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  • 1
    Digitale Medien
    Digitale Medien
    Springer
    Cellular and molecular life sciences 36 (1980), S. 861-863 
    ISSN: 1420-9071
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Biologie , Medizin
    Notizen: Summary The diuretic agent, furosemide, inhibits liver microsomal uridinediphosphate glucuronyltransferase (EC. 2.4.1.17), in monkey and rat. Inhibition is of the non-competitive type.
    Materialart: Digitale Medien
    Bibliothek Standort Signatur Band/Heft/Jahr Verfügbarkeit
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  • 2
    Digitale Medien
    Digitale Medien
    Springer
    Intensive care medicine 20 (1994), S. S14 
    ISSN: 1432-1238
    Schlagwort(e): Piperacillin ; Beta-lactamases ; Pharmacokinetics
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Abstract Piperacillin/tazobactam is a new combination of a broad-spectrum penicillin and a beta-lactamase inhibitor. In studies in healthy volunteers, the pharmacokinetics of piperacillin combined with tazobactam were similar to those of piperacillin alone. In contrast, tazobactam administered with piperacillin achieved higher plasma concentrations and had a longer half-life than tazobactam administered alone. Intravenous infusion of 4.0 g piperacillin with 0.5 g tazobactam over 5 min resulted in mean maximum plasma concentrations of 380 μg piperacillin/ml and 35.3 μg tazobactam/ml; half-lives were 1.14 h for piperacillin and 0.92 h for tazobactam. Within 30 min of infusion, piperacillin/tazobactam achieves 16–85% of plasma concentrations in skin, muscle, lung, gallbladder, and intestinal mucosa. Plasma and tissue levels remain above the MIC90s of major pathogens for 2 h post administration. These findings show that piperacillin/tazobactam is a truly synergistic combination which can be expected to be effective in treating a wide variety of infections in the clinical setting.
    Materialart: Digitale Medien
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  • 3
    Digitale Medien
    Digitale Medien
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 333 (1986), S. 457-461 
    ISSN: 1432-1912
    Schlagwort(e): Furosemide ; Hydrochlorothiazide ; Tizolemide ; Amiloride ; Triamterene ; Interactions ; Pharmacokinetics ; Micropuncture
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Summary The interaction between furosemide on the one hand and hydrochlorothiazide, tizolemide, amiloride and triamterene on the other was studied by clearance and micropuncture techniques in rats. Simultaneous administration of furosemide with hydrochlorothiazide and tizolemide distinctly increased the natriuresis compared to that induced by furosemide alone, whereas the potassium excretion diminished. In contrast, amiloride and triamterene primarily decreased furosemide-induced fractional potassium excretion by about 30%, whereas sodium excretion increased only slightly compared to that produced by furosemide alone. Hydrochlorothiazide and triamterene significantly decreased furosemide secretion and changed its pharmacokinetics. Furosemide plasma concentration increased, thus possibly prolonging the salidiuretic effect. Amiloride and tizolemide did not influence the secretion of furosemide at all.
    Materialart: Digitale Medien
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  • 4
    Digitale Medien
    Digitale Medien
    Springer
    Neuroradiology 32 (1990), S. 70-73 
    ISSN: 1432-1920
    Schlagwort(e): Intrathecal diatrizoate meglumine ; Lethal dysregulation
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Notizen: Summary A case of inadvertent intrathecal injection of diatrizoate meglumine is presented. After myelography with 10 ml i.e. 6.5 g Angiografin, a 76-year-old man rapidly developed myoclonus, drowsiness and excessive metabolic acidosis. He died only a few hours later. Postmortem showed non-specific brain edema. RP-HPL-Chromatography confirmed high concentration of the contrast medium in CSF (6 mg/ml) which must have induced refractory central nervous dysregulation. The lethal effects of the misapplication of this agent on the nervous system are discussed.
    Materialart: Digitale Medien
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  • 5
    Digitale Medien
    Digitale Medien
    Springer
    European journal of clinical pharmacology 54 (1998), S. 615-619 
    ISSN: 1432-1041
    Schlagwort(e): Key words Mefloquine ; Bioavailability ; Bioinequivalence
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Abstract Objective: To assess the bioequivalence between a generic tablet of mefloquine (Mephaquin® = M1) with the reference tablet (Lariam® = M2) in healthy volunteers. Methods: This open label, randomized two-way cross-over study was performed in a single centre. Following an overnight fast, eighteen healthy volunteers received a single oral dose of 750 mg mefloquine either in the form of three M1 lactabs or three M2 tablets. Serial blood samples were collected up to 8 weeks after drug administration. Plasma samples were analysed for mefloquine and its carboxylic acid metabolite using liquid chromatography and subsequent tandem mass spectrometry (LC-MS/MS). The pharmacokinetic parameters of mefloquine and its metabolite were estimated by non-compartmental methods. Results: The pharmacokinetics of mefloquine after administration of M1 and M2 tablets were significantly different as reflected by the respective mean values of maximum plasma concentration (Cmax 656 vs 1018 ng · ml−1), time to reach maximum concentration (tmax 46 vs 13 h) and area under the plasma concentration-time curve (AUC0→∞ 338 vs 432 μg · h · ml−1). No significant differences existed between the elimination half-lives of the two formulations (394 vs 396 h). The relative bioavailability (M1 vs M2) was 0.78 and ranged from 0.38 to 1.37. Bioequivalence could not be demonstrated for log-transformed data of AUC0→∞ or AUC0→last within a predefined range of 80–125% and for Cmax within a range of 70–143%. Conclusions: The observed differences in Cmax, tmax and AUC are consistent with a slower rate and lower extent of mefloquine absorption after administration of M1. Statistical evaluation of these kinetic data showed that the M1 tablet is not bioequivalent to the M2 tablet. Clinical consequences of this finding cannot be excluded.
    Materialart: Digitale Medien
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  • 6
    Digitale Medien
    Digitale Medien
    Springer
    European journal of clinical pharmacology 32 (1987), S. 625-629 
    ISSN: 1432-1041
    Schlagwort(e): disopyramide ; bioavailability ; saturable binding ; pharmacokinetics
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The pharmacokinetics of disopyramide were determined in 10 healthy volunteers after a 300 mg oral dose and again after a 2mg/kg i.v. dose. The unbound clearance was 599 ml/min and the unbound renal clearance 310 ml/min. The terminal elimination rate constant of unbound drug was 0.180 h−1 after the i.v. dose and 0.203 h−1 after the oral dose. The absorption rate constant was 0.53−1 and the maximum peak concentration occurred after 3.2 h. The bioavailability was 0.809 using the area under the unbound plasma concentration time curve. Although a saturable plasma protein binding was found in all subjects the bioavailability using the total concentration, in contrast to theoretical expectations, showed the same value (0.813) as the unbound concentrations.
    Materialart: Digitale Medien
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  • 7
    Digitale Medien
    Digitale Medien
    Springer
    European journal of clinical pharmacology 35 (1988), S. 313-317 
    ISSN: 1432-1041
    Schlagwort(e): disopyramide ; alpha1-acid glycoprotein ; renal dysfunction ; pharmacokinetics
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The pharmacokinetics of disopyramide was studied in 15 patients with renal dysfunction (4 with pyelonephritis, 7 with glomerular nephritis and 4 with interstitial nephritis). The elimination rate constant of unbound disopyramide was 0.094 h−1 and CLu/f (unbound clearance divided by bioavailability) was 245 ml/min. Both the unbound renal clearance (CLR) and CLu/f were highly correlated with the creatinine clearance (CLCR). The apparent unbound metabolic clearance in the patients was approximately two-fold lower than that previously reported in normal subjects. The estimated unbound metabolic clearance in the renal dysfunction patients showed a significant negative correlation with the α1-acid glycoprotein (AAG) concentration and only a weak, non-significant correlation with CLCR. As AAG in the renal dysfunction subjects was increased in comparison with normal values, it is possible that AAG is a factor in the decrease in the apparent unbound metabolic clearance.
    Materialart: Digitale Medien
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  • 8
    Digitale Medien
    Digitale Medien
    Springer
    European journal of clinical pharmacology 28 (1985), S. 665-670 
    ISSN: 1432-1041
    Schlagwort(e): tocainide ; renal failure ; pharmacokinetics ; oral dosing ; pharmacodynamics
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The plasma levels of tocainide have been followed after oral administration of 600 mg p.o. to 20 patients with renal failure due to various causes, and to 8 healthy controls. The peak plasma concentrations in the patients with pyelonephritis (3.80 µg/ml) and interstitial nephritis (3.74 µg/ml) but not in those with glomerulonephritis (3.17 µg/ml) differed from that in healthy volunteers (3.24 µg/ml). The renal clearance of tocainide was well correlated with the endogenous creatinine clearance and was dependent on urine pH. No difference in renal clearance was observed between the patients groups. It is suggested that the changes in plasma levels are a consequence of decreased renal clearance. Creatinine clearance was shown to be a poor estimator of tocainide clearance, which suggests that extrarenal clearance plays an important role in the handling of the drug in the body. The findings are used to suggest a safe dosage regimen.
    Materialart: Digitale Medien
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  • 9
    Digitale Medien
    Digitale Medien
    Springer
    European journal of clinical pharmacology 26 (1984), S. 133-135 
    ISSN: 1432-1041
    Schlagwort(e): co-dergocrine mesylate ; geriatric patients ; hydergine ; bioavailability ; steady state
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Chemie und Pharmazie , Medizin
    Notizen: Summary The relative bioavailability of the newly developed formulation of co-dergocrine mesylate (Hydergine spezial, 1×4 mg) was determined in elderly patients under steady state conditions, with conventional Hydergine forte tablets (2×2 mg) as a reference. Both formulations were given once a day for 8 days in a randomised cross-over design. The areas under the curve showed that the bioavailability of the new tablet was about 30% higher (28±6.3%) than that of Hydergine forte. The peak plasma concentration was reached 3±0.9 h after administration. Because of its greater relative bioavailability higher plasma levels were found 2–24 hours after the Hydergine spezial formulation than after Hydergine forte tablets.
    Materialart: Digitale Medien
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  • 10
    ISSN: 1439-0973
    Quelle: Springer Online Journal Archives 1860-2000
    Thema: Medizin
    Beschreibung / Inhaltsverzeichnis: Zusammenfassung Die minimalen Hemmkonzentrationen (MHK) von Enoxacin, Nalidixinsäure, Pipemidsäure, Norfloxacin, Ciprofloxacin, Ofloxacin und Pefloxacin wurden gegenüber 400 Erregern, angezüchtet aus dem Urin von 400 urologischen Patienten mit komplizierten Harnwegsinfektionen (HWI), mittels der Agar-Dilutionsmethode (104 KBE, Multipointer) bestimmt. 28 Patienten (21 Männer, sieben Frauen) im Alter von 36 bis 84 Jahren mit komplizierter HWI, verursacht durch empfindliche Erreger, wurden mit Enoxacin, 200 mg 2 × täglich, oral über einen Zeitraum von sechs bis 14 Tagen therapiert. Bei 19 Patienten wurden Plasma- und Urinproben vor und im Intervall nach Gabe von 400 mg Enoxacin auf die Enoxacin-Konzentrationen untersucht. Die Konzentrationsbestimmung erfolgte mit Hochdruckflüssigkeitschromatographie (HPLC). Die MHK-Werte von Enoxacin lagen gegenüber den 265 gramnegativen Erregern bei allen bis auf einen Erreger zwischen 0,03 und 4 mg/l. Die MHK gegenüber den 134 grampositiven Erregern lagen bei allen, mit Ausnahme von 2 Streptokokken-Stämmen, zwischen 0,25 und 16 mg/l. Bei einer Konzentration von 4 mg/l (8 mg/l) wurden 90,3% (98%) aller isolierten Erreger durch Enoxacin gehemmt. Von den Chinolonen, die getestet wurden, zeigte Ciprofloxacin die höchste Aktivitätin vitro und Cinoxacin die schwächste Aktivität. DieIn-vitro-Aktivität von Enoxacin kann man etwa mit der von Norfloxacin, Ofloxacin und Pefloxacin vergleichen. Nach oraler Gabe von 400 mg Enoxacin fanden sich bei den älteren Patienten Spitzenserumkonzentrationen, die zwischen 0,7 und 6,3 mg/l (Durchschnitt 3,6 mg/l) lagen. Diese Konzentrationen wurden ein bis sechs Stunden nach Medikamenteneinnahme erreicht. Die mittlere Urinausscheidung der unveränderten Substanz betrug innerhalb 24 Stunden 31,2% der verabreichten Dosis. 25 der 28 Patienten, die oral mit Enoxacin behandelt wurden, konnten fünf bis 14 Tage nach Beendigung der Therapie nachuntersucht werden. Bei diesen Patienten waren in 18 Fällen eine Heilung, einmal ein Therapieversagen und in sechs Fällen ein Rezidiv (gleiche Keimart) zu verzeichnen. Enoxacin wurde von allen Patienten gut vertragen. Aufgrund der Laboruntersuchungen ergab sich kein Hinweis für renale, hepatobiliäre oder hämatologische Toxizität. Aufgrund unserer Erfahrung eignet sich Enoxacin gut für die Behandlung von komplizierten Harnwegsinfektionen.
    Notizen: Summary Minimal inhibitory concentrations (MIC) of enoxacin, nalidixic acid, pipemidic acid, norfloxacin, ciprofloxacin, ofloxacin and pefloxacin against isolates from 400 urological in-patients with complicated urinary tract infections (UTI) were determined by means of an agar dilution technique (104 cfu, multipointer). 28 patients (21 male, seven female) aged 36 to 84 years with complicated UTI due to sensitive bacteria were treated orally with 200 mg enoxacin b.i.d. for six to 14 days. Plasma and urine samples were collected from 19 patients, at intervals prior to and following a 400 mg dose of enoxacin, and enoxacin concentrations were determined by a high pressure liquid chromatography (HPLC) method. The MICs of enoxacin against all but one of the gram-negative isolates cultured from 265 urological patients were between 0.03 and 4 mg/l. The MICs against 134 gram-positive isolates were between 0.25 and 16 mg/l except two strains of streptococci. At a concentration of 4 mg/l (8 mg/l), 90.3% (98%) of the total spectrum of isolates were inhibited by enoxacin. Of the quinolones tested, ciprofloxacin appeared to be the most active compoundin vitro and cinoxacin the least active antimicrobial agent. Thein vitro activity of enoxacin was comparable to that of norfloxacin, ofloxacin and pefloxacin. Oral administration of 400 mg enoxacin to elderly patients resulted in peak serum concentrations between 0.7 and 6.3 mg/l (mean 3.6 mg/l) attained between 1.0 and 6.0 h following drug ingestion. The mean urinary recovery of parent drug within 24 h was 31.2% of the administered dose. 25 of 28 patients treated orally with enoxacin could be followed-up for five to 14 days after the end of treatment. Enoxacin therapy in these patients resulted in 18 cures, one failure and six relapses (same species). The drug was well tolerated and there was no evidence of renal, hepatic or haematological toxicity. Enoxacin appears to be well suited for the treatment of complicated UTI.
    Materialart: Digitale Medien
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