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Oral cephalosporins
1Department of Bacteriology, U.Z. St Rafaël, Leuven, Belgium.
Abstract:
The arrival of new cephalosporins faces the clinician with an evergrowing confusion as to the drug of choice. The older agents (cephalexin, cephradine, cefadroxil and cefaclor) and the newer formulations cefatrizine and cefuroxime axetil are intensively used for treatment of mild and moderate infections. The oldest agents have a better pharmacokinetic profile but are less active against Gram-positives and Gram-negatives. Cefaclor, cefatrizine and cefuroxime axetil have improved in vitro activity against H. influenzae and/or against S. aureus and M. catarrhalis. However the mean free serum concentrations after proposed standard daily doses of cefaclor (3 x 250 mg/d), cefatrizine (2 x 500 mg/d) and cefuroxime-axetil (2 x 250 mg/d) are lower than those of the older cephalosporins. In comparison amoxicillin-clavulanate is equally efficacious, has a more reliable pharmacokinetic profile and is less expensive than cefaclor and cefuroxime axetil in a comparable dose (e.g. 3 x 500 mg/d).
Insights
Choosing the right cephalosporin is confusing. Newer agents like cefaclor and cefuroxime axetil show better in vitro activity but have lower serum concentrations than older cephalosporins, with amoxicillin-clavulanate offering a comparable alternative.
Area of Science:
- Pharmacology
- Infectious Diseases
- Microbiology
Background:
- The increasing number of cephalosporin antibiotics presents a challenge for clinicians in selecting the optimal drug.
- Older cephalosporins (cephalexin, cephradine, cefadroxil) and newer formulations (cefaclor, cefatrizine, cefuroxime axetil) are widely used for mild to moderate infections.
Purpose of the Study:
- To compare the pharmacokinetic profiles and in vitro activity of older and newer cephalosporins.
- To evaluate amoxicillin-clavulanate as a potential alternative to newer cephalosporins.
Main Methods:
- Comparative analysis of pharmacokinetic profiles (serum concentrations) and in vitro activity against key pathogens.
- Evaluation of efficacy and cost-effectiveness of amoxicillin-clavulanate versus cefaclor and cefuroxime axetil.
Main Results:
- Older cephalosporins possess better pharmacokinetic profiles but exhibit reduced activity against Gram-positive and Gram-negative bacteria compared to newer agents.
- Cefaclor, cefatrizine, and cefuroxime axetil demonstrate enhanced in vitro activity against specific pathogens like H. influenzae, S. aureus, and M. catarrhalis.
- Despite improved in vitro activity, newer cephalosporins achieve lower mean free serum concentrations than older agents at standard doses. Amoxicillin-clavulanate shows comparable efficacy, superior pharmacokinetics, and lower cost than cefaclor and cefuroxime axetil.
Conclusions:
- Clinicians must weigh the improved in vitro activity of newer cephalosporins against their less favorable pharmacokinetic profiles.
- Amoxicillin-clavulanate emerges as a cost-effective and pharmacokinetically reliable alternative for treating mild to moderate infections, comparable in efficacy to certain newer cephalosporins.