Clinical Pharmacokinetics of the Third Generation Cephalosporins

@article{Balant1985ClinicalPO,
  title={Clinical Pharmacokinetics of the Third Generation Cephalosporins},
  author={Luc P. Balant and Pierre Dayer and Raymond Auckenthaler},
  journal={Clinical Pharmacokinetics},
  year={1985},
  volume={10},
  pages={101-143}
}
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.

Pharmacokinetics of Intravenous Cefetamet and Oral Cefetamet Pivoxil in Human Subjects

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.

Crossover assessment of serum bactericidal activity and pharmacokinetics of five broad-spectrum cephalosporins in the elderly

Pharmacokinetic analysis revealed that cefoperazone and ceftriaxone had markedly different concentration-time profiles in the elderly volunteers than would have been expected on the basis of existing data from younger volunteers.

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.

The renal clearance of cefuroxime and ceftazidime and the effect of probenecid on their tubular excretion.

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.

Clinical Pharmacokinetics of Ceftriaxone

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.

The influence of chronic lobular hepatitis on pharmacokinetics of cefoperazone—a novel galactose single‐point method as a measure of residual liver function

Cefoperazone is a semisynthetic cephalosporin antibiotic containing a piperazine side chain, which results in antipseudomonal activity and may be more sensitive to changes in the liver function and/or plasma protein binding than other cep Halosporins, which are not primarily cleared by the liver.

Disposition of cefotaxime and its metabolite, desacetylcefotaxime, in rat: application of a pharmacokinetic-protein binding model.

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.
...

References

SHOWING 1-10 OF 252 REFERENCES

[Pharmacokinetics of a new cephalosporin, cefoperazone].

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

Phase I Study of Ceftizoxime, a New Cephalosporin. Repeated Dosing Study

The absence of adverse reactions in the single dosing study suggests that the drug can also be safely used for repeated dosing, and the relationship between the in vitro antibacterial activity and high serum and urine concentrations of the drug obtained in healthy volunteers suggests the clinical usefulness of theDrug.

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

Evidence that liver function impairment increases with both the apparent half-life of elimination and the urinary excretion of the drug is provided, raising the question of the desirability of cefoperazone dosage adjustment in patients with hepatic diseases.

Ceftizoxime. A review of its antibacterial activity, pharmacokinetic properties and therapeutic use.

Although only a few infections have been treated to date, ceftizoxime may be useful in the treatment of gonorrhoea in places where penicillinase-producing strains are common, and appears to be an effective addition to the growing number of third generation cephalosporins.

Cefoperazone (Cefobid, Pfizer)

Cefoperazone is a new β-lactam antibiotic that possesses a broad spectrum of activity against gram-positive and gram-negative organisms and has exceptional activity against P. aeruginosa.

Phase I Study of Ceftizoxime, a New Cephalosporin. Single‐Dose Study

Ceftizoxime is mainly excreted in the urine as unchanged drug, at an excretion rate in the 24‐hour urine of approximately 80 per cent, which exceeds the MIC80 against most pathogens tested.

Comparative pharmacokinetics of ceftazidime and moxalactam

The pharmacokinetics of ceftazidime and moxalactam were compared after intravenous and intramuscular administration of single 1-g doses to eight healthy volunteers in a crossover study. The

Pharmacokinetics of cefotaxime and desacetyl-cefotaxime in cirrhosis of the liver.

In 9 patients with advanced hepatic cirrhosis and a normal serum creatinine concentration, the pharmacokinetics of cefotaxime and its desacetyl metabolite were examined in serum and urine after intravenous administration and altered kinetics can be explained by altered metabolic function of the liver as well as by cirrhotic-linked alterations of renal elimination mechanisms.

Metabolism of cefotaxime: a review.

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.

Comparative pharmacokinetics of cefoperazone, cefotaxime, and moxalactam

The pharmacokinetics of cefoperazone, cefotaxime, and moxalactam were compared in a cross-over randomized study in 10 healthy volunteers and relevant pharmacokinetic parameters were calculated, using two- and three-compartment models.
...