Ertapenem sodium is a synthetic, parenteral carbapenem antibiotic.
The empirical formula is C22H24N3O7SNa and MW is 497.50.The chemical structure is:
The mechanism of action of ertapenem is similar to beta- lactam antibiotics. The bactericidal action of ertapenem is due to the inhibition of cell wall synthesis leading to death of bacteria.
After intramuscular administration peak plasma concentrations are reached in approximately 2 hours.
Ertapenem is active against wide range of gram-positive, gram negative and anaerobic bacteria. Ertapenem is stable against hydrolysis by a number of beta-lactamases, including penicillinases, and cephalosporinases and extended spectrum beta-lactamases.
|Condition||Daily Dose (IV or IM) Adults and Paediatric Patients >13 years of age||Daily Dose (IV or IM) Paediatric Patients 3 months to 12 years of age||Duration of treatment|
|Complicated intra-abdominal infections||1 g||15 mg/kg
|5 to 14 days|
|Complicated skin and skin structure infections, including
diabetic foot infections
|1 g||15 mg/kg
|5 to 14 days|
|Community acquired pneumonia||1 g||15 mg/kg
|10 to 14 days|
|Complicated urinary tract infections, including pyelonephritis||1 g||15 mg/kg
|10 to 14 days#|
|Acute pelvic infections including postpartum endomyometritis,
septic abortion and post-surgical gynecologic infections
|1 g||15 mg/kg
|3 to 10 days|
|Indication||Daily Dose (IV) –Adults||Duration of treatment|
|Prophylaxis of surgical site infection following elective colorectal surgery||1 g||Single IV dose given 1 hour prior to surgical incision|
Ertapenem is contraindicated in patients with prior history of hypersensitivity to any other drugs in the same class or to beta-lactams. Ertapenem is contraindicated in patients with a known hypersensitivity to local anesthetics of the amide type as lidocaine HCl is used as a diluent for Ertapenem.
Common side effects of ertapenem are infused vein complication, swelling, fever, abdominal pain, hypotension, constipation, diarrhoea, nausea, vomiting, altered status, dizziness, headache, insomnia, dyspnea, pruritis, rash, vaginitis.
Ertapenem sodium is a synthetically derived, parenteral carbapenem antibiotic.
Ertapenem is a 1-beta methyl-carbapenem which is chemically similar to beta lactams. Its molecular formula is C22H24N3O7SNa and MW is 497.50.The chemical structure is:
1 g ertapenem/vial for Intravenous or Intramuscular Use
The mechanism of action of ertapenem is similar to beta- lactam antibiotics. The bactericidal action of ertapenem is due to the inhibition of synthesis of the bacterial cell wall and is facilitated by the attachment of ertapenem to penicillin binding proteins.
Ertapenem is active against:
Gram positive bacteria
A varied number of beta lactamases do not cause much hydrolysis of ertapenem but it undergoes hydrolysis by the metallo beta-lactamases. In vitro studies have reported that the key forms of resistance to ertapenem in gram-negative bacilli, is due to combinations of decreased accumulation which is both because of increased influx and decreased influx and beta lactamase hydrolysis.
There is a possibility of cross-resistance between ertapenem and other carbapenems, but in vitro studies and surveillance studies designate that it is not complete. As β-lactams do not share mutual mechanisms of actions with non-β-lactam antimicrobials, there is no probability of target-based cross-resistance between them.
After intramuscular administration, the bioavailability is 90-92%. Mean peak plasma concentrations are reached in approximately 2 hours Protein binding is about 85% to 95%.Ertapenem is eliminated predominantly by the kidneys. The main metabolite of ertapenem is the bacteriologically inactive. Dehydropeptidase-1 catalyzes the metabolism of ertapenem. Approximately 80% excreted in urine and ten per cent in faeces.
The t1/2 of ertapenem ranges from 2.5 to 4 hours.
Ertapenem does not inhibit metabolism mediated by any of the six major cytochrome P450 (CYP) isoforms.
Ertapenem is indicated in the following conditions:
|Condition||Dose/day Adults and children aged >13 years (Intramuscular or IV)||Dose/day Children aged 3 months-12 years (Intramuscular or IV)||Duration of treatment|
|Infections of intra-abdominal origin and Infections of the skin and appendages (complicated)||1 g||15 mg/kg/BD||5 days to 2 weeks|
|Infections of urinary system (complicated) and Community acquired pneumonia||1 g||15 mg/kg/BD||10 days to 2 weeks|
|Acute pelvic infections||1 g||15 mg/kg/BD||Three to ten days|
A single dose of 1 g can be given by the intravenous route for prophylactic use in elective surgeries.
Simultaneous prescription of ertapenem and probenecid is not advised as probenecid causes inhibition of tubular secretion of ertapenem.
Ertapenem decreases the plasma levels of valproic acid.
Modifications in dose are required in persons with kidney dysfunction.
Not much data is available about the effect of liver dysfunction on the metabolism of ertapenem.
An extra dose of 150 mg should be given after haemodialysis.
It is a pregnancy Category B drug.
Ertapenem penetrates the placental barrier in rats and can cross the human placenta. No clinical trials have been conducted studying the teratogenic effects of ertapenem.
Ertapenem is secreted during lactation.
As no clinical data is available, ertapenem should not be prescribed in infants below three months of age.
As CSF penetration is poor, it should not be prescribed for the treatment of meningitis in the paediatric population.
Like other beta-lactam antibiotics serious and occasionally fatal hypersensitive reactions can occur with Ertapenem.
Convulsions and other CNS adverse effects have been seen with Ertapenem.
Like other antibiotics, it can also be seen with ertapenem.
Long-term carcinogenicity studies in animals have not been conducted to evaluate the carcinogenic potential of ertapenem. However, neither mutagenic nor carcinogenic potential nor impairment of fertility was found in a number of tests conducted in selected animals.
The common adverse effects are:
Other adverse effects rarely seen are: