Clinical Pharmacokinetics of the Third Generation Cephalosporins

  title={Clinical Pharmacokinetics of the Third Generation Cephalosporins},
  author={Luc P. Balant and Pierre Dayer and Raymond Auckenthaler},
  journal={Clinical Pharmacokinetics},
SummaryAt the present time, the third generation cephalosporins that are already on the market or close to this point include cefsulodin, cefotaxime, cefoperazone, latamoxef, ceftriaxone, ceftazidime, ceftizoxime and cefotetan. Other newer compounds are also under development but have not been included in this review.None of the third generation compounds is suitable for oral administration and, accordingly, their pharmacokinetics have been studied only after intravenous and intramuscular… 

Cefetamet Pivoxil Clinical Pharmacokinetics

Results following ascending intravenous doses of cefetamet in healthy young male volunteers demonstrated that the pharmacokinetics of intravenous cefETamet are independent of the dose.

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The predominant renal elimination of cefetamet and the lack of effect of age and disease on cefETamet pivoxil absorption make dosage adjustment in relation to renal dysfunction simple and reliable.

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Cefetamet Pivoxil

Preliminary data indicate that single dose cefetamet pivoxil can effectively eradicate N. Gonorrhoeae from both men and women and offers effective alternative oral therapy for outpatient treatment of community-acquired respiratory tract infections, with the advantage of improved activity against H. Influenzae and increased β-lactamase stability.

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The results indicate that in the therapeutic plasma concentration range of cefuroxime its renal clearance is not saturated, and probenecid at therapeutic doses will block tubular excretion of cafurxime almost completely.

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Because of its unusually long plasma half-life, the availability of intramuscular administration and its high intrinsic activity against many organisms, ceftriaxone has become a popular agent in once-daily therapy of infections in paediatric patients, gonococcal infections and outpatient management of pneumonia and osteomyelitis.

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The pharmacokinetics and protein binding of cefotaxime and desacetylcefotaxim were studied in rat and the binding characteristics were in good agreement with those of the metabolite produced in vivo, with a K value of 8.1.



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Comparison of in vitro studies with the pharmacokinetic properties show that 2 g cefoperazone given intravenously twice a day should inhibit most sensitive bacteria.

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[Pharmacokinetic study of a cephalosporin, cefoperazone, in liver failure].

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The metabolism of 14C-CTX in rats, dogs, and humans as well as in vitro studies in cells of rats and rabbits are discussed, showing differences in metabolism between the species.

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