Peringatan Keamanan

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

Cilastatin

DB01597

small molecule approved investigational

Deskripsi

Cilastatin is an inhibitor of renal dehydropeptidase, an enzyme responsible for both the metabolism of thienamycin beta-lactam antibiotics as well as conversion of leukotriene D4 to leukotriene E4. Since the antibiotic, imipenem, is one such antibiotic that is hydrolyzed by dehydropeptidase, cilastatin is used in combination with imipenem to prevent its metabolism. The first combination product containing both drugs was approved by the FDA in November of 1985 under the trade name Primaxin, marketed by Merck & Co.L7628 A newer triple-drug product was approved in July 2019 under the trade name Recarbrio which also contains relebactam.L4894

Struktur Molekul 2D

Berat 358.453
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half-life of cilastatin is approximately 1h.[L7568,L7526,A181271]
Volume Distribusi Cilastatin has a volume of distribution of 14.6-20.1L.[A181271]
Klirens (Clearance) Cilastatin has a total clearance of 0.2 L/h/kg and a renal clearance of 0.10-0.16 L/h/kg.[A181271]

Absorpsi

Data absorpsi tidak tersedia.

Metabolisme

Data metabolisme tidak tersedia.

Rute Eliminasi

Cilastatin is reported by official FDA labeling to be 70% excreted in the urine, however published literature has reported values as high as 98%.A181271

Interaksi Obat

80 Data
Succinic acid The excretion of Succinic acid can be decreased when combined with Cilastatin.
Citrulline The excretion of Citrulline can be decreased when combined with Cilastatin.
Pravastatin The excretion of Pravastatin can be decreased when combined with Cilastatin.
Oseltamivir The excretion of Oseltamivir can be decreased when combined with Cilastatin.
Cefotiam The excretion of Cefotiam can be decreased when combined with Cilastatin.
Conjugated estrogens The excretion of Conjugated estrogens can be decreased when combined with Cilastatin.
Tenofovir disoproxil The excretion of Tenofovir disoproxil can be decreased when combined with Cilastatin.
Piperacillin The excretion of Piperacillin can be decreased when combined with Cilastatin.
Indomethacin The excretion of Indomethacin can be decreased when combined with Cilastatin.
Aminohippuric acid The excretion of Aminohippuric acid can be decreased when combined with Cilastatin.
Trifluridine The excretion of Trifluridine can be decreased when combined with Cilastatin.
Allopurinol The excretion of Allopurinol can be decreased when combined with Cilastatin.
Zidovudine The excretion of Zidovudine can be decreased when combined with Cilastatin.
Cimetidine The excretion of Cimetidine can be decreased when combined with Cilastatin.
Cefdinir The excretion of Cefdinir can be decreased when combined with Cilastatin.
Methotrexate The excretion of Methotrexate can be decreased when combined with Cilastatin.
Cephalexin The excretion of Cephalexin can be decreased when combined with Cilastatin.
Valaciclovir The excretion of Valaciclovir can be decreased when combined with Cilastatin.
Levocarnitine The excretion of Levocarnitine can be decreased when combined with Cilastatin.
Leucovorin The excretion of Leucovorin can be decreased when combined with Cilastatin.
Fluorescein The excretion of Fluorescein can be decreased when combined with Cilastatin.
Hydrocortisone The excretion of Hydrocortisone can be decreased when combined with Cilastatin.
Tetracycline The excretion of Tetracycline can be decreased when combined with Cilastatin.
Estradiol The excretion of Estradiol can be decreased when combined with Cilastatin.
Acyclovir The excretion of Acyclovir can be decreased when combined with Cilastatin.
Cefaclor The excretion of Cefaclor can be decreased when combined with Cilastatin.
Ranitidine The excretion of Ranitidine can be decreased when combined with Cilastatin.
Quinapril The excretion of Quinapril can be decreased when combined with Cilastatin.
Bumetanide The excretion of Bumetanide can be decreased when combined with Cilastatin.
Dinoprostone The excretion of Dinoprostone can be decreased when combined with Cilastatin.
Famotidine The excretion of Famotidine can be decreased when combined with Cilastatin.
Fexofenadine The excretion of Fexofenadine can be decreased when combined with Cilastatin.
Benzylpenicillin The excretion of Benzylpenicillin can be decreased when combined with Cilastatin.
Rosuvastatin The excretion of Rosuvastatin can be decreased when combined with Cilastatin.
Captopril The excretion of Captopril can be decreased when combined with Cilastatin.
Sitagliptin The excretion of Sitagliptin can be decreased when combined with Cilastatin.
Cefazolin The excretion of Cefazolin can be decreased when combined with Cilastatin.
Ceftizoxime The excretion of Ceftizoxime can be decreased when combined with Cilastatin.
Cefacetrile The excretion of Cefacetrile can be decreased when combined with Cilastatin.
Ceftibuten The excretion of Ceftibuten can be decreased when combined with Cilastatin.
Tazobactam The excretion of Tazobactam can be decreased when combined with Cilastatin.
Cyclic adenosine monophosphate The excretion of Cyclic adenosine monophosphate can be decreased when combined with Cilastatin.
Cholic Acid The excretion of Cholic Acid can be decreased when combined with Cilastatin.
Glutaric Acid The excretion of Glutaric Acid can be decreased when combined with Cilastatin.
Oxalic Acid The excretion of Oxalic Acid can be decreased when combined with Cilastatin.
Taurocholic acid The excretion of Taurocholic acid can be decreased when combined with Cilastatin.
Doripenem The excretion of Doripenem can be decreased when combined with Cilastatin.
Saxagliptin The excretion of Saxagliptin can be decreased when combined with Cilastatin.
Ellagic acid The excretion of Ellagic acid can be decreased when combined with Cilastatin.
Cefaloridine The excretion of Cefaloridine can be decreased when combined with Cilastatin.
Avibactam The excretion of Avibactam can be decreased when combined with Cilastatin.
Eluxadoline The excretion of Eluxadoline can be decreased when combined with Cilastatin.
Silibinin The excretion of Silibinin can be decreased when combined with Cilastatin.
Tenofovir alafenamide The excretion of Tenofovir alafenamide can be decreased when combined with Cilastatin.
Baricitinib The serum concentration of Baricitinib can be increased when it is combined with Cilastatin.
Tenofovir The excretion of Tenofovir can be decreased when combined with Cilastatin.
Hydrochlorothiazide The excretion of Hydrochlorothiazide can be decreased when combined with Cilastatin.
Dexamethasone The excretion of Dexamethasone can be decreased when combined with Cilastatin.
Oxytetracycline The excretion of Oxytetracycline can be decreased when combined with Cilastatin.
Polythiazide The excretion of Polythiazide can be decreased when combined with Cilastatin.
Prednisolone phosphate The excretion of Prednisolone phosphate can be decreased when combined with Cilastatin.
Dexamethasone acetate The excretion of Dexamethasone acetate can be decreased when combined with Cilastatin.
Acamprosate The excretion of Acamprosate can be decreased when combined with Cilastatin.
Pemetrexed Cilastatin may decrease the excretion rate of Pemetrexed which could result in a higher serum level.
Mercaptopurine The excretion of Mercaptopurine can be decreased when combined with Cilastatin.
Valproic acid The excretion of Valproic acid can be decreased when combined with Cilastatin.
Clofarabine The excretion of Clofarabine can be decreased when combined with Cilastatin.
Grepafloxacin The excretion of Grepafloxacin can be decreased when combined with Cilastatin.
Cidofovir The excretion of Cidofovir can be decreased when combined with Cilastatin.
Stavudine The excretion of Stavudine can be decreased when combined with Cilastatin.
Lamivudine The excretion of Lamivudine can be decreased when combined with Cilastatin.
Adefovir dipivoxil The excretion of Adefovir dipivoxil can be decreased when combined with Cilastatin.
Didanosine The excretion of Didanosine can be decreased when combined with Cilastatin.
Zalcitabine The excretion of Zalcitabine can be decreased when combined with Cilastatin.
Levofloxacin The excretion of Levofloxacin can be decreased when combined with Cilastatin.
Cyclosporine The excretion of Cyclosporine can be increased when combined with Cilastatin.
Vadadustat The serum concentration of Vadadustat can be increased when it is combined with Cilastatin.
Sulbactam The excretion of Sulbactam can be decreased when combined with Cilastatin.
Seladelpar The excretion of Seladelpar can be decreased when combined with Cilastatin.
Sulopenem etzadroxil The serum concentration of Sulopenem etzadroxil can be increased when it is combined with Cilastatin.

Target Protein

Dipeptidase 1 DPEP1

Referensi & Sumber

Synthesis reference: Yatendra Kumar, "Process for the preparation of amorphous cilastatin sodium." U.S. Patent US20040152780, issued August 05, 2004.
Artikel (PubMed)
  • PMID: 7492120
    Keynan S, Hooper NM, Felici A, Amicosante G, Turner AJ: The renal membrane dipeptidase (dehydropeptidase I) inhibitor, cilastatin, inhibits the bacterial metallo-beta-lactamase enzyme CphA. Antimicrob Agents Chemother. 1995 Jul;39(7):1629-31.
  • 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: 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.
  • PMID: 3863619
    Koller M, Brom J, Raulf M, Konig W: Cilastatin (MK 0791) is a potent and specific inhibitor of the renal leukotriene D4-dipeptidase. Biochem Biophys Res Commun. 1985 Sep 16;131(2):974-9. doi: 10.1016/0006-291x(85)91335-x.

Contoh Produk & Brand

Produk: 33 • International brands: 0
Produk
  • Cilastatin Sodium Sterile
    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.

Sekuens Gen/Protein (FASTA)

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