Cilastatine
Cilastatine Uses, Dosage, Side Effects, Food Interaction and all others data.
Cilastatine 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. A newer triple-drug product was approved in July 2019 under the trade name Recarbrio which also contains relebactam.
Cilastatine is a chemical compound which inhibits the human enzyme dehydropeptidase. Renal Dehydropeptidase degrades the antibiotic imipenem. Cilastatine is therefore combined intravenously with imipenem in order to protect it from dehydropeptidase and prolong its antibacterial effect. However, cilastatin in and of itself does not have any antibacterial activity. The increased renal excretion of unchanged imipenem appears to prevent proximal tubular necrosis associated with high doses of imipenem.
| Trade Name | Cilastatine |
| Generic | Cilastatin |
| Cilastatin Other Names | Cilastatin, Cilastatina, Cilastatine, Cilastatinum |
| Type | |
| Formula | C16H26N2O5S |
| Weight | Average: 358.453 Monoisotopic: 358.156242642 |
| Protein binding | Cilastatin is plasma protein binding is reported to be 35-40%. |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Cilastatine is a renal dehydropeptidase inhibitor used to prevent degradation of imipenem. Both medications are used together to treat a variety of infections.
Cilastatine is indicated, in combination with imipenem with or without relebactam, for the treatment of bacterial infections including respiratory, skin, bone, gynecologic, urinary tract, and intra-abdominal as well as septicemia and endocarditis.
Cilastatine is also used to associated treatment for these conditions: Bloodstream Infections, Bone and Joint Infections, Complicated Intra-Abdominal Infections, Complicated Urinary Tract Infection, Endocarditis caused by staphylococcus aureus, Gynaecological infection, Intra-Abdominal Infections, Lower respiratory tract infection bacterial, Neutropenic Fever, Pyelonephritis, Skin and Subcutaneous Tissue Bacterial Infections, Surgical Site Infections, Uncomplicated Urinary Tract Infections, Hepatic abscess
How Cilastatine works
Cilastatine is a renal dehydropeptidase-I inhibitor. Since the antibiotic, imipenem, is hydrolyzed by dehydropeptidase-I, which resides in the brush border of the renal tubule, cilastatin is administered with imipenem to block the metabolism of imipenem.
Toxicity
In case of overdose with the combination product, including relebactam and imipenem, it is recommended to provide supportive care. Imipenem, cilastatin, and relebactam may be removed via hemodialysis.
Food Interaction
No interactions found.Volume of Distribution
Cilastatine has a volume of distribution of 14.6-20.1L.
Half Life
The half-life of cilastatin is approximately 1h.
Clearance
Cilastatine has a total clearance of 0.2 L/h/kg and a renal clearance of 0.10-0.16 L/h/kg.
Elimination Route
Cilastatine is reported by official FDA labeling to be 70% excreted in the urine, however published literature has reported values as high as 98%.
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