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  • 1
    ISSN: 1432-1041
    Keywords: pindolol ; beta-blockade ; slow release tablet ; plasma levels ; urinary excretion ; pharmacokinetics ; pharmacodynamics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary In 10 healthy volunteers the time course of cardiac beta-adrenoceptor blocking activity, plasma levels and cumulative urinary excretion of pindolol were compared during a 4-day course of pindolol 5 mg (Visken®) t. d. s., and one tablet of pindolol 20 mg retard (Visken® retard) once a day. After oral administration of the 20 mg retard tablet, plasma concentrations of pindolol higher than half the maximum value (1/2 Cp (tmax)) were maintained about 2.5 times as long as after administration of the conventional 5 mg tablet. This is evidence for an important and marked retardation of drug release. During treatment with pindolol 20 mg retard once daily, cardiac beta-adrenoceptor blockade, measured by the reduction in exercise-induced tachycardia and in the exercise-induced rise in systolic blood pressure, at almost all times throughout the 24 h period was at least as great as during treatment with pindolol 5 mg t. d. s. This suggests that patients successfully treated with pindolol 5 mg t. d. s. can be maintained with the same beta-adrenoceptor blockade by a single tablet of pindolol 20 mg retard once daily.
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 32 (1987), S. 367-372 
    ISSN: 1432-1041
    Keywords: endralazine ; severe hypertension ; food intake ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary A sensitive HPLC assay has been used to determine the effect of food on plasma endralazine levels in 8 patients with essential hypertension. Subjects were investigated whilst on maintenance therapy with endralazine combined with a fixed antihypertensive baseline treatment for at least 4 weeks, samples being collected after the usual oral morning dose of endralazine (5 mg and 10 mg), on two occasions at least 7 days apart. Endralazine was administered with the concomitant therapy in randomised order once 90 min before and once immediately after a standard breakfast. Acetylator status did not affect its pharmacokinetics in the postprandial study after a 5 mg dose, the peak endralazine concentration averaged 57.5% lower and the AUC had fallen significantly by 49.9%, whereas after 10 mg the postprandial peak level and the AUC were 82.9% and 64.7%, lower. In the 5 mg study the mean arterial blood pressure was decreased by 30 mm Hg in the fasting subjects and by 21 mm Hg in the post-prandial group. For the 10 mg dose the corresponding values were 35 and 24 mm Hg. The blood pressure lowering effect was only weakly correlated with the food — related reduction in the plasma endralazine levels. The results suggest that endralazine has a similar kinetic interaction with food as that found for hydralazine.
    Type of Medium: Electronic Resource
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  • 3
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 21 (1982), S. 451-455 
    ISSN: 1432-1041
    Keywords: pindolol ; plasma levels ; pindolol retard ; beta-adrenoceptor blockade
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary In a cross-over pharmacokinetic study in 8 healthy volunteers a retard formulation containing pindolol 30 mg was compared with the normal 15 mg pindolol tablet. The pindolol 30 mg retard tablet led to the same maximum plasma level as a single dose of the normal pindolol tablet. A plasma concentration higher than half of the maximum was maintained twice as long after the retard than after the normal 15 mg pindolol tablet. The bioavailability of the two forms was practically identical.
    Type of Medium: Electronic Resource
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  • 4
    Electronic Resource
    Electronic Resource
    Amsterdam : Elsevier
    Journal of Chromatography A 237 (1982), S. 399-406 
    ISSN: 0021-9673
    Source: Elsevier Journal Backfiles on ScienceDirect 1907 - 2002
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
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  • 5
    Electronic Resource
    Electronic Resource
    Oxford, UK : Blackwell Publishing Ltd
    Annals of the New York Academy of Sciences 80 (1959), S. 0 
    ISSN: 1749-6632
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Natural Sciences in General
    Type of Medium: Electronic Resource
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  • 6
    Electronic Resource
    Electronic Resource
    Springer
    Cellular and molecular life sciences 25 (1969), S. 103-104 
    ISSN: 1420-9071
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Zusammenfassung Es wird eine Methode zur fluorimetrischen Bestimmung von Thioridazin (Melleril®) und dessen Seitenkettensulfoxid Mesoridazin (Lidanil®) beschrieben. Die Erfassungsgrenze der Methode in Plasma und Urin liegt für beide Wirkstoffe bei 0.05Μg pro Probe.
    Type of Medium: Electronic Resource
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  • 7
    Electronic Resource
    Electronic Resource
    Springer
    Cellular and molecular life sciences 25 (1969), S. 802-803 
    ISSN: 1420-9071
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Zusammenfassung Eine empfindliche fluorimetrische Methode zur Bestimmung von 4-(2-Hydroxy-3-isopropylaminopropoxy)-indol, demβ-Blocker LB 46, in Plasma (Erfassungsgrenze 0,02 Μg) und in Urin (Erfassungsgrenze 0,05 Μg) wird beschrieben. Die mit dieser Methode gemessene biologische Halbwertszeit im Plasma beträgt nach peroraler Verabreichung beim Menschen 3 h und bei der Ratte etwa 30 min.
    Type of Medium: Electronic Resource
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  • 8
    Electronic Resource
    Electronic Resource
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 261 (1968), S. 360-378 
    ISSN: 1432-1912
    Keywords: Ergotamin ; Adrenerges System ; Phenoxybenzamin ; Nickhaut der Spinalkatze ; Isoliert durchströmte Milz der Katze ; Ergotamine ; Adrenergic System ; Phenoxybenzamine ; Nictitating Membrane of the Spinal Cat ; Isolated Perfused Spleen of the Cat
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Description / Table of Contents: Summary The direct effect of ergotamine and the effect of ergotamine on the responses of the nictitating membrane and the isolated perfused spleen of the cat to drugs and nerve stimulation were investigated and compared with the corresponding effects of phenoxybenzamine. Medium to high doses of ergotamine (2 to 500 μg i.a.) cause contraction of the nictitating membrane and the spleen. This contraction can be inhibited by phenoxybenzamine. The effect can be explained by direct stimulation of the α-receptors without involving norepinephrine liberation. Small doses of ergotamine (0.2 to 1 μg i.a. or 1 to 10 μg/kg i.v.) enhance the response of the nictitating membrane to epinephrine, norepinephrine, tyramine and serotonin and also—though less regularly—to sympathetic nerve stimulation. The amount of norepinephrine released into the perfusate from the isolated spleen after nerve stimulation is significantly increased by ergotamine (0.5 to 2 μg/min) but the concomitant organ contractions are not significantly inhibited and may even be enhanced at times. The increase of norepinephrine in the perfusate is best explained by inhibition of norepinephrine re-uptake into the special storage system of the spleen; it is not due to inhibition of enzymatic degradation of the hormone. Therefore, the reinforcement of sympathomimetic responses by ergotamine may be due to the fact that norepinephrine re-uptake is inhibited without the concomitant presence of a sympatholytic action. In the perfused spleen, phenoxybenzamine shows a sympatholytic action in amounts (0.01 to 0.1 μg/min) that are too small to inhibit norepinephrine reuptake; higher amounts (0.2 to 1 μg/min) are required for the latter effect. This fact explains why phenoxybenzamine in contrast to ergotamine does not reinforce sympathomimetic responses.
    Notes: Zusammenfassung Die Eigenwirkung von Ergotamin sowie die Wirkung von Ergotamin auf humorale und neuronale adrenerge Reaktionen an der Nickhaut der Spinalkatze und an der isoliert durchströmten Milz der Katze wurden im Vergleich zu Phenoxybenzamin untersucht. Ergotamin führt in mittleren bis hohen Dosen (2–500 μg i.a.) zu einer Kontraktion der Nickhaut und der Milz. Diese Wirkung ist mit Phenoxybenzamin hemmbar und auf eine α-Receptorenerregung zurückzuführen; sie ist eine direkte und kommt nicht über eine Noradrenalinfreisetzung zustande. In niedrigen Dosen (0,2–1 μg i.a. bzw. 1–10 μg/kg i.v.) potenziert Ergotamin die Adrenalin-, Noradrenalin-, Tyramin- und Serotoninreaktionen und — wenn auch weniger zuverlässig — den Sympathicusreizeffekt an der Nickhaut. An der isoliert durchströmten Milz erhöht Ergotamin (0,5–2 μg/min) die nach Nervenreizung im Perfusat bestimmte Noradrenalinmenge signifikant. Die durch Nervenreizung ausgelösten Milzkontraktionen werden nicht nennenswert gehemmt oder in einzelnen Fällen sogar verstärkt. Die Erhöhung des Noradrenalingehalts im Perfusat ist am ehesten Ausdruck einer Hemmung der Wiederaufnahme von Noradrenalin in die spezifischen Speicher und kommt nicht durch eine Hemmung des fermentativen Abbaus von Noradrenalin zustande. Die Hemmung der Wiederaufnahme von Noradrenalin durch Ergotamin bei gleichzeitig fehlender Sympathicolyse dürfte für die potenzierende Wirkung von Ergotamin auf adrenerge Reaktionen verantwortlich sein. Phenoxybenzamin wirkt an der Milz bereits in Dosen (0,01 bis 0,1 μg/min) deutlich sympathicolytisch, in denen noch keine Hemmung der Wiederaufnahme von Noradrenalin gefunden wird; erst höhere Dosen Phenoxybenzamin (0,2 bis 1 μg/min) hemmen die Wiederaufnahme von Noradrenalin. Dieser Befund erklärt, weshalb Phenoxybenzamin im Gegensatz zu Ergotamin keine verstärkende Wirkung auf adrenerge Reaktionen ausübt.
    Type of Medium: Electronic Resource
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  • 9
    Electronic Resource
    Electronic Resource
    Springer
    Fresenius' Zeitschrift für analytische Chemie 312 (1982), S. 455-461 
    ISSN: 1618-2650
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Zuammenfassung Durch Einsatz von 4-(6-Methylbenzothiazol-2-yl)phenylisocyanat können Verbindungen mit primärem, sekundärem oder teriärem Hydroxyl sowie primäre und sekundäre Amine in hochfluorescierende Derivate übergeführt werden. In Gegenwart einer äquimolaren Menge an Triethylendiamin als Katalysator wird zur Bildung der Urethane ein 5-fach molarer Reagensüberschuß und zur Bildung der Carbamate eine äquimolare Reagensmenge benötigt. Bei einer Reaktionstemperatur von 50° C ist die Reaktion von primären Alkoholen nach 3 h, von sekundären nach 3,5 und von tertiären nach 4h beendet. Primäre, aliphatische Amine reagieren bei Zimmertemperatur innerhalb 5 min und sekundäre, aliphatische Amine innerhalb 10 min. Heterocyclische, sekundäre Amine benötigen trotz Temperaturerhöhung eine längere Zeit. Nach Zerstörung von überschüssigem Isocyanat mit Diethylamin kann das beschriebene Verfahren sowohl mit DC als auch mit HPLC kombiniert werden. Je nach Polarität der zu analysierenden Verbindung ist die Verwendung von Kieselgel oder Reversed-Phase-Material möglich. Mittels DC können noch 250 pg Alkohol als fluorescierendes Urethan bzw. 50 pg Amin als fluorescierendes Carbamat detektiert werden. Bei Anwendung der HPLC liegen die Erfassungsgrenzen für Alkohole bei 500 pg und für Amine bei 250 pg pro 80 μl Einspritzvolu.
    Notes: Summary Compounds with a primary, secondary, or tertiary hydroxyl group and primary and secondary amines, may be converted into highly fluoresceing derivatives by means of 4-(6-methylbenzothiazol-2-yl)phenyl isocyanate. In the presence of an equimolar amount of triethylendiamine as a catalyst, a 5-molar reagent excess is necessary to form urethanes and an equimolar amount of reagent for the formation of carbamates. At a temperature of 50° C the reaction with primary alcohols is completed after 3 h, with secondary alcohols after 3.5 and with tertiary alcohols after 4h. Primary aliphatic amines react at room temperature within 5 min and secondary aliphatic amines within 10 min. In spite of the enhancement by temperature, heterocyclic secondary amines require more time. After the excess of isocyanate has been destroyed with diethylamine the described method may be combined both with TLC or HPLC. Depending on the polarity of the substance to be analyzed, the use of silica gel or reversed-phase material is possible. By means of TLC even 250 pg of alcohol can be detected as fluoresceing urethane and 50 pg of amine as fluoresceing carbamate. Using HPLC the detection limit for alcohols is 500 pg and for amines 250 pg per 80 μl injection volume.
    Type of Medium: Electronic Resource
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  • 10
    Electronic Resource
    Electronic Resource
    New York, NY : Wiley-Blackwell
    Helvetica Chimica Acta 39 (1956), S. 1156-1159 
    ISSN: 0018-019X
    Keywords: Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: Derivatives of 4-thiazolidone are obtained by reaction of mercaptoacetanilicle with 1, 1-dihalogen compounds.
    Additional Material: 1 Tab.
    Type of Medium: Electronic Resource
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