Comparative pharmacokinetics and serum bactericidal activities of SCE-2787 and ceftazidime

Abstract

Ceftazidime and the new SCE-2787 are parenteral cephalosporins with a broad antimicrobial spectrum. Pharmacokinetics, serum bactericidal activities, and side effects were investigated in a randomized crossover study. A total of 12 healthy volunteers received a 20-min infusion of 1.5 g of SCE-2787 or 2.0 g of ceftazidime. Serum and urine concentrations were determined by the bioassay method and by high-pressure liquid chromatography (HPLC) Infect. Dis. 136:196-204, 1977) against 40 clinically isolated strains. One hour after administration, we measured mean reciprocal bactericidal titers of SCE-2787 and ceftazidime, respectively, against Escherichia coli of 388 and 243, against KiebsieUla pneumoniae of 395 and 138, against Pseudomonas aeruginosa of 13.0 and 12.7, and against Staphylococcus aureus of 32.2 and 4.0. No severe side effects were observed in this single drug administration.

Population Pharmacokinetic Comparison and Pharmacodynamic Breakpoints of Ceftazidime in Cystic Fibrosis Patients and Healthy Volunteers

“…One limitation of our MCS is that it was based only on 15 subjects for whom we had frequent plasma samples. However, our results for the PK parameters of ceftazidime in healthy volunteers were in good agreement with those from other authors (5,27,40,52,57,70,78). We are aware of only two studies on the PK of ceftazidime in CF patients which included a healthy volunteer control group.…”

Pharmacokinetics of Cefozopran by Single and Multiple Intravenous Infusions in Healthy Chinese Volunteers

“…CL, V and t ½ did not vary significantly with dosage. The elimination half-lives proved to be independent of the dose, with values of 1.20–2.80 h, which was close to the values reported in previous studies [9, 14] and less than the value of 4.8 h that was reported in renal dysfunction patients [17]. Cefozopran was eliminated almost entirely through urinary excretion; this observation suggests a need for dosage adjustment in patients with the most severe degrees of renal impairment.…”

“…In addition to its clinically useful antibacterial activity, the pharmacokinetic characteristics of the drug have been studied in healthy Japanese volunteers [ 9 , 10 ] and adult patients [ 11 – 13 ] previously. Its blood concentration half-life is observed to extend as renal function is deteriorated, and this tendency is especially obvious in patients who are of old age or who have renal dysfunction.…”

Optimizing ceftazidime pharmacodynamics in patients with acute exacerbation of severe chronic bronchitis

“…In our study, maximal serum concentrations of ceftazidime (144 ± 9.8 mg/L to 168.9 ± 34.1 mg/L) at the end of a 30 min infusion in the C3 × 2 regimen, and pre-dose concentrations (9.14 and 13.4 mg/L), were in good agreement with the values reported previously. 6,7,11,19,20 Maximal ceftazidime concentrations in the C2 × 2 group were observed between 4 and 6 h after the start of infusion (54.2-60.1 mg/L); pre-dose concentrations varied between 16.6 and 17.7 mg/L. These pre-dose concentrations were again in excellent agreement with the steady-state concentration of ceftazidime 3 g applied in a 24 h infusion (18.2 ± 4.5 mg/L).…”