Ertapenem
Ertapenem
Generic Name
Ertapenem
Mechanism
- Inhibition of penicillin‑binding proteins (PBPs) in bacterial cell walls, preventing cross‑linking of peptidoglycan strands and leading to cell lysis.
- Highly potent against *Enterobacteriaceae*, *Staphylococcus aureus* (including MRSA), *Bacteroides fragilis*, and *Clostridioides difficile*.
- Unlike other carbapenems, lacks activity against Enterococcus spp. due to rapid β‑lactamase hydrolysis.
Pharmacokinetics
| Parameter | Value | Comment |
| Bioavailability | 100 % IV | No oral formulation. |
| Volume of distribution | 69 L (adult) | Reflects extensive tissue penetration. |
| Protein binding | 50–55 % | Moderate, necessitates monitoring in hypo‑albuminemia. |
| Half‑life | 4.5–6 h (normal renal function) | Supports once‑daily dosing. |
| Metabolism | Negligible | Primarily renal clearance. |
| Excretion | 70–90 % unchanged in urine | Requires dose adjustment in CKD. |
Indications
- Pelvic inflammatory disease (outpatient or inpatient).
- Complicated intra‑abdominal infections (e.g., peritonitis, appendicitis).
- Ventilator‑associated pneumonia and other hospitals’ *medically‑important* *Gram‑negative* infections.
- Skin and soft‑tissue infections (including necrotizing fasciitis when combined with other agents).
- Bone and joint infections (often as part of combination therapy).
Contraindications
- Immediate hypersensitivity to carbapenems or penicillins.
- Severe renal impairment (eGFR <15 mL/min) — requires dose reduction or avoidance.
- History of neurotoxicity (seizures, encephalopathy) — use with caution in elderly or hepatic dysfunction.
- Pregnancy: Category B; no proven risk but limited data.
- New‑borns: use only after 24 h of life due to immature renal clearance.
Warnings
• Risk of *Candida* overgrowth (superinfection) with prolonged therapy.
• Occasional cross‑reactivity with other β‑lactams; consider patch or graded challenge for penicillin allergy evaluation.
Dosing
- Adult dose: 1 g IV or IM once daily.
- Renal adjustment:
- CrCl 30–49 mL/min: 500 mg IV/IM once daily.
- CrCl <30 mL/min: 500 mg IV/IM every 48 h.
- Pediatric dose: 40 mg/kg IV/IM (max 1 g) once daily; adjust for renal function.
- Infusion time: 30‑60 min; can be extended to 90‑120 min if infusion reactions occur.
- Combination: Often paired with a β‑lactamase inhibitor (e.g., ampicillin‑sulbactam) or a cephalosporin against Enterococcus when required.
Monitoring
- Renal function: BUN/Creatinine, eGFR at baseline and every 2–3 days during long therapy.
- Neurologic: Evaluate for new seizures or CNS symptoms, particularly in CKD patients.
- Complete blood count: monitor for cytopenias when on prolonged treatment.
- Drug levels: not routine; use therapeutic drug monitoring only in special populations (pediatric, neonates, severe renal disease).
Clinical Pearls
- Once‑daily convenience lets *Ertapenem* bridge inpatient and outpatient therapy, improving compliance and reducing pharmacy burden.
- High anaerobic coverage makes it ideal for complex intra‑abdominal or pelvic infections where *Bacteroides* spp. are common.
- No activity against Enterococcus – remember to add an enterococcus‑active agent if that pathogen is suspected or proven.
- Overlap with other carbapenems: cross‑resistance may occur; choose *Ertapenem* when you want to avoid broader spectrum agents to preserve carbapenem efficacy.
- Infusion reaction mitigation: rate‑slow infusion or pretreatment with antihistamine/alcohol‑based skin prep can reduce hypersensitivity manifestations.
- Cost‑effectiveness: despite higher upfront cost, the single‑daily dose reduces infusion room time and nursing workload, making it a budget‑friendly option for many hospitals.
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• For detailed prescribing charts, see your institution’s formulary or the FDA label.