摘要:

Oral doses of 125, 250, and 500 mg of a new cephalosporin, CGP 9000 {7β-[D-2 -amino-2-(1,4-cyclohexadienyl)-acetamido]-3-methoxy-ceph-3-em-4-carboxylic acid}, given to healthy volunteers, were evaluated pharmacokinetically. The mean peak concentrations with the respective doses were 4.5 ± 1.4, 7.7 ± 2.7, and 12.3 ± 4.2 μg/ml. The maximum serum concentration occurred after 0.5–1.5 h. The amounts recovered unchanged in urine during 12 h were 96.4 ± 5.1, 92.4 ± 11.7 and 96.7 ± 7.6% of the respective doses. There was straight linear kinetics with a doubling of area under the serum curve for each dose, rising from 6.1 with the lowest, through 12.1 with the middle dose to 23.6 μg·h/ml with the highest dose. There was an apparent lag of 0.3–0.4 h before absorption. Absorption was relatively rapid, with mean absorption rate constants of 4.68–6.26 h-1. Serum half-life varied between 0.9 and 1.0 h with the different doses. The mean renal clearance values with the three doses ranged between 322

ISSN:0009-3157    

DOI:10.1159/000237910

出版商:S. Karger AG    

年代:1980

数据来源: Karger

摘要:

A cross-over study on metronidazole was carried out with 10 healthy adult volunteers who received tablets (250, 500 and 1,000 mg) and suppositories (500, 1,000 and 2,000 mg). The bioavailability of the suppositories was approximately 90% of the corresponding tablet dose as judged by area under the serum curves and amounts excreted in urine. The absorption was faster after the tablets. The mean curve peaks of unchanged metronidazole after the tablets occurred within 1 h and were 3.7 μg/ml after 250 mg, 9.8 μg/ml after 500 mg, and 11.8 μg/ml after 1,000 mg. The suppositories rendered peaks of 5.5, 9,5 and 14.0 μg/ml 4 h after doses of 500, 1,000 and 2,000 mg, respectively. In the dosage range 250–1,000 mg, the relationship between the dose and the total area under serum curves was similar for tablets and suppositories. Parts of the drug in serum and urine were antibacterially active metabolites. The mean recovery in urine within 36 h was 7–14% of the dose. The serum half-life of unchanged metronidazole (chemical assay) was 8.8–10.5 h. The terminal phase half-life of the total biologically active compound (microbiological assay) was 7

ISSN:0009-3157    

DOI:10.1159/000237911

出版商:S. Karger AG    

年代:1980

数据来源: Karger

摘要:

The pharmacokinetics of ceftezole, a new cephalosporin antibiotic, was studied in 15 patients with normal and impaired renal function after administering the drug in a 2-hour intravenous drip infusion of 2 g, 81% of the infused dose was excreted in the first 6 h urine of the patients with normal renal function. The pharmacokinetic parameters of ceftezole were obtained by analyzing the serum level data of the drug using a one-compartment open model. The mean serum half-life of ceftezole was 0.64 h in patients with normal renal function and was prolonged to 10.7 h in patients with severely impaired renal function (creatinine clearance: 0-2.6 ml/min.). There was a significant linear correlation between the elimination rate of the drug and creatinine clearance.

ISSN:0009-3157    

DOI:10.1159/000237912

出版商:S. Karger AG    

年代:1980

数据来源: Karger

摘要:

A method and an apparatus have been developed for the determination of the susceptibility of pathogenic bacteria to antibiotics. The method has the same applicability as the accepted Bauer-Kirby method. The method is rapid, the procedure for the performance of the test is simple, the supplies and equipment for the performance of the test are inexpensive and finally the test gives easily measurable end-points. The correlation of the method to the accepted Bauer-Kirby method against clinical isolates of gram-positive bacteria was 90–100% for the antibiotics tested with the exception of neomycin which was 80%. With gram-negative bacteria, the correlation was 92–100% for the antibiotics tes

ISSN:0009-3157    

DOI:10.1159/000237913

出版商:S. Karger AG    

年代:1980

数据来源: Karger

摘要:

The SbIII preparations available for clinical use were compared in vitro for their concentration/time/effect curves on Trypanosoma venezuelense (T. evansi), measuring decrease of motility and of parasite numbers. With these two criteria leading to similar relative results, the drugs are classified into a rapidly acting group, led by sodium emetic (AST), followed by its dimethylcysteine chelate (NAP) and Anthiomaline, and a less and more slowly acting one: Triostam, Astiban and Stibophen. The relative activity of these drugs in vitro is parallel to that encountered against Schistosoma mansoni, attributed to a similar pattern of intracellular absorption. In vivo effectiveness may depend on bio-availability of Sb in the host and the direct action on the parasite, reflected by its in vitro activity. The interplay of these two factors leads to a different in vitro/in vivo activity relationship of the antimonials even in the same host (mouse) and to its variation in other host species.

ISSN:0009-3157    

DOI:10.1159/000237914

出版商:S. Karger AG    

年代:1980

数据来源: Karger

摘要:

The in vitro activity of nitroxoline and its Mannich bases against bacteria and fungi was investigated. Nitroxoline and its derivative with diisopropylamine as an amino component, exhibited the highest antimicrobial activity. The optimum hydro/lipophilic properties (log P), both for antibacterial and antifungal activity, are about log P values of 2. The least effective compound was this nitroxoline Mannich base which has diethanolamine as an amino component.

ISSN:0009-3157    

DOI:10.1159/000237915

出版商:S. Karger AG    

年代:1980

数据来源: Karger

摘要:

Streptomycin-resistant enterobacteria were isolated from the faeces of 31 out of 35 patients under streptomycin therapy, in the University Hospital of Alexandria. The isolated bacteria were 26 Escherichia coli, 3 Klebsiella pneumoniae and 2 Enterobacter cloacae. Their resistance patterns have shown that 80% had multiple antibiotic resistance. The MIC of streptomycin for all strains was higher than 312 μg/ml.Nearly 90% of these strains carried resistance plasmids. However, 3 strains possessed no plasmids and were assumed to be mutants. 60% of the plasmid-carrying strains have been able to transfer the resistance by conjugation. The rest have shown small plasmids, some of them were characterized by streptomycin and sulphonamide resistance and a molecular weight of 4.1 mega-daltons

ISSN:0009-3157    

DOI:10.1159/000237916

出版商:S. Karger AG    

年代:1980

数据来源: Karger

摘要:

46 strains of Mycobacterium tuberculosis were studied as to their susceptibility to isoniazid (INH) or to INH + prothionamide (PTH) in the presence or absence of dapsone (DDS) by microdilution transfer plate technique. Synergy with DDS as defined by Berenbaum in 1978 was seen in 78% with INH and in 91% with INH + PTH. It concerned the minimal inhibitory concentration, whereas the minimal bactericidal concentration (MBC) was unaffected in the case of INH and it was increased in only 52% with INH + PTH. The latter MBC proportion mentioned would be decreased to roughly 16% accepting an only twofold decrease in the MBC as possibly due to dilution errors. The possible effect of dimethyl sulphoxide on the reported results is discussed.

ISSN:0009-3157    

DOI:10.1159/000237917

出版商:S. Karger AG    

年代:1980

数据来源: Karger

摘要:

The in vitro activity of the new semisynthetic ureidopenicillins azlocillin (AZ) and mezlocillin (MZ), and of the new cephalosporin cefsulodin (CEF) were determined against 50 carbenicillin-sensitive (CARS) and 50 carbenicillin-resistant (CARr) P. aeruginosa clinical isolates. In the CARS group the most active antibiotics are AZ and CEF with MICs between 0.5 and 8 μg/ml. Ticarcillin (TIC) and MZ showed more activity than CAR with MICs from 2 to 32 μ/ml. In this group there is a predominance of pyocine-type groups 1 and 3. In the CARr group, AZ is the most active antibiotic at low concentrations. At 64 μg/ml of CEF, 72% of strains are inhibited as compared to 70% with AZ, 62% with MZ and 50% with TIC. In this group there is predominance of non-typeable strains. Interaction with mecillinam (MEC) and these antibiotics was studied on three different culture media (MH, NIH and DST). There were few cases of synergism with MEC and TIC combinations, mostly on DST medium. No appreciable synergism was found with other combinations of antibioti

ISSN:0009-3157    

DOI:10.1159/000237918

出版商:S. Karger AG    

年代:1980

数据来源: Karger

摘要:

The oral administration of cyclacillin, a semisynthetic aminoalicyclic penicillin, results in the elimination of the lactobacilli from the gastrointestinal tract of mice. Although cyclacillin has a broad spectrum of activity similar to that of ampicillin, it does not, like ampicillin, affect the other flora of the gastrointestinal tract. Cyclacillin, unlike ampicillin, is rapidly absorbed from the stomach and upper small intestine, so that only small amounts reach the large bowel. Study of the dynamics of the lactobacillus population in the gut shows that in the mouse the prime site of localization and multiplication of lactobacilli is the stomach. The lactobacilli are transient in the small and large intestine, arriving there only after having been shed from the stomach.

ISSN:0009-3157    

DOI:10.1159/000237919

出版商:S. Karger AG    

年代:1980

数据来源: Karger