Imipenem

299.35

299.35

264-734-5

Q20IM7HE75

759901|717864

DTXSID2023143

J01DH51

29419000

148.25000

-2.78

Solid

1.6±0.1 g/cm3

106-111 C

530.2±60.0 °C at 760 mmHg

274.5±32.9 °C

1.721

7.76e-01 g/L

3.2None

169.26 Ų [M+H]+

36/37/38

26-27-36/37/39

Xi

In case of overdose with the combination product, including [relebactam] and [cilastatin], it is recommended to provide supportive care. Imipenem, cilastatin, and relebactam may be removed via hemodialysis.

In large clinical trials, imipenem was associated with transient and asymptomatic elevations in serum aminotransferase levels in approximately 6% of patients given the drug for 5 to 14 days. More serious hepatic injury from imipenem/cilastatin is rare, but jaundice and liver test abnormalities have been reported in 0.1% of patients in prospective trials of the agent. Several instances of cholestatic jaundice arising during or shortly after therapy have been reported with imipenem-cilastatin and other carbapenems. The latency to onset has been within 1 to 3 weeks and the pattern of enzyme elevations is usually cholestatic. Immunoallergic features can occur, but autoantibodies are rare. The course is usually self-limiting, but at least one case of vanishing bile duct syndrome related to the carbapenems has been reported. Imipenem and other carbapenems have not been linked to cases of acute liver failure in the published literature, but the product label for imipenem mentions that instances of jaundice and severe liver injury attributed to imipenem have been reported to the sponsor.

Imipenem is 20% bound to plasma proteins.

Imipenem is indicated, in combination with [cilastatin] with or without [relebactam], for the treatment of bacterial infections including respiratory, skin, bone, gynecologic, urinary tract, and intra-abdominal as well as septicemia and endocarditis.|FDA Label

AntiInfective Agents

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 Pseudomonas aeruginosa and the Enterococcus. It exerts a bactericidal effects by disrupting cell wall synthesis.

Substances that inhibit the growth or reproduction of BACTERIA. (See all compounds classified as Anti-Bacterial Agents.)

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.

Imipenem is metabolized by renal dehydropeptidase.

When given via IV injection imipenem has a half-life of 1 h. The apparent half-life of the IM injection ranges from 1.3-5.1 h, likely due to slower absorption form the injection site.

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.

Anhydrous Imipenem

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients