Brands, Medical Use, Clinical Data
- Antibacterials for Systemic Use
Brands / Synonyms
For the treatment the following moderate to severe infections caused by susceptible isolates of the designated microorganisms: (1) complicated intra-abdominal infections due to Escherichia coli, Clostridium clostridioforme, Eubacterium lentum, Peptostreptococcus species, Bacteroides fragilis, Bacteroides distasonis, Bacteroides ovatus, Bacteroides thetaiotaomicron, or Bacteroides uniformis, (2) complicated skin and skin structure infections, including diabetic foot infections without osteomyelitis due to Staphylococcus aureus (methicillin susceptible isolates only), Streptococcus agalactiae, Streptococcus pyogenes, Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, Bacteroides fragilis, Peptostreptococcus species, Porphyromonas asaccharolytica, or Prevotella bivia, (3) community acquired pneumonia due to Streptococcus pneumoniae (penicillin susceptible isolates only) including cases with concurrent bacteremia, Haemophilus influenzae (beta-lactamase negative isolates only), or Moraxella catarrhalis, (4) complicated urinary tract infections including pyelonephritis due to Escherichia coli, including cases with concurrent bacteremia, or Klebsiella pneumoniae, (5) acute pelvic infections including postpartum endomyometritis, septic abortion and post surgical gynecologic infections due to Streptococcus agalactiae, Escherichia coli, Bacteroides fragilis, Porphyromonas asaccharolytica, Peptostreptococcus species, or Prevotella bivia.
Ertapenem has in vitro activity against gram-positive and gram-negative aerobic and anaerobic bacteria.
Mechanism of Action
The bactericidal activity of ertapenem results from the inhibition of cell wall synthesis and is mediated through ertapenem binding to penicillin binding proteins (PBPs). In Escherichia coli, it has strong affinity toward PBPs 1a, 1b, 2, 3, 4 and 5 with preference for PBPs 2 and 3. Ertapenem is stable against hydrolysis by a variety of beta-lactamases, including penicillinases, and cephalosporinases and extended spectrum beta-lactamases. Ertapenem is hydrolyzed by metallo-beta-lactamases.
The mean bioavailability is approximately 90%.
Biotrnasformation / Drug Metabolism
The major metabolite is the inactive ring-opened derivative formed by hydrolysis of the β-lactam ring. Ertapenem did not inhibit metabolism mediated by cytochrome P450 (CYP) isoforms 1A2, 2C9, 2C19, 2D6, 2E1, or 3A4 when evaluated by in vitro studies in human liver microsomes.
INVANZ is contraindicated in patients with known hypersensitivity to any component of this product or to other
drugs in the same class or in patients who have demonstrated anaphylactic reactions to beta-lactams.
Due to the use of lidocaine HCl as a diluent, INVANZ administered intramuscularly is contraindicated in patients
with a known hypersensitivity to local anesthetics of the amide type. (Refer to the prescribing information for
When ertapenem is co-administered with probenecid (500 mg p.o. every 6 hours), probenecid competes for active
tubular secretion and reduces the renal clearance of ertapenem. Based on total ertapenem concentrations, probenecid
increased the AUC by 25% and reduced the plasma and renal clearances by 20% and 35%, respectively. The half-life
increased from 4.0 to 4.8 hours. Because of the small effect on half-life, the coadministration with probenecid to
extend the half-life of ertapenem is not recommended. In vitro studies indicate that ertapenem does not
inhibit P-glycoprotein-mediated transport of digoxin or vinblastine and that ertapenem is not a substrate for
In vitro studies in human liver microsomes indicate that ertapenem does not inhibit metabolism mediated by
any of the following six cytochrome p450 (CYP) isoforms: 1A2, 2C9, 2C19, 2D6, 2E1 and 3A4. Drug interactions caused
by inhibition of P-glycoprotein-mediated drug clearance or CYP-mediated drug clearance with the listed isoforms are
Other than with probenecid, no specific clinical drug interaction studies have been conducted.