摘要:

Limited data are available about cefixime pharmacokinetics and cerebrospinal fluid (CSF) penetration in infants and young children. Ten patients with bacterial meningitis and 8 undergoing CSF shunt placement, aged 2-22 months (mean 9.5 ± 6.5 months), were given a single dose of cefixime suspension, 8 mg/kg, before undergoing a routine lumbar puncture. Patients were fasted for 2 h before and 2 h after drug administration. Blood samples were collected just before drug administration (0 h) and at 1,2, 3, 4, 6, 8 h; CSF was obtained at 1-8.8 h after drug administration. Cefixime was measured by a high-performance liquid chromatographic method. The peak scrum concentration of cefixime ranged from 0.85 to 6.2 (mean 3.1) μg/ml and occurred at 2-8 h (mean 4.5). The area under the serum concentration-time curve ranged from 5.3 to 28.4 ug h/ml, and the elimination half-life ranged from 2.6 to 5.6 h. CSF concentrations ranged from 0.02 to 0.57 μg/ml. The mean CSF concentration of cefixime was 0.22 μg/ml in patients with meningitis and 0.10 ug/ml in those undergoing shunt placement (p < 0.02). The mean CSF concentration/serum concentration ratio was 11.7 in patients with meningitis compared with 5.4 in those undergoing shunt procedures (p < 0.02). These data indicate that cefixime can be considered as an alternative to other antimicrobials for infants and children with respiratory and urinary tract infections, since the observed peak serum concentration exceeded the minimum inhibitory concentrations of the common pathogens by severalfold. Cefixime should not be used for the treatment of bacterial meningitis, since the achievable CSF concentrations will most likely not exceed the minimum bactericidal concentration of common pathogens by 10-f

ISSN:0009-3157    

DOI:10.1159/000238966

出版商:S. Karger AG    

年代:1993

数据来源: Karger

摘要:

The pharmacokinetic profile of fluconazole, after 100 mg i.v. infusion or oral administration of a single 50 mg or 150 mg dose, was investigated in 18 healthy volunteers. At a dose of 100 mg i.v., the half-life (t½β) was 29.73 ± 8.05h. The mean residence time in the plasma was 27.56 ± 5.98 h. The post-distributive volume Vp = 52.16 ± 9.83 1, approximating that of total body water. Renal excretion accounted for 61.64 ± 8.80% of the drug elimination after 48 h, with renal clearance Clr = 12.91 ± 2.83 ml/min. Plasma clearance (Clp) was 21.03 ± 5.07 ml/min. At oral doses of 50 and 150 mg the distribution and elimination of fluconazole resembled that following i.v. infusion. The peak levels in plasma at 2.5 h were 0.93 ± 0.13 and 2.69 ± 0.43 μg/ml, respectively. The large distribution volume, the long half-life and mean residence times, combined with a rapid absorption after oral administration, suggest that fluconazole will be effective at a wide range of

ISSN:0009-3157    

DOI:10.1159/000238967

出版商:S. Karger AG    

年代:1993

数据来源: Karger

摘要:

The susceptibility of approximately 4,200 fresh clinical isolates to eleven different orally available compounds was assessed in ten Italian microbiology institutions during summer 1991. A standardized microdilution system including all the material necessary was employed to assess the antibacterial activity of ampicillin, ampicillin plus sulbactam, amoxicillin plus clavulanic acid, cefadroxil, cephalexin, cefaclor, cefuroxime, cefetamet, doxycycline, erythromycin, and clindamycin. The aminopenicillins (including the β-lactamase inhibitor combinations) were highly active against the streptococci, whereas cefetamet was the most active compound against Enterobacteriaceae, exhibiting good activity against the streptococci as well. The analysis of distribution of susceptibility revealed that there is a good discrimination between susceptible and resistant strains for cefetamet in any case, whereas the discrimination is low for the aminopenicillin/inhibitor combinations and the older cephalosporins in at least some of the gram-negative species

ISSN:0009-3157    

DOI:10.1159/000238968

出版商:S. Karger AG    

年代:1993

数据来源: Karger

摘要:

A viable counting technique was used to determine the postantibiotic effect (PAE) of ciprofloxacin against four bacterial species, treated with either one or four times the minimum inhibitory concentration for 1 or 3 h. PAE were demonstrated with Escherichia coli, Staphylococcus aureus or Streptococcus pyogenes after exposure to either concentration for both times. No clear PAE was demonstrated for Klebsiella pneumoniae after any treatment. In some cases, PAE was due to an increased post-treatment lag phase, which was followed by nearly normal multiplication, whereas in other cases a long lag was followed by abnormally rapid cell division, with the generation times of treated cultures being much less than those of the corresponding drug-free controls. This is evidence of recovery of cells that have completed DNA repair. S. aureus, E. coli and K. pneumoniae all exhibited evidence of this type of repair even though K. pneumoniae gave no significant PAE. However, the post-treatment generation times of S. pyogenes, which produced the greatest PAE, gave no evidence of such repair. It is concluded that PAEs may result from a variety of factors.

ISSN:0009-3157    

DOI:10.1159/000238969

出版商:S. Karger AG    

年代:1993

数据来源: Karger

摘要:

The in vitro activity of sparfloxacin, a new fluoroquinolone, was compared with ciprofloxacin and ofloxacin against 166 consecutive isolates from the upper respiratory tract of outpatients. The strains were fully susceptible to three quinolones. The antibacterial activity of sparfloxacin was comparable or better than that of ofloxacin and ciprofloxacin against all strains. Sparfloxacin was fourfold more active against Staphylococcus aureus and Streptococcus pneumoniae. The favourable MIC values and a prolonged half-life makes sparfloxacin interesting for treating respiratory tract infections in out-patient care.

ISSN:0009-3157    

DOI:10.1159/000238970

出版商:S. Karger AG    

年代:1993

数据来源: Karger

摘要:

Twelve strains of Streptococcus pneumoniae were serially exposed to increasing concentrations of levofloxacin, temafloxacin, ciprofloxacin and norfloxacin for five passages. Wild-type and passaged strains were tested for susceptibility to quinolones, macrolide and penicillin G. The MIC90 data showed a 2-fold increase for levofloxacin but a 32-fold increase for ciprofloxacin, a 16-fold increase for temafloxacin and an 8-fold increase for norfloxacin. Among 16 ciprofloxacin-induced resistant strains, 14 were susceptible to levofloxacin. No cross-resistance to other antibiotics was observed.

ISSN:0009-3157    

DOI:10.1159/000238971

出版商:S. Karger AG    

年代:1993

数据来源: Karger

摘要:

The susceptibility of 276 different strains of bacteria derived from the oropharyngeal flora to the tetrachlorodecaoxygen-anion complex (TCDO) was tested using the agar dilution method. The results showed that at therapeutic concentrations of the drug the growth of all the strains tested was inhibited, with the exception of Candida albicans. The pathogenic anaerobes proved to be particularly sensitive to TCDO.

ISSN:0009-3157    

DOI:10.1159/000238972

出版商:S. Karger AG    

年代:1993

数据来源: Karger

摘要:

The intracellular activity of flurithromycin, erythromycin, roxithromycin and miocamycin against susceptible clinical isolates of Staphylococcus aureus, phagocytosed by human monocytes, was investigated. Intracellular bioactivity was studied in a 24-hour assay, using experimental conditions which allowed the intracellular growth of bacteria. A colony counting method was used to differentiate between intracellular bacteriostatic and bactericidal activity of antibiotics. Moreover, the effect of macrolides against extracellular staphylococci was assessed. All agents showed higher intracellular than extracellular activity against staphylococci. At low concentration (O.f mg/l) they had intracellular bacteriostatic activity. At concentrations higher than the minimal inhibitory ones (1 and 5 mg/l), miocamycin only still produced a bacteriostatic effect while flurithromycin, erythromycin and roxithromycin also showed intracellular bactericidal activity.

ISSN:0009-3157    

DOI:10.1159/000238973

出版商:S. Karger AG    

年代:1993

数据来源: Karger

摘要:

In vitro response of 469 clinical isolates of gram-positive cocci was tested against MDL 62873 by the agar dilution method. The bacteria consisted of 407 isolates of staphylococci and 62 strains of enterococci. In vitro activity of MDL 62873 was compared with that of ampicillin, augmentin, erythromycin and vancomycin. All the isolates were completely inhibited by MDL 62873 at an MIC ranging between 0.25 and 8.0 ug/ml. In vitro activity of this new amide derivative of teicoplanin was far superior to that of ampicillin, augmentin and erythromycin and equal to or slightly better than that of vancomycin.

ISSN:0009-3157    

DOI:10.1159/000238974

出版商:S. Karger AG    

年代:1993

数据来源: Karger

摘要:

The antitumor effect of rubratoxin B, a mycotoxin, has been studied. Yoshida ascites sarcoma cells, in vitro in contact for 30 min with the drug and injected immediately afterwards into young rats by the intraperitoneal route, produced the survival of 80% of the animals and the doubling of the median survival time of the rats developing neoplasia. In vivo administration of the drug by the intraperitoneal route 24 h after implantation of tumor cells determined the prolongation of median survival time; supplied by other routes both against T8 sarcoma of Guerin and Yoshida ascites sarcoma it was ineffective. The differences between in vitro and in vivo results can be explained by a rapid neutralization of the drug on behalf of the organism’s enzymes or by being bound to proteins and peritoneal cells unlike tumor cell

ISSN:0009-3157    

DOI:10.1159/000238975

出版商:S. Karger AG    

年代:1993

数据来源: Karger