Brand name: INVanz
Drug class: Carbapenems
VA class: AM130
Chemical name: [4R-[3(3S*,5S*),4α,5β,6βS*)]]-(3-[[5-[[(3-Carboxyphenyl)amino]carbonyl]-3-pyrrolidinyl]thio]-6-(1-hydroxyethyl)-4-methyl-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid
Molecular formula: C₂₂H₂₄N₃NaO₇S
CAS number: 153832-38-3

Medically reviewed by Drugs.com on Jun 28, 2024. Written by ASHP.

Introduction

Antibacterial; carbapenem β-lactam antibiotic.

Uses for Ertapenem

Gynecologic Infections

Treatment of moderate to severe acute pelvic infections (including postpartum endomyometritis, septic abortion, postsurgical infections) caused by susceptible Streptococcus agalactiae (group B streptococci), Escherichia coli, Bacteroides fragilis, Porphyromonas asaccharolytica, Peptostreptococcus, or Prevotella bivia.

Intra-abdominal Infections

Treatment of complicated intra-abdominal infections caused by susceptible E. coli, Clostridium clostridioforme, Eubacterium lentum, Peptostreptococcus, B. fragilis, B. distasonis, B. ovatus, B. thetaiotaomicron, or B. uniformis.

Respiratory Tract Infections

Treatment of moderate to severe community-acquired pneumonia (CAP) caused by susceptible Streptococcus pneumoniae (penicillin-susceptible strains only), including cases with concurrent bacteremia.

Treatment of moderate to severe CAP caused by susceptible Haemophilus influenzae (non-β-lactamase-producing strains only) or Moraxella catarrhalis.

Skin and Skin Structure Infections

Treatment of complicated skin and skin structure infections, including diabetic foot infections without concurrent osteomyelitis, caused by susceptible Staphylococcus aureus (oxacillin-susceptible [methicillin-susceptible] strains only), Streptococcus agalactiae, S. pyogenes (group A β-hemolytic streptococci), E. coli, Klebsiella pneumoniae, Proteus mirabilis, Bacteroides fragilis, Peptostreptococcus species, Porphyromonas asaccharolytica, or Prevotella bivia.

Urinary Tract Infections (UTIs)

Treatment of complicated UTIs (including pyelonephritis) caused by susceptible E. coli (including cases with concurrent bacteremia) or Klebsiella pneumoniae.

Ertapenem Dosage and Administration

Administration

For solution and drug compatibility information, see Compatibility under Stability.

Administer by IV infusion or IM injection.

Administered once daily in adolescents ≥13 years of age and adults. Administered twice daily in children 3 months to 12 years of age.

IM route may be used as an alternative to the IV route in treatment of those infections for which IM therapy is appropriate. Duration of IM therapy should be ≤7 days. Solutions reconstituted for IM administration should not be given IV.

IV Infusion

Reconstitution and Dilution

Reconstitute 1-g vial with 10 mL of sterile water for injection, 0.9% sodium chloride injection, or bacteriostatic water for injection. Shake well to ensure complete dissolution of the drug. The appropriate dose should be withdrawn from the vial and diluted in 0.9% sodium chloride to provide a solution containing ≤20 mg/mL. For a 1-g dose, dilute in 50 mL of 0.9% sodium chloride.

Rate of Administration

Administer by IV infusion over 30 minutes.

IM Administration

Inject IM deeply into a large muscle mass, such as the gluteus or lateral part of the thigh. Use caution to avoid inadvertent injection into a blood vessel.

Reconstitution

Reconstitute 1-g vial with 3.2 mL of 1% lidocaine injection (without epinephrine) and shake thoroughly to ensure dissolution. Administer within 1 hour of reconstitution.

Dosage

Available as ertapenem sodium; dosage expressed in terms of ertapenem.

Duration of therapy depends on the type and severity of infection. IV route may be continued for ≤14 days; IM route may be continued for ≤7 days.

Pediatric Patients

Gynecologic Infections

IV or IM

Children 3 months to 12 years of age: 15 mg/kg twice daily (up to 1 g daily) for 3–10 days.

Adolescents ≥13 years of age: 1 g once daily for 3–10 days.

Intra-abdominal Infections

IV or IM

Children 3 months to 12 years of age: 15 mg/kg twice daily (up to 1 g daily) for 5–14 days.

Adolescents ≥13 years of age: 1 g once daily for 5–14 days.

Respiratory Tract Infections

Community-acquired Pneumonia

IV or IM

Children 3 months to 12 years of age: 15 mg/kg twice daily (up to 1 g daily). Usual duration is 10–14 days; treatment may be switched to an appropriate oral anti-infective after ≥3 days.

Adolescents ≥13 years of age: 1 g once daily. Usual duration is 10–14 days; treatment may be switched to an appropriate oral anti-infective after ≥3 days.

Skin and Skin Structure Infections

IV or IM

Children 3 months to 12 years of age: 15 mg/kg twice daily (up to 1 g daily) for 7–14 days.

Adolescents ≥13 years of age: 1 g once daily for 7–14 days.

Urinary Tract Infections (UTIs)

IV or IM

Children 3 months to 12 years of age: 15 mg/kg twice daily (up to 1 g daily). Usual duration is 10–14 days; treatment may be switched to an appropriate oral anti-infective after ≥3 days.

Adolescents ≥13 years of age: 1 g once daily. Usual duration is 10–14 days; treatment may be switched to an appropriate oral anti-infective after ≥3 days.

Adults

Gynecologic Infections

IV or IM

1 g once daily for 3–10 days.

Intra-abdominal Infections

IV or IM

1 g once daily for 5–14 days.

Respiratory Tract Infections

Community-acquired Pneumonia

IV or IM

1 g once daily. Usual duration is 10–14 days; treatment may be switched to an appropriate oral anti-infective after ≥3 days.

Skin and Skin Structure Infections

IV or IM

1 g once daily for 7–14 days. In adults with diabetic foot infections, anti-infective therapy (parenteral or parenteral followed by oral) has been given for up to 28 days.

Urinary Tract Infections (UTIs)

IV or IM

1 g once daily. Usual duration is 10–14 days; treatment may be switched to an appropriate oral anti-infective after ≥3 days.

Special Populations

Hepatic Impairment

Dosage recommendations not available; pharmacokinetics have not been studied.

Renal Impairment

Dosage adjustments recommended in patients with Cl_cr ≤30 mL/minute.

Adults with Cl_cr ≤30 mL/minute, including those with end-stage renal disease (Cl_cr ≤10 mL/minute) and those undergoing hemodialysis, should receive 500 mg once daily. If the dose is given within 6 hours prior to hemodialysis, a supplementary dose of 150 mg should be given after the hemodialysis session; supplemental dose not necessary if daily dose is given ≥6 hours prior to hemodialysis. Data not available in pediatric patients undergoing dialysis.

Geriatric Patients

No dosage adjustments except those related to renal impairment. (See Renal Impairment under Dosage and Administration.)

Cautions for Ertapenem

Contraindications

• Known hypersensitivity to ertapenem, other carbapenems, or any ingredient in the formulation.

• History of anaphylactic reaction to β-lactams.

• IM injections are prepared using lidocaine hydrochloride and are contraindicated in patients with known hypersensitivity to local anesthetics of the amide type.

Warnings/Precautions

Warnings

Superinfection/Clostridium difficile-associated Colitis

Possible emergence and overgrowth of nonsusceptible organisms. Careful observation of the patient is essential. Institute appropriate therapy if superinfection occurs.

Treatment with anti-infectives may permit overgrowth of clostridia. Consider Clostridium difficile-associated diarrhea and colitis (antibiotic-associated pseudomembranous colitis) if diarrhea develops and manage accordingly.

Some mild cases of C. difficile-associated diarrhea and colitis may respond to discontinuance alone. Manage moderate to severe cases with fluid, electrolyte, and protein supplementation; appropriate anti-infective therapy (e.g., oral metronidazole or vancomycin) recommended if colitis is severe.

CNS Effects

Seizures and other CNS effects reported, especially in those with CNS disorders (e.g., brain lesions, history of seizures) and/or renal impairment.

Do not exceed recommended dosage, especially in those with known factors that predispose to seizures. Anticonvulsant therapy should be continued in those with known seizure disorders.

If focal tremors, myoclonus, or seizures occur, evaluate the patient neurologically, initiate anticonvulsant therapy if necessary, and determine whether ertapenem dosage should be decreased or the drug discontinued.

Sensitivity Reactions

Hypersensitivity Reactions

Serious and occasionally fatal hypersensitivity reactions (e.g., anaphylaxis) reported with β-lactams.

If hypersensitivity occurs, discontinue ertapenem and institute appropriate therapy as indicated (e.g., epinephrine, corticosteroids, and maintenance of an adequate airway and oxygen).

Cross-hypersensitivity

Partial cross-allergenicity among β-lactam antibiotics, including penicillins, cephalosporins, and other β-lactams.

Prior to initiation of therapy, make careful inquiry concerning previous hypersensitivity reactions to ertapenem, cephalosporins, penicillins, or other drugs.

General Precautions

Laboratory Monitoring

Periodically assess organ system functions, including renal, hepatic, and hematopoietic, during prolonged therapy.

Sodium Content

Contains approximately 6 mEq (137 mg) of sodium per g of ertapenem.

Specific Populations

Pregnancy

Category B.

Lactation

Distributed into milk. Use with caution.

Pediatric Use

Safety and efficacy established in children 3 months to 17 years of age for the treatment of acute pelvic infections, complicated intra-abdominal infections, CAP, complicated skin and skin structure infections, and complicated UTIs. Not recommended for the treatment of meningitis; therapeutic concentrations not achieved in CNS. Not recommended in infants <3 months of age; data on use in this age group not available.

Geriatric Use

No substantial differences in safety and efficacy relative to younger adults, but increased sensitivity cannot be ruled out.

Substantially eliminated by kidneys; risk of toxicity may be greater in patients with impaired renal function. Select dosage with caution and assess renal function periodically since geriatric patients are more likely to have renal impairment.

No dosage adjustments except those related to renal function. (See Renal Impairment under Dosage and Administration.)

Hepatic Impairment

Pharmacokinetics not established.

Renal Impairment

Increased AUC. Dosage adjustments recommended in adults with Cl_cr ≤30 mL/minute, including those with end-stage renal disease and those undergoing hemodialysis. (See Renal Impairment under Dosage and Administration.)

Common Adverse Effects

GI effects (diarrhea, nausea, vomiting); local reactions (infused vein complication, phlebitis/thrombophlebitis); headache; vaginitis.

Drug Interactions

Drugs Metabolized by Hepatic Microsomal Enzymes

Does not inhibit CYP isoenzymes 1A2, 2C9, 2C19, 2D6, 2E1, or 3A4; pharmacokinetic interactions unlikely with drugs metabolized by these enzymes.

Drugs with p-Glycoprotein-mediated Clearance

Does not inhibit and is not a substrate for p-glycoprotein-mediated transport. Pharmacokinetic interaction unlikely with drugs that undergo p-glycoprotein-mediated clearance (e.g., digoxin, vinblastine).

Specific Drugs

Ertapenem Pharmacokinetics

Absorption

Bioavailability

Following IM injection, mean bioavailability is approximately 90%; peak plasma concentrations attained in approximately 2.3 hours.

Exhibits nonlinear pharmacokinetics because of concentration-dependent plasma protein binding.

Distribution

Extent

Distributed into blister fluid.

Therapeutic concentrations not achieved in CNS.

Crosses the placenta in rats; not known whether crosses the placenta in humans. Distributed into milk.

Plasma Protein Binding

Highly bound to plasma protein, principally albumin. 95% bound at plasma concentration <100 mcg/mL and 85% bound at 300 mcg/mL.

Elimination

Metabolism

Does not appear to undergo hepatic metabolism. The major metabolite is an inactive ring-opened derivative formed by hydrolysis of the β-lactam ring.

Elimination Route

Eliminated principally in urine.

Approximately 80% of an IV dose eliminated in urine (38% as unchanged drug and 37% as the ring-opened metabolite) and 10% eliminated in feces.

Half-life

Healthy young adults: 4 hours.

Pediatric patients 13–17 years of age: 4 hours.

Pediatric patients 3 months to 12 years of age: 2.5 hours.

Special Populations

Pharmacokinetics in patients with hepatic impairment not established.

In patients with severe renal impairment (Cl_cr 5–30 mL/minute per 1.73 m²) or end-stage renal disease, the extent of exposure to unbound drug is increased 4.4- or 7.6-fold, respectively.

Stability

Storage

Parenteral

Powder for IM Injection or IV Infusion

≤25°C.

Reconstituted and diluted IV solutions may be stored at room temperature, but the infusion should be completed within 6 hours. These solutions may be refrigerated at 5°C for up to 24 hours, but the infusion should be completed within 4 hours after removal from refrigeration. Do not freeze.

IM solutions should be used within 1 hour of reconstitution.

Compatibility

Reconstitute with sterile water for injection, 0.9% sodium chloride injection, or bacteriostatic water for injection, then dilute in 0.9% sodium chloride.

Do not reconstitute or dilute with dextrose-containing solutions or admix with other medications.

Parenteral

Solution CompatibilityHID

Incompatible by conventional standards, but recommended for dilution with use in shorter time periods. (See Storage under Stability.)

Drug Compatibility

Actions and Spectrum

• Synthetic carbapenem β-lactam antibiotic; structurally and pharmacologically related to imipenem and meropenem.

• Usually bactericidal in action.

• Like other β-lactam antibiotics, antibacterial activity results from inhibition of bacterial cell wall synthesis.

• Spectrum of activity includes many gram-positive and -negative aerobic bacteria and some gram-positive and -negative anaerobic bacteria. Stable in the presence of a variety of β-lactamases (including penicillinases, cephalosporinases, and extended-spectrum β-lactamases).

• Gram-positive aerobes: Active in vitro and in clinical infections against Staphylococcus aureus, Streptococcus agalactiae (group B streptococci), S. pneumoniae (penicillin-susceptible strains only), and S. pyogenes (group A β-hemolytic streptococci). Also active in vitro against S. pneumoniae (penicillin-intermediate strains) and S. epidermidis (oxacillin- susceptible strains only). Oxacillin-resistant (methicillin-resistant) staphylococci and Enterococcus are resistant.

• Gram-negative aerobes: Active in vitro and in clinical infections against Escherichia coli, Haemophilus influenzae (β-lactamase-negative strains only), Klebsiella pneumoniae, Moraxella catarrhalis, and Proteus mirabilis. Also active in vitro against Citrobacter, Enterobacter, H. influenzae (β-lactamase-producing strains), H. parainfluenzae, K. oxytoca, Morganella morganii, P. vulgaris, Providencia rettgeri, P. stuartii, and Serratia marcescens.

• Anaerobes: Active in vitro and in clinical infections against Bacteroides fragilis, B. distasonis, B. ovatus, B. thetaiotaomicron, B. uniformis, Clostridium clostridioforme, Eubacterium lentum, Peptostreptococcus, Porphyromonas asaccharolytica, and Prevotella bivia. Also active in vitro against B. vulgaris, C. perfringens, and Fusobacterium.

Advice to Patients

• Importance of informing clinicians of other medical conditions, including history of seizures.

• Importance of discontinuing therapy and informing clinician if an allergic or hypersensitivity reaction occurs.

• Importance of reporting persistent or worsening symptoms of infection.

• Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs.

• Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.

• Importance of informing patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

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