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  • 1
    Electronic Resource
    Electronic Resource
    Springer
    Applied microbiology and biotechnology 3 (1976), S. 193-202 
    ISSN: 1432-0614
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Process Engineering, Biotechnology, Nutrition Technology
    Notes: Summary Using mainly the Warburg technique, the effect of intermediates of tetradecane metabolism on tetradecane oxidation inPseudomonas aeruginosa was investigated. Precultivation and simultaneous incubation of bacteria with acetate, succinate, fumarate, glycolate and malonate inhibit the oxidation of tetradecane as well as of all primary oxidation products including myristic acid in a different manner. C2-units have a key function in the regulation of tetradecane oxidation. The inhibitory effect of tetradecane and its primary oxidation products on substrate oxidations may be unspecific. During the oxidation of tetradecane or its primary oxidation products O2-consumption increases exponentionally but CO2-production becomes stationary. The RQ-values obtained with myristic acid growing cells decrease to O.1, indicating that myristic acid is only partially oxidized via citric acid cycle.
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  • 2
    Electronic Resource
    Electronic Resource
    Springer
    Applied microbiology and biotechnology 3 (1976), S. 203-211 
    ISSN: 1432-0614
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Process Engineering, Biotechnology, Nutrition Technology
    Notes: Summary The effect of glucose on tetradecane oxidation and protein synthesis was investigated with a strain ofPseudomonas aeruginosa. Precultivation or simultaneous incubation with glucose or glucose-6-P inhibits substrate oxidation, CO2-production, and protein synthesis totally for several hours. This inhibitory effect is completely reversed by addition of adenosine-3′-,5′-mono-phosphate and diethoxymethane as inducer. The inhibitory effects of gluconate or 6-P-gluconate are transient. Substrate oxidations and synthesis of proteins are stopped immediately after addition of 6-P-gluconate or glucose-6-P, whereas non-phosphorylated glucose or gluconate decrease these functions after a lag period. From this fact it may be suggested that non-phosphorylated compounds must be phosphorylated to act as repressors.
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  • 3
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 22 (1982), S. 273-279 
    ISSN: 1432-1041
    Keywords: amoxycillin ; i.v. administration ; pharmacokinetics ; two- and three-compartment models
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetic characteristics of amoxycillin were studied in healthy volunteers after intravenous injection of 250 mg, 500 mg and 1,000 mg, and infusion of 2 g and 5 g. Serum concentrations were fitted using either bi- and tri- exponentional equations. Comparison of the regression curves obtained revealed that the three-compartment model gave a better fit to the serum concentration versus time curve. It was evident that there was a third, slow, dose dependent phase of disposition. This result has been confirmed by the fact that the terminal half life of amoxycillin on cessation of a continuous infusion is significantly greater than after acute administration.
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  • 4
    ISSN: 1439-0973
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Description / Table of Contents: Zusammenfassung Ticarcillin-Gewebespiegel wurden bei 77 Patienten nach einer 30minütigen Infusion von 5 g ermittelt; es wurden bei den gynäkologischen Indikationen Endometrium, Tube, Ovar und Myometrium untersucht. Die relativen Gewebespiegel betrugen 17% bis 30% der korrespondierenden Serumkonzentration wenn Ticarcillin nur einmalig verabreicht wurde; sie beliefen sich auf 22% bis 32% bei mehrfacher Applikation. Die Gewebespiegel waren in keinem Fall größer als die Serumkonzentrationen. Die mittleren relativen Gewebespiegel in der Frühschwangerschaft (Dezidua, Plazenta, Embryo) betrugen 10% der korrespondierenden Serumkonzentrationen. In der Spätschwangerschaft wurden Gewebespiegel in der Plazenta sowie im Fruchtwasser als auch in Serum aus der Nabelschnurarterie und -vene unmittelbar nach der Entbindung untersucht. Die maximalen Plazentakonzentrationen betrugen 30 mg/kg und nahmen exponentionell mit einer Halbwertszeit von 2,8 bis 1,3 Stunden nach einmaliger resp. mehrfacher Dosierung ab. Die Fruchtwasserspiegel stiegen von 10 mg/l unmittelbar nach der ersten auf 60 mg/l nach der siebten Infusion an. Die individuellen Nabelschnurspiegel in der Arterie und Vene waren signifikant unterschiedlich und deuten darauf hin, daß der Foet ein tiefes Kompartment darstellt. Die mit der Muttermilch ausgeschiedene Ticarcillin-Gesamttagesmenge war direkt zum totalen Volumen korreliert und betrug 2–2,5 mg/l.
    Notes: Summary Ticarcillin tissue concentrations were determined in 77 patients following an infusion of 5 g over 30 min. The tissues studied in gynecology were endometrium, tube, ovary and myometrium. The relative tissue levels ranged from 17% to 30% of the corresponding serum concentrations when ticarcillin was administered once, and from 22% to 32% when the drug was infused repeatedly. In no case did these tissue levels exceed the serum concentrations. The mean relative tissue levels in early pregnancy (decidua, placenta, embryo) were 10% of the corresponding serum concentrations. Levels in late pregnancy were determined in the placenta, amniotic fluid and in serum from the umbilical cord artery and vein immediately after delivery. Maximal placenta concentrations of 30 mg/kg were determined; these declined exponentionally with half-lives of 2.8 and 1.3 h, respectively, following single and repeated dosings. Amniotic fluid levels increased from 10 mg/l immediately after the first infusion to 60 mg/l after the seventh infusion. Individual umbilical cord levels in the artery and vein were significantly different, indicating that the fetus has properties of a deep compartment. The total amount of ticarcillin excreted daily in the mother's milk was strictly correlated to its total volume and ranged from 2–2.5 mg/l.
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  • 5
    Electronic Resource
    Electronic Resource
    Springer
    Infection 16 (1988), S. S3 
    ISSN: 1439-0973
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Description / Table of Contents: Zusammenfassung Die Fluorierung von Piperazin-substituierten Chinolonen hat zur Entwicklung einer interessanten Serie neuer Breitspektrum-Antibiotika geführt, die oral und parenteral verabreicht werden können und gut vertragen werden. Norfloxacin wurde bereits früh entwickelt, es folgten Ciprofloxacin, Enoxacin, Ofloxacin und Pefloxacin. In der vorliegenden Übersicht wird die am umfangreichsten untersuchte Verbindung am stärksten berücksichtigt und es werden, soweit verfügbar, Daten von Norfloxacin und Ofloxacin zum Vergleich herangezogen. Wegen ihrer Nebenwirkungs-Profile, die derzeit ihre therapeutische Anwendung einschränken, werden Enoxacin und Pefloxacin übergangen. Für Substanzen jüngeren Datums, wie Fleroxacin und Defloxacin liegen für eine Diskussion in diesem Rahmen noch nicht genügend Untersuchungen vor.
    Notes: Summary The fluorination of piperazinyl substituted quinolones has led to an interesting development of a series of new broad spectrum antibacterial agents that may be administered orally as well as parenterally and are well tolerated. Norfloxacin was an early compound, later followed by ciprofloxacin, enoxacin, ofloxacin and pefloxacin. In this overview the emphasis will be on the most extensively studied compound including comparisons, where data are available, with norfloxacin and ofloxacin. Enoxacin and pefloxacin will be omitted due to their pattern of side effects, which at present curtail their therapeutic use. More recent substances such as fleroxacin and defloxacin have not been sufficiently investigated to be considered in this context.
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  • 6
    Electronic Resource
    Electronic Resource
    Springer
    Infection 16 (1988), S. S14 
    ISSN: 1439-0973
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Description / Table of Contents: Zusammenfassung Die Penetration von Ciprofloxacin in Tonsillen wurde an 20 erwachsenen Patienten, die sich einer Tonsillektomie unterziehen mußten, untersucht. Zehn Patienten erhielten eine einmalige Infusion von 200 mg Ciprofloxacin (Gruppe A) und weitere 14 Patienten erhielten eine dreitägige orale Therapie mit 500 mg Ciprofloxacin zweimal täglich vor der anschließenden perioperativen Infusion von 200 mg (Gruppe B). Die Ciprofloxacin-Konzentrationen in Serum und Tonsillen wurden mikrobiologisch bestimmt. Die mittleren Ciprofloxacin-Serumkonzentrationen waren zwischen beiden Gruppen nicht signifikant verschieden. Gleichermaßen betrug das mittlere Verteilungsverhältnis zwischen Tonsillen und Serum 150% unabhängig, ob die Substanz einmal oder mehrfach verabreicht wurde. Somit wurde weder im intra- noch im extravaskulären Raum eine signifikante Kumulation von Ciprofloxacin beobachtet.
    Notes: Summary Penetration of ciprofloxacin into human tonsils was studied in 20 adult humans undergoing tonsilectomy. Ten patients received a single intravenous infusion of 200 mg ciprofloxacin within 15 min (group A) and 14 patients were treated orally for three days with 500 mg ciprofloxacin b.i.d. prior to a preoperative infusion of 200 mg (group B). Ciprofloxacin concentrations in serum and tonsils were determined microbiologically. Mean ciprofloxacin serum concentrations did not differ significantly between both groups. Similarly, mean distribution ratios between tonsils and serum were not dissimilar, being on average 150% irrespective of whether the drug was administered once or repeatedly. Thus, a significant accumulation of ciprofloxacin was not observed either in the intravascular or in the extravascular space.
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  • 7
    Electronic Resource
    Electronic Resource
    Springer
    Infection 16 (1988), S. S24 
    ISSN: 1439-0973
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Description / Table of Contents: Zusammenfassung In einer prospektiven pharmakokinetischen Studie wurden die Serumund Gewebespiegel von Ciprofloxacin (Bay O9867), einem neuen Chinolonderivat aus der Gruppe der Gyrasehemmer, bestimmt. 22 Patientinnen erhielten 300 mg Ciprofloxacin präoperativ infundiert (Gruppe A) und 19 Patientinnen erhielten zunächst drei Tage lang 500 mg Ciprofloxacin per os zweimal täglich, gefolgt von 300 mg Ciprofloxacin i. v. präoperativ (Gruppe B). Gewebeproben von etwa 2 g wurden intraoperativ aus den Eileitern, den Ovarien, dem Fundusmyometrium, sowie der Cervix entnommen. Die Konzentrationsbestimmungen erfolgten biologisch mit dem Agardiffusionstest. Die Ciprofloxacin-Konzentrationen lagen in beiden Untersuchungsgruppen im Serum und im gynäkologischen Gewebe in derselben Größenordnung. Die höchsten Serumkonzentrationen von 6 bzw. 4 mg/l wurden unmittelbar nach der Infusion gefunden. Nach zwei Stunden lagen die Serum-Konzentrationen in beiden Gruppen zwischen 0,6 mg/l und 1,3 mg/l. Die Gewebekonzentrationen zu denselben Zeitpunkten erreichten 0,62–3,3 mg/kg, was darauf hinweist, daß diese die simultanen Serumspiegel übersteigen. Im Durchschnitt liegen die Ciprofloxacin-Konzentrationen im Extravaskularraum zweifach höher als in den entsprechenden Serumproben. Ciprofloxacin kumuliert nicht. Die erzielten Gewebekonzentrationen sind zur Erzielung einer vollen antibakteriellen Wirkung bei gynäkologischen Infektionen voll ausreichend, da die MHK für die meisten pathogenen Bakterien weniger als 1 mg/l beträgt.
    Notes: Summary In a prospective pharmacokinetic study the serum and tissue concentrations of ciprofloxacin (Bay O9867), a new carboxyquinolone antimicrobial agent were studied. 22 patients were given 300 mg ciprofloxacin i. v. before the operation (group A), and 19 patients were premedicated with 500 mg ciprofloxacin orally twice daily for three days followed by 300 mg i. v. preoperatively. Tissue samples weighing approximately 2 g were taken from the fallopian tubes, the ovaries, the fundus myometrium and the cervix. Ciprofloxacin concentrations were measured biologically by the cup plate agar diffusion method. Ciprofloxacin concentrations in serum and gynecological tissues were within the same range in both groups. Maximal serum concentrations of 6 and 4 mg/l, respectively, were recorded immediately after infusion. After 2 h serum concentrations ranged from 0.6 to 1.3 mg/l in both groups. At the same time, the tissue concentrations ranged from 0.62 to 3.3 mg/kg, indicating that tissue levels exceed corresponding serum concentrations. On average ciprofloxacin is concentrated in the extravascular space two-fold, as compared to the corresponding serum concentrations. There is no drug accumulation. The tissue concentrations obtained provide a full antibacterial coverage for gynecological infections, since the MIC for the most pathogenic bacteria is less than 1 mg/l.
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  • 8
    ISSN: 1439-0973
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Description / Table of Contents: Zusammenfassung Die publizierten präklinischen sowie klinischen Daten zur Chinolonresistenz sind synoptisch dargestellt. Im Verlauf der klinischen Anwendung von Fluorochinolonen wurde bislang nur sporadisch das Auftreten Chinolon-resistenter Stämme beobachtet. Diese resistenten Stämme traten vor allem unter solchen klinischen Bedingungen auf, unter denen entweder hohe Bakterienzellzahlen chronische Infektionen verursachen und/oder in solchen Infektlokalisationen, in denen die Chinolonkonzentrationen nicht optimal sein können. Bezogen auf die individuelle Wahrscheinlichkeit des Auftretens Chinolon-resistenter Stämme treten diese vorrangig in hospitalisierten Patienten oder Pflegeheimbewohnern mit identifizierbaren Risikofaktoren auf. Epidemiologische Studien ergaben, daß in nahezu allen untersuchten Fällen ein oder ein vorherrschender Chinolon-resistenter Klon selektiert worden war, der sich anschließend horizontal ausbreitete. Somit ist das Auftreten einer Chinolonresistenz nicht auf eine unabhängige Selektion einer Vielzahl resistenter Stämme in entsprechend vielen Patienten zurück-zuführen, sondern vielmehr auf eine klonale Ausbreitung eines einzigen Stammes sobald dieser eine Chinolonresistenz erworben hat. Folglich ist die Rate der Chinolonresistenz sehr wahrscheinlich geringer als publiziert.
    Notes: Summary This review focuses on published information on the experimental as well as clinical data on the emergence of quinolone resistant isolates. In the course of clinical use of fluoroquinolones, only a sporadic emergence of quinolone resistance has been noted. The resistant organisms emerged particularly in certain clinical settings where large numbers of organisms frequently causing chronic infections are present and/or in loci where quinolone concentrations may not be optimal. In terms of occurrence in individuals, quinolone resistance has emerged most frequently in hospitalized and nursing-home patients with identifiable risk factors. Epidemiological studies revealed that in nearly all the cases studied one or one predominating quinolone resistant clone was selected that was horizontally transmitted. Thus, the emergence of quinolone resistance is not due to an independent selection of resistant strains in a number of patients, but to the clonal spread of one strain once it has acquired quinolone resistance. Therefore, the rate of quinolone resistance is very likely to be lower than reported.
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  • 9
    Electronic Resource
    Electronic Resource
    Springer
    Medical microbiology and immunology 175 (1986), S. 341-353 
    ISSN: 1432-1831
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The effect ofβ-lactam antibiotics on phagocytosis and intracellular killing of four isogenicEscherichia coli strains differing in their 0- and K antigens was studied by adopting the rat polyvinyl-sponge model. The penicillins mezlocillin, ticarcillin and piperacillin rendered all four isogenicE. coli strains more susceptible to intraleukocyte killing; the cefalosporins tested exhibited inhomogenous effects; lamoxactam was marginally effective, whereas cefoxitin was completely ineffective; cefotaxime caused an increase in intracellular killing of the capsule-defective mutant only. Theβ-lactam promoted increase in intracellular killing could be inhibited byα-methylmannoside but not byα-methylglucoside. Free-flow electrophoretic separation of mezlocillin-treated bacteria and guinea pig erythrocytes revealed that co-migration ofE. coli and erythrocytes respectively could be inhibited byα-methylmannoside but not byα-methylglucoside. These data indicate that mezlocillin interferes with the mannose sensitive adhesins ofE. coli.
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  • 10
    Electronic Resource
    Electronic Resource
    Springer
    Naturwissenschaften 62 (1975), S. 392-393 
    ISSN: 1432-1904
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology , Natural Sciences in General
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