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cefuroxime (Zinacef, Ceftin)
Tradename: Zinacef, Ceftin. 2nd generation cephalosporin.
Indications:
- treatment of moderate bacterial infections due to susceptible organisms
- empiric antibiotic therapy for community-acquired pneumonia
- step-down therapy for community-acquired pneumonia
- skin or soft tissue infections
- impetigo
- Lyme disease
- acute otitis media
- infectious arthritis, osteomyelitis
- urogenital infections
- gonorrhea
- proctitis [7]
- penetrates into CSF & may be used for the treatment of meningitis with susceptible organisms
- prophylaxis for perioperative infection
- open heart surgery
- empiric therapy for fever of unknown origin [7]
Contraindications:
- Enterococcus, MRSA & Pseudomonas aeruginosa
- anaerobic coverage
Dosage:
1) adults
a) 750-1500 mg IV/IM every 8 hours
b) 100-150 mg/kg/day divided every 8 hours
c) maximum: 6 g/day
d) 250-1000 mg PO BID-TID
2) children:
a) 75-150 mg/kg/day divided every 8 hours
b) 50-100 mg/kg/day IV divided 6-8 hours
c) 250-500 mg PO BID
d) meningitis 200-240 mg/kg/day IV/IM
e) maximum: 9 g/day
3) neonates
a) 20-30 mg/kg/day PO divided every 12 hours
b) 10-25 mg/kg/day IM/IV divided every 12 hours
Tabs: 125, 250, 500 mg, Suspension: 125 mg/5 mL.
Injection: 750 mg, 1.5 g.
Dosage adjustment in renal failure:
creatinine clearance dosage
10-30 mL/min every 12 hours
< 10 mL/min every 24 hours
dose after hemodialysis
Pharmacokinetics:
1) oral absorption increased 40-50% when taken with food
2) widely distributed to body tissues
a) therapeutic concentrations achieved in CSF even when meninges are not inflammed
b) crosses placenta
c) appears in breast milk
3) peak serum concentration within 15-60 minutes after IM injection
4) protein binding 33-50%
5) 1/2life 1-2 hours (17 hours ESRD)
6) eliminated unchanged in the urine by both glomerular filtration & tubular excretion
7) dose adjustment is necessary with renal insufficiency
Antimicrobial activity:
Gram positive
- Streptococcus
- Streptococcus group A
- Streptococcus group B
- Streptococcus group C
- Streptococcus group G
- Streptococcus pneumonia
- Streptococcus viridans, milleri
- Staphylococcus aureus (MSSA)
- Staphylococcus epidermidis (+/-)
Gram negative
- Neisseria gonorrhoeae
- Neisseria meningitidis
- Moraxella catarrhalis
- Haemophilus influenzae
- Haemophilus parainfluenzae [7]
- Escherichia coli
- Klebsiella species
- Enterobacter species (+/-)
- Salmonella species
- Shigella species
- Proteus mirabilis
- Providencia species
- Morganella species (+/-)
- Citrobacter species (+/-)
- Aeromonas species (+/-)
- Yersinia enterocolitica (+/-)
- Haemophilus ducreyi
Anaerobes
- Bacteroides melaninogenicus
- Clostridium species
- Peptostreptococcus species
Adverse effects:
1) not common (1-10%)
- thrombophlebitis, anemia, eosinophilia (hypersensitivity)
2) uncommon (< 1%)
- dizziness, fever, headache, rash, nausea/vomiting, diarrhea, epigastric pain, GI bleeding, colitis, neutropenia (transient), pain at site of injection, vaginitis, transient increase in serum transaminases & alkaline phosphatase, increase in serum creatinine &/or BUN
3) cross-reactivity with penicillin 2-5%
Drug interactions:
- probenecid increases & prolongs 1/2life of cefuroxime
Mechanism of action: inhibition of bacterial cell wall synthesis.
Interactions
drug interactions
drug adverse effects of cephalosporins
General
cephalosporin, 2nd generation
Properties
MISC-INFO: elimination route KIDNEY
1/2life 1-2 HOURS
protein-binding 33-50%
pregnancy-category B
safety in lactation ?
Database Correlations
PUBCHEM correlations
References
- The Pharmacological Basis of Therapeutics, 9th ed.
Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- Harrison's Principles of Internal Medicine, 13th ed.
Companion Handbook. Isselbacher et al (eds),
McGraw-Hill Inc. NY, 1995, pg 162
- Medical Knowledge Self Assessment Program (MKSAP) 11, American
College of Physicians, Philadelphia 1998
- Sanford Guide to antimicrobial therapy 1997
- Drug Information & Medication Formulary, Veterans Affairs,
Central California Health Care System, 1st ed., Ravnan et al
eds, 1998
- Kaiser Permanente Northern California Regional Drug
Formulary, 1998
- Deprecated Reference