BC. eds (2018). Goodman & Gilman's: The Pharmacological Basis of Therapeutics (13th ed.). McGraw-Hill Education.

Contoh Produk & Brand

Produk: 33 • International brands: 1
Produk
  • Imipenem
    Powder • 1 kg/1kg • Not applicable • US
  • Imipenem and Cilastatin
    Injection, powder, for solution • - • Intravenous • US • Generic • Approved
  • Imipenem and Cilastatin
    Injection, powder, for solution • - • Intravenous • US • Generic • Approved
  • Imipenem and Cilastatin
    Injection, powder, for solution • - • Intravenous • US • Generic • Approved
  • Imipenem and Cilastatin
    Injection, powder, for solution • - • Intravenous • US • Generic • Approved
  • Imipenem and Cilastatin
    Injection, powder, for solution • - • Intravenous • US • Generic • Approved
  • Imipenem and Cilastatin
    Injection, powder, for solution • - • Intravenous • US • Generic • Approved
  • Imipenem and Cilastatin for Injection
    Powder, for solution • - • Intravenous • Canada • Approved
Menampilkan 8 dari 33 produk.
International Brands
  • Tienamycin

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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