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First Oral 3rd Generation Cephalosporin


Mechanism of Action

- Bactericidal
- Inhibits bacterial cell wall synthesis


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


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


- 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


Clinical Uses

- Urinary Tract Infections
- Gonorrhoea
- Respiratory Tract Infections


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



- Single dose is effective
- High success rates > 95% in gonococcal urethritis


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


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


Adverse Effects

- Well tolerated
- Commonest adverse effects are diarrhoea and changes in the stools



Usual dosage is 400 mg daily in single or divided doses

Children 8 mg/kg/day


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