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cefotaxime (Claforan)
Tradename: Claforan. 3rd generation cephalosporin.
Indications:
- treatment of bacterial infections due to susceptible organisms
- gram negative rod infection (other than Pseudomonas)
- CNS infections
- documented or suspected meningitis
- lower respiratory tract infections
- pneumonia
- ventilator-associated pneumonia
- intra-abdominal infections
- peritonitis
- urogenital infections
- skin or soft tissue infections
- sepsis
- proctitis
- ophthalmia neonatorum
- prophylaxis for perioperative infection
- cesarean section
- empiric treatment of fever of unknown origin
Dosage:
1) 1-2g IV/IM every 6-8 hours.
2) Children: 50-180 mg/kg/day IV divided every 4-6 hours.
3) meningitis: 200 mg/kg/day
4) severe infection (> 50 kg) : 1-2 g every 4-6 hours
5) life-threatening infection 2 g every 4 hours
6) maximum: 12 g/day
Dosage adjustment in renal failure:
creatinine clearance dosage
> 50-90 mL/min 1-2 g every 8-12 hours
10-50 mL/min* 1-2 g every 12-24 hours
< 10 mL/min# 1-2 g every 24 hours
* same dose for continuous arteriovenous hemofiltration
# 1 g IV after hemodialysis
Pharmacokinetics:
1) widely distributed to body tissues & fluids, including
a) aqueous humor, ascitic fluid, prostatic fluid bone
b) penetrates CSF when meninges are inflammed
c) crosses placenta
d) appears in breast milk
2) protein bindng 31-50%
3) partially metabolized in the liver to an active metabolite, desacetylcefoxatime
4) elimination 1/2life:
a) cefotaxime: 1-1.5 hours, prolinged with renal &/or hepatic insufficiency (15-35 hours ESRD)
b) desacetylcefoxatime: 1.5-1.9 hours, prolonged with renal impairment
c) 60% excreted unchanged in the urine, 23% as metabolites
5) time to peak serum concentration:
a) 5 minutes after IV administration
b) within 30 minutes after IM administration
6) elimination by hemodialysis 20-50%
Antimicrobial activity:
Gram positive
- Streptococcus
- Streptococcus group A
- Streptococcus group B
- Streptococcus group C
- Streptococcus group G
- Streptococcus pneumonia
- Streptococcus viridans, milleri
- Staphylococcus
- Staphylococcus aureus (MSSA)
- Staphylococcus epidermidis (+/-)
Gram negative
- Neisseria
- Neisseria gonorrhoeae
- Neisseria meningitidis
- Moraxella catarrhalis
- Haemophilus
- Haemophilus influenzae
- Haemophilus parainfluenzae
- Haemophilus ducreyi
- Escherichia coli
- Klebsiella species
- Enterobacter species
- Serratia species
- Salmonella species
- Shigella species
- Proteus
- Proteus mirabilis
- Proteus vulgaris
- Providencia species
- Morganella species
- Morganella morganii [5]
- Citrobacter species
- Citrobacter diversus
- Aeromonas species
- Acinetobacter species
- Pseudomonas
- Pseudomonas aeruginosa (+/-)
- Pseudomonas cepacia
- Yersinia
- Yersinia enterocolitica
- Yersinia pseudotuberculosis
Anaerobes
- Bacteroides melaninogenicus
- Clostridium species
- Peptostreptococcus species
- Fusobacterium [5]
Adverse effects:
1) not common (1-10%)
- pain at injection site, rash, pruritus, fever, eosinophilia, colitis, diarrhea, nausea/vomiting
2) uncommon (< 1%)
- headache, pseudomembranous colitis, transient neutropenia, thrombocytopenia, phlebitis transient elevation of BUN, creatinine, transaminases
3) other
- Coomb's test may be positive
Drug interactions:
-> probenecid decreases renal clearance of cefotaxime by 50%
Laboratory:
1) specimen:
a) serum
b) keep specimen on ice-water
c) centrifuge at 4 degrees C
d) remove cells as soon as possible
e) freeze at -70 degrees C until assayed
2) methods: HPLC, MB
3) interferences:
-> desacetyl metabolite may interfere with microbiological assay (MB)
Interactions
drug interactions
drug adverse effects of cephalosporins
General
cephalosporin, 3rd generation
Properties
MISC-INFO: elimination route KIDNEY
LIVER
1/2life 1.1 +/- 0.2 HOURS
protein-binding 36%
pregnancy-category B
safety in lactation ?
elimination by hemodialysis +/-
Database Correlations
PUBCHEM correlations
References
- The Pharmacological Basis of Therapeutics, 9th ed.
Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- Sanford Guide to antimicrobial therapy 1997
- Kaiser Permanente Northern California Regional Drug
Formulary, 1998
- Clinical Guide to Laboratory Tests, 3rd ed. Teitz ed.,
W.B. Saunders, 1995
- Deprecated Reference
- Department of Veterans Affairs, VA National Formulary