摘要:

The pharmacokinetics of cephazolin given in intravenous dosages of 0.5 and 1.0 g and cephapirine, cephacetril and cephalothin in 1.0 g doses have been compared. The cefazolin appears to have favourable pharmacokinetic properties.

ISSN:0009-3157    

DOI:10.1159/000222009

出版商:S. Karger AG    

年代:1977

数据来源: Karger

摘要:

The elimination of para-aminosalicylic acid (PAS) after the intravenous injection of 20 mg PAS sodium/kg was estimated in patients with liver disease, in uremic patients and in volunteers without damage of the liver or kidneys. The drug was estimated with a colorimetric and fluorometric method. In the volunteers, the half-lives obtained with the fluorometric method were significantly longer than those estimated with the colorimetric method. This is caused by the estimation of more PAS metabolites by the used fluorometric method. In the patients with renal insufficiency (dialysis patients) the elimination rate of unchanged PAS – estimated with the colorimetric method – was not altered, whereas the elimination of PAS and its metabolites extractable by ethyl acetate was markedly slowed in comparison with the results obtained with the volunteers. The clearance of the unchanged PAS was even increased in the uremic patients. The serum protein binding of PAS was lowered significantly in the serum of uremic patients. In patients with liver cirrhosis, acute virus hepatitis and cholangitis the elimination rate of the drug was not altered in comparison with the volunteers. The results show that the dose of PAS in patients with renal insufficiency may not be reduced. The therapeutic level of the drug cannot otherwise be reached in these patie

ISSN:0009-3157    

DOI:10.1159/000222010

出版商:S. Karger AG    

年代:1977

数据来源: Karger

摘要:

Serum levels of FR10612 given orally to rats persisted significantly longer than did those of cephalexin. Since the elucidation of this phenomenon observed in rats is considered to be pertinent to the understanding of the drug kinetics of FR10612 in other animals including man, the present study was undertaken. From the dose-response curve of the serum levels of FR10612 in rats, it is apparent that the maximum oral absorption is obtained in the range of 100–400 mg/kg. Even when the doses were increased from 100 to 1,000 mg/kg, the tissue levels with the exception of the kidneys, did not increase significantly. However, the persistence of the tissue levels was enhanced. The serum and tissue levels of FR10612 in rats after repeated massive dosings did not increase accumulatively. From the experimental results of FR10612 in rats with ligated bile ducts and the results obtained after intravenous injection, it seems clear that the prolonged in vivo levels of FR10612 in rats after oral dosing are closely related to its enterohepatic circulatio

ISSN:0009-3157    

DOI:10.1159/000222011

出版商:S. Karger AG    

年代:1977

数据来源: Karger

摘要:

Carfecillin, the α-phenyl ester of carbenicillin, hydrolyses rapidly in the presence of serum or body tissues to liberate carbenicillin but hydrolysis is less rapid in aqueous solution. The activity of carfecillin in antibacterial tests in vitro depends upon the extent of hydrolysis to carbenicillin, and in conventional serial dilution tests carfecillin shows an antibacterial spectrum generally similar to that of carbenicillin due to extensive hydrolysis. However, in tests in which the extent of hydrolysis is reduced, carfecillin displays lesser activity than carbenicillin against gram-negative bacilli and greater activity against gram-positive cocci. In the presence of serum carfecillin is hydrolysed rapidly to carbenicillin and the activity shown is solely that of carbenicillin. Unlike carbenicillin, carfecillin is well absorbed in mice after oral administration, producing significant carbenicillin blood concentrations and the compound is as effective by the oral route in the treatment of various experimental mouse infections as is parenteral carbenicillin

ISSN:0009-3157    

DOI:10.1159/000222012

出版商:S. Karger AG    

年代:1977

数据来源: Karger

摘要:

Combined resistance against chloramphenicol (CHLOR), nalidixic acid (NA), and trimethoprim (TMP) was demonstrated in isolates and variants of a nosocomially significant, multiple-drug-resistant, nonconjugative strain of Serratia marcescens (bacteriocin type 18), either as a spontaneous event or after exposure of isolates and variants derived therefrom to increasing concentrations of CHLOR, NA, and TMP, respectively. This phenomenon was also noted among several selected mutants of two control strains of S. marcescens. The level of resistance was not absolute; the combined resistant mutants and variants were inhibited by 100–200 μg/ ml of CHLOR, 25–50 μg/ml of NA, and 12.5–25 μg/ml of TMP. However, the phenomenon of combined triple-resistance occurred irregularly with respect to the strain or variant of S. marcescens employed, and with regard to the selective drug utilized. Selection of mutants with CHLOR yielded a larger number of combined CHLOR-NA-TMP resistant mutants than selection with NA or TMP. Preliminary data obtained with spontaneously ‘cured’ variants of the multiple-drug-resistant strain of S. marcescens that had lost resistance against CHLOR, NA, TMP, penicillins, and aminoglycoside antibiotics, and which subsequently were shown to yield spontaneous mutants with combined triple-resistance against CHLOR, NA, and TMP, seem to indicate that this resistance phenomenon is not mediated extra-chromosomally, but rather chromosomally, and subject to phenotypic variation. The precise nature of this novel, unusual resistance mechanism against these three unrelated antimicrobial drugs remains to b

ISSN:0009-3157    

DOI:10.1159/000222013

出版商:S. Karger AG    

年代:1977

数据来源: Karger

摘要:

Both caffeine and theophyllme acting in subinhibitory concentrations inhibit the synthesis of peniciUinase in Staphylococcus aureus. Neither of these compounds inactivate the enzyme. Inhibition of peniciUinase synthesis is attributed to the lack of formation of peniciUinase rather than the elimination of the extrachromosomal plasmid.

ISSN:0009-3157    

DOI:10.1159/000222014

出版商:S. Karger AG    

年代:1977

数据来源: Karger

ISSN:0009-3157    

DOI:10.1159/000222015

出版商:S. Karger AG    

年代:1977

数据来源: Karger

ISSN:0009-3157    

DOI:10.1159/000222016

出版商:S. Karger AG    

年代:1977

数据来源: Karger

ISSN:0009-3157    

DOI:10.1159/000222017

出版商:S. Karger AG    

年代:1977

数据来源: Karger

ISSN:0009-3157    

DOI:10.1159/000222018

出版商:S. Karger AG    

年代:1977

数据来源: Karger