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Imipenem/ cilastatin is a broad spectrum beta-lactam antibiotic containing equal quantities of imipenem and cilastatin. It is related to the penicillin/cephalosporin family of antibiotics but is classified as belonging to the carbapenem class.
Imipenem is a potent inhibitor of bacterial cell wall synthesis and is bactericidal against a broad spectrum of pathogens. It is resistant to degradation by bacterial β-lactamases. Cilastatin is an inhibitor of dehydropeptidase I, an enzyme found in the brush border of the renal tubules. It is given as the sodium salt with imipenem to prevent its renal metabolism and protect against nephrotoxic effects.
Absorption: IM admin: 60-75% (imipenem); 95-100% (cilastatin).
Distribution: Rapidly and widely distributed to most tissues and fluids. Protein binding: 20% (imipenem) and 40% (cilastatin).
Metabolism Imipenem: Metabolised renally by dehydropeptidase I; cilastatin: Partly metabolised
Excretion Via urine (about 70% as unchanged drug). Half-life: 2-3 hours (imipenem after IM admin).