Cilastatin sodium

Cilastatin sodium is the sodium salt of cilastatin, which is a dipeptidase inhibitor of renal enzyme dehydropeptidase-I and leukotriene D4 peptidase. It inhibits metabolism of LTD4 to LTE4 and the hydrolysis of β-lactam antibiotics. It reduces toxic accumulation of cyclosporin A in kidney proximal tubule epithelial cells. It can be combined intravenously with imipenem in order to protect it from dehydropeptidase. It suppresses both host and target metabolism of the broad-spectrum antibiotic imipenem, improving its efficacy. It usually confers antibiotic resistance to certain bacteria because itself does not have antibiotic activity. It has nephroprotective effects.

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