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Pharmakokinetische Bedeutung der Proteinbindung

Pharmaco-kinetic aspects of protein-binding

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Summary

Binding of drugs to plasma proteins will influence distribution and elimination especially if factors interfere altering the extent of binding. These factors are: dependence on species, age, H+-concentration, speed of i.v. injection or the interaction of another drug for instance. Considering the quantitative aspects changes in binding to the plasma proteins will turn only then relevant to drug action if the extent of alteration is very large or the drugs are bound to a very high degree. But the scene changes completely if the binding to other proteins of the organism is considered. Experimental results concerning the binding of drugs to hemoglobin and muscle tissue suggest that this kind of binding is possibly more effective in pharmacokinetics than binding to plasma proteins.

Zusammenfassung

Auswirkungen der Bindung von Arzneimitteln an Plasmaproteine auf die Pharmakokinetik sind vor allem dann zu erwarten, wenn Faktoren wirksam werden, die das Ausmaß der Bindung verändern. Wichtige Beispiele dafür sind die Artspezifität der Bindung, der Einfluß von Alter, der H+-Konzentration, der Injektionsgeschwindigkeit und der Wechselwirkung durch ein zweites gleichzeitig verabreichtes Arzneimittel. Quantitative Überlegungen zeigen jedoch, daß die Auswirkungen der Bindungsänderungen an Plasmaproteinen nur dann für die Wirkung relevant werden, wenn diese Änderungen sehr groß sind, oder die Arzneimittel in besonders hohem Maße an die Plasmaproteine gebunden werden. Dies gilt nicht, wenn eine Bindung von Arzneimitteln an andere Proteine im Organismus mit berücksichtigt wird. Untersuchungsergebnisse zur Bindung von Arzneimitteln an Hämoglobin und an Muskelgewebe weisen darauf hin, daß dieser Bindungsart u.U. eine gewichtigere Bedeutung zukommt als der Bindung an Plasmaproteine.

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Kurz, H. Pharmakokinetische Bedeutung der Proteinbindung. Klin Wochenschr 56, 1195–1204 (1978). https://doi.org/10.1007/BF01477075

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