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  • Fibrinolysis  (2)
  • bioavailability  (2)
  • theophylline  (2)
  • 1
    Electronic Resource
    Electronic Resource
    The effects of a combination of cigarette smoking and oral contraception on coagulation and fibrinolysis in human females (1985)
    Springer
    Journal of molecular medicine 63 (1985), S. 221-224 
    Details
    ISSN: 1432-1440
    Keywords: Smoking ; Oral contraception ; Coagulation ; Fibrinolysis ; Fibrinopeptides
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Oral contraception as well as cigarette smoking influence haemostasis. The simulataneous effect of both on blood coagulation and fibrinolysis was studied in nine female smokers. While continuing oral contraception after a 4-week abstinence from smoking the concentration of fibrinogen, antithrombin III and alpha1-Antitrypsin decreased (P〈0.01 orP〈0.04) and of plasminogen increased (P〈0.03). The other coagulation parameters remained unchanged. Although all determinations of these parameters were in the normal range, the observed trends were statistically significant. The concentrations of the fibrinopeptide A and B 15–42 did not differ. It is concluded that the observed alteration is caused by cessation from cigarette smoking.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01731173
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  • 2
    Electronic Resource
    Electronic Resource
    The clinical pharmacokinetics of buflomedil in normal subjects after intravenous and oral administration (1981)
    Springer
    European journal of clinical pharmacology 20 (1981), S. 459-463 
    Details
    ISSN: 1432-1041
    Keywords: buflomedil ; vasodilatation ; pharmacokinetics ; bioavailability ; vasoactive drug
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary A dose-ranging pharmacokinetic study of buflomedil was carried out in eight subjects to determine the pharmacokinetic parameters of the drug after oral and intravenous administration. Based on AUC∞ analyses, the pharmacokinetics of buflomedil were found to be linear within the dose ranges studied (50 to 200 mg for i. v. injection and 150 to 450 mg for oral administration). In the oral study, the mean biological half-life of the drug was 2.97 h, while after intravenous dose it was 3.25 h. The apparent volume of distribution after the pseudodistribution equilibrium (Fdβ) and volume of distribution at the steady state (Vdss) were 1.43±0.24 l/kg and 1.32±0.26 l/kg, respectively. The mean urinary recovery of intact drug and the metabolite, paradesmethyl buflomedil, after intravenous dosing, were 23.6% and 18.7%, respectively, while after oral dosing, they were 18% and 14.8%, respectively. On the average, 72% of the dose was obserbed into the systemic circulation after oral administration. This level of bioavailability was attributed to the hepatic first-pass effect.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00542100
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  • 3
    Electronic Resource
    Electronic Resource
    Lack of clinically important interaction between erythromycin and theophylline (1984)
    Springer
    European journal of clinical pharmacology 26 (1984), S. 485-489 
    Details
    ISSN: 1432-1041
    Keywords: theophylline ; erythromycin ; interaction ; metabolism ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary In 11 healthy volunteers the kinetics of theophylline and the plasma levels and the urinary excretion of its metabolites were studied before and after treatment with erythromycin for 10 days. Theophylline was administered as an intravenous bolus injection (280 mg) followed by a constant intravenous infusion (23.8±4.1 mg/h) for 6 hours. The total clearance of theophylline at steady-state (63.4±9.9 vs 63.8±14.4 ml/min, before vs after erythromycin treatment) and the elimination half-life after cessation of the infusion (6.7±2.6 vs 7.5±1.8 h, before vs after treatment) did not change during the treatment with erythromycin. No difference in the formation of metabolites before and after treatment with erythromycin was detected; the findings in urine were 40.4±5.0 vs 42.1±5.4% 1,3-dimethyluric acid, 29.6±4.6 vs 30.1±5.9% 1-methyluric acid and 13.4±3.5 vs 12.5±2.2% 3-methylxanthine before and after erythromycin treatment, respectively. It is concluded that a clinically relevant interaction between erythromycin and theophylline does not occur.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00542146
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  • 4
    Electronic Resource
    Electronic Resource
    Intestinal absorption of levodopa in man (1983)
    Springer
    European journal of clinical pharmacology 25 (1983), S. 69-72 
    Details
    ISSN: 1432-1041
    Keywords: levodopa ; intestinal absorption ; small intestine ; bioavailability ; benserazide ; presystemic clearance
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary In four healthy subjects the intestinal absorption of levodopa (l-dopa) was investigated by measuring the plasma concentration of the amino acid following the administration of l-dopa at three different sites in the small intestine. In order to minimize presystemic clearance of l-dopa, the subjects were pretreated with the peripheral decarboxylase inhibitor benserazide 3×50 mg every 8 h on the previous day and 1×50 mg 2 h prior to administration of the l-dopa. L-dopa 100 mg dissolved in 0.05 N HCl and 50 mg benserazide dissolved in 0.05 N HCl were coadministered. Under these conditions no difference in tmax, cmax or AUC of l-dopa was observed between administration of the drug into the proximal or the distal part of duodenum, or into the upper part of jejunum. The results indicate that in healthy subjects, during inhibition of peripheral decarboxylase, the rate and extent of l-dopa absorption does not differ at any site in the upper small intestine.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00544017
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  • 5
    Electronic Resource
    Electronic Resource
    Non-linear elimination processes of theophylline (1983)
    Springer
    European journal of clinical pharmacology 24 (1983), S. 71-78 
    Details
    ISSN: 1432-1041
    Keywords: nonlinear kinetics ; theophylline ; dimethyluric acid ; theophylline metabolism ; 1-methyluric acid ; 3-methylxanthine ; renal clearance
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary After intravenous and oral administration of theophylline to four healthy subjects, the plasma concentration-time curve of theophylline could be described by linear pharmacokinetics, although total clearance in all subjects decreased when the dose was increased; the doses were theophylline 193.2 mg and 386.4 mg i.v. and 161 mg and 322 mg p.o. Total clearance was 65.5±11.3 ml/min. Renal clearance changed from 15.2±9.5 ml/min in the first two hours after administration to 4.9±5.5 ml/min between 16 and 24 h (p〈0.001). 1,3-dimethyluric acid (DMU), the major metabolite of theophylline, was determined in urine and in plasma. The renal clearance of DMU was constant at 496.7±180 ml/min. There was some evidence that at high plasma concentrations of theophylline the formation of DMU might be a zero-order process. The renal excretion rate of 1-methyluric acid (1-MU) paralleled that of DMU, which is in accordance with the assumption that DMU is demethylated to 1-MU. 3-methylxanthine (3-MX) was excreted in urine at a constant rate over 10 h, the rate being equivalent to the dose, which is contrary to the assumption of Michaelis-Menten-kinetics. 3-methyluric acid was found to be a minor metabolite of theophylline and 1-methylxanthine (1-MX) could not be detected. The cumulative amounts excreted in urine, expressed as a percentage of the dose and corrected for molecular weight, were theophylline 16.6±6.5%, DMU 44.3±7.0%, 1-MU 24.3±4.8%, 3-MX 12.9±3.4% and 3-MU 2.2±1.8%.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00613930
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  • 6
    Electronic Resource
    Electronic Resource
    Die intraindividuelle Streuung der fibrinolytischen Aktivität bei Probanden (1978)
    Springer
    Journal of molecular medicine 56 (1978), S. 445-448 
    Details
    ISSN: 1432-1440
    Keywords: Fibrinolysis ; Circadian rhythms ; Clinical trial ; Euglobulinlysis-time ; Fibrinolyse ; circadiane Rhythmik ; klinische Prüfung ; Euglobulinlyse-Zeit
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Description / Table of Contents: Zusammenfassung Bei 5 Probanden wurde über einen Zeitraum von 6 Wochen fünfmal die Anstiegsphase im Tagesrhythmus der fibrinolytischen Aktivität untersucht. Als Parameter wurden die Euglobulinlyse-Zeit und die Papierfibrinolyse, die Plasmaproteine, Fibrinogen, Plasminogen, α1-Antitrypsin und α2-Makroglobulin sowie die Thrombinocoagulase-Zeit und die Fibrinspaltprodukte erfaßt. Es zeigte sich bei allen Probanden der Anstieg der Fibrinolyse am Vormittag. Die Schwankungsbreite der fibrinolytischen Aktivität ist intraindividuell kleiner als bei einem interindividuellen Vergleich. Weiterhin zeigt sie mittags eine geringere Streuung als vormittags. Bei Untersuchungen zur klinischen Prüfung eines Soforteffektes von Arzneimitteln auf die Fibrinolyse sollte der Zeitraum der Plateauphase der fibrinolytischen Aktivität gewählt werden, um die Streuung der Ausgangswerte möglichst gering zu halten. Weiterhin ist die intraindividuelle Streuung der fibrinolytischen Aktivität in diesem Zeitraum geringer als während der Anstiegsphase im Rahmen des circadianen Rhythmus der Fibrinolyse. Eine intraindividuelle Kontrolle muß gewährleistet werden.
    Notes: Summary In five volunteers fibrinolytic activity has been measured five times over a period of six weeks during increasing values of circadian rhythm. Euglobulinlysis-time, paper fibrinolysis, fibrinogen, plasminogen, α1-antitrypsin, α2-makroglobulin, thrombinocoagulase-time and fibrin-split-products were used in one study. An increase of fibrinolytic activity in the mooning was observed in all volunteers. Intraindividual variation of values is considerable but less than variation of values compared interindividually. Moreover variation was smaller at noon than in the time before noon. In clinical trial of the short-time effect of drugs the period of the plateau of the fibrinolytic activity should be used because of its smaller variation of values. Furthermore, in this period the intraindividual variation of the fibrinolytic activity is smaller than during increasing slope of the circadian rhythm of fibrinolysis. Intraindividual control should be granted.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01477058
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