Ertapenem: a new carbapenem.

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Odenholt I

Ertapenem: a new carbapenem.

Expert Opin Investig Drugs. 2001 Jun;10(6):1157-66.

PubMed ID

11772242 [ View in PubMed

]

Abstract

Ertapenem is a new 1-beta-methyl carbapenem, stable to dehydropeptidase, which binds preferable to penicillin-binding proteins (PBP) 2 and 3. Ertapenem has a broad antibacterial spectrum with MIC90 values < 0.5 mg/l for penicillin-susceptible Streptococcus pneumoniae, Streptococcus pyogenes, methicillin-sensitive Staphylococcus aureus, Haemophilus influenzae, Moraxella catarrhalis, Escherichia coli, Citrobacter spp., Klebsiella spp., Serratia spp., Proteus spp., Clostridium perfringens, Fusobacterium spp. Peptostreptococcus spp. and anaerobic Streptococcus spp. Ertapenem exhibits a bactericidal mode of action as shown by time-killing curves and exhibits a short PAE of 1.4 - 2.6 h against the Gram-positive strains but no PAE against Gram-negative strains. In an infection model in mice, it has been shown that ertapenem and imipenem were highly efficacious at a level of 2 mg/kg in bacterial clearance in comparison to ceftriaxone, cefepime, ceftazidime, cefazolin, cefonicid, cefotaxime and meropenem. In comparison to other available carbapenems, ertapenem has a long half-life of 4.5 h and is developed as a single daily dose carbapenem. The protein binding is dose-dependent and is estimated to 94% at concentrations under 100 mg/l and approximately 85% at 300 mg/l. Cmax after a dose of 1 g in healthy volunteers has been estimated to 190 mg/l. Given the pharmacokinetic/pharmacodynamic data, it may be predicted that ertapenem will have an effect on most Gram-positive and Gram-negative bacteria with the exception of Pseudomonas aeruginosa, Enterococcus spp. and Acinetobacter spp. For pathogens with a MIC of 0.5 mg/l, the estimated T > MIC will be 50% (of 24 h) and for pathogens with a MIC of 1 mg/l 31%. For anaerobic bacteria with MIC values between 1-2 mg/l, the T > MIC may not be sufficient for bacterial eradication. However, clinical trials have to confirm this hypothesis.

DrugBank Data that Cites this Article

Drugs

Ertapenem

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Ertapenem	Penicillin-binding protein 2	Protein	Haemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd)	Yes	Inhibitor	Details