摘要:

Coupling of mitoxantrone (M), an intercalating cytostatic, to macromolecular polynucleotides may reduce side effects after direct intraperitoneal chemotherapy by interfering with systemic absorption of M. We have administered free M (30 mg/m2) or M mixed with poly(I).poly(C) (90 mg/m2) intraperitoneally to 5 patients with peritoneal carcinosis (cross-over study): peak plasma levels (HPLC assay) were 62 ± 12 versus 28 ± 4 ng/ml (p < 0.0025), AUC0-24 h were 583 ± 126 versus 481 ± 57 ng·h/ml (p < 0.025). Coupling of M to poly(I).poly(C) seems to reduce M absorption after intraperitoneal administra

ISSN:0009-3157    

DOI:10.1159/000238488

出版商:S. Karger AG    

年代:1987

数据来源: Karger

摘要:

The concentrations of trimethoprim (TMP) and sulfadiazine (SDZ) in serum, bile and gallbladder wall of 9 patients with acute cholecystitis were measured after b.i.d. treatment with 160 mg of TMP + 500 mg of SDZ. The samples were collected 2–4 h after the last dose. Mean TMP concentrations were 1.71 ± (SE) 0.51 μg/ml, 4.53 ± 5.26 μg/ml and 2.31 ± μg/g in serum, bile and gallbladder, respectively. Mean SDZ concentrations were 22.2 ± 14.9 μg/ml in serum, 9.37 ± 8.99 μg/ml in bile and 16.1. ± 10.1 μg/g in gallbladder. The average ratios of bile-serum and gallbladder-serum concentrations were 2.64 and 1.35 for TMP and 0.42 and 0.73 for SDZ. There was a significant correlation between serum and gallbladder concentrations of both TMP and SDZ. No correlation existed between serum an

ISSN:0009-3157    

DOI:10.1159/000238489

出版商:S. Karger AG    

年代:1987

数据来源: Karger

摘要:

Carumonam (Ro 17–2301/AMA-1080) is a new monobactam antibiotic. A comparative in vitro evaluation with ceftriaxone was undertaken against 153 gram-negative clinical aerobic or facultative bacteria, both producers and nonproducers of β-lactamase. Results indicated that carumonam had an enhancement of activity for Pseudomonas aeruginosa, Klebsiella oxytoca, Citrobacter freundii and Enterobacter cloacae and parallelled that of ceftriaxone against Escherichia coli, Klebsiella pneumoniae, Proteus spp. and Serratia marcescens. It can be concluded that carumonam could be an alternative of interest for the treatment of patients with infections due to gram-negative strains presumably or proven to be multiresista

ISSN:0009-3157    

DOI:10.1159/000238490

出版商:S. Karger AG    

年代:1987

数据来源: Karger

摘要:

Six isolates of Serratia marcescens were recovered sequentially from the respiratory tract of a single patient. The first three isolates were of the ‘opaque’ (wild-type) colony type and were susceptible to amikacin, cefotaxime, and lamoxactam. The following three isolates were of the small, ‘gray’ colony variety, significantly less susceptible to the three antibiotics, and revealed three altered outer membrane proteins, as determined with the SDS-PAGE pr

ISSN:0009-3157    

DOI:10.1159/000238491

出版商:S. Karger AG    

年代:1987

数据来源: Karger

摘要:

We evaluated the activity of teicoplanin against a type-III group B streptococcal strain in vitro and in vivo and compared the results with those of penicillin G. In vitro, the minimal inhibitory and minimal bactericidal concentrations of teicoplanin were 2- to 4-fold greater than those of penicillin G. In vivo studies were carried out with an experimental bacteremia and meningitis model in newborn rats. Eighty-one infected animals were randomized to receive teicoplanin 5, 10 or 20 mg/kg, twice daily, or penicillin G 50 or 200 mg/kg, twice daily, or saline (0.05 ml), twice daily. The mean serum levels of teicoplanin were maintained above 100 × the minimal bactericidal concentration for 7–8 h even with a dose of 5 mg/kg. The mean penetration of teicoplanin into the cerebrospinal fluid was estimated as 2.4–8.2% of those of concomitant levels in serum. The overall efficacy of teicoplanin was similar to that of penicillin G as judged by mortality rates. However, two bacteremic animals which were free of meningitis at the beginning of therapy developed this complication during 4 days of teicoplanin therapy, in contrast with none in the penicillin group. Further studies are needed to understand the reason(s) for these failures with teicoplanin the

ISSN:0009-3157    

DOI:10.1159/000238492

出版商:S. Karger AG    

年代:1987

数据来源: Karger

摘要:

Although imipenem inhibits most bacteria at very low concentrations, some Pseudomonas aeruginosa, Serratia marcescens and Enterobacter species are resistant or become resistant after exposure. At concentrations of rifampin equivalent to those attainable in man after daily oral ingestion of 600 mg, synergy of imipenem and rifampin was found for 52% of 62 P. aeruginosa and an additive effect for 37%. Against 30 S. marcescens synergy of imipenem and rifampin was not found, but an additive effect was noted for 47% of the isolates. With 32 Enterobacter isolates 35% were synergically inhibited, and an additive effect was found against 38% of the strains. Imipenem and ciprofloxacin were synergistic for 8% of P. aeruginosa and 22% of Enterobacter. Eighty-seven percent of P. aeruginosa isolates with imipenem MIC ≥4 μg/ml were synergistically inhibited by the combination of imipenem-rifampin. Imipenem MIC and MBC were lowered to 1-2 μg/ml and to 2–4 μg/ml for rifampin. MIC of imipenem and ciprofloxacin were 0.5–2 and 0.05–0.1 μg/ml, respectively. When a triple combination of imipenem-rifampin-ciprofloxacin was studied, 62% of P. aeruginosa, 32% of Enterobacter spp. and 47 % of S. marcescens were synergisticall

ISSN:0009-3157    

DOI:10.1159/000238493

出版商:S. Karger AG    

年代:1987

数据来源: Karger

摘要:

Single and combined resistance to quinolones and beta-lactams was determined after serial transfers of 18 selected strains of Pseudomonas aeruginosa (5), Acinetobacter calcoaceticus (3) and beta-lactamase producing enterobacterial strains (10), in broth dilutions of 4 quinolones and 8 beta-lactams. Two definitions for resistance were used: (I) 8-fold MIC increase and stability of acquired resistance after five transfers in drug-free broth; and (II) 8-fold MIC increase over the breakpoint level. Using definition I, after transfers on a beta-lactam, resistance to one or more beta-lactams was noted in 45%, to one or more quinolones in 7% of strains. After transfers on a quinolone, the frequency of resistance to quinolones was 82%, to beta-lactams 26%. When all tests were counted separately, the resistance percentages were lower, but they showed the same trend. Calculation according to definition II showed quinolone resistance in 5.4% of all tests after transfer on a beta-lactam and beta-lactam resistance in 23% after transfer on a quinolone. Serial transfers on imipenem led to fewer cases of resistance (13%) to beta-lactams than transfers on any other beta-lactam (19–39%). There were no conclusive differences between the 7 other beta-lactam

ISSN:0009-3157    

DOI:10.1159/000238494

出版商:S. Karger AG    

年代:1987

数据来源: Karger

摘要:

The in vitro antibacterial activity of Ro 23–6240 was assessed and compared with those of ciprofloxacin and beta-lactam antibiotics including several oral compounds against members of the family Enterobacteriaceae (n = 130) and Pseudomonas spp. (n = 31). In general, Ro 23–6240 was 2 dilution steps less active than ciprofloxacin. For the Pseudomonas spp. the MICs for 90% inhibition were 2 and 0.5 mg/l for Ro 23–6240 and ciprofloxacin, respectively. For the other species tested, the MIC90 values for Ro 23–6240 ranged from 0.031 to 1 mg/l and for ciprofloxacin from 0.016 to 0.25 mg/l. Spontaneous Ro 23–6240-resistant mutants were only isolated from Enterobacter cloacae with a frequency similar to that of ciprofloxacin (4.8 × 10-8 and 2.4 × 10-8, respectively). No resistant mutants were isolated from Escherichia coli, Proteus mirabilis, Klebsiella pneumoniae and Pseudomonas aeruginosa at concentrations of 4 and 8 times the MIC of Ro 23–6240 or ciprofloxacin (frequency < 10<

ISSN:0009-3157    

DOI:10.1159/000238495

出版商:S. Karger AG    

年代:1987

数据来源: Karger

摘要:

The effects of the anti-tuberculosis (TB) drugs isoniazid, rifampicin, streptomycin, pyrazinamide and ethambutol on the synthesis of prostaglandin E2 (PGE2) by polymorphonuclear leucocytes were investigated. Only rifampicin at a concentration of 100 μg/ml caused statistically significant stimulation of PGE2 production whereas the other compounds had no effect. Immunomodulatory properties of the compounds individually and in combination were investigated using phytohaemagglutinin-stimulated mononuclear leucocyte transformations. Rifampicin caused dose-dependent inhibition of blastogenesis and combinations containing this agent also had an inhibitory effect. The prostaglandin synthesis inhibitor indomethacin caused stimulation of phytohaem-agglutinin responsiveness and this effect was not influenced by the presence of the anti-TB drugs

ISSN:0009-3157    

DOI:10.1159/000238496

出版商:S. Karger AG    

年代:1987

数据来源: Karger

摘要:

The effect of deficiency of vitamin A and its supplementation on growth of murine sarcoma 180 was evaluated. The efficacy of cyclophosphamide under depleted and supplemented condition of the vitamin was also scrutinized. Supplemental vitamin A helped to check progression of tumour growth and also increased the effectiveness of chemotherapy. The action is possibly mediated through the host immune system.

ISSN:0009-3157    

DOI:10.1159/000238497

出版商:S. Karger AG    

年代:1987

数据来源: Karger