Cilapenem
Cilapenem Uses, Dosage, Side Effects, Food Interaction and all others data.
Cilapenem is a semisynthetic thienamycin that has a wide spectrum of antibacterial activity against gram-negative and gram-positive aerobic and anaerobic bacteria, including many multiresistant strains. It is stable to many beta-lactamases. Similar compounds include meropenem, known for having greater activity against Gram negative bacteria, and the newer ertapenem which exhibits a longer half-life due to increased binding to plasma proteins. Cilapenem is commonly used in combination with cilastatin and is now available in a triple-drug product with cilastatin and relebactam which was recently approved by the FDA. Cilapenem was first approved by the FDA in November 1985 as the combination product Primaxin marketed by Merck & Co.
Cilapenem is a beta-lactam antibiotic belongings to the subgroup of carbapenems. Cilapenem 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.
| Trade Name | Cilapenem |
| Generic | Imipenem |
| Imipenem Other Names | Imipenem, Imipenemum |
| Weight | 500mg |
| Type | Injection |
| Formula | C12H17N3O4S |
| Weight | Average: 299.346 Monoisotopic: 299.093976737 |
| Protein binding | Imipenem is 20% bound to plasma proteins. |
| Groups | Approved |
| Therapeutic Class | |
| Manufacturer | Matrix Pharma |
| Available Country | Pakistan |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Cilapenem is a carbapenem antibiotic normally administered with cilastatin to treat a variety of infections.
Cilapenem 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.
Cilapenem is also used to associated treatment for these conditions: Bloodstream Infections, Bone and Joint Infections, Complicated Intra-Abdominal Infections, Complicated Urinary Infection, Complicated Urinary Tract Infection, Endocarditis caused by staphylococcus aureus, Gynaecological infection, Intra-Abdominal Infections, Lower respiratory tract infection bacterial, Pyelonephritis, Skin and Subcutaneous Tissue Bacterial Infections, Uncomplicated Urinary Tract Infections
How Cilapenem works
Cilapenem 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.
Toxicity
In case of overdose with the combination product, including relebactam and cilastatin, it is recommended to provide supportive care. Cilapenem, cilastatin, and relebactam may be removed via hemodialysis.
Food Interaction
No interactions found.Volume of Distribution
The reported volume of distribution for imipenem ranges from 0.23-0.31 L/kg.
Elimination Route
Cilapenem is not effectively absorbed from the gastrointestinal tract and therefore must be administered parenterally. The bioavailability of the IM injection is 89%.
Half Life
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.
Clearance
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.
Elimination Route
Approximately 70% of imipenem is excreted in the urine as the parent drug.
Innovators Monograph
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