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Pronunciation
(sef PROE zil)
Generic Available (U.S.)
Yes
Index Terms
Brand Names: Canada
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
Treatment of otitis media and infections involving the respiratory tract and skin and skin structure; active against methicillin-sensitive staphylococci, many streptococci, and various gram-negative bacilli including E. coli, some Klebsiella, P. mirabilis, H. influenzae, and Moraxella.
Pregnancy Risk Factor
B
Pregnancy Considerations
Adverse events were not observed in animal reproduction studies; therefore, cefprozil is classified as pregnancy category B. It is not known if cefprozil crosses the human placenta. Other cephalosporins cross the placenta and are considered safe for use during pregnancy.
Lactation
Enters breast milk/use caution (AAP rates “compatible”; AAP 2001 update pending)
Breast-Feeding Considerations
Small amounts of cefprozil are excreted in breast milk. The manufacturer recommends that caution be exercised when administering cefprozil to nursing women. Nondose-related effects could include modification of bowel flora.
Contraindications
Hypersensitivity to cefprozil, any component of the formulation, or other cephalosporins
Warnings/Precautions
Concerns related to adverse effects:
• Penicillin allergy: Use with caution in patients with a history of penicillin allergy, especially IgE-mediated reactions (eg, anaphylaxis, angioedema, urticaria).
• Superinfection: Prolonged use may result in fungal or bacterial superinfection, including C. difficile-associated diarrhea (CDAD) and pseudomembranous colitis; CDAD has been observed >2 months postantibiotic treatment.
Disease-related concerns:
• Renal impairment: Use with caution in patients with renal impairment; modify dosage in severe impairment.
Dosage form specific issues:
• Phenylalanine: Some products may contain phenylalanine.
Adverse Reactions
1% to 10%:
Central nervous system: Dizziness (1%)
Dermatologic: Diaper rash (2%)
Gastrointestinal: Diarrhea (3%), nausea (4%), vomiting (1%), abdominal pain (1%)
Genitourinary: Vaginitis, genital pruritus (2%)
Hepatic: Transaminases increased (2%)
Miscellaneous: Superinfection
<1%: Anaphylaxis, angioedema, pseudomembranous colitis, rash, urticaria, erythema multiforme, serum sickness, Stevens-Johnson syndrome, hyperactivity, headache, insomnia, confusion, somnolence, leukopenia, eosinophilia, thrombocytopenia, BUN increased, creatinine increased, arthralgia, cholestatic jaundice, fever
Reactions reported with other cephalosporins: Seizure, toxic epidermal necrolysis, renal dysfunction, interstitial nephritis, toxic nephropathy, aplastic anemia, hemolytic anemia, hemorrhage, pancytopenia, agranulocytosis, colitis, vaginitis, superinfection
Metabolism/Transport Effects
None known.
Drug Interactions
Aminoglycosides: Cephalosporins (2nd Generation) may enhance the nephrotoxic effect of Aminoglycosides. Risk C: Monitor therapy
BCG: Antibiotics may diminish the therapeutic effect of BCG. Risk X: Avoid combination
Probenecid: May increase the serum concentration of Cephalosporins. Risk C: Monitor therapy
Typhoid Vaccine: Antibiotics may diminish the therapeutic effect of Typhoid Vaccine. Only the live attenuated Ty21a strain is affected. Management: Vaccination with live attenuated typhoid vaccine (Ty21a) should be avoided in patients being treated with systemic antibacterial agents. Use of this vaccine should be postponed until at least 24 hours after cessation of antibacterial agents. Risk D: Consider therapy modification
Ethanol/Nutrition/Herb Interactions
Food: Food delays cefprozil absorption.
Mechanism of Action
Inhibits bacterial cell wall synthesis by binding to one or more of the penicillin-binding proteins (PBPs) which in turn inhibits the final transpeptidation step of peptidoglycan synthesis in bacterial cell walls, thus inhibiting cell wall biosynthesis. Bacteria eventually lyse due to ongoing activity of cell wall autolytic enzymes (autolysins and murein hydrolases) while cell wall assembly is arrested.
Pharmacodynamics/Kinetics
Absorption: Well absorbed (94%)
Protein binding: 35% to 45%
Half-life elimination: Normal renal function: 1.3 hours
Time to peak, serum: Fasting: 1.5 hours
Excretion: Urine (61% as unchanged drug)
Dosage
Usual dosage range:
Infants and Children >6 months to 12 years: Oral: 7.5-15 mg/kg/day divided every 12 hours
Children >12 years and Adults: Oral: 250-500 mg every 12 hours or 500 mg every 24 hours
Indication-specific dosing:
Infants and Children >6 months to 12 years: Oral:
Otitis media: 15 mg/kg every 12 hours for 10 days
Children 2-12 years: Oral:
Pharyngitis/tonsillitis: 7.5-15 mg/kg/day divided every 12 hours for 10 days (administer for >10 days if due to S. pyogenes); maximum: 1 g/day
Uncomplicated skin and skin structure infections: 20 mg/kg every 24 hours for 10 days; maximum: 1 g/day
Children >12 years and Adults: Oral:
Pharyngitis/tonsillitis: 500 mg every 24 hours for 10 days
Secondary bacterial infection of acute bronchitis or acute bacterial exacerbation of chronic bronchitis: 500 mg every 12 hours for 10 days
Uncomplicated skin and skin structure infections: 250 mg every 12 hours or 500 mg every 12-24 hours for 10 days
Dosing adjustment in renal impairment: Clcr <30 mL/minute: Reduce dose by 50%
Hemodialysis: Reduced by hemodialysis; administer dose after the completion of hemodialysis
Administration: Oral
Administer around-the-clock to promote less variation in peak and trough serum levels. Chilling the reconstituted oral suspension improves flavor (do not freeze).
Monitoring Parameters
Assess patient at beginning and throughout therapy for infection; monitor for signs of anaphylaxis during first dose
Test Interactions
Positive direct Coombs', false-positive urinary glucose test using cupric sulfate (Benedict's solution, Clinitest®, Fehling's solution), false-positive serum or urine creatinine with Jaffé reaction
Dietary Considerations
May be taken with food. Oral suspension may contain phenylalanine; consult product labeling.
Patient Education
Take at regular intervals around-the-clock, with or without food. Chilling oral suspension improves flavor (do not freeze). Maintain adequate hydration, unless instructed to restrict fluid intake. May cause false test results with Clinitest®; use of another type of glucose testing is preferable. May cause dizziness, nausea, vomiting, or diarrhea. Report rash; breathing or swallowing difficulty; persistent diarrhea, nausea, vomiting, or abdominal pain; changes in urinary pattern or pain on urination; opportunistic infection (eg, vaginal itching or drainage, sores in mouth, blood in stool or urine, unusual fever or chills); or CNS changes (eg, irritability, agitation, nervousness, insomnia, hallucinations).
Geriatric Considerations
Has not been studied exclusively in the elderly. Adjust dose for estimated renal function.
Dental Health: Effects on Dental Treatment
No significant effects or complications reported
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Mental Health: Effects on Mental Status
May cause nervousness; case reports of euphoria, delusion, illusions, and depersonalization with cephalosporins
Mental Health: Effects on Psychiatric Treatment
May rarely cause neutropenia; use caution with clozapine and carbamazepine
Nursing: Physical Assessment/Monitoring
Assess results of culture/sensitivity tests and patient's allergy history prior to therapy. Monitor for interstitial nephritis, hemolytic anemia, and hemorrhage. Advise patients with diabetes about use of Clinitest® (may cause false-positive test). Teach patient to report opportunistic infection and hypersensitivity reactions.
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Powder for suspension, oral: 125 mg/5 mL (50 mL, 75 mL, 100 mL); 250 mg/5 mL (50 mL, 75 mL, 100 mL)
Tablet, oral: 250 mg, 500 mg
References
American Academy of Pediatrics Committee on Drugs, “Transfer of Drugs and Other Chemicals Into Human Milk,” Pediatrics, 2001, 108(3):776-89.
Arguedas AG, Zaleska M, Stutman HR, et al, “Comparative Trial of Cefprozil vs Amoxicillin Clavulanate Potassium in the Treatment of Children With Acute Otitis Media With Effusion,” Pediatr Infect Dis J, 1991, 10(5):375-80.
Barriere SL, “Review of In Vitro Activity, Pharmacokinetic Characteristics, Safety, and Clinical Efficacy of Cefprozil, a New Oral Cephalosporin,” Ann Pharmacother, 1993, 27(9):1082-9.
Bradley JS, Byington CL, Shah SS, et al. “The Management of Community-Acquired Pneumonia in Infants and Children Older Than 3 Months of Age: Clinical Practice Guidelines by the Pediatric Infectious Diseases Society and the Infectious Diseases Society of America”, Clin Infect Dis, 2011, 53(7):e25-76.
Gainer RB 2nd, “Cefprozil: A New Cephalosporin; Its Use in Various Clinical Trials,” South Med J, 1995, 88(3):338-46.
Lowery N, Kearns GL, Young RA, et al, “Serum Sickness-Like Reactions Associated With Cefprozil Therapy,” J Pediatr, 1994, 125(2):325-8.
Marshall WF and Blair JE, “The Cephalosporins,” Mayo Clin Proc, 1999, 74(2):187-95.
Schatz BS, Karavokiros KT, Taeubel MA, et al, “Comparison of Cefprozil, Cefpodoxime Proxetil, Loracarbef, Cefixime, and Ceftibuten,” Ann Pharmacother, 1996, 30(3):258-68.
Shukla UA, Pittman KA, and Barbhaiya RH, “Pharmacokinetic Interactions of Cefprozil With Food, Propantheline, Metoclopramide, and Probenecid in Healthy Volunteers,” J Clin Pharmacol, 1992, 32(8):725-31.
Shyu WC, Pittman KA, Wilber RB, et al, “Pharmacokinetics of Cefprozil in Healthy Subjects and Patients With Hepatic Impairment,” J Clin Pharmacol, 1991, 31(4):372-6.
International Brand Names
Lexi-Comp.com
Last full review/revision December 2011
Content last modified December 2011
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