PRECEF
Clinical safety rating: caution
Comprehensive clinical and safety monograph for PRECEF (PRECEF).
Cefoperazone is a third-generation cephalosporin antibiotic that inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs), leading to cell lysis and death.
| Metabolism | Primarily excreted unchanged in bile; minor hepatic metabolism. Not significantly metabolized by cytochrome P450 enzymes. |
| Excretion | Primarily renal (80-90% as unchanged drug via glomerular filtration and tubular secretion); biliary/fecal <10%. |
| Half-life | 0.5-1 hour in adults with normal renal function; prolonged to 2-8 hours in moderate to severe renal impairment (CrCl <30 mL/min). |
| Protein binding | 20-30% bound to serum albumin. |
| Volume of Distribution | 0.15-0.25 L/kg, consistent with extracellular fluid distribution. |
| Bioavailability | Intramuscular: 90-100%. |
| Onset of Action | Intravenous: 2-5 minutes; Intramuscular: 10-30 minutes. |
| Duration of Action | 4-6 hours after IV/IM administration; sustained up to 12 hours in renal impairment. |
| Molecular Weight | 415.47 |
1-2 g IV every 6-8 hours; maximum 12 g/day.
| Dosage form | INJECTABLE |
| Renal impairment | CrCl >50 mL/min: no adjustment. CrCl 10-50 mL/min: 1 g every 12-24 hours. CrCl <10 mL/min: 1 g every 24-48 hours. |
| Liver impairment | No specific Child-Pugh based adjustments; use caution in severe impairment. |
| Pediatric use | 50-100 mg/kg/day IV divided every 6-8 hours; maximum 12 g/day. |
| Geriatric use | Start at lower end of dosing range; adjust based on renal function. |
| 1st trimester | Avoid in first trimester unless essential; risk of teratogenicity based on animal studies. |
| 2nd trimester | Use only if clearly needed; no adequate human studies. |
| 3rd trimester | Risk of kernicterus in neonates if given near term; avoid if possible. |
Clinical note
Comprehensive clinical and safety monograph for PRECEF (PRECEF).
| Placental transfer | Crosses placenta readily; achieves therapeutic concentrations in fetal circulation. |
| Breastfeeding | Excreted in small amounts into breast milk; unlikely to cause adverse effects in infants due to poor oral absorption. However, monitor for diarrhea or rash. |
| Lactation Rating |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
Hypersensitivity to cephalosporins or any componentHistory of anaphylactic reaction to penicillins or other beta-lactams
| Precautions | Hypersensitivity reactions, including anaphylaxis, may occur, Pseudomembranous colitis has been reported, Bleeding risk due to hypoprothrombinemia (contains N-methylthiotetrazole side chain), Disulfiram-like reaction with alcohol consumption |
| Food/Dietary | Avoid alcohol and alcohol-containing foods, medications, and mouthwash during therapy and for 2 days after completion. No other significant food interactions reported. |
| Clinical Pearls |
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| Teratogenic Risk | FDA Pregnancy Category B. No evidence of teratogenicity in animal studies; no adequate human studies. Caution in first trimester; weigh risk vs benefit. |
| Fetal Monitoring | Monitor maternal renal function and CBC; fetal growth ultrasound if used in severe infections during pregnancy. |
| Fertility Effects | No reported adverse effects on fertility in animal studies. |
| PRECEF (cefoperazone) is a third-generation cephalosporin with enhanced activity against Pseudomonas aeruginosa. Monitor for disulfiram-like reaction if alcohol is consumed within 48 hours of administration. Prolonged use may cause vitamin K deficiency due to inhibition of gut flora; consider prophylactic vitamin K in malnourished patients. Dosage adjustment required in hepatic impairment but not in renal impairment. Use with caution in patients with history of penicillin allergy due to cross-sensitivity. |
| Patient Advice | Avoid alcohol and alcohol-containing products during treatment and for 48 hours after the last dose to prevent severe nausea, vomiting, and flushing. · Complete the full course of therapy even if you feel better to ensure the infection is fully treated. · Report any signs of bleeding (unusual bruising, blood in urine/stool) or prolonged diarrhea, as this may indicate a serious side effect. · Inform your doctor if you are pregnant, planning to become pregnant, or breastfeeding. · Do not stop taking this medication without consulting your healthcare provider. |