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  • 1
    Electronic Resource
    Electronic Resource
    Increased activity of enzymes of the tricarboxylic acid cycle in response to aldosterone in the toad bladder (1968)
    Springer
    Pflügers Archiv 300 (1968), S. 213-225 
    Details
    ISSN: 1432-2013
    Keywords: Biological Transport, active ; Aldosterone ; Sodium ; Enzymes ; Tricarboxylic Acid Cycle ; Aktiver Transport ; Aldosteron ; Natrium ; Enzyme ; Trikarbonsäurecyclus
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary 1. The activities of condensing enzyme, isocitrate dehydrogenase, glutamate dehydrogenase, glutamate-oxaloacetate transaminase, and malate dehydrogenase increase in toad bladder mucosa in vitro 2 hours after addition of d-aldosterone (10−7 M) to the serosal bathing medium whereas no change in activity of lactate dehydrogenase, aldolase and pyruvate kinase was noted. 2. The increase in enzyme activities has approximately the same time course as the stimulation of sodium transport by aldosterone. 3. The response of sodium transport to d-aldosterone was studied in the same tissue which was assayed for enzymatic activity. A significant, positive correlation between relative increments in sodium transport and in condensing enzyme activity per milligram of mucosal protein was found to exist. 4. The effects of aldosterone on both sodium transport and enzyme enhancement were abolished by actinomycin D and puromycin. 5. The increase in activity of mitochondrial enzymes due to d-aldosterone was not dependent on the presence of sodium in the mucosal bathing medium and hence was independent of any possible direct stimulatory effect of transepithelial sodium transport on enzyme activity. 6. The increase in activity of enzymes contributing to the supply of aerobic energy for the enhanced sodium transport induced by aldosterone is regarded as complementary to an independent action of the hormone to increase the entry of sodium into the transport process.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00364295
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  • 2
    Electronic Resource
    Electronic Resource
    Der Einfluß von Aldosteron auf die Aktivität mitochondrialer und cytoplasmatischer Enzyme in der Rattenniere (1968)
    Springer
    Pflügers Archiv 300 (1968), S. 244-254 
    Details
    ISSN: 1432-2013
    Keywords: Aldosterone ; Adrenalectomy ; Sodium Transport ; Tricarboxylic Acid Cycle ; Enzyme Activity ; Aldosteron ; Adrenalektomie ; Natriumtransport ; Citronensäurecyclus ; Enzymaktivität
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Description / Table of Contents: Zusammenfassung In Nieren normaler und adrenalektomierter Ratten wurde die Aktivität des condensing enzyme, der TPN-Isocitrat-Dehydrogenase, DPN-Isocitrat-Dehydrogenase, Succinat-Dehydrogenase, Malat-Dehydrogenase, Glutamat-Oxalacetat-Transaminase, Glutamat-Dehydrogenase, β-Hydroxybutyrat-Dehydrogenase, α-Glycerophosphat-Oxydase, Glyceraldehydphosphat-Dehydrogenase, Lactat-Dehydrogenase, Pyruvat-Kinase und des malic enzyme bestimmt. Adrenalektomie bewirkt eine Abnahme der Aktivität des condensing enzyme um 44%, der TPN-Isocitrat-Dehydrogenase um 20%, der Glutamat-Oxalacetat-Transaminase um 23%, der Glutamat-Dehydrogenase um 23% und der Glyceraldehydphosphat-Dehydrogenase um 17%. Gabe von Aldosteron bei adrenalektomierten Tieren normalisiert die Aktivität des condensing enzyme, der TPN-Isocitrat-Dehydrogenase und der Glutamat-Dehydrogenase, die Aktivität der Glutamat-Oxalacetat-Transaminase und der Glyceraldehydphosphat-Dehydrogenase zeigt eine nicht zur Normalisierung ausreichende Steigerung. Außerdem wird die durch Adrenalektomie nicht veränderte Aktivität der Succinat-Dehydrogenase um 10% erhöht.
    Notes: Summary The activity of the following enzymes was determined in kidneys of normal and adrenalectomized rats: condensing enzyme, isocitrate dehydrogenase (NADP and NAD), succinate dehydrogenase, malate dehydrogenase, aspartate aminotransferase, glutamate dehydrogenase, hydroxybutyrate dehydrogenase, glycerophosphat dehydrogenase, glyceraldehydphosphat dehydrogenase, pyruvate kinase, lactate dehydrogenase, malate dehydrogenase (decarboxylating, NADP). Adrenalectomy lowers the activity of condensing enzyme by 44%, of isocitrate dehydrogenase (NADP) by 20%, of aspartate aminotransferase by 23%, of glutamate dehydrogenase by 23% and of glyceraldehydphosphat dehydrogenase by 17%. Aldosterone given to adrenalectomized rats normalises the activity of condensing enzyme, isocitrate dehydrogenase (NADP), and glutamate dehydrogenase, the activity of aspartate aminotransferase and glyceraldehydphosphat dehydrogenase increases without reaching the control levels. The activity of succinate dehydrogenase is not influenced by adrenalectomy but is augmented by aldosterone treatment of adrenalectomized animals.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00364297
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  • 3
    Electronic Resource
    Electronic Resource
    Pharmacodynamics and pharmacokinetics of three different doses of urapidil infused in hypertensive patients (1986)
    Springer
    European journal of clinical pharmacology 30 (1986), S. 549-552 
    Details
    ISSN: 1432-1041
    Keywords: urapidil ; pharmacodynamics ; pharmacokinetics ; hypertension
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The study was designed to follow the haemodynamic effects and pharmacokinetics under steady-state conditions of three different doses of urapidil infused continuously. Nine male hypertensive patients received three randomly assigned intravenous infusions of 32.5, 65 and 130 mg urapidil, over 14 h during 6 consecutive days, in a change-over fashion. Blood pressure and heart rate were measured over a period of 28 h after the infusion began and were compared with a reference profile obtained prior to the treatment periods. Urapidil and its main metabolite, parahydroxylated urapidil, were also determined for 28 h after the infusion began using HPLC. The 32.5 mg dose of urapidil caused a maximum decrease in systolic blood pressure of 33±8 mmHg, the 65 mg dose a maximum decrease of 39±12 mmHg and the 130 mg dose a maximum decrease of 50±12 mmHg. The 32.5 and 65 mg doses resulted in similar serum urapidil concentrations, with maximum levels in the 100 to 200 ng/ml range, and the 130 mg dose caused a maximum level approximately four times that achieved with the 32.5 mg dose. The serum concentration of parahydroxy urapidil was proportional to the corresponding dose of urapidil. Four patients reported mild headache, fatigue, weakness, pressure in the head, perspiration and orthostatic dysregulation. The side-effects were probably drug related but required no specific therapy. In summary, the 32.5 mg dose of urapidil resulted in a pronounced decrease in blood pressure. The average pressure reduction over the 14-h infusion period showed further dose-dependent increases after the 65 and 130 mg doses. In severe hypertension, the 130 mg dose can be employed, since it does result in a further, significantly larger decrease in blood pressure.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00542413
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  • 4
    Electronic Resource
    Electronic Resource
    New aspects of the pharmacokinetics and pharmacodynamics of clonidine in man (1983)
    Springer
    European journal of clinical pharmacology 24 (1983), S. 21-30 
    Details
    ISSN: 1432-1041
    Keywords: clonidine ; bioavailability ; blood pressure ; elimination half-life ; pharmacokinetics ; plasma catecholamines ; rebound phenomenon
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Using considerably improved analytical methods, the kinetics and effects of clonidine were observed in healthy volunteers over periods of time more than 3 times longer than those previously reported. The high sensitivity and small work load of the newly developed method permitted the performance of low-dose and multipledose trials. 1. The complete bioavailability of clonidine and its elimination half-life (20 to 25.5 h) remained constant after single and multiple doses. 2. Approximately 62% of a given dose was excreted unchanged in the urine, independent of the quantity administered (0.075, 0.15, 0.2, 0.25 or 0.3 mg), the drug formulation (solution, tablet, Perlonget) or of the mode of administration (i.v., p.o.; single or multiple doses). 3. As the pharmacokinetics of the drug were affected by entero-hepatic circulation, it cannot be described by a conventional, open one or two compartment model. 4. The time courses of the plasma clonidine concentration and its drug effects ran asynchronously. 5. On cessation of chronic clonidine administration, blood pressure and plasma catecholamine levels increased to pretreatment levels without exhibiting any “overshoot” reaction.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00613922
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  • 5
    Electronic Resource
    Electronic Resource
    Pharmacodynamics and pharmacokinetics of urapidil in hypertensive patients: A crossover study comparing infusion with an infusion-capsule combination (1987)
    Springer
    European journal of clinical pharmacology 32 (1987), S. 61-65 
    Details
    ISSN: 1432-1041
    Keywords: urapidil ; hypertension ; alpha-adrenoceptor blocker ; antihypertensive agent ; pharmacodynamics ; pharmacokinetics ; adverse effects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics and haemodynamic effects of infused urapidil and an infusion-capsule combination were followed to study the correlation between the serum urapidil level and the blood pressure. Prior to urapidil administration, basal blood pressure and heart rate were measured for 16 h in 12 male hypertensive patients. Six patients received infusions lasting for 4 h of urapidil 10, 2.5 and 5 mg/h. Six patients were infused with urapidil 10 mg/h for 4 h and 2 h after the end of the infusion each took a 60-mg capsule. After a 5 day washout period the procedures were crossed over. A maximum serum urapidil level of 625±232 ng/ml was achieved at the end of the 10 mg/h infusion, when the fall in blood pressure was 37/21 mmHg. During the 2.5 and 5 mg/h infusions the serum urapidil level was 330 and 420 ng/ml, respectively, and the corresponding decreases in blood pressure were 28/16 mmHg and 31/8 mmHg. Although the urapidil concentration 1 hour after beginning the infusion was only 184±89 ng/ml a near maximal blood pressure decrease had already occurred 33±9/20±8 mmHg, whereas, 1 h after the end of the infusion the reduction in blood pressure was only 10±12/3±8 mm, with a urapidil concentration of 358±120 ng/ml. During the plateau phases of both the infusion and infusion-capsule treatments the falls in blood pressure followed the serum urapidil levels. Only in the initial rising and final falling phases of the treatments were the pharmacodynamics and pharmacokinetics of urapidil not correlated.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00609958
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