Ticagrelor

What it is and how it works

Mechanism of Action Ticagrelor and its major metabolite reversibly interact with the platelet P2Y 12 ADP-receptor to prevent signal transduction and platelet activation. Ticagrelor and its active metabolite are approximately equipotent.

Mechanism class: P2Y12 Receptor Antagonists · Cytochrome P450 3A4 Inhibitors · P-Glycoprotein Inhibitors

Indications

Ticagrelor tablets are a P2Y 12 platelet inhibitor indicated to reduce the risk of cardiovascular (CV) death, myocardial infarction (MI), and stroke in patients with acute coronary syndrome (ACS) or a history of MI. For at least the first 12 months following ACS, it is superior to clopidogrel. Ticagrelor tablets also reduces the risk of stent thrombosis in patients who have been stented for treatment of ACS. to reduce the risk of a first MI or stroke in patients with coronary artery disease (CAD) at high risk for such events. While use is not limited to this setting, the efficacy of ticagrelor tablets were established in a population with type 2 diabetes mellitus (T2DM). to reduce the risk of stroke in patients with acute ischemic stroke (NIH Stroke Scale score ≤5) or high-risk transient ischemic attack (TIA). Acute Coronary Syndrome or a History of Myocardial Infarction Ticagrelor tablets are indicated to reduce the risk of cardiovascular (CV) death, myocardial infarction (MI), and stroke in patients with acute coronary syndrome (ACS) or a history of MI.

Dosage and administration (summary)

or History of MI Initiate treatment with 180 mg oral loading dose of ticagrelor tablets. Then administer 90 mg twice daily during the first year. After one year, administer 60 mg twice daily. Patients with CAD and No Prior Stroke or MI Administer 60 mg ticagrelor tablets twice daily. Acute Ischemic Stroke Initiate treatment with a 180 mg loading dose of ticagrelor tablets then continue with 90 mg twice daily for up to 30 days. Use ticagrelor tablets with a daily maintenance dose of aspirin of 75 to 100 mg. However, in patients who have undergone PCI, consider single antiplatelet therapy with ticagrelor tablets based on the evolving risk for thrombotic versus bleeding events.

Contraindications

· History of intracranial hemorrhage. · Active pathological bleeding. · Hypersensitivity to ticagrelor or any component of the product. History of Intracranial Hemorrhage Ticagrelor tablet is contraindicated in patients with a history of intracranial hemorrhage (ICH) because of a high risk of recurrent ICH in this population . Active Bleeding Ticagrelor tablet is contraindicated in patients with active pathological bleeding such as peptic ulcer or intracranial hemorrhage .

Warnings and precautions

Dyspnea was reported more frequently with ticagrelor tablets than with control agents in clinical trials. Dyspnea from ticagrelor tablets are self-limiting. Severe Hepatic Impairment: Likely increase in exposure to ticagrelor. Laboratory Test Interference: False negative platelet functional test results have been reported for Heparin Induced Thrombocytopenia (HIT). Ticagrelor tablets are not expected to impact PF4 antibody testing for HIT. Risk of Bleeding Drugs that inhibit platelet function including ticagrelor tablets increase the risk of bleeding .

Pregnancy

Pregnancy Risk Summary Available data from case reports with ticagrelor tablets use in pregnant women have not identified a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes.

Storage and supply

Ticagrelor tablets 60 mg is supplied as a round, biconvex, pink to light pink, film coated tablet debossed with “60” on one side and on other side. Bottles of 14 – NDC 67877-522-14 Bottles of 60 – NDC 67877-522-60 Bottles of 180 – NDC 67877-522-18 Bottles of 500 – NDC 67877-522-05 Carton of 100 Tablets (10×10 Unit-dose) – NDC 67877-522-38 Storage a…

Source: Ticagrelor (Ticagrelor) — US FDA prescribing information, 2025-10-29, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.