Bioavailability
Intramuscular injection:

imipenem: 60–75%
cilastatin: 95–100%

Distribution
The drug is distributed rapidly and widely to most tissues and fluids, including sputum, pleural fluid, peritoneal fluid, interstitial fluid, bile, aqueous humor, reproductive organs, and bone; highest concentrations occur in pleural fluid, interstitial fluid, peritoneal fluid, and reproductive organs; low concentrations occur in CSF; it crosses the placenta, and enters breast milk

Protein binding
imipenem: 13–21%
cilastatin, 40%

Metabolism
Imipenem is metabolized in the kidney by dehydropeptidase 1; activity is blocked by cilastatin. Elimination
Half-life (both drugs): 60 min; prolonged with renal impairment. Excretion (both drugs): Urine (~70% as unchanged drug)

Availability and description
Primaxin IV is a combination of imipenem, cilastatin sodium, and sodium bicarbonate which is added as a buffer. Primaxin IM lacks the sodium bicarbonate buffer. See also
Imipenem/cilastatin/relebactam

References
External links
"Cilastatin mixture with Imipenem". Drug Information Portal. U.S. National Library of Medicine.
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