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Pronunciation |
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(se
fyoor OKS
eem) |
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U.S. Brand
Names |
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Ceftin® Oral; Kefurox® Injection;
Zinacef®
Injection |
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Generic
Available |
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No |
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Synonyms |
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Cefuroxime Axetil; Cefuroxime Sodium |
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Pharmacological Index |
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Antibiotic, Cephalosporin (Second Generation) |
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Use |
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Treatment of infections caused by staphylococci, group B streptococci, H.
influenzae (type A and B), E. coli, Enterobacter,
Salmonella, and Klebsiella; treatment of susceptible infections of
the lower respiratory tract, otitis media, urinary tract, skin and soft tissue,
bone and joint, sepsis and gonorrhea |
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Pregnancy Risk
Factor |
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B |
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Contraindications |
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Hypersensitivity to cefuroxime, any component, or
cephalosporins |
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Warnings/Precautions |
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Modify dosage in patients with severe renal impairment, prolonged use may
result in superinfection; use with caution in patients with a history of
penicillin allergy, especially IgE-mediated reactions (eg, anaphylaxis,
urticaria); may cause antibiotic-associated colitis or colitis secondary to
C. difficile |
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Adverse
Reactions |
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1% to 10%:
Hematologic: Eosinophilia (7%), decreased hemoglobin and hematocrit (10%)
Hepatic: Increased transaminases (4%), increased alkaline phosphatase (2%)
Local: Thrombophlebitis (1.7%)
<1%: Anaphylaxis, erythema multiforme, toxic epidermal necrolysis,
Stevens-Johnson syndrome, interstitial nephritis, dizziness, fever, headache,
rash, nausea, vomiting, diarrhea, stomach cramps, GI bleeding, colitis,
neutropenia, leukopenia, increased creatinine, increased BUN, pain at injection
site, vaginitis, seizures, angioedema, pseudomembranous colitis
Other reactions with cephalosporins include toxic nephropathy, cholestasis,
agranulocytosis, colitis, pancytopenia, aplastic anemia, hemolytic anemia,
hemorrhage, prolonged PT, encephalopathy, asterixis, neuromuscular excitability,
serum-sickness reactions, superinfection |
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Overdosage/Toxicology |
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After acute overdose, most agents cause only nausea, vomiting, and diarrhea,
although neuromuscular hypersensitivity and seizures are possible, especially in
patients with renal insufficiency; many beta-lactam antibiotics have the
potential to cause neuromuscular hyperirritability or seizures
Hemodialysis may be helpful to aid in the removal of the drug from the blood
but not usually indicated, otherwise most treatment is supportive or symptom
directed following GI decontamination |
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Drug
Interactions |
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Increased effect: High-dose probenecid decreases clearance
Increased toxicity: Aminoglycosides increase nephrotoxic potential
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Stability |
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Reconstituted solution is stable for 24 hours at room temperature and 48
hours when refrigerated; I.V. infusion in NS or D5W solution is
stable for 24 hours at room temperature, 7 days when refrigerated, or 26 weeks
when frozen; after freezing, thawed solution is stable for 24 hours at room
temperature or 21 days when refrigerated |
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Mechanism of
Action |
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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. |
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Pharmacodynamics/Kinetics |
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Absorption: Oral (cefuroxime axetil): Increased when given with or shortly
after food or infant formula (37% to 52%)
Distribution: Widely distributed to body tissues and fluids; crosses
blood-brain barrier; therapeutic concentrations achieved in CSF even when
meninges are not inflamed; crosses placenta and reaches breast milk
Protein binding: 33% to 50%
Bioavailability, axetil: Oral: 37% to 52%
Half-life:
Neonates: less than or equal to 3 days: 5.1-5.8 hours; 6-14 days: 2-4.2
hours; 3-4 weeks: 1-1.5 hours
Adults: 1-2 hours (prolonged in renal impairment)
Time to peak serum concentration: I.M.: Within 15-60 minutes
Elimination: Primarily excreted 66% to 100% as unchanged drug in urine by
both glomerular filtration and tubular secretion |
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Usual Dosage |
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Children:
Pharyngitis, tonsillitis: Oral:
Suspension: 20 mg/kg/day (maximum: 500 mg/day) in 2 divided doses
Tablet: 125 mg every 12 hours
Acute otitis media, impetigo: Oral:
Suspension: 30 mg/kg/day (maximum: 1 g/day) in 2 divided doses
Tablet: 250 mg every 12 hours
I.M., I.V.: 75-150 mg/kg/day divided every 8 hours; maximum dose: 6 g/day
Meningitis: Not recommended (doses of 200-240 mg/kg/day divided every 6-8
hours have been used); maximum dose: 9 g/day
Adults:
Oral: 250-500 mg twice daily; uncomplicated urinary tract infection: 125-250
mg every 12 hours
I.M., I.V.: 750 mg to 1.5 g/dose every 8 hours or 100-150 mg/kg/day in
divided doses every 6-8 hours; maximum: 6 g/24 hours
Dosing adjustment in renal impairment:
Clcr 10-20 mL/minute: Administer every 12 hours
Clcr <10 mL/minute: Administer every 24 hours
Hemodialysis: Dialyzable (25%)
Note: Cefuroxime axetil film-coated tablets and oral suspension are
not bioequivalent and are not substitutable on a mg/mg basis
Continuous arteriovenous or venovenous hemodiafiltration (CAVH) effects: Dose
as for Clcr 10-20 mL/minute |
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Dietary
Considerations |
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May be taken with food, however, bioavailability is increased with
food |
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Monitoring
Parameters |
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Observe for signs and symptoms of anaphylaxis during first dose; with
prolonged therapy, monitor renal, hepatic, and hematologic function
periodically |
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Test
Interactions |
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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 |
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Mental Health: Effects
on Mental Status |
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May cause nervousness; case reports of euphoria, delusion, illusions, and
depersonalization with cephalosporins |
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Mental Health:
Effects on Psychiatric
Treatment |
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May rarely cause neutropenia; use caution with clozapine and
carbamazepine |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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No information available to require special precautions |
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Dental Health:
Effects on Dental Treatment |
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No effects or complications reported |
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Patient
Information |
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Take as directed, at regular intervals around-the-clock (with or without
food). Chilling oral suspension improves flavor (do not freeze). Complete full
course of medication, even if you feel better. Drink 2-3 L fluid/day. If
diarrhea occurs, yogurt or buttermilk may help. May cause false-positive test
with Clinitest®; use another form of testing. May
interfere with oral contraceptives; additional contraceptive measures are
necessary. Report severe, unresolved diarrhea; vaginal itching or drainage;
sores in mouth; blood, pus, or mucus in stool or urine; easy bleeding or
bruising; unusual fever or chills; rash; or respiratory difficulty.
Breast-feeding precautions: Consult prescriber if
breast-feeding. |
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Nursing
Implications |
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Do not admix with aminoglycosides in same bottle/bag; obtain specimens for
culture and sensitivity prior to the first dose |
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Dosage Forms |
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Infusion, as sodium, premixed (frozen) (Zinacef®): 750
mg (50 mL); 1.5 g (50 mL)
Powder for injection, as sodium: 750 mg, 1.5 g, 7.5 g
Powder for injection, as sodium (Kefurox®,
Zinacef®): 750 mg, 1.5 g, 7.5 g
Powder for oral suspension, as axetil (tutti-frutti flavor)
(Ceftin®): 125 mg/5 mL (50 mL, 100 mL, 200 mL); 250 mg/5
mL (50 mL, 100 mL)
Tablet, as axetil (Ceftin®): 125 mg, 250 mg, 500 mg
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References |
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American Thoracic Society,
"Guidelines for the Initial Management of Adults With Community-Acquired Pneumonia: Diagnosis Assessment of Severity and Initial Antimicrobial Therapy,"
Am Rev Respir Dis, 1993, 148(5):1418-26.
"Antimicrobial Prophylaxis in Surgery," Med Lett Drugs Ther, 1993,
35(906):91-4.
Broekhuysen J, Deger F, Douchamps J, et al,
"Pharmacokinetic Study of Cefuroxime in the Elderly," Br J Clin
Pharmacol, 1981, 21(6):801-5.
de Louvois J, Mulhall A, and Hurley R,
"Cefuroxime in the Treatment of Neonates," Arch Dis Child, 1982,
57(1):59-62.
Donowitz GR and Mandell GL, "Beta-Lactam Antibiotics," N Engl J Med,
1988, 318(7):419-26 and 318(8):490-500.
Douglas JG, Bax RP, and Munro JF,
"The Pharmacokinetics of Cefuroxime in the Elderly," J Antimicrob
Chemother, 1980, 6(4):543-9.
Gentry LO, Zeluff BJ, and Cooley DA,
"Antibiotic Prophylaxis in Open-Heart Surgery: A Comparison of Cefamandole, Cefuroxime, and Cefazolin,"
Ann Thorac Surg, 1988, 46(2):167-71.
Gooch WM 3rd, Blair E, Puopolo A, et al,
"Effectiveness of Five Days of Therapy With Cefuroxime Axetil Suspension for Treatment of Acute Otitis Media,"
Pediatr Infect Dis J, 1996, 15(2):157-64.
Marshall WF and Blair JE, "The Cephalosporins," Mayo Clin Proc, 1999,
74(2):187-95.
Nelson JD,
"Cefuroxime: A Cephalosporin With Unique Applicability to Pediatric Practice,"
Pediatr Infect Dis, 1983, 2(5):394-6.
Perry CM and Brogden RN,
"Cefuroxime Axetil. A Review of Its Antibacterial Activity, Pharmacokinetic Properties and Therapeutic Efficacy,"
Drugs, 1996, 52(1):125-58.
Peterson CD, Lake KD, Arom KV, et al,
"Antibiotic Prophylaxis in Open-Heart Surgery Patients: Comparison of Cefamandole and Cefuroxime,"
Drug Intell Clin Pharm, 1987, 21(9):728-32.
Thoene DE and Johnson CE, "Pharmacotherapy of Otitis Media,"
Pharmacotherapy, 1991, 11(3):212-21. |
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