Which medications in the drug class Adenosine diphosphate receptor antagonists are used in the treatment of Acute Coronary Syndrome?

Updated: Sep 30, 2020
  • Author: David L Coven, MD, PhD; Chief Editor: Eric H Yang, MD  more...
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Answer

Adenosine diphosphate receptor antagonists

Thienopyridine adenosine 5'-diphosphate (ADP) antagonists approved for antiplatelet activity in the United States include clopidogrel, ticlopidine, prasugrel, and ticagrelor. All but ticagrelor have irreversible antiplatelet activity and take several days to manifest an effect, whereas, ticagrelor is a reversible P2Y12 receptor inhibitor. A potential additive benefit exists when ADP antagonists are used in conjunction with aspirin. These drugs may be considered alternatives to aspirin in patients with aspirin intolerance or who are allergic to aspirin.

Clopidogrel (Plavix)

Clopidogrel (Plavix) inhibits ADP-dependent activation of the glycoprotein IIb/IIIa complex, a necessary step for platelet aggregation. This process results in intense inhibition of platelet function, particularly in combination with aspirin.

Clopidogrel can be considered an alternative to aspirin in patients with aspirin intolerance or who are allergic to aspirin. The CURRENT-OASIS 7 trial suggests that a 7-day double-dose clopidogrel regimen can be considered for patients with acute coronary syndromes, as the efficacy and safety did not differ from that of a high- and low-dose aspirin regimen. However, there is no benefit in the double-dose treatment for patients who are undergoing an early invasive strategy.

Clopidogrel is a class I recommendation for patients when an early noninterventional approach is planned in therapy. When percutaneous coronary intervention (PCI) is planned, clopidogrel is started and continued for at least 1 month and for up to 9 months, if the patient is not at high risk for bleeding.

Clopidogrel is generally preferred over ticlopidine (Ticlid), because it more rapidly inhibits platelets and appears to have a more favorable safety profile.

Clopidogrel has been suggested to be less effective in reducing the rate of cardiovascular events in individuals who carry the loss-of-function CYP2C19 alleles. However, a 2010 study concluded that patients with ACS or atrial fibrillation respond well to clopidogrel, regardless of CYP2C19 loss-of-function carrier status.

Ticlopidine (Ticlid)

Beneficial effects were noted in patients with UA after 2 wk of use in one randomized trial. When compared to controls, ticlopidine use decreased vascular deaths and nonfatal MIs.

Prasugrel (Effient)

Thienopyridine drug that inhibits platelet activation and aggregation through the irreversible binding of its active metabolite to ADP platelet receptors (specifically the P2Y12 receptor). Platelet inhibition is the result of this action.

Indicated to reduce thrombotic cardiovascular (CV) events (including stent thrombosis) with acute coronary syndrome (ACS) that is managed with percutaneous coronary intervention (PCI). Specifically for unstable angina or non – ST-elevation myocardial infarction (NSTEMI) or with ST-elevation myocardial infarction (STEMI) when managed with primary or delayed PCI.

Reduces rate of combined endpoint of CV death, nonfatal MI, or nonfatal stroke compared with clopidogrel.

Ticagrelor (Brilinta)

Ticagrelor and its major metabolite reversibly interact with the platelet P2Y12 ADP-receptor to prevent signal transduction and platelet activation. It is indicated to reduce the rate of thrombotic cardiovascular (CV) events in patients with ACS (unstable angina, non-ST elevation MI, or ST elevation MI). It also reduces the rate of stent thrombosis in patients who have undergone stent placement for treatment of ACS and is indicated in patients with a history of MI more than 1 year previously.

Clinical trial results showed a reduced rate of combined endpoint of CV death, MI, or stroke compared to clopidogrel. Difference between treatments was driven by CV death and MI with no difference in stroke. In patients treated with PCI, ticagrelor also reduces the rate of stent thrombosis.

The drug is administered with aspirin (loading dose of 325 mg PO once, then 75-100 mg/day). Note that exceeding an aspirin dose of 100 mg/day decreases ticagrelor effectiveness.


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