Calcium-Antagonisten, 1st Edition by Prof. Dr. med. Winifred G. Nayler (auth.)

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By Prof. Dr. med. Winifred G. Nayler (auth.)

Dieses Buch gibt einen hervorragenden Überblick über den Stand der wissenschaftlichen Forschungen auf dem Gebiet der Pharmakologie der Calcium-Antagonisten. Die Pharmakokinetik der verschiedenen Calcium-Antagonisten wird ebenso beschrieben, wie die Anwendung in der Praxis bei den verschiedensten Erkrankungen des Herz-Kreislauf-Systems. Nebenwirkungen, Risiken und Kontraindikationen sind ein weiteres wichtiges Thema. Zum Schluß wird ein Ausblick auf die Zukunft dieses vielseitigen Medikamentes gegeben.

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Extra resources for Calcium-Antagonisten, 1st Edition

Sample text

5) zu bezeichnen. L steht fUr "langdauernde groBe Kapazitat" und T fUr "voriibergehend" (transitorisch). N stand zu Anfang fUr "weder T noch L", heute bedeutet es aber "neural" (Spedding 1987). 2): a) ihre Aktivierungsschwelle (die Spannung, die zur Offnung der Kanale fUr den Ca2+-FluB erforderlich ist); b) die Empfindlichkeit gegeniiber Ca2+ - Antagonisten, sowohl anorganische als auch organische; c) ihre Fahigkeit, Ba2+ statt Ca2+ als Ladungstrager zu akzeptieren; d) ihre Ca2+ -Leitung; e) ihre Stabilitat in isolierten Partikeln; f) ihre Empfindlichkeit gegeniiber natiirlich vorkommenden Toxinen; g) der zeitliche Ablauf ihrer Aktivierung und Inaktivierung.

Zusatzlich, wie bereits erwahnt, wirken viele Dihydropyridine vorzugsweise auf die GefaBe (Kap. 8). Die wesentliche Struktur der Calcium-Antagonisten auf Dihydropyridin-Basis wird in Abb. 8 dargestellt. Die Substituenten bei X beeinflussen die Potenz der Verbindungen, die Substituenten bei R in der 3,5-Estergruppe des heterozyklischen Rings beeinflussen die vaskulare Selektivitat. Nifedipin ist z. B. ein starkerer Vasodilatator als Nicardipin (Abb. 9), doch dilatiert der letztgenannte, namlich 1,4-Dihydro-2,6-dimethyl-4-(m- nitrophenyl )pyridin-3 ,5dicarbonsaure-3-[2-(N-benzyl-N-methyl-amino) ]iithyl, 5-methylester selektiv die Koronar- und HimgefaBe.

12) und Niguldipin (Abb. 15). Zweifellos wird diese Liste noch langer werden, da man noch nach potenteren und langer wirkenden Medikamenten sucht. 58 Calcium-Antagonisten Hel Abb. 15 Strukturfonnel von Niguldipin, einem Nifedipin-Analogon. 3). Obwohl der Prototyp Nifedipin relativ gleich selektiv fUr Myokard und GefaBsystem ist, sind einige der kiirzlich entwickelten Analoga - darunter Nitrendipin, Nisoldipin, Felodipin und Amlodipin - selektiv fUr die GefaBe. Daneben sind viele dieser neueren Dihydropyridine langwirkende Verbindungen (Kap.

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