Ertapenem

Uses

To reduce the development of drug-resistant bacteria and maintain the effectiveness of Ertapenem and other antibacterial drugs, Ertapenem should be used only to treat or prevent infections that are proven or strongly suspected to be caused by susceptible bacteria. W hen culture and susceptibility information are available, they should be considered in selecting or modifying antibacterial therapy. In the absence of such data, local epidemiology and susceptibility patterns may contribute to the empiric selection of therapy.

Complicated Intra-Abdominal Infections: Ertapenem is used for the treatment of 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.

Complicated Skin And Skin Structure Infections, Including Diabetic Foot Infections: Without Osteomyelitis Ertapenem is used for the treatment of complicated skin and skin structure infections, including diabetic foot infections without osteomyelitisdue 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. Ertapenem has not been studied in diabetic foot infections with concomitant osteomyelitis

Community Acquired Pneumonia: Ertapenem is used for the treatment of 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.

Complicated Urinary Tract Infections Including Pyelonephritis: Ertapenem is used for the treatment of complicated urinary tract infections including pyelonephritis due to Escherichia coli, including cases with concurrent bacteremia, or Klebsiella pneumoniae.

Acute Pelvic Infections Including Postpartum Endomyometritis, Septic Abortion And Post Surgical Gynecologic Infections: Ertapenem is used for the treatment of acute pelvic infections including postpartum endomyometritis, septic abortion and post surgical gynecological infections due to Streptococcus agalactiae, Escherichia coli, Bacteroides fragilis, Porphyromonas asaccharolytica, Peptostreptococcus species, or Prevotella bivia.

Prophylaxis Of Surgical Site Infection Following Elective Colorectal Surgery: Ertapenem is used for the prevention of surgical site infection following elective colorectal surgery.

Ertapenem is also used to associated treatment for these conditions: Gynaecological infection, Moderate, severe Community Acquired Pneumonia (CAP), Moderate, severe Complicated Intra-Abdominal Infections, Moderate, severe Complicated Skin and Soft Tissue Infection, Moderate, severe Complicated Urinary Tract Infection, Moderate, severe Diabetic Foot Infection, Moderate, severe Postpartum Endomyometritis, Moderate, severe Septic Abortion

How Ertapenem works

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.

Dosage

Ertapenem dosage

Prophylaxis of surgical infections:

• Adult:1 g as a single dose, to be given 1 hr before the surgery.

Community-acquired pneumonia, Intra-abdominal infections, Skin and skin structure infections, Urinary tract infections:

• Adult:1 g once daily IM (for up to 7 days) or IV infusion over 30 min (for up to 14 days)
• Child:3 mth to 13 yr15 mg/kg bid. Max: 1 g/day.

IV: Dilute powd for inj in 10 mL of sterile water for inj, NaCl 0.9% inj or bacteriostatic water for inj then reconstituted soln should be further diluted with 50 mL NaCl 0.9%. IM: Reconstitute with 3.2 mL of lidocaine 1% inj (witho epinephrine).

Side Effects

Drug rash with eosinophilia and systemic symptoms (DRESS), pruritus, diarrhoea, nausea, vomiting, infused vein complication, phlebitis or thrombophlebitis, headache, muscular weakness, gait disturbance, abnormal coordination, vaginitis; elevations in ALT, AST, alkaline phosphatase and platelet count. Dry mouth, taste disturbances, dyspepsia, abdominal pain, anorexia, constipation, melaena, bradycardia, hypotension, chest pain, oedema, pharyngeal discomfort, dyspnoea, dizziness, sleep disturbances, confusion, asthenia, seizures, raised glucose, petechiae.

Precaution

Patient with known or suspected CNS disorders (e.g. brain lesions, history of seizures). Renal impairment. Pregnancy and lactation.

Interaction

May decrease plasma levels of valproic acid thus, increasing the risk of seizures. Increased plasma concentrations with probenecid.

Food Interaction

Ertapenem Hypertension interaction

[Moderate] Parenteral ertapenem contains approximately 137 mg (6.0 mEq) of sodium per each gram of ertapenem activity.

The sodium content should be considered in patients with conditions that may require sodium restriction, such as congestive heart failure, hypertension, and fluid retention.

Ertapenem Drug Interaction

Unknown: sulfamethoxazole / trimethoprim, sulfamethoxazole / trimethoprim, diphenhydramine, diphenhydramine, lvp solution, lvp solution, polyethylene glycol 3350, polyethylene glycol 3350, sodium chloride, sodium chloride, acetaminophen, acetaminophen, acetaminophen, acetaminophen, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol, ondansetron, ondansetron

Ertapenem Disease Interaction

Major: colitis, renal dysfunctionModerate: CNS disorders, hemodialysis, sodium

Volume of Distribution

• 0.12 liter/kg [adults]
• 0.2 liter/kg [pediatric, 3 months to 12 years]
• 0.16 liter/kg [pediatric patients 13 to 17 years]

Elimination Route

Ertapenem is almost completely absorbed following intramuscular administration. The bioavailability of a 1 g intramuscular dose approximated 92% in 26 healthy subjects [77% male; median (range) age, 29 (22–41) years]. Plasma concentrations of total ertapenem were similar whether given intramuscularly or intravenously.

Half Life

The mean plasma half-life is approximately 4 hours.

Clearance

• 1.8 L/h

Elimination Route

Of the 80% recovered in urine, approximately 38% is excreted as unchanged drug and approximately 37% as the ring-opened metabolite.

Pregnancy & Breastfeeding use

Pregnancy Category B. Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies in women in the 1st trimester (and there is no evidence of a risk in later trimesters).

Contraindication

Hypersensitivity to ertapenem, other carbapenems; history of anaphylactic reaction to β-lactams (e.g. penicillins, cephalosporins). Known hypersensitivity to local anaesth of the amide type due to use of lidocaine as diluent in IM use.

Special Warning

Patient undergoing haemodialysis: 500 mg/day; if daily dose given w/in 6 hr prior to haemodialysis, supplemental dose of 150 mg should be administered following the dialysis period.CrCl ≤30 and ESRD: 500 mg/day.

Innovators Monograph

You find simplified version here Ertapenem