CEFPROZIL
Clinical safety rating: safe
Human studies have proved safety
Cefprozil, a second-generation cephalosporin, exerts bactericidal activity by binding to penicillin-binding proteins (PBPs) and inhibiting bacterial cell wall synthesis, leading to cell lysis.
| Metabolism | Cefprozil is primarily eliminated unchanged in the urine via glomerular filtration and tubular secretion; metabolism is minimal. |
| Excretion | Renal (primarily), approximately 60-70% unchanged in urine; biliary/fecal excretion accounts for <10%. |
| Half-life | 1.2-1.4 hours in adults with normal renal function; prolonged to 5-6 hours in severe renal impairment (CrCl <30 mL/min). |
| Protein binding | Approximately 36%, primarily to albumin. |
| Volume of Distribution | 0.23 L/kg; indicates limited distribution primarily into extracellular fluid. |
| Bioavailability | Oral: approximately 95% (well absorbed); not available parenterally. |
| Onset of Action | Oral: peak serum concentrations achieved in 1.5 hours; clinical effect begins within 2-4 hours. |
| Duration of Action | Approximately 6-8 hours for susceptible organisms; dose adjustment needed for renal impairment. |
250-500 mg orally every 12 hours for 10 days; for pharyngitis/tonsillitis: 500 mg orally every 24 hours for 10 days.
| Dosage form | FOR SUSPENSION |
| Renal impairment | CrCl >=30 mL/min: no adjustment; CrCl <30 mL/min (not on dialysis): 50% of usual dose at usual interval; hemodialysis: administer dose after dialysis. |
| Liver impairment | No dosage adjustment required for hepatic impairment. |
| Pediatric use | For pharyngitis/tonsillitis: 7.5 mg/kg orally every 12 hours for 10 days (max 500 mg/day); for other infections: 7.5-15 mg/kg orally every 12 hours for 10 days (max 500 mg/dose). |
| Geriatric use | No specific adjustment; monitor renal function and adjust dose based on creatinine clearance. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Probenecid may decrease cephalosporin excretion May cause diarrhea including Clostridium difficile-associated diarrhea.
| Breastfeeding | Excreted in human milk in small amounts. M/P ratio not reported. Use with caution, monitor infant for diarrhea, candidiasis, and allergic reactions. |
| Teratogenic Risk | Pregnancy Category B. Animal studies show no evidence of fetal harm, but no adequate human studies. Use only if clearly needed. |
| Fetal Monitoring |
■ FDA Black Box Warning
None
| Common Effects | Diarrhea |
| Serious Effects |
["Hypersensitivity to cefprozil or any component of the formulation","Hypersensitivity to other cephalosporins"]
| Precautions | ["Hypersensitivity reactions (including anaphylaxis) reported; cross-allergy with penicillins and other beta-lactams","Clostridioides difficile-associated diarrhea (CDAD) may occur","Use caution in renal impairment; dose adjustment required for CrCl < 30 mL/min","Possible superinfection with prolonged use","In patients with phenylketonuria, note that oral suspension contains phenylalanine"] |
| Food/Dietary | Cefprozil absorption is not significantly affected by food; it may be taken with or without meals. However, taking with food may reduce gastrointestinal upset. |
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| Monitor for signs of hypersensitivity reactions, diarrhea, and superinfection. No specific fetal monitoring required. |
| Fertility Effects | No known effects on fertility in animal studies. No human data. |
| Clinical Pearls | Cefprozil is a second-generation cephalosporin with good activity against Streptococcus pyogenes, Streptococcus pneumoniae, and Haemophilus influenzae, but not against methicillin-resistant Staphylococcus aureus (MRSA). It is approved for upper respiratory tract infections, including acute sinusitis, pharyngitis/tonsillitis, and otitis media, as well as uncomplicated skin and skin structure infections. Renal dose adjustment is required for creatinine clearance <30 mL/min. False-positive urinary glucose tests may occur with copper reduction methods (e.g., Clinitest) but not with enzymatic glucose oxidase tests. |
| Patient Advice | Take this medication exactly as prescribed; complete the full course even if you feel better. · Shake the oral suspension well before each use to ensure proper dosing. · Notify your healthcare provider if you develop watery or bloody diarrhea, which may indicate Clostridioides difficile infection. · Report any skin rash, hives, or difficulty breathing immediately; this may indicate an allergic reaction. · If you have a history of penicillin allergy, discuss this with your doctor as cross-sensitivity may occur. · Store the oral suspension in the refrigerator; do not freeze. Discard any unused portion after 14 days. |