Ticagrelor (Brilinta)

An antiplatelet agent.

Fast, potent inhibitor of platelet function.

P2SY12 Platelet inhibitor.

A reversible platelet antagonist.

Blocks the P2Y12 platelet ADP receptor.

Not a prodrug, but undergoes transformation in the liver to an effective metabolite.

Releases adenosine, which may contribute to its antiplatelet effect and side effects of bradycardia, dyspnea, and gastrointestinal symptoms.

Indicated to reduce the rate of thrombotic cardiovascular events in patients with acute coronary syndrome including unstable angina, non-ST-elevation myocardial infarction, or ST-elevation myocardial infarction.

It exhibits more profound platelet inhibition with more rapid onset on the basis of platelets function testing, compared with clopidogrel.

At 30 days ticagrelor plus aspirin reduced the primary composite of cardiovascular death, myocardial infarction, stroke versus clopidogrel plus aspirin in acute coronary syndromes.

In patients with stable coronary artery disease and diabetes without a history of myocardial infarction a stroke who receives ticagrelor plus aspirin had a lower incidence of ischemic cardiovascular events but a higher incidence of major bleeding in those who receive placebo plus aspirin (Steg PG).

Reduces the rate of cardiovascular death, myocardial infarction or stroke compared to clopidogrel in patients with acute coronary syndromes.

For at least the first 12 months following ACS, it is superior to clopidogrel.

In the PLATO (Platelet Inhibition and Patient Outcomes) trial a study of 18,000 patients with ACS with ST segment elevation myocardial infarction or non–STEMI: Ticagrelor was associated with fewer recurrent ischemic events at 12 months compared with clopidogrel group, with reductions in AMI, vascular mortality, and total mortality, but not in stroke.

In a retrospective cohort study that includes 62,580 patients, ticagrelor  use compared with clopidogrel was not associated with a significant difference in the risk of net clinical adverse events at 12 months in patients with acute coronary syndrome treated with PCI in clinical practice (You SC).
Among patients with mild-moderate acute non-cardio embolic ischemic stroke the risk of stroke or death within 30 days was lower with ticagrelor-aspirin than aspirin alone, but the incidence of disability did not differ significantly between the two groups (Johnston SJ). 

In the above study Ticagrelor was associated with a higher rate of bleeding unrelated to coronary artery bypass procedures, including more episodes of intracranial bleeding.

Studies in acute coronary syndromes have been done in combination with aspirin and maintenance doses of aspirin greater than one hundred milligrams decreases the effectiveness of this agent and should be avoided.

Can cause significant bleeding, and is contraindicated in patients with active bleeding or with a history of intracranial hemorrhage.

Should be discontinued at least 5 days prior to any surgery.

Discontinuing this agent increases the risk of subsequent cardiovascular events.

Dyspnea reported in 14% of patients taking this drug.

Metabolized by CYP3A4/5 and not CYP2C19 cytochrome system.

Simvastatin and lovastatin doses of greater than 40 mg should be avoided.

Risk of bleeding increased in patients of older age, created history of bleeding disorders, following percutaneous invasive procedures, and concomitant use of agents that increase the risk of bleeding such as anticoagulants, fibrinolytic therapy, higher doses of aspirin and non steroidal anti-inflammatory drugs.

Associated with major bleeding 11.6%.

Associated with increased risk of bradycardias.

Dosage initially 180 mg, two 90 mg tablets loading dose and continued therapy with 90 mg b.i.d.

No known treatment to reverse the effects of this drug.

Needs to be discontinued 48-72 hours prior to any surgery.

Among patients who underwent PCI for high-risk cardiovascular disease and completed three months of dual antiplatelet therapy, ticagrelor monotherapy had a lower incidence of clinically relevant bleeding than antiplatelet therapy with ticagrelor plus aspirin, with no higher risk of death, myocardial infarction, or stroke (Mehran R).

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