Cilastatin inhibits the human

enzyme An enzyme () is a protein that acts as a biological catalyst by accelerating chemical reactions. The molecules upon which enzymes may act are called substrate (chemistry), substrates, and the enzyme converts the substrates into different mol ...

dehydropeptidase Dipeptidases are enzymes secreted by enterocytes into the small intestine. Dipeptidases hydrolyze bound pairs of amino acid Amino acids are organic compounds that contain both amino and carboxylic acid functional groups. Although over 500 ...

Uses

Dehydropeptidase is an enzyme found in the

kidney In humans, the kidneys are two reddish-brown bean-shaped blood-filtering organ (anatomy), organs that are a multilobar, multipapillary form of mammalian kidneys, usually without signs of external lobulation. They are located on the left and rig ...

and is responsible for degrading the

antibiotic An antibiotic is a type of antimicrobial substance active against bacteria. It is the most important type of antibacterial agent for fighting pathogenic bacteria, bacterial infections, and antibiotic medications are widely used in the therapy ...

imipenem Imipenem (trade name Primaxin among others) is a synthetic beta-lactam, β-lactam antibiotic belonging to the carbapenems chemical class. developed by Merck scientists Burton Christensen, William Leanza, and Kenneth Wildonger in the mid-1970s. Car ...

. Cilastatin can therefore be combined

intravenously Intravenous therapy (abbreviated as IV therapy) is a medical technique that administers fluids, medications and nutrients directly into a person's vein. The intravenous route of administration is commonly used for rehydration or to provide nutr ...

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-dependent

beta-lactamase Beta-lactamases (β-lactamases) are enzymes () produced by bacteria that provide multi-resistance to beta-lactam antibiotics such as penicillins, cephalosporins, cephamycins, monobactams and carbapenems ( ertapenem), although carbapene ...

that usually confers antibiotic resistance to certain bacteria, more precisely, the

carbapenem Carbapenems are a class of very effective antibiotic agents most commonly used for treatment of severe bacterial infections. This class of antibiotics is usually reserved for known or suspected multidrug-resistant (MDR) bacterial infections. Si ...

family of antibiotics. This property is due to the physicochemical similarities between

membrane dipeptidase Membrane dipeptidase (, ''renal dipeptidase'', ''dehydropeptidase I (DPH I)'', ''dipeptidase'', ''aminodipeptidase'', ''dipeptide hydrolase'', ''dipeptidyl hydrolase'', ''nonspecific dipeptidase'', ''glycosyl-phosphatidylinositol-anchored renal di ...

(MDP), the compound it is usually set to target, and the bacterial metallo-beta-lactamase carried by the CphA gene. The combination allows the antibiotic to be more effective by changing the

pharmacokinetics Pharmacokinetics (from Ancient Greek ''pharmakon'' "drug" and ''kinetikos'' "moving, putting in motion"; see chemical kinetics), sometimes abbreviated as PK, is a branch of pharmacology dedicated to describing how the body affects a specific su ...

involved. Thus imipenem/cilastatin, like

amoxicillin/clavulanic acid Amoxicillin/clavulanic acid, also known as co-amoxiclav or amox-clav, sold under the brand name Augmentin, among others, is an antibiotic medication used for the treatment of a number of bacterial infections. It is a combination consisting of ...

, is a commonly used combination product.

References

{{Leukotrienergics Hydrolase inhibitors Alpha-Amino acids Amino acid derivatives Thioethers Dicarboxylic acids