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| AHFS/Drugs.com | International Drug Names |
| MedlinePlus | a686013 |
| Routes of administration | IV |
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| CompTox Dashboard(EPA) | |
| ECHA InfoCard | 100.072.592 |
| Chemical and physical data | |
| Formula | C16H26N2O5S |
| Molar mass | 358.45 g·mol−1 |
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Cilastatin inhibits the humanenzymedehydropeptidase.[1]
Dehydropeptidase is an enzyme found in thekidney and is responsible for degrading theantibioticimipenem. Cilastatin can therefore be combinedintravenously with imipenem in order to protect it from degradation, prolonging its antibacterial effect.
Imipenem alone is an effective antibiotic and can be given without cilastatin. Cilastatin itself does not have antibiotic activity, although it has been proved to be active against a zinc-dependentbeta-lactamase that usually confers antibiotic resistance to certain bacteria, more precisely, thecarbapenem family of antibiotics. This property is due to the physicochemical similarities betweenmembrane dipeptidase (MDP), the compound it is usually set to target, and the bacterial metallo-beta-lactamase carried by the CphA gene.[1] The combination allows the antibiotic to be more effective by changing thepharmacokinetics involved. Thusimipenem/cilastatin, likeamoxicillin/clavulanic acid, is a commonly used combination product.
