Ertapenem

Molecular formula C22H2SN3O7S Molecular weight 475.52 CAS Registry No 153832-46-3 Merck Index 13, 3706 

Sample preparation Filter (Amicon Centrifree) 1 mL plasma while centrifuging at 1500 g for 15 min, mix an aliquot of the filtrate with an equal volume of buffer, inject a 50 jiL aliquot. (Prepare the buffer by dissolving 15.5 g sodium 2-[2V-morpholino]ethane sulfonate (MES) and 5.58 g 2-[2V-morpholino]ethane sulfonic acid in 100 mL water. Dilute this stock solution 10-fold before use, pH 6.5.) 

Mobile phase MeOH 25 mM phosphate buffer 10 90, apparent pH 6.5 Flowrate 2 Injection volume 50 Detector UV 300 

Musson, D.G. Birk, K.L. Kitchen, C.J. Zhang, J. Hsieh, J.Y.K. Fang, W. Majumdar, A.K. Rogers, J.D. Assay methodology for the quantitation of unbound ertapenem, a new carbapenem antibiotic, in hmnan plasma, J.Chromatogr.B, 2003, 783, 1-9. 

Sample preparation Mix 50 p,L 50 xg/mL IS with 200 p.L serum, add 800 p.L MeCN, vortex briefiy, centrifuge at 2600 g for 10 min. remove the supernatant and add it to 2.5 mL dichloromethane, vortex hriefiy, centrifuge, inject an aliquot of the aqueous layer. 

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Injection drug use MSSA GAS Gram-negatives Anaerobes CA-MRSAd Amoxicillin-clavulanate 500 mg every 8 hours Fluoroquinolone + clindamycin 300 mg every 6 hours TMP-SMX DS 1-2 tabs every 12 hours + clindamycin 300 mg every 6 hours Ampicillin-sulbactam 3 g every 6 hours Piperacillin-tazobactam 3.375 g every 6 hours Ceftriaxone 1 g daily + clindamycin 600 mg every 8 hours Ertapenem 1 g daily... 

Other Imipenem/cilistatin, meropenem, ertapenem, or extended-spectrum penicillins with B-lactamase inhibitor 1. Ciprofloxacin with metronidazole 2. Aztreonam with clindamycin or metronidazole 3. Antianaerobic cephalosporins.3... 

Gangrenous or Imipenem/cilastatin, meropenem, ertapenem, 1. Aztreonam with clindamycin or metronidazole... 

These agents have broad-spectrum activity, including gram-positive, gram-negative, and anaerobic bacteria. Imipenem and meropenem are active against P. aeruginosa and enterococci, but ertapenem is not. All may be associated with Candida superinfections. Rarely used for UTIs. 

Pediatric6 100-150 mg/kg per day IV in divided doses every 8 hours Ertapenem 5 ... 

Community-acquired pneumonia Health care-associated, ventilator-asociated, or nosocomial pneumonia (Early onset no risk factors for MDR pathogens) Third-generation cephalosporin plus a macrolide or doxycycline Third-generation cephalosporin OR Fluoroquinolone OR Ampicillin-sulbactam OR Ertapenem... 

Treatment for septic patients with hospital-acquired, ventilator-acquired, and health care-associated pneumonia is dependent on risk factors for multi-drug resistant (MDR) organisms (Fig. 79-2). Recommended treatment for patients with no MDR risk factors are third-generation cephalosporins, fluoroquinolones, ampicillin-sulbactam, or ertapenem (see Table 79-3).35 Recommended treatment for patients with MDR risk factors are P-lactam/p-lactamase inhibitors (piperacillin-tazobactam), antipseudomonal cephalosporin, or carbapenem, plus an aminoglycoside, plus vancomycin or linezolid (see Table 79-3).35 If an aminoglycoside is undesirable, a antipseudomonal fluoroquinolone may be utilized with a P-lactam/p-lactamase inhibitor. 

Metronidazole, clindamycin, doxycydine,e cefazolin,c imipenem," meropenem," or ertapenem"... 

Cefuroximej fluoroquinolone,b,r BLIQg imipenem,0 meropenem,0 or ertapenem Legionella spp. 

Trimethoprim-sulfamethoxazole, aztreonam/ imipenem," meropenem," or ertapenem Pseudomonas aeruginosa... 

Cefotaxime, ceftriaxone, ampicillin-sulbactam, or ertapenem ertapenem was recently approved for such use (in once-daily parenteral treatment) but little experience is available. 

Monotherapy with imipenem 0.5 g IV every 6-8 hours, meropenem 1 g IV every 8 hours, ertapenem 1 g IV every 24 hours, extended-spectrum penicillins with a /3-lactamase inhibitor (piperacillin/tazobactam 4.5 g IV every 6 hours), or tigecycline 100 mg IV as loading dose, then 50 mg IV every 12 hours... 

Patients with serious injuries or clenched-fist injuries should be started on IV antibiotics (cefoxitin 1 g every 6 to 8 hours), ampiciUin-sulbactam (1.5 to 3 g every 6 hours), or ertapenem (1 g every 24 hours). 

A number of recent publications indicate that the antibacterial field has adopted the concept of comparing free drug concentration at the site of action to in vitro drug potency reported as MIC [24-26]. A study of the antibacterial ertapenem in healthy volunteers was carried out to provide support for its use in skin and skin-structure infections [27]. Using microdialysis techniques, unbound drug concentrations in muscle and subcutaneous tissues were sampled at... 

Livermore DM, Sefton AM, Scott GM. (2003) Properties and potential of 274 ertapenem. J Antimicrob Chemother 52 331-344. 

Hammond ML. (2004) Ertapenem A Group 1 carbapenem with distinct antibacterial and pharmacological properties. J Antimicrob. Chemother 53 ii7-9. 

Livermore DM, Mushtaq S, Warner M. (2005) Selectivity of ertapenem for Pseudomonas Aeruginosa mutants cross-resistant to other carbapenems. J Antimicrob Chemother 55 306-311. 

Gesser RM, Carrol KA, Teppler H. (2003) Efficacy of ertapenem in the treatment of serious infections caused by Enterobacteriaceae Analysis of pooled clinical trial data. J Antimicrob Chemother 51 1253-1260. 

Bassetti M, Righi E, Fasce R, Molinari MR Rosso R, Di Biagio A, Mussap M, Pallavicini FB, Viscoli C. (2007) Efficacy of Ertapenem in the treatment of early ventilator-associated pneumonia caused by extended-spectrum beta-lactamase-producing organisms in an intensive care unit. J Antimicrob Chemother 60 433 35. 

Parakh A, Krishnamurthy S, Bhattacharya M. (2009) Ertapenem. Kathmandu UnivMedJl 454 60. 

Nix DE, Majumdar AK, DiNubile MJ. (2004) Pharmacokinetics and pharmacodynamics of ertapenem An overview for clinicians. J Antimicrob Chemother 53 23-28. 

Teppler H, Gesser RM, Friedland IR, Woods GL, Meibohm A, Herman G Mistry G Isaacs R. (2004) Safety and tolerability of ertapenem. J Antimicrob Chemother 53 75-81. 

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