摘要:

20 patients (0.4–5.6 years old) receiving ceftriaxone for the treatment of bacterial meningitis were studied. Simultaneous serum and cerebrospinal fluid concentrations of ceftriaxone were determined by HPLC in 15 patients at 11.4–12.8 h after an intravenous loading dose of 75 mg/kg. Serum and cerebrospinal fluid concentrations ranged from 20.5 to 44.9 (31.3 ± 7.8) and from 1.1 to 8.0 (3.7+1.8) μg/ml, respectively. Cerebrospinal fluid concentrations ranged from 3 to 25% (12 ± 6%) of the simultaneous serum concentrations. In 6 patients, serum and cerebrospinal fluid concentrations were determined after maintenance doses of 50 mg/kg/l2 h. Serum and cerebrospinal fluid concentrations ranged from 120 to 144 and 2.3–4.9 μg/ml at 1.8–5.5 h after the first maintenance dose in 2 patients; 74–139 and 5.7–7.9 μg/ml at 1.3–5.8 h after the second dose in 3 patients and was 101 and 4.1 μg/ml at 4 h after the 3rd dose in 1 patient. Multiple blood samples were collected after the loading dose in 5 patients and after 9–10 days of maintenance doses in 3 patients. Steady-state peak and trough serum concentrations ranged from 295 to 440 and 32.6–44.8 μ 0.05); and elimination half-life averaged 3.7 and 4.6 h (p = 0.01), respectively. These results suggest that (1) adequate cerebrospinal fluid concentrations of ceftriaxone can be achieved in patients with meningitis with the dosage regimen studied; (2) ceftriaxone kinetics may vary among infants and children with meningitis, and (3) the higher clearance of ceftriaxone noted at the higher dose may be partly due to its concentration-dependen

ISSN:0009-3157    

DOI:10.1159/000238395

出版商:S. Karger AG    

年代:1986

数据来源: Karger

摘要:

The concentrations of ceftazidime attained in cardiac and leg muscles of rabbits were compared after a single intramuscular injection of 100 mg/kg. Simultaneous measurements of muscle and muscle fluid over an 8-hour period showed that ceftazidime penetrated heart muscle more rapidly and to a greater extent than leg muscle. Although the half-lives did not vary, the areas under the time/concentration curves for heart muscle and heart muscle fluid were significantly greater than those for leg muscle and leg muscle fluid. It is suggested that an increased fluid content and vascularity of cardiac muscle may explain these results. This study also confirms previous reports that whole muscle tissue levels of β-lactam antibiotics substantially underestimate the actual concentrations present in the extracellular fluid

ISSN:0009-3157    

DOI:10.1159/000238396

出版商:S. Karger AG    

年代:1986

数据来源: Karger

摘要:

Twelve patients with syphilis were treated weekly with injections of 1.44 g (2.4 x 106 IU) of benzathine penicillin G for up to 3 weeks. Almost daily, serum penicillin concentrations were measured by a sensitive microbiological agar cup method. An individual and interindividual variation was found. Concentrations below the recommended 0.018 μg/ml were found 7 days after the first or second injection in 5 samples. Shorter intervals between injections are recommended

ISSN:0009-3157    

DOI:10.1159/000238397

出版商:S. Karger AG    

年代:1986

数据来源: Karger

摘要:

Ceftriaxone (Rocephin®), a broad-spectrum parenteral cephalosporin with an exceptionally long elimination half-life, has a marked activity against both Salmonella typhimurium infections in mice and typhoid fever in man. This study investigates autoradiographically the penetration of ceftriaxone into murine cells of liver, spleen and kidney, with emphasis on the cells of the reticuloendothelial system (RES). The RES is an important site of localization of the pathogenic agent of typhoid fever. An incorporation of ceftriaxone was found in several cell types of the three investigated organs, in particular the cells of the RES and in precursors, e.g. monocytes of the blood stream, Kupffer cells or reticular cells. Besides long biological half-life, satisfactory penetration into phagocytes and other tissue cells has been shown, which is essential to the good in vivo activity of ceftriaxone against systemic Salmonella infections

ISSN:0009-3157    

DOI:10.1159/000238398

出版商:S. Karger AG    

年代:1986

数据来源: Karger

摘要:

The influence of normal human serum on bactericidal activity of ceftizoxime sodium (CZX) was studied in vitro against Escherichia coli and Staphylococcus aureus. Subminimal inhibitory concentrations of CZX inhibited the growth of bacteria. Normal human serum as a source of complement and low doses of CZX, such as 1/20 or 1/10 the minimal inhibitory concentration, had a strong synergic action on the gram-negative bacteria E. coli, but not on the gram-positive bacteria S. aureus. However, the combination of CZX and fresh human serum had a stronger inhibitory effect on the growth of S. aureus than CZX alone. It is concluded that subminimal inhibitory concentrations of CZX inhibited the growth of bacteria in vitro in the presence of human serum, indicating that smaller dosages of CZX may act to eliminate the invading bacteria in vivo together with serum complement.

ISSN:0009-3157    

DOI:10.1159/000238399

出版商:S. Karger AG    

年代:1986

数据来源: Karger

摘要:

Cefotaxime has extremely low MIC values in comparison with amoxycillin against Enterobacteriaceae, but studies of antibacterial activity using turbidimetric and viable count methods show no advantage for cefotaxime. Superior rates of killing have been demonstrated for amoxycillin and amoxycillin/clavulanic acid using both constant antibiotic concentrations and changing concentrations to simulate conditions in vivo. Slow bactericidal activity was seen with cefotaxime even at levels greatly in excess of the MIC and could be correlated with filament formation by this compound over a wide range of concentrations.

ISSN:0009-3157    

DOI:10.1159/000238400

出版商:S. Karger AG    

年代:1986

数据来源: Karger

摘要:

In vitro activity of cefpimizole, an experimental third generation cephalosporin, and 10 other antimicrobials (ampicillin, azlocillin, cefamandole, cefoperazone, cefotaxime, mezlocillin, moxalactam, piperacillin, rifampin and sulfamethoxazole/trimethoprim) were determined for 181 isolates of Haemophilus obtained from pediatric patients. For 156 β-lactamase-negative isolates, MIC50 values of cefoperazone, cefpimizole, and cefamandole were 4, 8, and 16 times greater than those of moxalactam and cefotaxime (0.06 μg/ml). 25 β-lactamase-producing isolates were resistant to ampicillin, azlocillin, mezlocillin, and piperacillin, however, MIC50 of all third generation cephalosporin were similar to those obtained for β-lactamase-negative organisms. Refampin and SMX/TMP demonstrated low MIC50 values for all isola

ISSN:0009-3157    

DOI:10.1159/000238403

出版商:S. Karger AG    

年代:1986

数据来源: Karger

摘要:

Three new nitrosourea analogs (CNCC, RFCNU, and chlorozotocin) had comparable activities in vivo against L1210 leukemia cells. In addition to the antileukemia effect, these drugs also decreased both the humoral immune response to sheep red blood cells and the delayed hypersensitivity reaction to oxazolone. The immunodepression induced by these agents lasted at least 25 days, and could not be reversed by the transplantation of normal syngenic bone marrow cells into treated animals.

ISSN:0009-3157    

DOI:10.1159/000238404

出版商:S. Karger AG    

年代:1986

数据来源: Karger

摘要:

The in vitro studies on the growth of cultured Ehrlich ascites tumour cells showed similar results as the in vivo studies reported previously. The growth of tumour cells was inhibited when cultured in 0.02 or 0.03 M L-histidine. At these concentrations, L-glycine shows no significant effect.

ISSN:0009-3157    

DOI:10.1159/000238405

出版商:S. Karger AG    

年代:1986

数据来源: Karger

摘要:

Aclacinomycin (ACM) a new cytotoxic antibiotic employed in cancer chemotherapy, can either enhance or inhibit the NK-cell activity of the immune system, depending on the dose administered. A single intraperitoneal injection of 2–4 mg/kg of ACM augments the cytolytic activity by spleen and peritoneal exudate cells of normal mice and spleen cells depleted of nylon-adherent cells and peritoneal exudate cells of tumor-bearing mice. In contrast to the stimulatory effect of NK-cell activity by low doses of ACM, a single injection of 8 mg/kg of this agent leads to depression in the level of NK-cell activity in both normal and tumor-bearing animals. We suggest that the mechanism through which the ACM enhances NK-cell activity may be through the deletion of a suppressor cell population acting on the NK cell

ISSN:0009-3157    

DOI:10.1159/000238406

出版商:S. Karger AG    

年代:1986

数据来源: Karger