Cilastatin (as sodium), Imipenem (as monohydrate)

Indications

Cilastatin (as sodium), Imipenem (as monohydrate) is used for: CILASTATIN
Combined intravenously with imipenem in order to protect it from dehydropeptidase and prolong its antibacterial effect
IMIPENEM
For the treatment of bacterial infections caused by susceptible bacteria

Adult Dose

Child Dose

Renal Dose

Administration

Contra Indications

Precautions

Pregnancy-Lactation

Interactions

Adverse Effects

Side effects of Cilastatin (as sodium), Imipenem (as monohydrate) :

Mechanism of Action

CILASTATIN
Cilastatin is a specific and reversible renal dehydropeptidase-i inhibitor. Since the antibiotic, imipenem, is hydrolyzed by dehydropeptidase-i, which resides in the brush border of the renal tubule, cilastatin is administered with imipenem to block the metabolism and thus the inactivation of imipenem so that antibacterial levels of imipenem can be attained in the urine. The drug also prevents the metabolism of leukotriene d4 to leukotriene e4 through the inhibition of leukotriene d4 dipeptidase
IMIPENEM
Imipenem acts as an antimicrobial through the inhibition of cell wall synthesis of various gram-positive and gram-negative bacteria. This inhibition of cell wall synthesis in gram-negative bateria is attained by binding to pencillin binding proteins (pbps). In e. Coli and selected strains of p. Aeruginosa, imipenem has shown to have the highest affinity to pbp-2, pbp-1a, and pbp-1b. This preferential binding to pbp-2 and pbp-1b results in the direct conversion of the individual cell to a spheroblast, which leads to rapid cell lysis and death without filament formation