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. |
| Molecular Weight | 500.44 Da |
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 | Generally avoided due to lack of safety data; animal studies have shown teratogenic effects at high doses. |
| 2nd trimester | Use only if clearly needed; consider alternative agents with established safety. |
| 3rd trimester | Avoid near term due to potential for kernicterus in neonates via displacement of bilirubin. |
Clinical note
Comprehensive clinical and safety monograph for PENTACEF (PENTACEF).
| Placental transfer | Significant placental transfer; achieves therapeutic concentrations in fetal plasma. |
| Breastfeeding | Pentacef is excreted into breast milk in low concentrations. Use with caution in nursing mothers, especially in infants with jaundice or glucose-6-phosphate dehydrogenase deficiency. |
| Lactation Rating |
■ FDA Black Box Warning
None.
| Serious Effects |
Known hypersensitivity to cephalosporins or any component of the formulationPrevious immediate-type hypersensitivity reaction to penicillins (risk of cross-sensitivity)
| Precautions | Hypersensitivity reactions (including anaphylaxis), Clostridioides difficile-associated diarrhea, superinfection, altered coagulation (with prolonged therapy), and renal impairment (dose adjustment required). |
| Food/Dietary | Avoid alcohol and any products containing alcohol (e.g., mouthwash, over-the-counter medications, cooking wines, some fruit juices) during treatment and for 72 hours after the last dose due to the risk of a disulfiram-like reaction. No other significant food interactions reported. |
Loading safety data…
| L3 (Moderately Safe) |
| 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. |
| 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. |
| Clinical Pearls | PENTACEF (cefoperazone) is a third-generation cephalosporin with a high rate of biliary excretion; use caution in patients with biliary obstruction. It has a disulfiram-like reaction with alcohol; avoid concurrent use. Monitor prothrombin time as it may cause hypoprothrombinemia, especially in malnourished patients. Dose adjustment required in hepatic impairment, not renal. |
| Patient Advice | Take this medication exactly as prescribed, even if you feel better. · Avoid alcohol and alcohol-containing products during treatment and for 72 hours after last dose to prevent severe nausea, vomiting, and headache. · Report any unusual bleeding or bruising to your healthcare provider immediately. · Complete the full course of therapy; do not skip doses. · If you miss a dose, take it as soon as you remember, but skip if almost time for next dose; do not double dose. · This medication may cause diarrhea; if severe or persistent, contact your doctor. · Inform your healthcare provider if you are pregnant, planning to become pregnant, or breastfeeding. |