Zusammenfassung
Der ADP-Rezeptor (P2Y12)-Antagonist Clopidogrel hat
sich in der Therapie des akuten Koronarsyndroms sowie nach koronarer
Stent-Implantation zur dualen Thrombozytenaggregationshemmung neben
Aspirin bewährt. Vor allem aufgrund der Metabolisierung
in die aktive Form sowie seines irreversiblen Effektes hat Clopidogrel
allerdings Nachteile, die seine Effektivität in der Reduktion
klinischer Ereignisse beeinflussen könnten. Zwei Neuentwicklungen
zur Thrombozytenaggregationshemmung bei akutem Koronarsyndrom könnten
anwendungsrelevant werden. Der irreversible ADP-Rezeptor-Antagonist
Prasugrel führt zu einer stärkeren Thrombozytenaggregationshemmung
als Clopidogrel und zeigte in der TRITON-Studie weniger ischämische,
aber mehr Blutungskomplikationen. Der ohne Metabolisierung wirksame,
reversible ADP-Rezeptorantagonist Ticagrelor ist ebenfalls potenter
als Clopidogrel in der Thrombozytenaggregationshemmung. Ticagrelor
zeigte in der PLATO-Studie eine Reduktion ischämischer
Ereignisse bei insgesamt nicht mehr schweren Blutungskomplikationen
im Vergleich zu Clopidogrel, und führte außerdem
zu einer Reduktion der Gesamtmortalität. Diese Übersichtsarbeit
stellt bisherige Daten zu den neuen Substanzen zusammen und leitet
mögliche Konsequenzen für die klinische Praxis
ab.
Abstract
Use of the ADP (P2Y12)-receptor antagonist clopidogrel
is a cornerstone of dual platelet inhibition in acute coronary syndromes
and following stent implantation. Because of the metabolization
into its active form and the irreversible inhibition of the ADP
receptor there are disadvantages to clopidogrel which could limit
its efficacy in reducing clinical events. This is particularly problematic
in so-called poor responders with reduced metabolizing activity
and hence reduced platelet inhibition. Two novel drugs for platelet inhibition
in acute coronary syndrome could become relevant in clinical practice.
The irreversible ADP-receptor antagonist prasugrel led to stronger
platelet inhibition, fewer ischemic events but more bleeding complications
compared to clopidogrel in the TRITON-TIMI-38 trial. The reversibly
binding, direct-acting ADP-receptor antagonist ticagrelor, which
is effective without metabolization, is also superior over clopidogrel
in reducing platelet aggregation and decreased the number of ischemic events
in the PLATO-trial. However, it did not increase the rate of overall
major bleeding and was shown to reduce total mortality. This review
article summarizes current data on novel platelet inhibitors and
delineates their potential influence on clinical practice.
Schlüsselwörter
Thrombozytenaggregationshemmung - akutes Koronarsyndrom - perkutane Koronarintervention
(PCI) - Ticagrelor - Prasugrel - Clopidogrel - Myokardinfarkt - Stentthrombose
Keywords
platelet inhibition - acute coronary syndrome - PCI - ticagrelor - prasugrel - clopidogrel
- myocardial infarction - stent thrombosis
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Dr. Dr. med. Stephan H. Schirmer
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Universitätsklinikum
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