摘要:

Pharmacokinetics were evaluated for piperacillin given as doses of 15, 30 and 60 mg/kg body weight to 12 healthy volunteers subdivided into three groups which were each given different dosage levels. For the 15, 30 and 60 mg/kg doses, the serum half-lives were 0.8, 1.0 and 0.9 hand the disposition phase distribution volume coefficients, Δd,β 0.31, 0.30, and 0.25 1/kg, The total body clearances for the three doses normalized to 70 kg body weight were 18.53, 14.00 and 13.53 1/h for the 15, 30 and 60 mg/kg doses, respectively. The corresponding values for the total area under the curves per 1.0 g dose were 57.1, 75.0 and 79.6 μg/ml. The urinary elimination of the antibiotic corresponding to the antimicrobial activity of unchanged drug rose from 50.0 to 71.3% of the dose, for a dose increment of 15 to 60 mg/kg. These results document that piperacillin is subject to dose-dependent pharmacokinetics. Capacity-limited kinetics is a property shared by other ureidopenicilli

ISSN:0009-3157    

DOI:10.1159/000238070

出版商:S. Karger AG    

年代:1982

数据来源: Karger

摘要:

The pharmacokinetics of azlocillin at intravenous doses of 1.0, 2.0 and 5.0 g and of 2.0 g mezlocillin were studied in a cross-over study on 10 healthy volunteers. The serum concentrations and total area under the serum curves for azlocillin increased more than expected from the multiples of the dose size. Likewise, the percentage of urinary excretion of an antibacterially active agent increased steadily with higher doses. The same applied to the serum half-life (t½), whereas the total body clearance was reduced. All these characteristics are indicative of dose-dependent, i.e. capacity-limited pharmacokinetics. The t½ was 0.89, 0.98, and 1.53 h for each dose. For 2.0 g mezlocillin, the serum values, urinary recovery, and t½ were lower than the values after the same dose of azlocillin. The t½ was 0.64 h. The total body clearance was 12.0, 9.2, and 6.4 liters/h for the three doses of azlocillin and 14.4 liters/h for 2.0 g mezlocillin. Dose dependence appears to be more pronounced with azlocillin than found previously with mezlocillin. Unchanged azlocillin and its biotransformation products are excreted more slowly than mezlocillin and its metaboli

ISSN:0009-3157    

DOI:10.1159/000238071

出版商:S. Karger AG    

年代:1982

数据来源: Karger

摘要:

It was documented that in clinical studies amoxycillin administered in the form of continuous perfusion (150 mg/kg/day) induces high antibacterial concentrations in patients with purulent meningitis. The drug was well tolerated.

ISSN:0009-3157    

DOI:10.1159/000238072

出版商:S. Karger AG    

年代:1982

数据来源: Karger

摘要:

Pharmacokinetics of a new preparation of microencapsulated erythromycin base was studied in 16 healthy subjects. They received 250 mg base 6-hourly or 500 mg 12-hourly for 7 days. The mean maximal serum peaks ( ± SD) after morning doses on days 1, 2, 3, and 7 were 1.4 ± 0.9, 3.2 ± 1.1, 3.6 ± 0.6, 3.5 ± 1.2 mg/l after the 250-mg dose and 3.2 ± 1.5, 3.7 ± 2.1, 3.6 ± 1.8, and 3.0 ± 2.0 mg/1 after the 500-mg dose. The mean 24-hour urine recoveries were 1.8 and 1.2°/o, the serum half-lives were (days 1–7) 1.4–2.1 h and 1.9–2.8 h for the 250-mg and 500-mg doses. The mean areas under the serum concentration curves ( ± SD) were 5.8 ± 2.2, 11.9 ± 2.2, and 15.3 ± 5.1 mg h 1-1 after 250 mg and 14.2 ± 4.9, 16.4 ± 7.6, and 14.3 ± 9.0 mg · h-1 after 500 mg on days 1, 2, and 7. The inter- and intrasubject variability was larger after the 500-mg dose. The pharmacokinetic results indicate that both dosage alternatives are suitable and result in similar steady-state peak levels, but the initia

ISSN:0009-3157    

DOI:10.1159/000238073

出版商:S. Karger AG    

年代:1982

数据来源: Karger

摘要:

The pharmacokinetics of alafosfalin and ampicillin were studied in rabbits. Serum concentrations were compared to levels in subcutaneous tissue fluid obtained from implanted tissue cages. The concentrations of alafosfalin exceeded those of ampicillin and the drugs were eliminated at similar rates from serum and tissue fluid.

ISSN:0009-3157    

DOI:10.1159/000238074

出版商:S. Karger AG    

年代:1982

数据来源: Karger

摘要:

Biliary excretion of cefaclor, a new orally active cephalosporin, was studied in vitro using an isolated rabbit liver preparation perfused for 3 h (n = 5). Under these conditions, bile recovery amounted to 2.3% of the cefaclor dose added to the circulating blood (10 mg). In humans, after oral administration of a 1-gram dose of cefaclor to cholecystec-tomized patients provided with a T tube (n = 10), a mean biliary peak concentration of 7.6 ± 2.4 μg/ml was observed at the 3rd hour. Cumulative biliary excretion amounted to 0.05% of the administered dose. Assays performed on samples collected during chole-cystectomy in 10 patients 1 h after intake of a 1-gram dose of cefaclor showed mean concentrations of 13.7 ± 1.2 μg/ml in serum, 8.1 ± 1.3 μg/ml in common duct bile and 5.9 ± 1.4 μg/ml in gallbladder bile. These results were compared with the data obtained after administration of seven other cephalosporins studied under identical con

ISSN:0009-3157    

DOI:10.1159/000238075

出版商:S. Karger AG    

年代:1982

数据来源: Karger

摘要:

The antimicrobial efficacy of BU-2313B, a new antibiotic, was evaluated in comparison with clindamycin, chloramphenicol and cefoxitin against 265 clinical anaerobic isolates. BU-2313B inhibited 88% of 66 isolates of Bacteroides fragilis tested at 2 μg/ml, whereas clindamycin, chloramphenicol and cefoxitin inhibited 98, 97 and 92% of them at 2, 8 and 16 μg/ml, respectively. BU-2313B was severalfold more effective than chloramphenicol and cefoxitin, but it was eight times less effective than clindamyci

ISSN:0009-3157    

DOI:10.1159/000238076

出版商:S. Karger AG    

年代:1982

数据来源: Karger

摘要:

The in vitro activities of moxalactam, GR 20263, and N-formimidoyl thienamycin were compared to those of cephalothin, cefazolin, cefamandole, cefoxitin, and tobramycin against 152 strains of Enterobacteriaceae and staphylococci. The results showed that moxalactam, GR 20263, and N-formimidoyl thienamycin each had significantly improved activity toward the gram-negative organisms tested compared to the other β-lactams and tobramycin. N-formimidoyl thienamycin was particularly impressive with respect to its activity toward Staphylococcus auteus and S. epidermidis as compared to moxalactam, GR 20263 and the older β-lactam drug

ISSN:0009-3157    

DOI:10.1159/000238077

出版商:S. Karger AG    

年代:1982

数据来源: Karger

摘要:

The induction of complete resistance to adriamycin in L1210 leukaemia was accomplished after 10 transplant generations. The adriamycin-resistant subline showed cross-resistance to vincristine and bouvardin. It was sensitive to methotrexate; this was observed by a 50% increase in life span compared to the life span of untreated control animals.

ISSN:0009-3157    

DOI:10.1159/000238078

出版商:S. Karger AG    

年代:1982

数据来源: Karger

摘要:

We describe a method, based on Selye’s granuloma pouch, for establishing reproducible Bacteroides fragilis infections in both mice and rats starting from rather low inocula. The infected pouches resemble abscesses and phlegmons. This model is promising for studies of antibiotic therapy in that both bacterial kinetics and antibiotic levels can be followed in the exudate

ISSN:0009-3157    

DOI:10.1159/000238079

出版商:S. Karger AG    

年代:1982

数据来源: Karger