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  • 1
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    German Medical Science GMS Publishing House; Düsseldorf
    In:  Infektiologie Update 2016; 25. Jahrestagung der Paul-Ehrlich-Gesellschaft für Chemotherapie (PEG); 20161006-20161008; Rostock; DOC16peg24 /20160930/
    Publication Date: 2016-09-30
    Keywords: ddc: 610
    Language: German
    Type: conferenceObject
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  • 2
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    German Medical Science GMS Publishing House; Düsseldorf
    In:  Bad Honnef-Symposium 2019; 20190429-20190430; Bonn; DOC19bhs10 /20190425/
    Publication Date: 2019-04-26
    Keywords: ddc: 610
    Language: German
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  • 3
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    German Medical Science GMS Publishing House; Düsseldorf
    In:  GMS Infectious Diseases; VOL: 5; DOC03 /20170203/
    Publication Date: 2017-02-03
    Description: The mean (SD) unbound fraction of moxifloxacin in plasma from patients with severe sepsis or septic shock was determined by ultrafiltration to 85.5±3.0% (range 81.9 and 91.6%) indicating a decreased protein binding of moxifloxacin in this population compared with the value of 58-60% provided in the Summary of Product Characteristics. However, previous investigations neglected the influence of pH and temperature on the protein binding of moxifloxacin. Maintaining physiological conditions (pH 7.4, 37°C) - as in the present study - the unbound fraction of moxifloxacin in plasma from healthy volunteers was 84%. In contrast, the unbound fraction of moxifloxacin was 77% at 4°C and 66-68% in unbuffered plasma or at pH 8.5 in fair agreement with previously published data. PK/PD parameters e.g. f AUC/MIC or ratios between interstitial fluid and free plasma concentrations, which were obtained assuming a protein binding rate of moxifloxacin of 40% or more, should be revised.
    Keywords: fluoroquinolone ; unbound fraction ; ultrafiltration ; septic shock ; ddc: 610
    Language: English
    Type: article
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  • 4
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    German Medical Science GMS Publishing House; Düsseldorf
    In:  Bad Honnef-Symposium 2015; 20150330-20150331; Königswinter; DOC15bhs22 /20150320/
    Publication Date: 2015-03-21
    Keywords: ddc: 610
    Language: German
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  • 5
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    German Medical Science; Düsseldorf, Köln
    In:  Deutscher Kongress für Orthopädie und Unfallchirurgie; 70. Jahrestagung der Deutschen Gesellschaft für Unfallchirurgie, 92. Tagung der Deutschen Gesellschaft für Orthopädie und Orthopädische Chirurgie und 47. Tagung des Berufsverbandes der Fachärzte für Orthopädie; 20061002-20061006; Berlin; DOCW.6.1-1681 /20060928/
    Publication Date: 2007-03-09
    Keywords: ddc: 610
    Language: German
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  • 6
    ISSN: 1435-1803
    Keywords: neurogenic hypertension ; rats ; haemodynamics ; catecholamines ; tissue ; plasma
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary To study the role of peripheral catecholamines in plasma and different tissues in neurogenic hypertension we measured directly blood pressure, maximum rate of left ventricular pressure rise (dp/dtmax) and heart rate through an aortic catheter 5 weeks after total sino-aortic baroreceptor deafferentation in male Sprague-Dawley rats. Blood samples were collected through the same catheter to determine plasma catecholamine concentrations. Blood pressure and dp/dtmax were significantly higher in neurogenic-hypertensive rats when compared with sham operated rats. Plasma noradrenaline concentrations and plasma adrenaline concentrations reached significantly higher levels in neurogenic-hypertensive rats. In the heart noradrenaline content was lower (when calculated per g wet weight) and in the adrenal medulla adrenaline content was higher in neurogenic-hypertensive rats, when compared with sham operated controls. A significant positive correlation was found between dp/dtmax and plasma noradrenaline concentrations. It is concluded that sino-aortic baroreceptor deafferentation produces a significant chronic hypertension, probably supported by elevated plasma catecholamine concentrations and enhanced synthesis and release of adrenaline from adrenal medulla.
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  • 7
    ISSN: 1439-0973
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Description / Table of Contents: Zusammenfassung Zehn Patienten wurden je 2 g Cefotaxim i. v. injiziert. In der Galleflüssigkeit wurden die antibakterielle Aktivität mittels Agardiffusionstest und die Konzentrationen von Cefotaxim und Desacetyl-Cefotaxim mit Hochdruckflüssigkeitschromatographie bestimmt, Die gefundenen Werte erlauben den Einsatz von Cefotaxim bei infektiösen Gallenwegserkrankungen.
    Notes: Summary Ten patients were injected with 2 g cefotaxime i. v. The antibacterial activity in the bile was measured by the agar diffusion test and the concentrations of cefotaxime and desacetyl cefotaxime were determined by high performance liquid chromatography. The values found allow the use of cefotaxime in infectious biliary diseases.
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  • 8
    ISSN: 1439-0973
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Description / Table of Contents: Summary In eleven volunteers and 39 patients undergoing transurethral resection of the prostate or bladder tumor, concentrations of enoxacin were measured in seminal fluid (volunteers), in prostatic fluid (volunteers, patients) and in prostatic adenoma tissue (patients) after oral (400 mg) administration and intravenous (428 mg) infusion (60 min) of enoxacin. Simultaneously 2.534 g of ioxitalamic acid was i.v. injected to identify possible urinary contamination. The concentrations of enoxacin in seminal fluid after 2–4 h and in prostatic tissue after about 1–4 h and 14–16 h exceeded plasma concentrations more than two-fold. The concentrations in prostatic fluid after 1–4 h were about half the plasma concentrations. Venous blood samples were taken after intravenous infusion at intervals of up to 24 h in a total of 14 patients. The mean plasma concentration of enoxacin decreased from its maximum of 6.9 mg/l at the end of infusion to 0.5 mg/l at 12 h after administration. A terminal half life of 6.65 h was calculated according to an open two-compartment model.
    Notes: Zusammenfassung Bei elf Probanden und 39 Patienten, die sich einer transurethralen Resektion der Prostata oder eines Blasentumors unterziehen mußten, wurden Enoxacinkonzentrationen in der Samenflüssigkeit (Probanden), im Prostatasekret (Probanden, Patienten) und im Prostataadenomgewebe (Patienten) nach oraler Gabe von 400 mg bzw. intravenöser Infusion (60 min) von 428 mg Enoxacin gemessen. Gleichzeitig wurde 2,534 g Ioxitalaminsäure intravenös verabreicht, um mögliche Urinkontaminationen zu identifizieren. Die Enoxacinkonzentrationen in der Samenflüssigkeit nach 2–4 h und im Prostataadenomgewebe nach 1–4 h und nach 14–16 h waren mehr als doppelt so hoch wie die Plasmakonzentrationen. Die Prostatasekretkonzentrationen lagen dagegen nach 1–4 h bei etwa der Hälfte der Plasmakonzentrationen. Nach intravenöser Infusion bei 14 Patienten wurden in Intervallen bis zu 24 h venöse Blutproben entnommen, die Plasmakonzentrationen bestimmt und die pharmakokinetischen Parameter berechnet. Die mittlere maximale Plasmakonzentration von Enoxacin lag am Ende der Infusion bei 6,9 mg/l und sank auf 0,5 mg/l nach 12 h. Eine terminale Halbwertszeit von 6,65 h wurde entsprechend einem offenen Zwei-Kompartiment-Modell errechnet.
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  • 9
    ISSN: 1439-0973
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Description / Table of Contents: Zusammenfassung Zwölf gesunde freiwillige Probanden erhielten in einer offenen, randomisierten Cross-Over-Studie zweimal 250 mg Clarithromycin täglich und einmal 500 mg täglich. Am ersten und fünften Tag der Therapie wurden die pharmakokinetischen Parameter von Clarithromycin und seinem aktiven Metaboliten, 14-Hydroxy-Clarithromycin, in Serum, Speichel und Blutzellen (polymorphkernige Leukozyten (PMNs) und mononukleären Zellen (MNCs; nur Clarithromycin) bestimmt. Die mittleren Maximalkonzentrationen von Clarithromycin an Tag fünf waren nach 500 mg Clarithromycin einmal täglich mindestens doppelt so hoch wie nach 250 mg zweimal täglich (Serum: 2,3 vs. 1,2 mg/l; Speichel: 1,1 vs. 0,3 mg/l; MNCs 60 vs. 26 mg/l; PMNs 29 vs. 14 mg/l), die Talspiegel hingegen waren deutlich niedriger (Serum: 0,09 vs. 0,28 mg/l; Speichel: 0,06 vs. 0,13 mg/l; MNCs: 〈1 vs. 6,8 mg/l; PMNs: 0,8 vs. 2,8 mg/l). Die mittleren, relativen Serumkonzentrationen des aktiven Metaboliten, 14-Hydroxy-Clarithromycin, waren hingegen niedriger nach 500 mg Clarithromycin vs. 250 mg (0,78 vs. 0,46 mg/l). Die mittleren Maximalkonzentrationen in Speichel betrugen bei Clarithromycin 25–40% und bei Hydroxy-Clarithromycin 50–80% der maximalen Serumkonzentrationen. Clarithromycin zeigt eine gute und schnelle Diffusion in intrazelluläre und extrazelluläre Körperkompartimente. Im Hinblick auf Bioverfügbarkeit und Maximalkonzentrationen kann das Therapieschema von 500 mg einmal täglich gut mit dem Schema zweimal 250 mg täglich konkurrieren, die Talspiegel am Ende des 24-Stunden-Dosierungsintervalls sind jedoch niedriger.
    Notes: Summary In an open-label, randomized, crossover study 12 healthy volunteers were given clarithromycin orally 250 mg twice daily (b.i.d.) and 500 mg once a day (q.d.). Blood and saliva samples were collected on study days 1 and 5 to determine the pharmacokinetics of clarithromycin and its 14-hydroxy metabolite in plasma and saliva, and to measure concentrations of clarithromycin in mononuclear cells (MNCs) and polymorphonuclear leucocytes (PMNs). The mean peak levels of clarithromycin on day 5 of therapy in serum (2.3 vs. 1.2 mg/l), saliva (1.1 vs. 0.3 mg/l) and blood cells 60 vs. 26 mg/l in MNCs and 29 vs. 14 mg/l in PMNs) were at least doubled, the trough levels were lower with 500 mg q.d. vs. 250 mg b.i.d. (0.09 vs. 0.28 mg/l in serum; 0.06 vs. 0.13 mg/l in saliva; 〈1 vs. 6.8 mg/l in MNCs; 0.8 vs. 2.8 mg/l in PMNs). The mean relative peak serum concentrations of the 14-hydroxy metabolite were somewhat lower with the 500 mg dosage (0.78 vs. 0.46 mg/l). The peak concentrations of clarithromycin and its 14-hydroxy metabolite in saliva were 25–40% and 50–80% of the maximum serum concentrations with both dosage regimens. Clarithromycin exhibits good and rapid penetration into intracellular as well as into extravasal extracellular body compartments. Clarithromycin 500 mg q.d. compares favourably with 250 mg b.i.d., as far as peak serum levels and bioavailability are concerned, but trough levels are lower at the end of the 24-hour dosing interval.
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  • 10
    ISSN: 1439-0973
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Description / Table of Contents: Summary The pharmacokinetic parameters of cefixime were determined in healthy volunteers following oral administration of 200 mg cefixime as tablet, syrup and dry suspension, respectively. All three galenic formulations showed reliable absorption. Mean peak plasma concentrations amounted to 2.4–3.4 mg/l and were reached after 3.3–3.5 h. Mean terminal half-lives were 2.9–3.1 h. The mean areas under the plasma concentration-time curves ranged between 18 and 26 mg/l·h; 18–24% of the dose administered were recovered unchanged in the urine. The best bioavailability was obtained with the dry suspension followed by the tablet and the syrup. With respect to the ester pro-drug cephalosporins, cefuroxime axetil, cefetamet pivoxyl and cefotiam hexetil, cefixime exhibits higher plasma half-life and area under the curve as well as, comparable absolute bioavailability but consistently lower urinary recovery which indicates higher non-renal clearance.
    Notes: Zusammenfassung In einer vergleichenden Untersuchung an gesunden Probanden wurden die pharmakokinetischen Parameter von Cefixim nach oraler Applikation von 200 mg als Trockensuspension, Fertigsaft und Tablette bestimmt. Alle drei galenischen Formulierungen zeigten eine zuverlässige Resorption. Die maximalen mittleren Plasmakonzentrationen betrugen 2,4–3,4 mg/l und wurden nach 3,3 bis 3,5 h erreicht. Die mittleren Plasmahalbwertszeiten waren 2,9 bis 3,1 h, die Fläche unter der Plasmakonzentrations-Zeit-Kurve 18–26 mg/l·h, die Wiederfindung im Urin 18–24% der applizierten Dosis. Die höchste Bioverfügbarkeit wurde gemessen nach Applikation der Trockensuspension gefolgt von Tablette und Fertigsaft. Vor den Prodrug-Cephalosporinen, Cefuroxim Axetil, Cefetamet Pivoxyl und Cefotiam Hexetil, zeichnet sich Cefixim durch längere Plasmahalbwertszeit und größere, dosiskorrigierte Fläche unter der Plasmakonzentrations-Zeit-Kurve aus. Die im Vergleich zu den genannten anderen Cephalosporinen niedrigere Wiederfindung im Urin bei gleicher absoluter Bioverfügbarkeit läßt auf eine größere extrarenale Clearance schließen.
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