Brand name: Cefzil
Drug class: Second Generation Cephalosporins
Chemical name: (6R, 7R)-7-[(R)-2-amino-2-(p-hydroxyphenyl)acetamido]-8-oxo-3-propenyl-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid monohydrate
CAS number: 92665-29-7

Medically reviewed by Drugs.com on Sep 29, 2023. Written by ASHP.

Introduction

Antibacterial; β-lactam antibiotic; second generation cephalosporin.

Uses for Cefprozil

Acute Otitis Media (AOM)

Treatment of AOM caused by Streptococcus pneumoniae, Haemophilus influenzae (including β-lactamase-producing strains), or Moraxella catarrhalis (including β-lactamase-producing strains).

When anti-infectives indicated, AAP recommends high-dose amoxicillin or amoxicillin and clavulanate as drugs of choice for initial treatment of AOM; certain cephalosporins (cefdinir, cefpodoxime, cefuroxime, ceftriaxone) recommended as alternatives for initial treatment in penicillin-allergic patients without a history of severe and/or recent penicillin-allergic reactions.

Pharyngitis and Tonsillitis

Treatment of pharyngitis and tonsillitis caused by S. pyogenes (group A β-hemolytic streptococci). Generally effective in eradicating S. pyogenes from nasopharynx; efficacy in prevention of subsequent rheumatic fever not established to date.

AAP, IDSA, AHA, and others recommend a penicillin regimen (10 days of oral penicillin V or oral amoxicillin or single dose of IM penicillin G benzathine) as treatment of choice for S. pyogenes pharyngitis and tonsillitis; other anti-infectives (oral cephalosporins, oral macrolides, oral clindamycin) recommended as alternatives in penicillin-allergic patients.

If an oral cephalosporin used, 10-day regimen of first generation cephalosporin (cefadroxil, cephalexin) preferred instead of other cephalosporins with broader spectrums of activity (e.g., cefaclor, cefdinir, cefixime, cefpodoxime, cefuroxime).

Respiratory Tract Infections

Treatment of acute sinusitis caused by S. pneumoniae, H. influenzae (including β-lactamase-producing strains), or M. catarrhalis (including β-lactamase-producing strains). Because of variable activity against S. pneumoniae and H. influenzae, IDSA no longer recommends second or third generation oral cephalosporins for empiric monotherapy of acute bacterial sinusitis. Oral amoxicillin or amoxicillin and clavulanate usually recommended for empiric treatment. If an oral cephalosporin used as an alternative in children (e.g., in penicillin-allergic individuals), combination regimen that includes a third generation cephalosporin (cefixime or cefpodoxime) and clindamycin (or linezolid) recommended.

Treatment of secondary bacterial infections of acute bronchitis caused by susceptible S. pneumoniae, H. influenzae (including β-lactamase-producing strains), or M. catarrhalis (including β-lactamase-producing strains).

Treatment of acute bacterial exacerbation of chronic bronchitis caused by susceptible S. pneumoniae, H. influenzae (including β-lactamase producing strains), or M. catarrhalis (including β-lactamase producing strains).

Treatment of mild to moderate community-acquired pneumonia^{† [off-label]} (CAP). If an oral cephalosporin used as an alternative to penicillin G or amoxicillin for treatment of CAP caused by penicillin-susceptible S. pneumoniae, ATS and IDSA recommend cefdinir, cefditoren, cefpodoxime, cefprozil, or cefuroxime.

Skin and Skin Structure Infections

Treatment of uncomplicated skin and skin structure infections caused by Staphylococcus aureus (including penicillinase-producing strains) or S. pyogenes.

Also has been used for treatment of uncomplicated skin and skin structure infections caused by S. epidermidis^{† [off-label]}, S. saprophyticus^{† [off-label]}, group B or G streptococci^{† [off-label]}, E. coli^{† [off-label]}, or K. pneumoniae^†.

Cefprozil Dosage and Administration

Administration

Oral Administration

Administer orally without regard to meals.

Reconstitution

Reconstitute oral suspension at time of dispensing by adding the amount of water specified on the container in 2 equal portions; shake after each addition.

Reconstituted suspensions contain 125 or 250 mg of cefprozil/5 mL.

Shake oral suspension well prior to administration of each dose.

Dosage

Available as cefprozil monohydrate; dosage expressed as anhydrous cefprozil.

Pediatric Patients

General Pediatric Dosage

Oral

Children beyond neonatal period: AAP recommends 15–30 mg/kg daily in 2 equally divided doses for treatment of mild or moderate infections. AAP states the drug is inappropriate for treatment of severe infections.

Acute Otitis Media (AOM)

Oral

Children 6 months to 12 years of age: 15 mg/kg every 12 hours for 10 days.

Pharyngitis and Tonsillitis

Oral

Children 2–12 years of age: 7.5 mg/kg every 12 hours for 10 days.

Children ≥13 years of age: 500 mg once daily for 10 days.

Respiratory Tract Infections

Acute Sinusitis

Oral

Children 6 months to 12 years of age: 7.5 mg/kg every 12 hours for 10 days. For moderate to severe infections, 15 mg/kg every 12 hours for 10 days.

Children ≥13 years of age: 250 mg every 12 hours for 10 days. For moderate to severe infections, 500 mg every 12 hours for 10 days.

Secondary Bacterial Infections of Acute Bronchitis

Oral

Children ≥13 years of age: 500 mg every 12 hours for 10 days.

Acute Exacerbations of Chronic Bronchitis

Oral

Children ≥13 years of age: 500 mg every 12 hours for 10 days.

Skin and Skin Structure Infections

Oral

Children 2–12 years of age: 20 mg/kg once every 24 hours for 10 days.

Children ≥13 years of age: 250 or 500 mg every 12 hours for 10 days or 500 mg once daily for 10 days.

Adults

Pharyngitis and Tonsillitis

Oral

500 mg once daily for 10 days.

Respiratory Tract Infections

Acute Sinusitis

Oral

250 mg every 12 hours for 10 days. For moderate to severe infections, 500 mg every 12 hours for 10 days.

Secondary Bacterial Infections of Acute Bronchitis

Oral

500 mg every 12 hours for 10 days.

Acute Exacerbations of Chronic Bronchitis

Oral

500 mg every 12 hours for 10 days.

Skin and Skin Structure Infections

Oral

250 or 500 mg every 12 hours for 10 days or 500 mg once daily for 10 days.

Special Populations

Hepatic Impairment

Dosage adjustments not required.

Renal Impairment

Dosage adjustments not required in patients with Cl_cr ≥30 mL/minute.

Patients with Cl_cr <30 mL/minute: Administer 50% of the usual dose using usual dosing intervals.

Hemodialysis patients: Administer cefprozil doses after dialysis sessions.

Geriatric Patients

No dosage adjustments required except those related to renal impairment. Cautious dosage selection because of age-related decreases in renal function. See Renal Impairment under Dosage and Administration.

Cautions for Cefprozil

Contraindications

• Known allergy to cefprozil or other cephalosporins.

Warnings/Precautions

Warnings

Superinfection/Clostridium difficile-associated Diarrhea and Colitis

Possible emergence and overgrowth of nonsusceptible bacteria or fungi with prolonged use. Careful observation of the patient is essential. Institute appropriate therapy if superinfection occurs.

Treatment with anti-infectives alters normal colon flora and may permit overgrowth of Clostridium difficile. C. difficile infection (CDI) and C. difficile-associated diarrhea and colitis (CDAD; also known as antibiotic-associated diarrhea and colitis or pseudomembranous colitis) reported with nearly all anti-infectives, including cefprozil, and may range in severity from mild diarrhea to fatal colitis. C. difficile produces toxins A and B which contribute to development of CDAD; hypertoxin-producing strains of C. difficile are associated with increased morbidity and mortality since they may be refractory to anti-infectives and colectomy may be required.

Consider CDAD if diarrhea develops during or after therapy and manage accordingly. Obtain careful medical history since CDAD has been reported to occur as late as 2 months or longer after anti-infective therapy is discontinued.

If CDAD is suspected or confirmed, discontinue anti-infectives not directed against C. difficile whenever possible. Initiate appropriate supportive therapy (e.g., fluid and electrolyte management, protein supplementation), anti-infective therapy directed against C. difficile (e.g., metronidazole, vancomycin), and surgical evaluation as clinically indicated.

Sensitivity Reactions

Hypersensitivity Reactions

Hypersensitivity reactions (anaphylaxis, serum-sickness-like reactions, erythema, Stevens-Johnson syndrome ) have been reported.

If a hypersensitivity reaction occurs, discontinue cefprozil immediately and institute appropriate therapy as indicated (e.g., epinephrine, corticosteroids, and maintenance of an adequate airway and oxygen).

Cross-hypersensitivity

Partial cross-sensitivity among cephalosporins and other β-lactam antibiotics, including penicillins and cephamycins.

Prior to initiation of therapy, make careful inquiry concerning previous hypersensitivity reactions to cephalosporins, penicillins, or other drugs. Cautious use recommended in patients with a history of hypersensitivity to penicillins: avoid use in those who have had an immediate-type (anaphylactic) hypersensitivity reaction and administer with caution in those who have had a delayed-type (e.g., rash, fever, eosinophilia) reaction.

General Precautions

Selection and Use of Anti-infectives

To reduce development of drug-resistant bacteria and maintain effectiveness of cefprozil and other antibacterials, use only for treatment or prevention of infections proven or strongly suspected to be caused by susceptible bacteria.

When selecting or modifying anti-infective therapy, use results of culture and in vitro susceptibility testing. In the absence of such data, consider local epidemiology and susceptibility patterns when selecting anti-infectives for empiric therapy.

Phenylketonuria

Depending on the manufacturer, oral suspensions containing 125 or 250 mg of cefprozil/5 mL contain aspartame (NutraSweet), which is metabolized in the GI tract to provide 28 mg of phenylalanine per 5 mL.

History of GI Disease

Cephalosporins should be used with caution in patients with a history of GI disease, particularly colitis. (See Superinfection/Clostridium difficile-associated Diarrhea and Colitis under Cautions.)

Specific Populations

Pregnancy

Category B.

Lactation

Distributed into milk; use with caution.

Pediatric Use

Safety and efficacy not established in infants <6 months of age for treatment of AOM or acute sinusitis.

Safety and efficacy not established in children <2 years of age for treatment of pharyngitis or tonsillitis or for uncomplicated skin and skin structure infections.

Geriatric Use

Safety and efficacy in those ≥65 years of age similar to that in younger adults, but possibility exists of greater sensitivity to the drug in some geriatric patients.

Substantially eliminated by kidneys; risk of toxicity may be greater in patients with impaired renal function. Select dosage with caution and consider renal function monitoring since geriatric patients are more likely to have renal impairment.

Hepatic Impairment

Half-life only slightly prolonged. Dosage adjustments not required.

Renal Impairment

Decreased clearance.

Use with caution in those with known or suspected renal impairment. Monitor closely and assess renal function prior to and during therapy.

Reduce dosage in those with Cl_cr <30 mL/minute. See Renal Impairment under Dosage and Administration.

Common Adverse Effects

Diarrhea, nausea, vomiting, abdominal pain, rash, genital pruritus or vaginitis, dizziness.

Drug Interactions

Specific Drugs and Laboratory Tests

Cefprozil Pharmacokinetics

Absorption

Bioavailability

Bioavailability is 90–95% in fasting adults; peak plasma concentrations attained within 1.5 hours.

Tablets and oral suspension are bioequivalent under fasting conditions.

Food

Food does not affect absorption or peak plasma concentrations, but time to peak plasma concentrations may be prolonged by 15–45 minutes.

Distribution

Extent

Distributed into various body tissues and fluids including blister fluid, middle ear fluid, and tonsillar and adenoidal tissue.

Distributed into milk in low concentrations.

Plasma Protein Binding

35–45%.

Elimination

Metabolism

Not appreciably metabolized.

Elimination Route

Eliminated principally in urine by glomerular filtration and tubular secretion.

54–70% of a single dose eliminated unchanged in urine within 24 hours.

Half-life

Adults with normal renal function: 1–1.4 hours.

Children 6 months to 12 years of age: 0.94–2.1 hours.

Special Populations

In geriatric patients, clearance decreased and AUC increased.

Plasma half-life increased slightly in patients with hepatic impairment (about 2 hours).

Prolonged plasma half-life (up to 5.2–5.9 hours) in patients with renal impairment.

Stability

Storage

Oral

Tablets

20–25°C in tight, light-resistant container.

For Suspension

20–25°C. After reconstitution, store in a refrigerator; discard after 14 days.

Actions and Spectrum

• Second generation cephalosporin active against some aerobic gram-negative bacteria that generally are resistant to first generation cephalosporins, but has a narrower spectrum of activity than third generation cephalosporins.

• Usually bactericidal.

• Like other β-lactam antibiotics, antibacterial activity results from inhibition of bacterial cell wall synthesis.

• In vitro spectrum of activity includes many gram-positive aerobic bacteria, some gram-negative aerobic bacteria, and some anaerobic bacteria. Inactive against fungi and viruses.

• Gram-positive aerobes: active in vitro and in clinical infections against Staphylococcus aureus (including β-lactamase-producing strains), Streptococcus pneumoniae, and S. pyogenes (group A β-hemolytic streptococci). Also active in vitro against Enterococcus durans, E. faecalis, Listeria monocytogenes, Staphylococcus epidermidis, S. saprophyticus, S. warneri, Streptococcus agalactiae (group B streptococci), and groups C, D, F, and G streptococci. E. faecium and methicillin-resistant (oxacillin-resistant) staphylococci are resistant.

• Gram-negative aerobes: active in vitro and in clinical infections against Haemophilus influenzae (including β-lactamase producing strains) and Moraxella catarrhalis (including β-lactamase-producing strains). Also active in vitro against Citrobacter diversus, Escherichia coli, Klebsiella pneumonia, Neisseria gonorrhoeae, (including β-lactamase-producing strains), Proteus mirabilis, Salmonella, Shigella, and Vibrio. Inactive against most strains of Acinetobacter, Enterobacter, Morganella morganii, P. vulgaris, Providencia, Pseudomonas, and Serratia.

• Anaerobes: active in vitro against Prevotella melaninogenicus, Clostridium difficile, C. perfringens, Fusobacterium, Peptostreptococcus, and Propionibacterium acnes. Most strains of Bacteroides fragilis are resistant.

• Strains of staphylococci resistant to penicillinase-resistant penicillins (methicillin-resistant [oxacillin-resistant] staphylococci) should be considered resistant to cefprozil, although results of in vitro susceptibility tests may indicate that the organisms are susceptible to the drug. In addition, β-lactamase-negative, ampicillin-resistant (BLNAR) strains of H. influenzae should be considered resistant to cefprozil despite the fact that results of in vitro susceptibility tests may indicate that the organisms are susceptible to the drug.

Advice to Patients

• Advise patients that antibacterials (including cefprozil) should only be used to treat bacterial infections and not used to treat viral infections (e.g., the common cold).

• Importance of completing full course of therapy, even if feeling better after a few days.

• Advise patients that skipping doses or not completing the full course of therapy may decrease effectiveness and increase the likelihood that bacteria will develop resistance and will not be treatable with cefprozil or other antibacterials in the future.

• Advise patients that diarrhea is a common problem caused by anti-infectives and usually ends when the drug is discontinued. Importance of contacting a clinician if watery and bloody stools (with or without stomach cramps and fever) occur during or as late as 2 months or longer after the last dose.

• Advise individuals with phenylketonuria and other individuals who must restrict their intake of phenylalanine that cefprozil oral suspensions contain aspartame (NutraSweet), which is metabolized in the GI tract to phenylalanine.

• Importance of notifying clinician of persistent or worsening symptoms of infection.

• Importance of informing clinician if history includes allergy or sensitivity to cephalosporins or penicillins.

• Importance of discontinuing cefprozil and informing clinician if an allergic or hypersensitivity reaction occurs.

• Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.

• Importance of informing clinician of existing or contemplated concomitant therapy, including prescription and OTC drugs.

• Importance of informing patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

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