Ertapenem: review of a new carbapenem

Abstract

The carbapenems are beta-lactam-type antibiotics with an exceptionally broad spectrum of activity. Ertapenem is a new carbapenem developed to address the pharmacokinetic shortcomings (short half-life) of imipenem and meropenem. Ertapenem shares similar structural features with meropenem, including its stability to dehydropeptidase-1, allowing it to be administered without a dehydropeptidase-1 inhibitor. Ertapenem, like imipenem and meropenem, demonstrates broad-spectrum antimicrobial activity against many Gram-positive and -negative aerobes and anaerobes and is resistant to nearly all beta-lactamases, including extended-spectrum beta-lactamases and AmpCs. However, it differs from both imipenem and meropenem in demonstrating limited activity against Enterococcusspp., Pseudomonasaeruginosa and other nonfermentative Gram-negative bacteria commonly associated with nosocomial infections. The extensive protein binding of ertapenem extends the half-life and allows for once-daily dosing. Prospective, multicenter, randomized, double-blind, comparative clinical studies demonstrate similar clinical efficacy of ertapenem compared with other agents. Clinical trials of complicated intra-abdominal infection, acute pelvic infection, complicated skin and soft-structure infection, community-acquired pneumonia and complicated urinary tract infections demonstrated that ertapenem has equivalent efficacy and safety compared with ceftriaxone and piperacillin/tazobactam. Ertapenem is a promising new carbapenem with excellent efficacy and safety for the treatment of a variety of community-acquired infections. It also appears to be of great value as an outpatient parenteral antimicrobial therapy.

Phase 2, Randomized, Double-Blind Study of the Efficacy and Safety of Two Dose Regimens of Eravacycline versus Ertapenem for Adult Community-Acquired Complicated Intra-Abdominal Infections

“…This phase 2, randomized, double-blind study compared two dose regimens of eravacycline with ertapenem, a carbapenem antibiotic with demonstrated effectiveness in cIAI (17)(18)(19) and a recommended first-line empirical monotherapy for the treatment of community-acquired cIAIs (1). Eravacycline, at both dose regimens of 1.5 mg/kg q24h and 1.0 mg/kg q12h, had efficacy comparable to that of ertapenem on clinical and microbiological endpoints.…”

Acinetobacter baumannii: biology and drug resistance — role of carbapenemases

“…Moreover, the MIC values of doripenem are lower than presented by imipenem and meropenem for A. baumannii. The studies concerning analysis of carbapenems MIC 90 values among Acinetobacter spp., revealed more than eightfold higher MIC 90 for ertapenem, comparing to other carbapenems [45][46][47].…”

“…In consequence, increasing of the molecular weight and lipophilicity of the molecule was observed. Structural changes of the molecule also resulted in the increased half-life and decreased permeation through the Gram-negative bacteria cell wall [47].…”

Antibiotics Against Endocarditis – Past, Present and Future (Experimental Data)

“…Subsequent to that study, the carbapenem ertapenem was investigated in combination with linezolid using the same experimental model (Jacqueline et al, 2006). Ertapenem is a parenteral carbapenem antibiotic with a broad antibacterial spectrum and once-a-day dosing that is supported by clinical studies and an extended half-life (Zhanel et al, 2005). In this study, animals were randomly assigned to receive either no treatment (controls), a linezolid regimen mimicking the human dose of 10 mg/kg/12 h, an ertapenem regimen mimicking the human dose of 1 g/day, or a combination of both regimens.…”