無水イミペネム

Pharmaceuticals -> Listed in ZINC15

Pharmaceuticals -> Antibiotics

Pharmaceuticals -> Antibiotics

FDA approved drugs -> Active ingredient

FDA approved drugs -> Active ingredient

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.

Drug-Induced Liver Injury Severity and Toxicity (DILIst)

Imipenem

DILI Positive

Intravenous

DOI:10.1016/j.drudis.2019.09.022

Imipenem is a beta-lactam antibiotic belongings to the subgroup of carbapenems. Imipenem is active against aerobic and anaerobic Gram positive as well as Gram negative bacteria including <i>Pseudomonas aeruginosa</i> and the <i>Enterococcus</i>. It exerts a bactericidal effects by disrupting cell wall synthesis.

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 penicillin-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 inhibition of PBPs prevents the bacterial cell from adding to the peptidoglycan polymer which forms the bacterial cell wall eventually leading to cell death.

Imipenem is metabolized by renal dehydropeptidase.

Renal. Half Life: 1 hour

Q20IM7HE75

IMIPENEM ANHYDROUS

Chemical Structure [CS] - Carbapenems

Established Pharmacologic Class [EPC] - Penem Antibacterial

Imipenem anhydrous is a Penem Antibacterial.

Imipenem is not effectively absorbed from the gastrointestinal tract and therefore must be administered parenterally. The bioavailability of the IM injection is 89%.

Approximately 70% of imipenem is excreted in the urine as the parent drug.

The reported volume of distribution for imipenem ranges from 0.23-0.31 L/kg.

The total clearance of imipenem is 0.2 L/h/kg. When used alone, the renal clearance is 0.05 L/h/kg. In combination with cilastatin the renal clearance of imipenem is 0.15 L/h/kg, likely due to the increased concentration of the parent drug.

Use (kg) in Switzerland (2009): >100

For the treatment of bacterial infections caused by susceptible bacteria.