Cefixime
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Cefixime
First Oral 3rd Generation Cephalosporin
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Mechanism of
Action
- Bactericidal
- Inhibits bacterial cell wall synthesis
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Antibacterial Activity
- Greater coverage
of Gram negative bacteria than cephalexin and cefadroxil
- Superior binding to penicillin binding proteins than cephalexin and
cefadroxil for greater antibacterial activity
- Greater stability against beta-lactamases that cephalexin and cefadroxil;
beta-lactamase stability similar to cefuroxime and ceftizoxime
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Antibacterial
Spectrum
Gram positive
and gram negative bacteria including streptococci, gonococci, Enterobacteriaceae
(e.g., E. coli, Salmonella, Klebsiella pneumoniae, Proteus mirabilis,
P. vulgaris), H. influenzae
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Pharmacokinetics
-
Peak plasma concentration 3-4 hours
- Half life 3 hours approx.
- Increased AUC in elderly
- Food/antacids - no significant effect on absorption
- Well distributed in body
- Not metabolised in body; excreted unchanged in urine
- Renal impairment - dose adjustment only required if creatinine clearance
< 20 ml/min
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Clinical Uses
- Urinary
Tract Infections
- Gonorrhoea
- Respiratory Tract Infections
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Urinary Tract
Infections (UTI)
- Good
efficacy in complicated and uncomplicated UTI
- Covers important causes of UTI, including E.coli, K.pneumoniae and
P.mirabilis
- Efficacy > 90%
- Similar success rates compared to norfloxacin and amoxycillin
- Tolerability similar to amoxycillin, but diarrhoea may be commoner
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Gonorrhoea
- Single
dose is effective
- High success rates > 95% in gonococcal urethritis
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Lower Respiratory
tract infections
- Good
coverage of H.influenzae and Strep. pneumoniae
- Similar results to cefaclor and amoxycillin-clavulanic acid
- Better results in acute than chronic infections
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Upper respiratory
tract infections and otitis media
- Effective
in URTI including pharyngitis, tonsillitis and otitis media
- Excellent results = 100% success in some studies
- Efficacy in otitis media better than cefaclor
- Superior to amoxycillin against H.influenzae in otitis media
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Adverse Effects
- Well
tolerated
- Commonest adverse effects are diarrhoea and changes in the stools
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Dosage
Usual dosage
is 400 mg daily in single or divided doses
Children 8 mg/kg/day
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Salient Features
- 3rd generation
cephalosporin with once daily oral administration
- Compared to oral 2nd generation cephalosporins, less active against
gm +ve cocci and more active against Enterobacteriaceae and beta-lactamase
producing H.influenzae and N.gonorrhoeae. Poor activity against Staph
aureus
- Dosage 400 mg daily
- Useful in UTI, gonorrhoea, RTI and otitis media
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