Basic mechanisms and classification of calcium entry blockers

  • T. Godfraind
Part of the Developments in Cardiovascular Medicine book series (DICM, volume 40)


Calcium antagonists may exert the following actions at the level of the cell membrane:
  1. 1.

    they may interfere with specific Ca2+ channels e.g. the slow Ca2+ channels of the heart, voltage-operated or receptor-operated channels in smooth muscles;

  2. 2.

    they may diminish intracellular Ca2+ entry by blocking the continuous leakage of the cell membrane;

  3. 3.

    they might restore or improve Ca2+ extrusion via the Na-Ca exchange pump or the Ca-ATP pump. Calcium antagonists may exert additional actions, related or not to calcium metabolism or to calcium function. Calcium entry blockers do specifically act on membrane Ca channels operated by depolarization or by receptors.



Calcium Antagonist Entry Blocker Calcium Modulator Calcium Entry Blocker Elsevier Biomedical 
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Les antagonistes du calcium peuvent exercer les actions suivantes au niveau de la membrane cellulaire:
  1. 1.

    IIs peuvent interférer avec les canaux spécifiques de Ca2+, par exemple les lents canaux de Ca2+ du coeur, les canaux activés par voltage ou par récepteur dans les muscles lisses.

  2. 2.

    IIs peuvent diminuer l’entrée de Ca2+ dans la cellule en bloquant l’infiltration s’effectuant par la membrane cellulaire.

  3. 3.

    IIs pourraient restaurer ou améliorer l’expulsion du Ca2+ via la pompe à échange Na-Ca ou la pompe Ca-ATP.


Les antagonistes du calcium peuvent exercer d’autres actions, reliées ou non au métabolisme du calcium ou à la fonction du calcium. Les agents bloqueurs de l’entrée de calcium agissent spécifiquement sur les canaux de calcium de la membrane activés par dépolarisation ou par des récepteurs.


Los antagonistes de calcio pueden ejercer las acciones siguientes a nivel de la membrana celular:
  1. 1.

    pueden interferir con canales Ca2+ específicos p.ej. los canales Ca2+ “lentos” del corazón, los canales accionados por voltaje o por receptores en músculos lisos;

  2. 2.

    pueden disminuir la entrada intracelular de Ca2+ bloqueando la gota continua de la membrana celular;

  3. 3.

    podrían restablecer o mejorar la extrusión de Ca2+ via la bomba de cambio Na-Ca o la bomba Ca-ATP.


Los antagonistas de calcio pueden ejercer acciones adicionales, relacionadas o no con el metabolismo cálcico o con la función cálcica. Los inhibidores de la entrada de Ca2+ actüúan específicamente en canales membranosos de Ca2+, accionados por depolarización o por receptores.


Kalzium-Einstromhemmer können an der Zellmembran die folgenden Wirkungen ausüben:
  1. 1.

    1. Beeinflussung spezifischer Ca2+-Kanäle, z.B. der langsamen Ca2+- Kanäle des Herzens, oder der potential- bzw. rezeptorabhängigen Kanäle glatter Muskeln;

  2. 2.

    2. Herabsetzung des intrazellulären Ca2+ -Einstroms durch Hemmung des kontinuierlichen Durchlasses durch die Zellmembran;

  3. 3.

    3. Wiederherstellung bzw. Verbesserung der Ca2+ -Ausfuhr über die Na-Ca-Austauschpumpe oder über die Ca-ATP-Pumpe.


Kalzium-Einstromhemmer können auch zusätzliche Wirkungen ausüben, die nicht unbedingt mit Calciummetabolismus oder Calciumfunktion zusammenhängen müssen. Sie wirken spezifisch auf Membran-Ca-Kanäle ein, die durch Depolarisierung oder Rezeptoren reguliert werden.


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© Martinus Nijhoff Publishers, The Hague 1984

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  • T. Godfraind

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