[In vitro evaluation of lomefloxacin].

Lomefloxacin (1-ethyl-6,8-difluoro-1,4-dihydro-7-(3-methyl-1-piperazinyl)-4- oxoquinoline-3-carboxylic acid monohydrochloride, SC-47111) is a broad-spectrum antibiotic of the 4-quinolone group. In this comparative study the antimicrobial in-vitro activity of lomefloxacin was tested against 863 gram-negative and 415 gram-positive strains from fresh clinical isolates. As comparative agents ciprofloxacin, norfloxacin and ofloxacin were used.

Serotyping, sites of isolation and resistance of Pseudomonas aeruginosa.

407 strains of pseudomonas aeruginosa form in-patients and out-patients were serotyped according to Habs' schema. 11.3% of the isolates were non-typable and among the other strains serotypes 6 and 10 were the most prevalent (20.

Kinetics of erythromycin uptake into Ehrlich mouse ascites tumor cells.

The uptake was studied with freshly isolated Ehrlich ascites tumor (EMAT) cells and with 14C-labelled erythromycin. Erythromycin was accumulated by EMAT cells. The uptake rates and quotes of erythromycin increased with increasing temperature and with increasing pH value (alkaline pH).

Modifying effects of pH and temperature on (14C)erythromycin uptake into Staphylococcus aureus--relation to antimicrobial activity.

The uptake of (14C)erythromycin into Staphylococcus aureus was investigated by use of a rapid centrifugation method. Erythromycin uptake was saturable with time and with increasing erythromycin concentrations (apparent uptake constant Km = 6.0 x 10(-7) moles/l).

Whole body tissue distribution of [14C]-erythromycin in the guinea pig. An autoradiographic study.

The distribution of 14C-labelled erythromycin following intravenous administration to the guinea pig has been studied by whole body autoradiographic technique. Erythromycin was quickly and extensively distributed throughout the body although penetration into some compartments like brain, spinal cord or vitreous body was limited. High radioactivity concentrations were detected in kidney, liver, lung, upper respiratory tract and in bone marrow.

Comparative in vitro activity, serum binding and binding activity interactions of the macrolides A-56268, RU-28965, erythromycin and josamycin.

The minimal inhibitory concentrations of macrolide antibiotics against staphylococci, streptococci and Haemophilus influenzae were determined in vitro. A-56268 was the most active and RU-28965 was the least active of the macrolides tested. The interaction at erythromycin binding sites in serum and at alpha 1-acid glycoprotein was studied.

Kinetics of erythromycin uptake and release by human lymphocytes and polymorphonuclear leucocytes.

The uptake of 14C-labelled erythromycin by human lymphocytes and polymorphonuclear leucocytes was studied. Erythromycin was concentrated by the cells. The amount of accumulated erythromycin was correlated with the cell count and was found to increase with alkaline pH and with increasing temperature of the incubation medium.

Pharmacokinetics, in-vitro activity, therapeutic efficacy and clinical safety of aztreonam vs. cefotaxime in the treatment of complicated urinary tract infections.

The minimal inhibitory concentrations (MICs) of aztreonam and cefotaxime were determined against 400 isolates from urological in-patients with complicated and/or hospital acquired urinary tract infections (UTI). Against the Gram-negative rods the activities of both antibiotics were comparable except for higher activity of aztreonam against Pseudomonas aeruginosa. The pharmacokinetic study in nine elderly patients showed a prolonged plasma half life of aztreonam (2.

The binding protein of erythromycin in human serum.

Erythromycin binding to human serum albumin and to alpha 1-acid glycoprotein was measured under conditions of binding equilibrium. At therapeutical concentrations of erythromycin the binding to albumin is not saturable. The fraction of total erythromycin bound to alpha 1-acid glycoprotein is proportionally related to the protein concentration and is bound to a single class of binding sites with an apparent association constant Ka = 0.

Impact of injectable cephalosporins on the gastrointestinal microflora: observations in healthy volunteers and hospitalized patients.

A disturbed microbiological ecosystem of the gut flora is frequently seen as a consequence of antibiotic therapy. Because this impact on the physiological balance is known to be causative for severe nosocomial infections and is mainly seen with antibiotics that are massively excreted via the bile (e.g.

Comparative study of fosfomycin activity in Mueller-Hinton media and in tissues.

Fosfomycin utilizes two uptake systems as ways of entry into microorganisms: the L-a-glycerophosphate and the hexose phosphate transport system. The latter is inducible by glucose-6-phosphate. The relationship between glucose-6-phosphate (concentration range 0-100 mg/l) and the susceptibility of Staphylococcus aureus was studied in Mueller-Hinton broth.

The current state of cephalosporin antibiotics: microbiological aspects.

An increasing number of new cephalosporins continue to become available in the clinic so that the clinician requires something akin to Ariadne's thread to work through the labyrinth of confusing names and product claims. The parenteral cephalosporins may be grouped on the basis of structure, antimicrobial activity and metabolic stability as follows: 1. cephacetrile, cephalothin, cefapirin; 2.

Cefotetan: antimicrobial activity in-vitro compared with that of cefotaxime.

The antimicrobial activity of cefotetan and cefotaxime were compared in vitro against 547 strains of aerobes and 24 strains of Bacteroides fragilis. The strains were recent clinical isolates from 20 hospitals. Cefotetan was found to exhibit an activity two- to fourfold lower than that of cefotaxime against most of the enterobacteriaceae.

Erythromycin binding to human serum.

Erythromycin binding to human serum was measured under conditions of binding equilibrium. The binding is sensitive to pH changes, decreasing at acid pH. Over a great range of serum dilution, the bound fraction is semilogarithmically related to serum concentration.

[Binding, distribution and efficacy of erythromycin (author's transl)].

The significance of the binding of antibiotics in humans in still a controversial question. In principle, only free, unbound antibiotic is considered to be diffusible and biologically active. With unimpaired measurements and a binding balance within the normal therapeutic concentration range, the free portion of erythromycin in the human serum is found to depend significantly on the total concentration of erythromycin.

The in-vitro activity of ceftazidime against clinically important pathogens.

A total of 1414 strains of Gram-negative bacilli and 250 strains of Gram-positive cocci were tested for antimicrobial susceptibility using the broth dilution method. The strains were clinical isolates from 26 hospitals in the Rhein-Main area. All the strains were tested against ceftazidime and ten other cephalosporin antibiotics.

The role of sialic acid in 5-HT binding to synaptic membranes.

The high affinity binding of [14C]5-HT to nerve ending membranes isolated from rat brain is not affected by neuraminidase treatment. The specificity of ligand receptor interaction was demonstrated by displacement studies with tryptamine derivatives, noradrenaline, and acetylcholine.

[Tissue penetration of erythromycin (author's transl)].

Although erythromycin has been used in therapy for more than 25 years, until now there has been no paper summarizing the data on tissue penetration. The present review documents in detail dose- and time-related peak serum levels of erythromycin derivatives after oral administration, in addition to the erythromycin tissue levels. The erythromycin tissue levels often manifoldly exceed the corresponding MIC values of pathogens sensitive to erythromycin.

[Erythromycin determination in organ tissues (author's transl)].

The recovery rates of erythromycin after in vitro and in vivo administration were studied comparatively in liver, lung, and kidney. Using buffer standards the recovery rate in homogenates of in vitro administered erythromycin decreased with increasing protein concentration. At constant protein concentration the erythromycin administered recovered correlated linearly.

On the significance of sialic acid in high affinity 5-hydroxytryptamine uptake by synaptosomes.

Synaptosomes isolated from rat brain cortex incorporated [14C]5-hydroxytryptamine at 37 degrees C with high affinity. An apparent transport constant of Kt = 50nM was found. The high affinity uptake was decreased by treatment of synaptosomes with neuraminidase from Vibrio cholerae or Clostridium perfringens prior to incubation with [14C]5-hydroxytryptamine.

[Diagnostic Methods in the Bulbus Duodeni. Agreement and Disagreement between Endoscopic, Roentgenological and Histological Examination (author's transl)].

In a collective of 1012 patients (700 m., 312f.), 346 (268 m.