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  • 11
    Electronic Resource
    Electronic Resource
    Plasma concentrations and haemodynamic effects of nitroglycerin during and after intravenous infusion in healthy volunteers (1982)
    Springer
    European journal of clinical pharmacology 23 (1982), S. 99-106 
    Details
    ISSN: 1432-1041
    Keywords: nitroglycerin ; i.v. infusion ; plasma level ; haemodynamic effects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The effects of nitroglycerin, infused intravenously at 3.4 and 7.5 µg/min over 30 min, on haemodynamic parameters were determined in the morning and the afternoon in a randomized, placebo-controlled study in 5 healthy volunteers. The mean steady-state concentrations of nitroglycerin reached in the plasma during the infusions of 3.4 and 7.5 µg/min were 0.35±0.06 ng/ml and 0.64±0.22 ng/ml, respectively. Wide inter-individual variation was noted. The nitroglycerin-induced increase in the orthostatic rise in heart rate and the change in digital-pulse-wave morphology roughly paralleled the plasma concentration, whereas the reduction in systolic blood pressure in the upright position was still evident 15 mins after the infusion, i.e. when nitroglycerin was no longer measurable in plasma. No significant diurnal variation in vascular sensitivity to the vasodilative action of nitroglycerin was demonstrable. The change in pulse-wave morphology resulting from the reduction in peripheral resistance (shift of the dicrotic wave in the descending limb towards the base-line) proved to be the most sensitive haemodynamic parameter.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00545962
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  • 12
    Electronic Resource
    Electronic Resource
    Studies of the bioavailability of nitroglycerin from a transdermal therapeutic system (Nitroderm TTS) (1984)
    Springer
    European journal of clinical pharmacology 27 (1984), S. 7-12 
    Details
    ISSN: 1432-1041
    Keywords: nitroglycerin ; plasma concentration ; transdermal administration ; bioavailability ; pharmacodynamics ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary In 6 healthy volunteers, intravenous infusions of nitroglycerin 4.8 and 10.6 µg/min yielded mean steady-state plasma concentrations of 0.5±0.02 and 0.82±0.04 ng/ml as determined by a gas chromatographic/mass spectrometric method. The plasma concentrations reached in the same subjects 17 h after application of Nitroderm TTS 5 and 10 with in vivo release rates of 3.7 and 5.7 µg/min were 0.28±0.01 and 0.37±0.01 ng/ml, respectively. Thus, 75% of the quantity of nitroglycerin released by the systems passed into the circulation. The inter-individual and intra-individual variations in plasma concentrations were similar for both modes of administration. The nitroglycerin-induced morphological changes in the fingerpulse wave were clearly dose-dependent, but it seems that this pharmacodynamic parameter is determined less by the plasma concentration than by the nitroglycerin content of the vascular wall.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF02395198
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  • 13
    Electronic Resource
    Electronic Resource
    Effects of α- and β-receptor blockade on systolic time intervals (1974)
    Springer
    European journal of clinical pharmacology 7 (1974), S. 1-10 
    Details
    ISSN: 1432-1041
    Keywords: α- and β-blockade ; systolic time intervals ; oxprenolol ; phentolamine ; man
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The effects of single oral doses of oxprenolol (20 and 80 mg), phentolamine (20 and 40 mg), and combinations of oxprenolol and phentolamine (80:20 and 20:40 mg, respectively) on blood pressure, heart rate and the systolic time intervals (Q—S2c, PEPc, LVETc and PEP/LVET) have been studied under double-blind conditions in seven healthy volunteers during recumbency and passive tilting. Heart rate was slowed by oxprenolol and slightly increased by phentolamine, but was not affected by either of the combinations. There were only minimal non-significant changes in blood pressure in the subjects, all of whom were normotensive. Of the systolic time intervals, PEPc was most affected: it was prolonged by oxprenolol because of reduction in myocardial contractility, and shortened by phentolamine as a result of the cardiostimulant effect of this compound. When the two drugs were administered in combination, the negative inotropic effects of the β-blocker always predominated. The changes induced by the drugs were more pronounced during upright titling than in the recumbent position. Measurement of PEPc provides a suitable means of assessing the influence of cardiovascular drugs on left ventricular function in pharmacological studies in man.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00614383
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  • 14
    Electronic Resource
    Electronic Resource
    Experience with a new beta-receptor blocking agent (Trasicor®) in the management of cardiac arrhythmias (1969)
    Springer
    European journal of clinical pharmacology 1 (1969), S. 123-130 
    Details
    ISSN: 1432-1041
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Twenty-six Swiss physicians took part in a study in which the effects of an orally administered new beta-receptor blocking agent, Trasicor®, were assessed in out-patients with disturbances of cardiac rhythm. Ninety-eight patients were treated for 3 weeks with daily doses ranging from 20 to 120 mg, the most commonly employed daily dose being 60 mg. The patients were examined before treatment and again after 1, 3, 7, 14 and 21 days of treatment. The compound proved highly effective in decreasing heart rate in sinus tachycardia and ventricular rate in chronic auricular fibrillation, both at rest and during effort. Trasicor also abolished, or substantially reduced, the frequency of attacks of paroxysmal supraventricular tachycardia and ventricular ectopic beats. — In hypertensive patients, Trasicor elicited a statistically significant decrease in both the systolic and diastolic blood pressures, whereas in normotensives only the systolic blood pressure was affected to a statistically significant extent. - Side effects were usually mild and transient; treatment had to be withdrawn in only a small percentage of patients.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00404658
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  • 15
    Electronic Resource
    Electronic Resource
    Studies of the bioavailability of nitroglycerin from a transdermal therapeutic system (Nitroderm TTS) (1984)
    Springer
    European journal of clinical pharmacology 27 (1984), S. 7-12 
    Details
    ISSN: 1432-1041
    Keywords: nitroglycerin ; plasma concentration ; transdermal administration ; bioavailability ; pharmacodynamics ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary In 6 healthy volunteers, intravenous infusions of nitroglycerin 4.8 and 10.6 µg/min yielded mean steady-state plasma concentrations of 0.5±0.02 and 0.82±0.04 ng/ml as determined by a gas chromatographic/mass spectrometric method. The plasma concentrations reached in the same subjects 17 h after application of Nitroderm TTS 5 and 10 with in vivo release rates of 3.7 and 5.7 µg/min were 0.28±0.01 and 0.37±0.01 ng/ml, respectively. Thus, 75% of the quantity of nitroglycerin released by the systems passed into the circulation. The inter-individual and intra-individual variations in plasma concentrations were similar for both modes of administration. The nitroglycerin-induced morphological changes in the fingerpulse wave were clearly dose-dependent, but it seems that this pharmacodynamic parameter is determined less by the plasma concentration than by the nitroglycerin content of the vascular wall.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00553146
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  • 16
    Electronic Resource
    Electronic Resource
    Inhibition of adrenaline-induced platelet aggregation by the orally administered α-adrenergic receptor blocker phentolamine (regitine®) (1977)
    Springer
    European journal of clinical pharmacology 11 (1977), S. 7-10 
    Details
    ISSN: 1432-1041
    Keywords: Platelets ; phentolamine ; aggregation ; adrenaline
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary In eight healthy volunteers pretreatment with phentolamine 40 mg p o inhibited platelet aggregation (1st and 2nd phases) induced by low concentrations of adrenaline (2, 1 and 0.5 µM) in plasma from blood sampled 30 min after administration of the compound. The lower the concentration of adrenaline used, the greater was the degree of inhibition elicited. These results are indicative of competitive inhibition of the action of adrenaline on the platelet membrane by phentolamine. Four to six hours after administration of the compound, the aggregation characteristics had reverted to normal. It is concluded that the increased tendency toward platelet aggregation associated with elevated blood levels of catecholamines can be prevented by therapeutic doses of phentolamine.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00561780
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  • 17
    Electronic Resource
    Electronic Resource
    Human pharmacological studies of a new transdermal system containing nitroglycerin (1982)
    Springer
    European journal of clinical pharmacology 22 (1982), S. 473-480 
    Details
    ISSN: 1432-1041
    Keywords: nitroglycerin ; transdermal system ; transdermal absorption ; plasma concentration ; haemodynamic effects ; tolerability ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary A new transdermal therapeutic system (TTS) for the administration of nitroglycerin (NTG) was tested in human pharmacological studies in 26 healthy volunteers. Plasma concentrations and haemodynamic responses were determined after the application of the system in different dosages. The concentrations of NTG reached in the plasma were uniform and dose-related, i.e. dependent on the drug-release area, and showed only minor inter-individual variation. They remained almost constant as long as the system was in contact with the skin. Renewal of the system caused no appreciable change in the plasma concentration. The haemodynamic effects, like those of all nitrates, were not clearly related to the dose administered, and were not always dependent on the plasma concentration. Upon repeated application, NTG-TTS was well tolerated locally and systemically and led to no alteration in blood chemistry or haematological parameters. The typical nitrate headaches disappeared after a few days. The presence of the system on the skin caused no discomfort or inconvenience.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00609617
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  • 18
    Electronic Resource
    Electronic Resource
    Antihypertensive therapy with adrenergic beta-receptor blockers and vasodilators (1972)
    Springer
    European journal of clinical pharmacology 4 (1972), S. 177-181 
    Details
    ISSN: 1432-1041
    Keywords: Hypertension ; treatment with Nepresol ; Trasicor and combination of both
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary In a single-blind trial the antihypertensive effects of Nepresol, Nepresol and Trasicor and Trasicor alone were tested in 18 patients with mild to moderate hypertension. After a control period of 2 weeks during which a placebo was administered, each active compound was given for 3 weeks. Two patients failed to complete the trial and three of the remaining 16 did not respond satisfactorily to any of the treatments. The other 13 patients showed statistically significant reductions in systolic and diastolic blood pressures (systolic 8.6–13.2%; diastolic 7.4–8.2%) in response to each of the three treatments. Trasicor counteracted the increase in heart rate caused by Nepresol without impairing its hypotensive effect; the reduction in blood pressure was slightly greater, although not by a statistically significant amount. — The side-effects observed during treatment with Nepresol appeared to be less marked when the two drugs were given in combination. Doses of 75 mg Nepresol and 120 mg Trasicor, either alone or in combination, only produced an adequate response in two patients with mild hypertension. In all other patients the dose had to be doubled. — This study confirms the therapeutic usefulness of a combination of vasodilators and β-receptor blockers in the treatment of hypertension.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00561142
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  • 19
    Electronic Resource
    Electronic Resource
    Über die Eliminierungsgeschwindigkeit von Glutethimid (Doriden®) und die Natur der Ausscheidungsprodukte beim Menschen (1962)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 244 (1962), S. 97-108 
    Details
    ISSN: 1432-1912
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Zusammenfassung Mit Hilfe der radioaktiven Markierung wurde das Stoffwechselverhalten von Doriden beim Menschen aufgeklärt. Doriden wird rasch resorbiert und praktisch quantitativ in Form von wasserlöslichen, pharmakologisch unwirksamen Glucuroniden in kurzer Zeit im Harn ausgeschieden. Die Glucuronide sind identisch mit denjenigen aus Hundeversuchen, bei welchen die chemische Struktur sowie die pharmakologischen Eigenschaften dieser Doriden-Derivate nach Isolierung untersucht worden waren. Die Bestimmung der biologischen Halbwertszeit bezüglich der Inaktivierung des Wirkstoffes ergab 10 Std, in bezug auf die renale Ausscheidung der Metaboliten 16 Std. Der erste Wert wurde als effektive, der zweite als maximale Halbwertszeit definiert.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00246121
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