PENTACEF
Clinical safety rating: caution
Comprehensive clinical and safety monograph for PENTACEF (PENTACEF).
Cephalosporin antibiotic that inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs), disrupting peptidoglycan cross-linking.
| Metabolism | Hepatically metabolized; primarily eliminated unchanged in urine via glomerular filtration and tubular secretion. |
| Excretion | Approximately 80-90% renal excretion as unchanged drug via glomerular filtration and tubular secretion; 10-20% biliary/fecal elimination. |
| Half-life | Terminal elimination half-life is 1.5-2 hours; prolonged to 3-5 hours in moderate renal impairment (CrCl 30-50 mL/min) and up to 10-20 hours in severe impairment (CrCl <10 mL/min); dosing adjustment required for CrCl <50 mL/min. |
| Protein binding | 20-30% bound to serum albumin. |
| Volume of Distribution | 0.15-0.25 L/kg, indicating predominantly extracellular fluid distribution; higher in neonates (0.3-0.5 L/kg). |
| Bioavailability | Oral: 75-90% (fasting); reduced by ~25% with food. Intramuscular: 100%. |
| Onset of Action | Oral: 30-60 minutes; Intramuscular: 15-30 minutes; Intravenous: within minutes. |
| Duration of Action | 8-12 hours for susceptible organisms; shorter (6-8 hours) for moderately susceptible pathogens; no post-antibiotic effect. |
1-2 g IV/IM every 8-12 hours; maximum 6 g/day.
| Dosage form | INJECTABLE |
| Renal impairment | CrCl 30-50 mL/min: 1-2 g every 12 hours; CrCl 10-29 mL/min: 1-2 g every 24 hours; CrCl <10 mL/min: 1-2 g every 48 hours. |
| Liver impairment | No specific Child-Pugh based adjustments; use with caution in severe impairment. |
| Pediatric use | Neonates: 50 mg/kg IV every 12 hours; Infants/Children: 50-100 mg/kg/day IV/IM divided every 8-12 hours; maximum 6 g/day. |
| Geriatric use | Reduce dose based on renal function; monitor renal status closely. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for PENTACEF (PENTACEF).
| Breastfeeding | Cefoperazone is excreted into breast milk in low concentrations (M/P ratio approximately 0.1–0.2). Considered compatible with breastfeeding by the American Academy of Pediatrics. Potential for gastrointestinal disturbances or allergic sensitization in the infant, but usually not a concern. Monitor infant for diarrhea or rash. |
| Teratogenic Risk | PENTACEF (Cefoperazone) is a cephalosporin antibiotic classified as FDA Pregnancy Category B. No evidence of teratogenicity in animal studies; however, adequate human studies are lacking. First trimester: no known risk, but use only if clearly needed. Second and third trimesters: generally considered safe, but caution due to limited data. Risk of kernicterus in neonates if used near term due to bilirubin displacement. |
■ FDA Black Box Warning
None.
| Serious Effects |
Hypersensitivity to cephalosporins or any component of the formulation; history of severe immediate reaction (e.g., anaphylaxis) to penicillins or other beta-lactams.
| Precautions | Hypersensitivity reactions (including anaphylaxis), Clostridioides difficile-associated diarrhea, superinfection, altered coagulation (with prolonged therapy), and renal impairment (dose adjustment required). |
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| Fetal Monitoring | No specific fetal monitoring required. Monitor maternal renal function and gastrointestinal symptoms. In prolonged therapy, monitor for superinfection and bleeding tendencies due to vitamin K deficiency. Observe neonate for signs of adverse effects if used near delivery. |
| Fertility Effects | No known adverse effects on fertility in animals or humans. Cefoperazone does not affect spermatogenesis or oogenesis. No specific studies on human fertility, but no reports of impairment. |