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  • Articles  (112)
  • Articles: DFG German National Licenses  (112)
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  • Articles  (112)
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  • Articles: DFG German National Licenses  (112)
  • Latest Papers from Table of Contents or Articles in Press
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  • Springer  (112)
  • American Chemical Society (ACS)
  • Molecular Diversity Preservation International
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Year
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  • 1
    Electronic Resource
    Electronic Resource
    Springer
    The journal of membrane biology 94 (1986), S. 205-215 
    ISSN: 1432-1424
    Keywords: Na,K-ATPase ; vanadate ; rubidium ; shark rectal gland ; ouabain ; cAMP ; theophylline ; furosemide
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: Summary Scatchard analysis of3H ouabain bound to isolated rectal gland cells as a function of increasing ouabain concentrations produced a concave curvilinear plot that was resolved into two specific sites with either a high (I) or low (II) affinity for ouabain. Cyclic cAMP/theophylline (±furosemide, 10−4 m) increased the amount of3H ouabain bound to the high-affinity site I. Vanadate, a phosphate congener which promotes formation of the ouabain-binding state of the enzyme, mimicked the effects of cAMP/theophylline at low concentrations of ouabain, suggesting that cAMP/theophylline increases binding to site I by enhancing the rate of turnover of resident enzyme. Enhanced86Rb uptake seen following cAMP/theophylline administration was primarily associated with increased flux through the high-affinity ouabain site, and this stimulation was not obliterated by the co-administration of furosemide. A model was presented which suggested the presence of two noninteracting pools of enzyme or isozymes which exhibit either a high or low affinity for ouabain. Cyclic AMP both stimulated turnover via site I, and modified the kinetics of binding of3H ouabain to site II. The (ave)K d of3H ouabain for site II was increased from 3.6 μm (controls) to 0.5 μm (cAMP/theophylline) and the Hill coefficient was modified from 0.45 (controls) to 1.12 (caMP/theophylline), suggesting a transition from a negative- to a noncooperative binding state. While furosemide reversed the effects of cAMP/theophylline on site II kinetics, it did not obliterate cAMP/theophylline effects on site I. This suggests that cAMP may alter the intrinsic turnover rate of this particular pool of Na,K-ATPase in shark rectal gland.
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  • 2
    Electronic Resource
    Electronic Resource
    Springer
    Microchimica acta 96 (1988), S. 207-221 
    ISSN: 1436-5073
    Keywords: theophylline ; insulin ; competitive binding assays ; flow injection analysis ; ion-selective electrode
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract A fast, non-equilibrium enzyme-linked flow-injection immunoassay (FIIA) system using an immobilized secondary-antibody reactor is described. The assay method is based on the competition between the enzyme-labeled antigen and analyte (unlabeled antigen) for a limited amount of soluble primary-antibody binding sites. This mixture is then introduced via flow-injection into the secondaryantibody reactor. The reactor bound enzyme activity, as measured by flowing an appropriate substrate solution through the reactor, is inversely proportional to the concentration of free analyte in the sample. By using non-equilibrium conditions, a single assay takes a total time of 13 min or less including regeneration of the reactor. To illustrate the application of this system, theophylline and insulin were chosen as model hapten and macromolecule analytes, respectively. Preliminary studies suggest that the new FIIA system is suitable for determining theophylline in serum with acceptable accuracy and precision.
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  • 3
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 32 (1987), S. 431-432 
    ISSN: 1432-1041
    Keywords: theophylline ; fluoroquinolones ; drug interaction ; pharmacokinetics ; ofloxacin ; norfloxacin
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Pretreatment for 3 days with oral ofloxacin or norfloxacin had no significant effect on the disposition of a single i.v. dose the theophylline in healthy volunteers.
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  • 4
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 33 (1987), S. 85-88 
    ISSN: 1432-1041
    Keywords: theophylline ; aminophylline ; incremental concentration ; occlusion pressure ; maximum inspiratory pressure ; transdiaphragmatic pressure ; ventilatory function
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary To investigate the possible mechanisms by which theophylline affects the control of ventilation, neuromuscular drive and ventilatory function were examined in 7 healthy men receiving an incremental intravenous aminophylline dosing schedule to achieve plasma theophylline concentrations of 5, 10, and 15 µg/ml. As compared with the baseline (predose) values, the 3 incremental aminophylline doses significantly (p〈0.05 to 0.01) increased occlusion pressure (P0.1) and maximum inspiratory pressure static (MIPS) at functional residual capacity (FRC). This was not observed for ventilatory flow $$(\dot V)$$ , tidal volume (VT), inspiratory time to total breathing cycle time ratio (Ti/Ttot), VT/Ti, and effective impedance [P0.1/(VT/Ti)]. When maximum electrical activity of diaphragm (Edimax) and transdiaphragmatic pressure (Pdimax) were examined in 3 of the 7 subjects, Pdi/Edi tended to increase with increasing theophylline concentrations, while Edimax did not. Our results suggest that the increase in P0.1 during the increase in aminophylline dose is caused by an improvement in respiratory muscle contractility, rather than by a central effect or by an increase in neural drive.
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  • 5
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 33 (1987), S. 227-230 
    ISSN: 1432-1041
    Keywords: enoxacin ; theophylline ; drug interaction ; healthy volunteers ; adverse effects ; pharmacokinetics ; renal tubular excretion
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The mechanism of the theophylline-enoxacin interaction has been studied in six healthy subjects. Theophylline 250 mg was administered p.o., twice daily for 11 days in a sustained release dosage form. On the 4th day of treatment, blood samples were taken every 2 h and urine was collected over 1 dose interval. From Days 5 to 11 coated tablets of enoxacin 400 mg b.i.d. were coadministered. On Day 11 blood and urine were collected as on Day 4. The mean plasma theophylline concentration rose from 4.4 to 15.1 mg/l, corresponding to a 73.6% reduction in total clearance. The urinary excretion of unchanged theophylline increased from 12.7 to 35.3%, whereas the production of metabolites was reduced (1-demethylation 81.4%; 3-demethylation 83.1%, 8-hydroxylation 74.6%). The results indicate that the theophylline-enoxacin interaction may be due to inhibition of the cytochrome P-450 isozymes responsible for theophylline metabolism. Unexpectedly, the renal clearance of theophylline metabolites was found to be drastically reduced when enoxacin was coadministered. This led to unchanged or even to elevated plasma levels of the metabolites. The mechanism of this interaction is still to be elucidated, but it may be due to competition for renal tubular secretion.
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  • 6
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 33 (1987), S. 487-491 
    ISSN: 1432-1041
    Keywords: theophylline ; furosemide ; drug interaction ; urinary flow ; renal clearance ; urinary excretion
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary In new of previous contradictory results, the possible interaction between the loop diuretic furosemide and theophylline was re-evaluated in 12 healthy volunteers with a steady-state plasma theophylline level. Two doses of furosemide 20 mg at a 4 h interval did not influence the steady-state plasma concentration of theophylline despite causing a moderate diuresis. Urinary recovery of theophylline and its metabolites amounted to 106±21% of the dose without furosemide and 96±19% of the dose with furosemide, demonstrating that there was no influence on the enteral absorption of theophylline of the furosemide treatment. After the first dose of furosemide the fractional renal clearance (CLR1) of theophylline (fractional = hourly sampling period) changed in parallel with the urinary flow rate, without a significant difference between treatment with and without furosemide. After the second dose of furosemide, CLR1 was increased in the first hour and then it declined to levels far lower than the control value. This unexpected result could explain the unchanged plasma concentration of theophylline during furosemide treatment.
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  • 7
    ISSN: 1432-1041
    Keywords: theophylline ; absolute bioavailability ; aminophylline infusion ; sustained-release formulation
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The effect of different intravenous infusions on the absolute bioavailability of theophylline from a sustained-release formulation has been investigated. Oral administration of 750 mg theophylline (2 capsules Euphylong 375) was referenced to intravenous aminophylline infusions corresponding to 506 mg theophylline over 8 h (63 mg·h−1) in Study 1, and to 749 mg theophylline over 14 h in Study 2. A reduction in the infusion rate from 69 to 33 mg·h−1 was made in Study 2 after 8 h in order to mimic the concentration/time profile of the oral formulation as closely as possible. The absolute bioavailability was 100 (89, 115) % in Study 1 and 88 (73, 105) % in Study 2. The lower clearance values and, as a consequence, the lower bioavailability ratios observed with the higher intravenous dose, although not significant, indicate that the absolute bioavailability of theophylline might appear to depend on the choice of the intravenous reference standard.
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  • 8
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 34 (1988), S. 309-310 
    ISSN: 1432-1041
    Keywords: kidney failure ; theophylline ; immunoassay ; drug interference
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary We studied the validity of plasma theophylline measurements in renal failure. Patients with increased serum creatinine receiving theophylline had drug measurements by four methods: high pressure liquid chromatography (HPLC) fluorescence polarization immunoassay (FPIA), enzyme immunoassay (EIA) and dipstick immunoassay (DI). The mean±SD (µmol/l) for plasma theophylline in the 18 patients with renal impairment was: HPLC 63.4±36.7; EIA 64.4±35.9; FPIA 70±3.43; DI 122±65.9. A significant correlation (r=0.94, p〈0.01) was obtained between serum creatinine and the difference in theophylline concentrations between HPLC and DI. Plasma theophylline results should be interpreted with caution in patients with renal failure.
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  • 9
    ISSN: 1432-1041
    Keywords: theophylline ; enprofylline ; liver cirrhosis ; renal failure ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary We have studied the pharmacokinetics of theophylline and enprofylline in patients with liver cirrhosis, patients with chronic renal failure, and healthy subjects, and have assessed the predictive value of routine tests of liver function and renal function (creatinine clearance) for theophylline and enprofylline total body clearances. Theophylline clearance was significantly decreased in the patients with liver cirrhosis compared with both the patients with renal failure and the healthy subjects (the mean values in the three groups were 24, 47, and 46 ml·h−1·kg−1 respectively. Enprofylline clearance was significantly decreased in the patients with chronic renal failure, compared with both the patients with liver cirrhosis and the healthy subjects (the values in the three groups were 64, 250, and 289 ml·h−1·kg−1 respectively. There was a strong correlation between creatinine clearance and enprofylline clearance, while there was only a poor correlation between the liver function tests and theophylline clearance. It appears that in various clinical situations enprofylline elimination can be predicted more precisely than theophylline elimination, which may make the drug safer in clinical practice.
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  • 10
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 34 (1988), S. 145-150 
    ISSN: 1432-1041
    Keywords: asthma ; ketotifen ; prednisolone ; lymphocyte beta2-adrenoceptors ; beta-adrenoceptor desensitization ; tachyphylaxis ; salbutamol ; terbutaline ; theophylline
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary In 13 patients with bronchial asthma, who were onβ 2-adrenergic bronchodilator therapy, the effects of prednisolone and ketotifen on lymphocyteβ 2-adrenoceptor density and -responsiveness were investigated. The mean lymphocyteβ 2-adrenoceptor density and -responsiveness was significantly lower than in healthy controls, presumably due to the long-termβ 2-adrenergic bronchodilator treatment. Both prednisolone 100 mg i.v. and ketotifen 1 mg b.d.p.o. for 6 days rapidly improved lymphocyteβ 2-adrenoceptor function. 16 h after prednisolone and about 6 days after the first dose of ketotifen lymphocyteβ 2-adrenoceptor density and-responsiveness had risen to values within the range in normal volunteers. The improvement of lymphocyteβ 2-adrenoceptor function was accompanied by a significant increase in peak expiratory flow rate before and after inhalation of salbutamol. It is concluded that prednisolone and ketotifen may act beneficially on the recovery ofβ 2-adrenoceptor responsiveness toβ 2-adrenergic bronchodilators in tolerant asthmatic patients.
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