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Cefprozil

Pronunciation

Pronunciation

(sef PROE zil)

Index Terms

  • Cefzil

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Suspension Reconstituted, Oral:

Generic: 125 mg/5 mL (50 mL, 75 mL, 100 mL); 250 mg/5 mL (50 mL, 75 mL, 100 mL)

Tablet, Oral:

Generic: 250 mg, 500 mg

Pharmacologic Category

  • Antibiotic, Cephalosporin (Second Generation)

Pharmacology

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.

Absorption

Well absorbed (95%)

Distribution

Vd: 0.23 L/kg

Excretion

Urine (~60% as unchanged drug)

Time to Peak

Serum: Fasting: 1.5 hours

Half-Life Elimination

Infants and Children (6 months to 12 years): 1.5 hours

Adults:

Normal renal function: 1.3 hours

Renal impairment: 5.2 hours

Renal failure: 5.9 hours

Hepatic impairment: 2 hours

Protein Binding

~36%

Special Populations: Elderly

AUC is about 35% to 60% higher.

Use: Labeled Indications

Pharyngitis/tonsillitis: Treatment of mild to moderate pharyngitis/tonsillitis caused by Streptococcus pyogenes.

Limitations of use: Cefprozil is generally effective in the eradication of S. pyogenes from the nasopharynx; however, substantial data establishing the efficacy of cefprozil in the subsequent prevention of rheumatic fever are not available at present.

Otitis media: Treatment of mild to moderate infection caused by S. pneumoniae, Haemophilus influenzae (including beta-lactamase–producing strains), and Moraxella (Branhamella) catarrhalis (including beta-lactamase–producing strains).

Secondary bacterial infection of acute bronchitis and acute bacterial exacerbation of chronic bronchitis: Treatment of secondary bacterial infections in acute bronchitis and acute bacterial exacerbations of chronic bronchitis caused by S. pneumoniae, H. influenzae (including beta-lactamase–producing strains), and M. catarrhalis (including beta-lactamase–producing strains).

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

Contraindications

Hypersensitivity to cefprozil, any component of the formulation, or other cephalosporins

Dosing: Adult

Pharyngitis/tonsillitis: Oral: 500 mg every 24 hours for 10 days (administer for ≥10 days if due to S. pyogenes)

Secondary bacterial infection of acute bronchitis or acute bacterial exacerbation of chronic bronchitis: Oral: 500 mg every 12 hours for 10 days

Skin and skin-structure infections, uncomplicated: Oral: 250 to 500 mg every 12 hours, or 500 mg every 24 hours for 10 days

Dosing: Geriatric

Refer to adult dosing.

Dosing: Pediatric

Otitis media: Oral: Infants ≥6 months and Children: 15 mg/kg/dose every 12 hours for 10 days (maximum: 500 mg/dose)

Pharyngitis/tonsillitis:

Children 2 to 12 years: Oral: 7.5 mg/kg/dose every 12 hours for 10 days (administer for ≥10 days if due to S. pyogenes) (maximum: 500 mg/day)

Children >12 years and Adolescents: Refer to adult dosing.

Secondary bacterial infection of acute bronchitis or acute bacterial exacerbation of chronic bronchitis: Children >12 years and Adolescents: Refer to adult dosing.

Skin and skin-structure infections, uncomplicated:

Children 2 to 12 years: Oral: 20 mg/kg/day once every 24 hours for 10 days (maximum: 1,000 mg/day)

Children >12 years and Adolescents: Refer to adult dosing.

Urinary tract infection (off-label use): Infants and Children 2 to 24 months: Oral: 15 mg/kg/dose twice daily for 7 to 14 days (AAP, 2011)

Dosing: Renal Impairment

Manufacturer's labeling: Infants, Children, Adolescents, and Adults: Oral:

CrCl ≥30 mL/minute: No dosage adjustment necessary.

CrCl <30 mL/minute: Reduce dose by 50%.

End-stage renal disease (ESRD) on hemodialysis: Give dose after dialysis on dialysis days.

Alternative recommendations (Aronoff, 2007):

Adults: Oral:

CrCl >50 mL/minute: No dosage adjustment necessary

CrCl <50 mL/minute: Administer 50% of usual dose every 12 hours

Intermittent hemodialysis (IHD): Supplement with 250 mg after dialysis on dialysis days

Peritoneal dialysis: Administer 50% of usual dose every 12 hours

Infants, Children, and Adolescents: Oral:

Recommendations based on 30 mg/kg/day divided every 12 hours in patients with normal renal function:

GFR ≥30 mL/minute/1.73 m2: No dosage adjustment necessary.

GFR <29 mL/minute/1.73 m2: 7.5 mg/kg/dose every 12 hours

ESRD on hemodialysis: 7.5 mg/kg/dose every 12 hours; supplement with 5 mg/kg/dose after dialysis on dialysis days

Peritoneal dialysis: 7.5 mg/kg/dose every 12 hours

Dosing: Hepatic Impairment

No dosage adjustment necessary.

Reconstitution

Oral suspension: Refer to manufacturer’s product labeling for reconstitution instructions. Shake well.

Administration

Oral: Administer without regard to meals. Administer around the clock to promote less variation in peak and trough serum levels.

Dietary Considerations

Oral suspension may contain phenylalanine; consult product labeling.

Storage

Store at 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°F). Refrigerate suspension after reconstitution; discard after 14 days.

Drug Interactions

Aminoglycosides: Cephalosporins (2nd Generation) may enhance the nephrotoxic effect of Aminoglycosides. Monitor therapy

BCG (Intravesical): Antibiotics may diminish the therapeutic effect of BCG (Intravesical). Avoid combination

BCG Vaccine (Immunization): Antibiotics may diminish the therapeutic effect of BCG Vaccine (Immunization). Monitor therapy

Cholera Vaccine: Antibiotics may diminish the therapeutic effect of Cholera Vaccine. Avoid combination

Lactobacillus and Estriol: Antibiotics may diminish the therapeutic effect of Lactobacillus and Estriol. Monitor therapy

Probenecid: May increase the serum concentration of Cephalosporins. Monitor therapy

Sodium Picosulfate: Antibiotics may diminish the therapeutic effect of Sodium Picosulfate. Management: Consider using an alternative product for bowel cleansing prior to a colonoscopy in patients who have recently used or are concurrently using an antibiotic. Consider therapy modification

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 3 days after cessation of antibacterial agents. Consider therapy modification

Vitamin K Antagonists (eg, warfarin): Cephalosporins may enhance the anticoagulant effect of Vitamin K Antagonists. Monitor therapy

Test Interactions

Positive direct Coombs, false-positive urinary glucose test using cupric sulfate (Benedict's solution, Clinitest, Fehling's solution), but not with enzyme-based tests for glycosuria (eg, Clinistix). A false-negative reaction may occur in the ferricyanide test for blood glucose.

Adverse Reactions

Frequency not always defined.

1% to 10%:

Central nervous system: Dizziness (1%)

Dermatologic: Diaper rash (2%), genital pruritus (2%)

Gastrointestinal: Nausea (4%), diarrhea (3%), abdominal pain (1%), vomiting (1%)

Genitourinary: Vaginitis

Hepatic: Increased serum transaminases (2%)

Infection: Superinfection

<1% (Limited to important or life-threatening): Anaphylaxis, angioedema, arthralgia, cholestatic jaundice, confusion, drowsiness, eosinophilia, erythema multiforme, fever, headache, hyperactivity, increased blood urea nitrogen, increased serum creatinine, insomnia, leukopenia, pseudomembranous colitis, serum sickness, skin rash, Stevens-Johnson syndrome, thrombocytopenia, urticaria

Warnings/Precautions

Concerns related to adverse effects:

• Hypersensitivity: If a serious hypersensitivity reaction occurs, discontinue and institute emergency supportive measures, including airway management and treatment (eg, epinephrine, antihistamines and/or corticosteroids).

• Penicillin allergy: Use with caution in patients with a history of penicillin allergy.

• 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:

• Gastrointestinal disease: Use with caution in patients with a history of gastrointestinal disease, particularly colitis.

• Renal impairment: Use with caution in patients with renal impairment; modify dosage in severe impairment.

Concurrent drug therapy issues:

• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

Dosage form specific issues:

• Benzyl alcohol and derivatives: Some dosage forms may contain sodium benzoate/benzoic acid; benzoic acid (benzoate) is a metabolite of benzyl alcohol; large amounts of benzyl alcohol (≥99 mg/kg/day) have been associated with a potentially fatal toxicity ("gasping syndrome") in neonates; the "gasping syndrome" consists of metabolic acidosis, respiratory distress, gasping respirations, CNS dysfunction (including convulsions, intracranial hemorrhage), hypotension, and cardiovascular collapse (AAP ["Inactive" 1997]; CDC 1982). Some data suggest that benzoate displaces bilirubin from protein-binding sites (Ahlfors 2001); avoid or use dosage forms containing benzyl alcohol derivative with caution in neonates. See manufacturer’s labeling.

• Phenylalanine: Some products may contain phenylalanine.

• Polysorbate 80: Some dosage forms may contain polysorbate 80 (also known as Tweens). Hypersensitivity reactions, usually a delayed reaction, have been reported following exposure to pharmaceutical products containing polysorbate 80 in certain individuals (Isaksson, 2002; Lucente 2000; Shelley, 1995). Thrombocytopenia, ascites, pulmonary deterioration, and renal and hepatic failure have been reported in premature neonates after receiving parenteral products containing polysorbate 80 (Alade, 1986; CDC, 1984). See manufacturer's labeling.

Monitoring Parameters

Monitor renal function at baseline and as clinically indicated. Monitor for signs of anaphylaxis during first dose.

Pregnancy Risk Factor

B

Pregnancy Considerations

Adverse events were not observed in animal reproduction studies.

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience nausea or diarrhea. Have patient report immediately to prescriber bruising, bleeding, severe loss of strength and energy, seizures, urinary retention, change in amount of urine passed, vaginitis, or signs of Clostridium difficile (C. diff)-associated diarrhea (abdominal pain or cramps, severe diarrhea or watery stools, or bloody stools) (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.

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