摘要:

αα-Diethyl-1-naphthylacetic acid (DA 808) and α-methyl-α-(2-morpholinoethyl)-1-naphthylacetic acid (DA1627) are compared with dehydrocholic acid for activity on biliary excretion of penicillin G, ampicillin, methicillin, rifamycin SV, tetracycline and demethylchlortetracycline in rats. Unlike to dehydrocholic acid, DA 808 and DA 1627 do not decrease the concentrations of penicillins and tetracycline in the bile. The concentrations of rifamycin SV and demethylchlortetracycline are partially reduced by the two naphthylacetic acid derivatives and markedly reduced by dehydrocholic acid. DA 808 and DA 1627 increase, however, the total amount of the penicillins and tetracycline excreted in the bile but not that of demethylchlortetracycline and rifamycin SV. Dehydrocholic acid does not increase the amount of the antibiotics excreted in the bile. On the basis of these results some remarks of clinical therapy about the association of choleretics-antibiotics in the biliary infections are m

ISSN:0009-3157    

DOI:10.1159/000220749

出版商:S. Karger AG    

年代:1971

数据来源: Karger

摘要:

A study aimed at contributing to the elucidation of the decrease in serum rifampicin concentrations observed during repeated administration of the antibiotic was carried out in a group of 18 healthy subjects. Three dose levels were investigated: 900 mg once daily, 600 mg once daily and 300 mg 12-hourly, and the behaviour over a period of 14 days of the peak and 12-hour serum concentrations and of the biological half-life was evaluated. The study demonstrates that during treatment with repeated doses of rifampicin the kinetics of the antibiotic undergo definite changes. While the peak serum concentrations do not appear to be affected in a consistent way by the duration of treatment, the 12-hour serum concentrations show a definite decrease, which takes place mainly during the first 6 days of treatment; a further decrease between 6 and 14 days was seen but was found not to be significant. A definite decrease in biological half-life is also observed during the first 6 days of treatment; such a decrease is directly correlated with the dose given on each administration. As a consequence, the half-life values, which are correlated with the doses on the first day of treatment, are no longer different for the different doses on the sixth day. The hypothesis that the increase in rate of disappearance of rifampicin from blood, which takes place mainly during the first 6 days of treatment, is due to an increased rate of biliary excretion is discussed.

ISSN:0009-3157    

DOI:10.1159/000220750

出版商:S. Karger AG    

年代:1971

数据来源: Karger

摘要:

Sixty-four chemicals representing groups of alkylating agents, chelating agents, redox inhibitors, antimetabolites and miscellaneous chemicals were tested for their in vitro scolicidal action upon the hydatid scolices of Echinococcus granulosus. Scolices death was determined by their motility and staining properties and confirmed by their ability to undergo cystic development when inoculated i. p. into young albino mice. Thirteen chemicals displayed effective scolicidal activity after 10 min of exposing the scolices to the chemical. Of these 9 were effective in 5 min and 7 in 1 min. All the chemicals were of organic nature amenable to structural modifications which might lead to drugs useful in systemic treatment and prophylaxis of hydatid disease. The lethal dose (LD50) and scolicidal value of each chemical were determined. The significance of these findings is discussed.

ISSN:0009-3157    

DOI:10.1159/000220751

出版商:S. Karger AG    

年代:1971

数据来源: Karger

摘要:

Rifampicin is oxidized with hydrogen peroxide to a product that is fluorescent in alkaline solutions. Maximum fluorescence is measured at 480 nm with an excitation wavelength of 370 nm. The lower limit of detection of rifampicin in water is 0.1 μg/ml. A microbiological assay with Staphylococcus aureus 560 as the assay organism verified the reliability of the fluorometric assay. The fluorametric and microbiological assays were applied to the estimation of rifampicin in serum and were used to obtain concentration-time data for dogs that had been treated orally with 10 mg/kg rifampicin. Half-life of rifampicin in the dog was 8 h

ISSN:0009-3157    

DOI:10.1159/000220752

出版商:S. Karger AG    

年代:1971

数据来源: Karger

摘要:

Sulfalene has a marked inhibitory action against a drug-sensitive strain of P. berghei in mice. The ED90 ranges between 0.25 and 1.0 mg/kg (given intraperitoneally daily for 4 days). The action is potentiated when the sulphonamide is given in a 1:1 mixture with pyrimethamine. This mixture shows a high level of potentiation against strains resistant to chloroquine, primaquine and sulphaphenazole, as well as against strains resistant to cycloguanil or pyrimethamine. These observations provide an experimental rationale for the application of such combinations in the treatment of individuals infected with multiple-resistant strains of P. falciparum. Other factors must be taken into consideration where large-scale administration is concerned.

ISSN:0009-3157    

DOI:10.1159/000220753

出版商:S. Karger AG    

年代:1971

数据来源: Karger

ISSN:0009-3157    

DOI:10.1159/000220754

出版商:S. Karger AG    

年代:1971

数据来源: Karger

ISSN:0009-3157    

DOI:10.1159/000220755

出版商:S. Karger AG    

年代:1971

数据来源: Karger

ISSN:0009-3157    

DOI:10.1159/000220756

出版商:S. Karger AG    

年代:1971

数据来源: Karger

ISSN:0009-3157    

DOI:10.1159/000220748

出版商:S. Karger AG    

年代:1971

数据来源: Karger