摘要:

Because of the extremely long terminal elimination half-life of mefloquine it is practically impossible to measure quantitatively its urinary excretion after a single dose. Indeed, a correct estimation would require collection of urine over a period of several months. This difficulty was overcome by measuring excretion in the course of a multiple-dose study when steady-state conditions had been reached. Six male African volunteers were given at an interval of 1 week 250 mg mefloquine base in the form of its hydrochloride. Urine was quantitatively collected from each subject during the 11th week and analyzed for unchanged drug and its alcohol and acid metabolites. Excretion of the unchanged drug and of its acid metabolite amounted respectively to 9% (5.2–13.1%) and 4.2% (2.9–6.2%) of the weekly dose. Concentrations of the alcohol metabolite were too low to be measu

ISSN:0009-3157    

DOI:10.1159/000238513

出版商:S. Karger AG    

年代:1987

数据来源: Karger

摘要:

Cinoxacin is an antibacterial drug belonging to the quinolone class used in the treatment of urinary tract infections due to common gram-negative pathogens. Considering the high frequency of urinary tract infections in elderly people where aging represents a physiopathological condition frequently requiring an adjustment of the dosage regimen, the pharmacokinetic behaviour of cinoxacin (500mg/l2h) in aged patients was investigated to find out if age-dependent differences may be established. The main differences detected were a shift to 4 h of the Tmax and a partly reduced clearance in comparison with data referred to younger people. On the other hand the findings showed that no accumulation occurred. High urinary concentrations of cinoxacin, exceeding the MICs for most urinary tract pathogens were found up to the 12th hour after administration.

ISSN:0009-3157    

DOI:10.1159/000238514

出版商:S. Karger AG    

年代:1987

数据来源: Karger

摘要:

In order to avoid gentamicin toxicity trough serum concentrations when drug monitoring is not available, a correction factor for serum creatinine was calculated and evaluated. In a first group of 35 patients under aminoglycoside treatment with variable serum creatinine (SCr) values, the regression plot of SCr concentrations versus half-life (T½) values was established: log T½ = log 2.28 + 1.45 log SCr, r = 0.90, p < 0.01. A second group of 18 patients was treated with doses of 1.0 mg/kg of gentamicin. Dose intervals equivalent to 3 T½ were daily adjusted. The T½ was calculated from SCr according to the relationship established for the patients of the first group. All the patients studied maintained trough levels within the therapeutic ra

ISSN:0009-3157    

DOI:10.1159/000238515

出版商:S. Karger AG    

年代:1987

数据来源: Karger

摘要:

Chloramphenicol serum concentration is often monitored to assure efficacy and prevent toxicity. We studied the relationship between steady-state chloramphenicol serum concentration and hematologic adverse effects in 45 pediatric patients. The mean peak serum concentration of chloramphenicol in patients with and without toxicity were not different (p > 0.1): 22.7 μg/ml in neutropenic patients versus 23.1 μg/ml in those without neutropenia; 18.2 μg/ml in leukopenic patients versus 23.3 μg/ml in those without leukopenia; 22.2 μg/ml in patients with eosinophilia versus 23.9 μg/mlin those without eosinophilia; 23.7 μg/mlin patients with anemia versus 22.1 μg/ml in those without anemia. None of the patients developed thrombocytopenia. These data clearly demonstrate that chloramphenicol toxicity may not be predictable by serum concentration in pediatric patients receiving therapeutic doses of chloramphenicol succinate. Thus, frequent monitoring of chloramphenicol serum concentration does not appear warranted unless a patient appears unresponsive to a therapeutic dose or has received an excessi

ISSN:0009-3157    

DOI:10.1159/000238516

出版商:S. Karger AG    

年代:1987

数据来源: Karger

摘要:

16 patients received an intravenous infusion of 200 mg ciprofloxacin 1, 2, 3 and 6 h, respectively, before cataract extraction. This dosage produced mean aqueous humor levels of 0.165 ± 0.09 and 0.12610.028 μg/ml after 1 and 3 h, respectively. The mean serum levels were 1.76010.873 and 0.85410.283 μg/mlafter 1 and 3 h, respectively. These levels are above the minimum inhibitory concentration of ciprofloxacin for sensitive organis

ISSN:0009-3157    

DOI:10.1159/000238517

出版商:S. Karger AG    

年代:1987

数据来源: Karger

摘要:

The killing kinetics of Staphylococcus aureus, exposed to various concentrations of dicloxacillin in broth and in broth with 40 g/l human albumin was studied. When the free concentrations of dicloxacillin were identical in the two media, no difference in killing capacity could be demonstrated at concentrations above MIC, indicating that only the free antibiotic fraction is antibacterially active. However, at concentrations identical to the MIC, a better bactericidal effect in the medium containing albumin was found. In experiments where equal total concentrations were compared in the two media, an increasing bactericidal effect in the medium containing albumin could be demonstrated at concentrations between 10–100 × MIC. The most probable explanation for this was a prominent paradoxical effect with increasing antibiotic concentrations on the killing rate of S.aureus in broth. This effect was neutralized in the presence of albumin due to the lower free antibiotic concentration in this medi

ISSN:0009-3157    

DOI:10.1159/000238518

出版商:S. Karger AG    

年代:1987

数据来源: Karger

摘要:

A total of 500 clinical isolates of Pseudomonas aeruginosa and 14 isolates of Pseudomonas maltophilia were examined for susceptibility to ticarcillin and timentin (ticarcillin plus clavulanic acid). Clavulanic acid enhanced the activity of ticarcillin against only 34 of 500 isolates of P. aeruginosa. Among 23 isolates of P. aeruginosa, that had yielded divergent disk diffusion results, there were 3 major discrepancies (3 = ticarcillin-resistant by disk diffusion, but susceptible by broth dilution test criteria) and 1 very major discrepancy (timentin-susceptible by disk diffusion, but resistant by broth dilution test criteria). Clavulanic acid enhanced the activity of ticarcillin against 12 of 14 isolates of P. maltophilia; there were 2 major discrepancies (ticarcillin resistance in terms of disk diffusion, but susceptibility according to ticarcillin MICs). Consequently, it was decided to continue employing timentin disks alone, rather than add ticarcillin disks in our Bauer-Kirby test battery for Pseudomonadaceae.

ISSN:0009-3157    

DOI:10.1159/000238519

出版商:S. Karger AG    

年代:1987

数据来源: Karger

摘要:

A series of novel 9-acridanones and 9-iminoacridines has been prepared and investigated by a number of spectroscopic techniques in order to determine the nature and extent of the binding of these compounds to DNA. Results are discussed with reference to antiamebic activity in vitro.

ISSN:0009-3157    

DOI:10.1159/000238520

出版商:S. Karger AG    

年代:1987

数据来源: Karger

摘要:

Norfloxacin and adriamycin were tested alone and in combination for bactericidal activity against different strains of gram-negative bacteria. The antitumoral effect of a combination of norfloxacin and adriamycin was determined in mice bearing Ehrlich ascites carcinoma and in mice bearing P 388 leukemia. No interference with the antibacterial activity of norfloxacin or with the antitumoral activity of adriamycin was observed.

ISSN:0009-3157    

DOI:10.1159/000238521

出版商:S. Karger AG    

年代:1987

数据来源: Karger

摘要:

Thirteen nosocomially significant, gentamicin- and methicillin-resistant (GRMR) Staphylococcus aureus isolates, all of phage group III/M (lysotype 42E/47/53/54/75/77/83A/84/85/94/96), were uniformly resistant against augmentin, erythromycin, fosfomycin, gentamicin, methicillin, oxacillin, penicillin G, tetracycline, and tobramycin, but differed in susceptibility to cefamandole, ciprofloxacin, clindamycin, imipenem, josamycin, the synthetic chinolone Ro 23–6240, and ofloxacin. All isolates were susceptible to chloramphenicol, coumermycin, fusidic acid, novobiocin, rifampin, teicoplanin, trimethoprim-sulfamethoxazole (cotrimoxazole), and vancomycin. One isolate was of intermediate susceptibility to netilmicin. On a weight-for-weight basis, the 7 most active drugs were rifampin, coumermycin, cotrimoxazole, novobiocin, teicoplanin, fusidic acid, and vancomycin (in decreasing order) in terms of minimal inhibitory concentrations. With regard to minimal bactericidal concentrations, coumermycin, rifampin, vancomycin, teicoplanin, cotrimoxazole, ofloxacin, and ciprofloxacin (in decreasing order) were the 7 most potent antimicrobial drugs. Freshly defibrinated human blood [65% (v/v)] combined with chloramphenicol and rifampin, respectively, resulted in a weak additive effect (time kill curves). Indifferent effects were observed following combination of blood with ciprofloxacin, cotrimoxazole, coumermycin, fusidic acid, imipenem, netilmicin, novobiocin, ofloxacin, compound Ro 23–6240, teicoplanin, and vancomycin. Rifampin combined with novobiocin, teicoplanin, and vancomycin, respectively, in the presence of 65% (v/v) human blood, resulted in an additive effect. Combinations of rifampin with 9 other antimicrobial drugs in blood yielded essentially indifferent effe

ISSN:0009-3157    

DOI:10.1159/000238522

出版商:S. Karger AG    

年代:1987

数据来源: Karger