Ertapenem

Trade Names:Invanz- Powder for injection, lyophilized 1.046 g ertapenem sodium (equivalent to 1 g ertapenem)

Pharmacology

Inhibits cell wall synthesis.

Pharmacokinetics

Absorption

Bioavailability for IM dose is approximately 90%. T _max is approximately 2.3 h (IM).

Distribution

Approximately 85% to 95% protein bound (concentration dependent). Vd is approximately 0.12 L/kg in adults; 0.2 L/kg in children 3 mo to 12 yr of age; 0.16 L/kg in children 13 to 17 yr of age (at steady state).

Metabolism

Major metabolite is the inactive ring-opened derivative formed by hydrolysis of the beta-lactam ring.

Elimination

The t _½ is approximately 4 h. Approximately 80% excreted in urine (approximately 38% as unchanged drug) and 10% in feces.

Special Populations

Unbound AUC increased 1.5- and 2.3-fold in those with mild and moderate renal function impairment, respectively. No dosage adjustment necessary. Unbound AUC increased 4.4- and 7.6-fold in those with advanced and end-stage renal function impairment, respectively. Dosage adjustment required.

Pharmacokinetics have not been established.

The total and unbound AUC increased 37% and 67%, respectively.

Indications and Usage

Treatment of moderate to severe complicated intra-abdominal infections, complicated skin and skin structure infections, community-acquired pneumonia, complicated UTIs (eg, pyelonephritis), and acute pelvic infections (eg, postpartum endomyometritis, septic abortion, postsurgical gynecologic infections) caused by susceptible microorganisms; prophylaxis of surgical-site infection following elective colorectal surgery.

Contraindications

Hypersensitivity to any component of this product or to other drugs in the same class; patients who have demonstrated anaphylactic reactions to beta-lactams; because of the lidocaine diluent, patients with known sensitivity to local anesthetics of the amide type.

Dosage and Administration

IV/IM 1 g/day for 7 to 14 days.

IV/IM 15 mg/kg twice daily for 5 to 14 days.

IV/IM 1 g/day for 7 to 14 days.

IV/IM 15 mg/kg twice daily for 7 to 14 days.

IV/IM 1 g/day for 10 to 14 days.

IV/IM 15 mg/kg twice daily for 10 to 14 days.

IV/IM 1 g/day for 3 to 10 days.

IV/IM 15 mg/kg twice daily for 3 to 10 days.

IV/IM Ccr 30 mL/min or less: 500 mg/day.

IV/IM No data available.

IV/IM 500 mg within 6 h prior to hemodialysis and a supplemental dose of 150 mg following the hemodialysis session.

IV/IM No data available.

IV 1 g 1 h prior to surgical incision.

General Advice

• For IV infusion, reconstitute with 10 mL of compatible diluent (water for injection, sodium chloride 0.9% injection, or bacteriostatic water for injection). Do not use diluents containing dextrose. Shake well to dissolve powder, and immediately transfer contents of the reconstituted vial to 50 mL of sodium chloride 0.9% injection. Infuse prescribed dose over 30 min. Complete infusion within 6 h of reconstitution. Do not mix or co-infuse with other medications.
• Do not administer if reconstituted solution is cloudy, discolored, or contains particulate matter.
• For IM administration, reconstitute with 3.2 mL of lidocaine hydrochloride 1% injection (without epinephrine). Shake vial thoroughly to form clear solution. Immediately withdraw contents of vial and administer by deep IM injection into large muscle mass. Do not administer IV. Use reconstituted IM solution within 1 h after preparation.
• Reconstituted solution may exhibit a pale yellow color, which is normal and does not affect potency.
• If other drugs are being administered through the same IV line, flush IV line before and after infusion with sodium chloride 0.9% injection.
• Do not mix or coinfuse with other medications; do not use diluents containing dextrose.

Storage/Stability

Store lyophilized powder below 77°F. Reconstituted solution for IV administration, diluted in sodium chloride 0.9% injection, may be stored at room temperature and used within 6 h or stored under refrigeration for 24 h and used within 4 h after removal from refrigeration. Protect from freezing. Use reconstituted solution for IM administration within 1 h of preparation.

Drug Interactions

Inhibits renal excretion of ertapenem; coadministration not recommended.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Hypertension, hypotension, tachycardia (2%).

CNS

Headache (7%); altered mental status (5%); insomnia (3%); dizziness (2%); anxiety, asthenia/fatigue (1%).

Pyrexia (5%); headache (4%); dizziness (2%).

Hallucinations.

Dermatologic

Erythema, pruritus, rash (2%).

Diaper dermatitis (5%); rash (3%); pruritus (2%); dermatitis (1%).

EENT

Pharyngitis (1%).

Nasopharyngitis (2%); viral pharyngitis (1%).

GI

Diarrhea (10%); nausea (8%); abdominal swelling, constipation, vomiting (4%); acid regurgitation, small intestine obstruction (2%); dyspepsia, oral candidiasis (1%).

Diarrhea (12%); vomiting (10%); abdominal pain (5%); constipation, loose stools, nausea (2%); abdominal abscess, upper abdominal pain (1%).

Genitourinary

UTIs (4%); vaginitis (3%).

Hematologic-Lymphatic

Anemia (6%)

Lab Tests

Increased ALT (9%); increased AST (8%); increased platelet count, increased serum alkaline phosphatase (7%); decreased Hgb (5%); decreased Hct (3%); decreased segmented neutrophils, decreased serum albumin, decreased serum potassium, decreased WBC, increased eosinophils, increased serum glucose, increased total serum bilirubin, increased urine RBC and WBC (2%); decreased platelet count, increased PT, increased serum creatinine, increased serum potassium (1%).

Decreased neutrophil count (6%); increased ALT, increased AST (4%); increased alkaline phosphatase, increased eosinophil count, increased platelet count (1%).

Local

Infused vein complication (7%); extravasation, phlebitis/thrombophlebitis (2%).

Pain (7%); erythema (4%); phlebitis, swelling (2%); induration, warmth (1%).

Musculoskeletal

Leg pain (1%).

Respiratory

Dyspnea (3%); cough, pneumonia (2%); rales/rhonchi, respiratory distress (1%).

Cough (4%); upper respiratory tract infection (2%); wheezing (1%).

Miscellaneous

Wound infections (6%); fever (5%); edema/swelling (3%); anastomotic leak, C. difficile infection/colitis, cellulitis, chest pain, death, postoperative infection (2%); seroma (1%).

Hypothermia (2%); herpes simplex (1%).

Anaphylaxis/anaphylactoid reactions.

Precautions

Pregnancy

Category B .

Lactation

Excreted in breast milk.

Children

Safety and efficacy not established in children younger than 3 mo of age.

Elderly

Because elderly patients are more likely to have decreased renal function, select dose with caution.

Hypersensitivity

Hypersensitivity reactions may occur; do not administer to patients who have demonstrated anaphylactic reactions to beta-lactams, carbapenams, or penicillin.

Renal Function

Adjust dose accordingly.

Superinfection

May result in bacterial or fungal overgrowth of nonsusceptible organisms.

CNS

Seizures and other CNS adverse reactions may occur.

Pseudomembranous colitis

Consider possibility in patients with diarrhea.

Overdosage

Symptoms

Diarrhea, dizziness, nausea.

Patient Information

• Explain to patient that medication will be prepared and administered by health care provider.
• Review dosing schedule and prescribed length of therapy with patient. Advise patient that dose and duration of therapy are dependent on site and cause of infection and response to therapy.
• Advise patient to notify health care provider if infection does not improve or appears to worsen.
• Instruct patient to report the following symptoms to health care provider: black, furry tongue; diarrhea; difficulty breathing; hives; itching; loose, foul-smelling stools; rash; vaginal itching or discharge.

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