摘要:

The pharmacokinetics and elimination of ciprofloxacin and its three major metabolites desethylene ciprofloxacin (Ml), sulfonylciprofloxacin (M2), and oxocipro-floxacin (M3) were determined in 18 volunteers with normal and varying degrees of reduced renal functions. One dose of 500 mg ciprofloxacin was given orally. Samples were assayed by high-pressure liquid chromatography. Serum concentrations of both ciprofloxacin and its metabolites were only slightly influenced by the renal function. The serum concentrations of the metabolites were less than 10% of the ciprofloxacin levels, even in reduced renal function, and were overlapping within groups of patients arranged according to renal function. Dialysis reduced the serum concentration of the parent compound and its metabolites. The serum half-life of ciprofloxacin in normal renal function was 5.8 ± 1.2 h; this rose to 10.8 ± 2.3 h in the group with clearances of 10–30 ml/min. Compared to the latter group, the t1/2 was lower (7.0 ± 2.9 h) in the patients with terminal renal failure. The period of monitoring has a distinct consequence for the t1/2 of ciprofloxacin. The shorter t1/2values emanate if monitoring had stopped after 10 or 12 h. A slower gamma-phase of elimination was observed and this was particularly distinct in subjects with renal functions within the normal range. The total renal elimination of the parent compound and its metabolites was approximately 60% over the 48-hour collection period in normal renal function and was reduced by about 20% in the group with clearances within the range of 10–30 ml/min. In renal impairment, there was a shift towards a higher proportion of the dose being eliminated as M2. Ml contributed only up to 2% of the dose in urine. Irrespective of the renal capacity, the amount of M3 recovered in urine was 3

ISSN:0009-3157    

DOI:10.1159/000238702

出版商:S. Karger AG    

年代:1989

数据来源: Karger

摘要:

Antibiotics poorly penetrate the vitreous humor after periocular or systemic administration. Sometimes a direct intravitreal injection is necessary for the treatment of bacterial endophthalmitis. The kinetics of the intravitreally injected antibiotics, netilmicin (500 μg/0.1 ml), piperacillin (2,000 μg/0.1 ml), ampicillin (2,000 μg/0.1 ml) and aztreonam (2,000 p.g/0.1 ml), were examined in rabbits. Aqueous and vitreous antibiotic concentrations were assayed by microbiological methods. The results show that active levels of all drugs studied are present in the vitreous body for 48 h. In aqueous humor pMactam antibiotics are present in very small concentrations, whereas the aminoglycoside netilmicin (vitreous/aqueous ratio) have higher levels (%) than other dru

ISSN:0009-3157    

DOI:10.1159/000238703

出版商:S. Karger AG    

年代:1989

数据来源: Karger

摘要:

Cephalosporins do not reach active therapeutical concentrations in the prostatic tissue in patients suffering from chronic bacterial prostatitis. Cefoperazone is an exception. Its efficacy in the treatment of chronic bacterial prostatitis in 20 patients was studied and the concentrations, obtained after intramuscular administration, evaluated in patients who underwent transurethral operation due to prostatic hypertrophy (in 14 patients). The cefoperazone concentrations in the prostate have been evaluated 60, 90 and in some cases 120 min after the administration of the drug and compared to those obtained in serum. The clinical cure has been obtained in 16 patients. The average drug concentration in the prostate after 60 min was 22.8 ± 13.6 versus 39.8 ± 20.0 (μg/ml in serum; 90 min after administration the average concentration in the prostate was 23.2 ± 14.1 versus 35.7 ± 18.1 (ig/ml in serum. The correlation was significant both at 60 min (r = 64, p < 0.05) and at 90 min (r = 64, p < 0

ISSN:0009-3157    

DOI:10.1159/000238704

出版商:S. Karger AG    

年代:1989

数据来源: Karger

摘要:

The elimination kinetics of cefpiramide, a parenteral semisynthetic cephalosporin derivative, were studied in 6 healthy volunteers and 31 patients with renal dysfunction after a single 500-mg intravenous injection. Cefpiramide concentrations in serum and urine were determined by an agar-well diffusion method. The serum levels in patients with renal impairment were slightly higher than those in volunteers during the period from 30 min to 24 h after the administration. The mean serum half-life during the (3-phase was 4.06 h in the volunteers and was slightly prolonged in the patients. The mean urinary recovery during 24 h amounted to 21.5% in the volunteers and decreased with reduced renal function. Hemodialysis did not enhance the clearance of cefpiramide.

ISSN:0009-3157    

DOI:10.1159/000238705

出版商:S. Karger AG    

年代:1989

数据来源: Karger

摘要:

Fleroxacin, a new long-acting quinolone, induces rapid killing and bacterial filamentation as do other quinolones. Ten strains of Escherichia coli were exposed comparatively to fleroxacin and ampicillin in order to determine the effect of sub- and supra-inhibitory concentrations of each of these two compounds on turbidimetric growth curves and viable counts. By comparing the maximal early increase in optical density (OD, PIOD) as colony-forming units per milliliter (CFU/ml) after 2 and 6 h of exposure to antibiotics, we observed a reduced number of CFU/ml in comparison with the control after the 2-hour exposure at 1/4 the minimum inhibition concentration (MIC) and after 6 h at 1/8 MIC, but a high OD value was also seen among the fleroxacin exposed bacteria. For ampicillin, PIOD rates and killing rates were slower and dose dependent. This discrepancy was due to filament formation, which increased the PIOD value to the same extent as the control curve. After exposure to fleroxacin at 1/2 MIC the PIOD decreased significantly and after 2 and 6 h E. coli killing rates of 99 and 99.9%, respectively, were observed. With exposure to 2 and 4 x MIC, both PIOD values and CFU/ml decreased substantially. Combined analysis of continuous turbidimetric monitoring and viable counts showed that subinhibitory concentrations of fleroxacin and p-lactam had different effects on E. coli. Fleroxacin’s rapid killing rate, despite filament formation, contrasted with the result obtained with ampicillin. The minimum antibiotic concentration of fleroxacin against E. coli was around Vs MIC.424, Yourassowsky/Van der Linden/Crokae

ISSN:0009-3157    

DOI:10.1159/000238706

出版商:S. Karger AG    

年代:1989

数据来源: Karger

摘要:

The effect of dactimicin on the inner ear of guinea pigs was investigated by comparing it with the effects of ribostamycin, astromicin and amikacin. At doses of 200 and 400 mg/kg/day for 4 weeks, no pinna reflex loss was observed, but 2 animals receiving 400 mg dactimicin/kg/day showed unilateral loss of the outer hair cells in the cochlea and very scattered loss of the hair cells in the vestibular organ. At doses of 400 and 500 mg dactimicin/kg/day for 5 weeks, all surviving animals showed no abnormality of the outer hair cells, the inner hair cells and the spiral ganglion cells in the cochlea except for scattered unilateral loss of the outer hair cells and loss of the stria vascularis. Based on these observations, it is concluded that the ototoxicity of dactimicin on the inner ear of guinea pigs is the same as or a little stronger than that of ribostamycin, weaker than or the same as that of astromicin and weaker than amikacin.

ISSN:0009-3157    

DOI:10.1159/000238707

出版商:S. Karger AG    

年代:1989

数据来源: Karger

摘要:

The highest minimum inhibitory concentrations of ceftriaxone and cefotaxime in 89 analysed Neisseria gonorrhoeae isolates amounted to 0.008 and 0.031 μg/ml, respectively. In a randomized controlled trial the single intramuscular injection of ceftriaxone 250 mg and cefotaxime 500 mg cured bacteriologically 35 out of 35, and 29 out of 30 patients, respectively, with uncomplicated gonorrhoea. Facing the different pheno-types of the isolates grown before and after therapy in the case of the non-cured patient within the cefotaxime treatment group, reinfection rather than failure has to be presumed. Postgonococcal urethritis occurred about as often in both groups, the percentage amounting to 24.2 and 28.6%, respectively. If side effects were noted at all, they were considered minor: 4 patients belonging to the first and 3 belonging to the second treatment group complained temporarily about pain at the injection site. Due to the data presented here, ceftriaxone and cefotaxime appear equally effective and safe when used in the dose generally preferred, irrespective of differences in in vitro activity and pharmacokinetic behaviour

ISSN:0009-3157    

DOI:10.1159/000238708

出版商:S. Karger AG    

年代:1989

数据来源: Karger

摘要:

Five cases (3.5%) of reversible cephapirin-induced neutropenia were observed in 132 patients receiving this antibiotic. The disorder was severe (agranulocytosis) in 3 cases. Simultaneous maculopapular rash was observed in all of them and in 4 cases fever occured. All the cases observed were female (p not significant). Neutropenia developed only after administration of high doses of the antibiotic for a prolonged period of time. In contrast to another 127 patients treated with cephapirin who did not develop neutropenia, neutropenic patients had received a mean daily dose, total dose, mean daily dose per kilogram and total dose per kilogram of body weight significantly larger (p = 0.05, 0.02, 0.001 and 0.001, respectively). The duration of therapy was significantly longer in the neutropenic group (p = 0.001). Neutropenia did not occur below 90 g of total dose, but when this amount was exceeded, the incidence of the disorder reached 26.3% (p < 0.001). We conclude that when this drug must be used either for long periods of time or at high doses, a hematologic vigilance is recommendable.

ISSN:0009-3157    

DOI:10.1159/000238709

出版商:S. Karger AG    

年代:1989

数据来源: Karger

ISSN:0009-3157    

DOI:10.1159/000238710

出版商:S. Karger AG    

年代:1989

数据来源: Karger

ISSN:0009-3157    

DOI:10.1159/000238711

出版商:S. Karger AG    

年代:1989

数据来源: Karger