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  • Articles: DFG German National Licenses  (7)
  • 1995-1999  (7)
  • PTCA  (3)
  • Morphine-3-O-β-D-Glucuronide  (2)
  • thrombolytic therapy  (2)
  • Picea abies
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  • Articles: DFG German National Licenses  (7)
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Year
  • 1
    ISSN: 1432-1912
    Keywords: µ-, δ-, κ-Opioid-Receptor ; Morphine ; Morphine-3-O-β-D-Glucuronide ; Morphine-6-O-β-D-Glucuronide ; Cerebral membranes ; In-vitro-binding
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract We investigated the nature of interaction of morphine-3-O-β-D-glucuronide (M3G) and morphine6-O-β-D-glucuronide (M6G) with opioid binding sites at the µ-, δ- and κ-opioid receptors (µ-OR, δ-OR and κ-OR) in cerebral membranes. Saturation binding experiments revealed a competitive interaction of M6G with all three opioid receptors. Inhibition binding experiments at the µ-OR employing combinations of morphine and M6G resulted in a rightward shift of the IC50 for morphine proportional to the M6G concentration, thus strengthening the finding of competitive interaction of M6G at the µ-opioid binding site. Data in absence and presence of M6G were included in a three-dimensional model. Compared to a model with one binding site a model with two binding sites significantly improved the fits. This might indicate that different µ-OR subtypes are involved. Hydrolysis of M6G to morphine was investigated and did not occur. Therefore the effects of M6G on binding to the μ-OR were due to M6G and not due to morphine. In contrast, M3G at the three opioid receptors was found to inhibit binding being about 300 times weaker than morphine. This effect was well explained by the amount of contaminating morphine (about 0.3%) identified by HPLC. We conclude that M6G binds to µ-, δ- and κ-OR in a competitive manner. Some of our results on the µ-OR suggest two binding sites for agonists at the μ-OR and that M6G binds to both sites. Our results suggest that the high potency of M6G as an analgesic is mediated through opioid receptors. In contrast, M3G does not interact with the µ-, δ- or κ-OR. We therefore doubt that any effect of M3G is mediated via opioid receptors.
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    Springer
    Der Internist 39 (1998), S. 713-719 
    ISSN: 1432-1289
    Keywords: Schlüsselwörter Koronarreserve ; Myokardinfarkt ; Therapie ; PTCA ; Koronare Herzkrankheit ; Diagnostik ; Hibernation ; Stunned Myokardium
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Zum Thema Ein bei Belastung zunehmender Sauerstoffbedarf des Myokards kann im wesentlichen nur durch eine Steigerung der Koronardurchblutung gedeckt werden. Dies geschieht zu ca. 90% durch Dilatation der arteriolären Widerstandsgefäße und nur zu ca. 10% durch Dilatation der epikardialen Koronargefäße, die angiographisch sichtbar gemacht werden können. Die Differenz zwischen Ruhe- und maximal möglichem Blutfluß wird als Koronarreserve bezeichnet. Die Messung des koronaren Blutflusses, der Perfusion, des myokardialen Stoffwechsels sowie der Auswirkung auf die Myokardfunktion erfolgt durch verschiedenste Verfahren: Thallium-Szintigraphie, Positionen-Emissions-Tomographie, Magnetresonanztomographie, Clearance-Methoden, Doppler- und Kontrastechokardiographie, intrakoronare Doppleruntersuchungen u.s.w. Die mittels Koronarangiographie mögliche morphologische Beschreibung und Quantifizierung von Stenosedurchmessern ist hierzu nicht die Methode der Wahl. Die Ergebnisse dieser Untersuchungen bei verschiedenen koronarbedingten Erkrankungen und die Evaluierung von Therapiestrategien stehen im Mittelpunkt dieser Arbeit.
    Type of Medium: Electronic Resource
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  • 3
    ISSN: 1432-1912
    Keywords: Key words μ- ; δ- ; κ-Opioid-Receptor ; Morphine ; Morphine-3-O-β-D-Glucuronide ; Morphine-6-O-β-D-Glucuronide ; Cerebral membranes ; In-vitro-binding
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract  We investigated the nature of interaction of morphine-3-O-β-D-glucuronide (M3G) and morphine-6-O-β-D-glucuronide (M6G) with opioid binding sites at the μ-, δ- and κ-opioid receptors (μ-OR, δ-OR and κ-OR) in cerebral membranes. Saturation binding experiments revealed a competitive interaction of M6G with all three opioid receptors. Inhibition binding experiments at the μ-OR employing combinations of morphine and M6G resulted in a rightward shift of the IC50 for morphine proportional to the M6G concentration, thus strengthening the finding of competitive interaction of M6G at the μ-opioid binding site. Data in absence and presence of M6G were included in a three-dimensional model. Compared to a model with one binding site a model with two binding sites significantly improved the fits. This might indicate that different μ-OR subtypes are involved. Hydrolysis of M6G to morphine was investigated and did not occur. Therefore the effects of M6G on binding to the μ-OR were due to M6G and not due to morphine. In contrast, M3G at the three opioid receptors was found to inhibit binding being about 300 times weaker than morphine. This effect was well explained by the amount of contaminating morphine (about 0.3%) identified by HPLC. We conclude that M6G binds to μ-, δ- and κ-OR in a competitive manner. Some of our results on the μ-OR suggest two binding sites for agonists at the μ-OR and that M6G binds to both sites. Our results suggest that the high potency of M6G as an analgesic is mediated through opioid receptors. In contrast, M3G does not interact with the μ-, δ- or κ-OR. We therefore doubt that any effect of M3G is mediated via opioid receptors.
    Type of Medium: Electronic Resource
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  • 4
    Electronic Resource
    Electronic Resource
    Springer
    Der Internist 38 (1997), S. 1179-1190 
    ISSN: 1432-1289
    Keywords: Schlüsselwörter Koronare Herzkrankheit ; Therapie ; Koronare Herzkrankheit ; PTCA ; Koronare Herzkrankheit ; interventionelle Therapie ; Stents ; PTCA ; Myokardinfarkt ; Therapie
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Zum Thema In der Behandlung des akuten Myokardinfarkts ist die PTCA fest etabliert. Bezüglich der koronaren Herzkrankheit konkurriert die PTCA allerdings besonders in Hinblick auf die Prognose des Leidens mit der medikamentösen Therapie und der aortokoronaren Bypassoperation. Welche Behandlungsstrategien und welche Indikationsstellungen im Einzelfall favorisiert werden können oder auch nicht, haben zahlreiche Studien in den letzten Jahren gesichert. Über das technische Vorgehen bei PTCA, Ergebnisse, Management und Restenosen nach PTCA sowie über den Vergleich der verschiedenen Therapieformen wird hier eingehend berichtet. Breiten Raum nimmt die Darstellung von Indikationen und Kontraindikationen und schließlich die interventionelle Behandlung des akuten Myokardinfarkts ein. Die bemerkenswerten Methoden der Stentimplantation zur Prävention von Reokklusionen einschließlich der technischen Weiterentwicklung von Stents sind faszinierend und für die erfolgreiche Senkung von Morbidität und Mortalität der koronaren Herzkrankheit und ihrer Komplikationen von hoher Bedeutung.
    Type of Medium: Electronic Resource
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  • 5
    ISSN: 1573-742X
    Keywords: thrombolytic therapy ; saruplase ; myocardial infarction
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Saruplase (unglycosylated human-type high molecular weight single-chain urokinase-type plasminogen activator) was given to 1698 patients in the open-label Practical Applicability of Saruplase Study (PASS), which assessed the safety and efficacy of saruplase in the treatment of acute myocardial infarction. Thirty-seven hospitals in Europe participated in the study. All patients received 20 mg saruplase as a bolus followed by an infusion of 60 mg saruplase over 1 hour. Prior to the infusion of saruplase, 62% of the patients received a bolus of 5000 U of heparin, and after saruplase a 24-hour intravenous infusion of heparin was given to 95% of patients. The mean age of the patients was 59 years and 80.1% were male. The median delay from the onset of chest pain to the start of saruplase infusion was 145 minutes. Acute angiography was performed in 8 of the participating 37 centers in 350 patients (20.6%), on average 85 minutes (median) after the start of the saruplase infusion. TIMI 3 flow was obtained in 186 patients (53.1%) and TIMI 2 flow in 61 patients (17.4%). Patency rates were similar for patients with anterior and inferior infarction. ECG signs suggestive of reperfusion were seen in 63% of the patients. In-hospital mortality was low (92 patients; 5.4%), and nonfatal recurrent myocardial infarction was seen in 60 patients (3.5%). Severe bleeding complications occurred in 92 patients (5.4%), 21 of whom (1.2%) needed a blood transfusion. An intracerebral hemorrhage was observed in eight patients (0.5%), and seven patients (0.4%) suffered from a thromboembolic stroke. At discharge 85.9% of the patients were in NYHA functional class I. One-year mortality was low (142 patients; 8.4%). Mortality was high in patients with TIMI 0 or 1 flow at the acute angiography who did not undergo rescue PTCA (9/39; 23.1%), lower in patients with TIMI 0 or 1 flow followed by successful rescue PTCA (7/64; 10.9%), and low in patients with TIMI 2 flow (1/61; 1.6%) or with TIMI 3 flow (2/186; 1.1%). Patency rates and (bleeding) complications did not differ between patients with a body weight greater than or less than 70 kilograms. No antibodies against saruplase were detected in samples from 455 patients. In conclusion, it can be stated that saruplase, given in combination with aspirin and intravenous heparin, can be given safely and effectively to patients with acute myocardial infarction.
    Type of Medium: Electronic Resource
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  • 6
    ISSN: 1573-742X
    Keywords: thrombolytic therapy ; acute myocardial infarction ; patency
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract To study the safety and efficacy of the thrombolytic agent saruplase as a bolus, the angiographic and clinical outcomes of three bolus regimens were investigated in a pilot study conducted in 192 patients with an acute myocardial infarction and were compared with the standard regimen. Fifty-two patients received a double bolus of 40 mg and 40 mg after 30 minutes, 51 patients a bolus of 80 mg, and 36 patients a bolus of 60 mg. Fifty-three patients received the standard regimen (a bolus of 20 mg and 60 mg IV infusion over 1 hour). At 60 minutes TIMI 2 and 3 flow were, respectively, 9.6% and 61.5% with the 40/40-mg bolus, 15.7% and 51.0% with the 80-mg bolus, 16.7% and 30.6% with the 60-mg bolus, and 7.5% and 54.7% with the standard 20/60-mg infusion. At 90 minutes TIMI 2 and 3 flow improved to 9.6% and 73.1%, 15.7% and 56.9%, 13.9% and 36.1%, and 5.7% and 71.7%, respectively. The primary endpoint, persistent patency (TIMI 2 + 3) at 24–45 hours, was seen in 69.2%, 64.7%, 44.4%, and 67.9% of patients who had no rescue PTCA, respectively. Inclusion in the 60-mg bolus group was prematurely stopped because of their low patency rates. The 40/40-mg bolus group had the highest mortality rate (13.5%), whereas the 60-mg bolus group had no deaths. Other adverse event rates were similar in the four groups. This clinical outcome is highly influenced by rescue PTCA of patients with insufficient TIMI flow. This pilot study indicates that in patients with an acute myocardial infarction, a double bolus of 40/40 mg resulted in the highest patency but also had the highest complication rate. The 80-mg single bolus is an attractive alternative for further evaluation because of its acceptable patency and event profile, and its easy form of administration.
    Type of Medium: Electronic Resource
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  • 7
    Electronic Resource
    Electronic Resource
    Springer
    Intensivmedizin und Notfallmedizin 34 (1997), S. 266-270 
    ISSN: 1435-1420
    Keywords: Key words Coronary intervention ; PTCA ; acute myocardial infarction ; stent-implantation ; rescue-PTCA ; direct-PTCA ; primary PTCA ; Schlüsselwörter Koronarintervention ; PTCA ; akuter Myokard-infarkt ; Stent-Implantation ; Rescue-PTCA ; direkte PTCA ; primäre PTCA
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Description / Table of Contents: Zusammenfassung Während die intravenöse Thrombolysetherapie weiterhin als Goldstandard der Reperfusionsbehandlung des akuten Myokardinfarktes gilt, sind in den vergangenen Jahren auch zunehmend mechanische Reperfusionsstrategien untersucht worden. Zunächst wurde das Konzept der routinemäßigen Sofort-PTCA nach Thrombolysebehandlung untersucht, das wegen einer höheren Komplikationsrate im Vergleich zur alleinigen Thrombolysetherapie jedoch keine Verbreitung fand. Beim Konzept der Rescue-PTCA erfolgt eine mechanische Rekanalisation und Dilatation nur im Falle eines dokumentierten persistierenden Gefäßverschlusses nach Thrombolysetherapie. Für dieses Konzept konnte eine verbesserte Überlebensrate und Ventrikelfunktion belegt werden. Das zuletzt untersuchte Konzept der primären PTCA, bei dem die PTCA ohne vorhergehende thrombolytische Therapie routinemäßig durchgeführt wird, zeigte im Vergleich zur Thrombolysetherapie eine signifikant geringere Letalität, Reinfarktrate und Inzidenz zerebraler Insulte. Der erhebliche logistische Aufwand steht jedoch einer weiteren Verbreitung dieser Therapieform entgegen. Gegenwärtig sollten daher mechanische Reperfusionsmaßnahmen, insbesondere bei den Patienten mit akutem Myokardinfarkt erwogen werden, bei denen eine thrombolytische Therapie kontraindiziert ist, ein kardiogener Schock vorliegt oder ein anderes Krankheitsbild differentialdiagnostisch abgegrenzt werden muß. Gegebenenfalls sollte auch bei älteren Patienten (〉75 Jahre) von einer Thrombolysebehandlung zugunsten mechanischer Reperfusionsmaßnahmen Abstand genommen werden. Nach erfolgter Thrombolysetherapie sollte bei fehlenden Reperfusionszeichen eine Herzkatheteruntersuchung und im Falle eines persistierenden Gefäßverschlusses eine mechanische Rekanalisation im Sinne der Rescue-PTCA angestrebt werden.
    Notes: Summary Although thrombolysis remains the gold standard in the treatment of acute myocardial infarction, mechanical reperfusion strategies have been introduced into the clinical routine within recent years. The concept of a routinely performed immediate PTCA following thrombolysis was combined with a higher complication rate compared to thrombolysis alone and was therefore abandoned. The concept of rescue-PTCA, where PTCA is performed only in case of persistent occlusion of the infarct-related artery, led to a better left ventricular function and higher survival rate. The relatively new concept of primary PTCA, which is performed routinely without preceding thrombolysis, revealed a significantly lower mortality, reinfarction rate and incidence of cerebral bleedings compared to thrombolysis. Currently, the following strategy for patients with acute myocardial infarction is recommended. In patients with cardiogenic shock, contraindications to thrombolysis, an unclear diagnosis or advanced age (more than 75 years) mechanical reperfusion should be the preferred strategy. In case of persistent or recurrent ischemia, electrical or hemodynamic instability following thrombolysis, coronary angiography and, in case of need, rescue-PTCA should be performed.
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