Ticagrelor

What is Ticagrelor

Ticagrelor is an oral platelet P2Y₁₂ adenosine-5′-diphosphate (ADP) receptor antagonist that inhibits platelet aggregation.

Ticagrelor is indicated to reduce the rate of thrombotic cardiovascular events in patients with acute coronary syndrome (ACS) (unstable angina, non-ST elevation myocardial infarction, or ST-elevation myocardial infarction) and to reduce the risk of first myocardial infarction or stroke in patients with coronary artery disease at high risk for these events, such as patients with type 2 diabetes.

It has been shown to reduce the rate of a combined endpoint of cardiovascular death, myocardial infarction, or stroke compared to clopidogrel.

The difference between treatments was driven by CV death and MI with no difference in stroke. In patients treated with percutaneous coronary intervention (PCI), it also reduces the rate of stent thrombosis. Ticagrelor should be used in combination with aspirin (see Indications/Dosage).

Unlike clopidogrel, ticagrelor does not require hepatic activation to an active form and does not have irreversible effects on platelets.

Ticagrelor was approved by the FDA in July 2011.

In August 2015, the FDA approved a 60 mg tablet to be administered, along with aspirin, beyond 12 months following ACS.

In May 2020, ticagrelor received FDA-approval for use in patients with coronary artery disease.

Brand Name

BRILINTA

Indications

1. acute myocardial infarction
2. arterial thromboembolism prophylaxis
3. coronary artery disease
4. myocardial infarction prophylaxis
5. percutaneous coronary intervention (PCI)
6. stroke prophylaxis
7. unstable angina

Side Effects

1. angioedema
2. atrial fibrillation
3. AV block
4. back pain
5. bleeding
6. bradycardia
7. chest pain (unspecified)
8. cough
9. diarrhea
10. dizziness
11. dyspnea
12. fatigue
13. gynecomastia
14. headache
15. hypertension
16. hyperuricemia
17. hypotension
18. intracranial bleeding
19. nausea
20. rash
21. syncope
22. thrombotic thrombocytopenic purpura (TTP)

Monitoring Parameters

• CBC
• LFTs

Contraindications

• abrupt discontinuation
• aspirin coadministration
• AV block
• bleeding
• bradycardia
• breast-feeding
• children
• coronary artery bypass graft surgery (CABG)
• geriatric
• GI bleeding
• heparin-induced thrombocytopenia (HIT)
• hepatic disease
• infants
• intracranial bleeding
• labor
• neonates
• obstetric delivery
• pregnancy
• sick sinus syndrome
• surgery
• syncope

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