Product: Brilinta

Company: AstraZeneca

Pharmacologic class: P2Y12 platelet inhibitor (cyclopentyltriazolopyrimidine)

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Active ingredient: Ticagrelor 90 mg; tablets.

Indication: To reduce the rate of thrombotic cardiovascular (CV) events in patients with acute coronary syndrome  (ACS; unstable angina or non-ST-elevation MI or ST-elevation MI).

Pharmacology: Ticagrelor is a platelet activation and aggregation inhibitor mediated by the P2Y12 class of adenosine diphosphate (ADP) receptors. Ticagrelor and its major metabolite reversibly interact with the platelet P2Y12 ADP-receptor to prevent signal transduction and platelet activation. Both ticagrelor and its active metabolite are approximately equipotent.

Clinical trials: In a randomized, double-blind study, the use of ticagrelor was compared with a regimen of clopidogrel, both given in combination with aspirin and other standard therapy in patients with acute coronary syndromes. Patients were treated for at least six months and for up to 12 months.

The primary endpoint was the composite of first occurrence of cardiovascular death, nonfatal MI (excluding silent MI) or nonfatal stroke. The components were assessed as secondary endpoints.

At study completion, ticagrelor had been shown to significantly reduce the rate of a combined endpoint of cardiovascular death, MI, or stroke compared with clopidogrel (9.8% vs. 11.7%, respectively, hazard ratio=0.84).

The difference between treatments on the composite resulted from effects on CV death (HR=0.79) and MI (HR=0.84); each was statistically significant when considered as a secondary endpoint and there was no difference on strokes. There was also a decrease in all-cause mortality.

Among 11,298 patients with percutaneous coronary intervention (PCI) receiving any stent during this study, there was a lower risk of stent thrombosis (1.3% for adjudicated “definite”) than with clopidogrel (1.9%).

Adults: Initiate loading dose at 180 mg once, then continue with 90 mg twice daily. After the initial loading dose of aspirin (usually 325 mg), take ticagrelor with maintenance dose of aspirin 75-100 mg daily. ACS patients may start ticagrelor after receiving a loading dose of clopidogrel.

Children: Not established.

Contraindications: History of intracranial hemorrhage. Active pathological bleeding (e.g., peptic ulcer, intracranial hemorrhage). Severe hepatic impairment.

Warnings/Precautions: Do not start in patients planned to undergo urgent coronary artery bypass graft (CABG). When possible, discontinue at least five days before any surgery. Suspect bleeding in hypotensive patients who have recently undergone coronary angiography, PCI, CABG or other surgery.

Older age, history of bleeding disorders, undergoing percutaneous invasive procedures, concomitant anticoagulants, fibrinolytics, higher doses of aspirin and chronic nonsteroidal anti-inflammatory drug use increased the risk of bleeding.

Avoid interruption of treatment; if temporarily discontinued, restart as soon as possible. Premature discontinuation increases risk for CV events (e.g., MI, stent thrombosis, death). Effectiveness reduced with aspirin maintenance dose >100 mg; avoid. Moderate hepatic impairment. Pregnancy (Cat. C). Nursing mothers: not recommended.

Interactions: Concomitant strong CYP3A inhibitors (e.g., ketoconazole, itraconazole, voriconazole, clarithromycin, nefazodone, ritonavir, saquinavir, nelfinavir, indinavir, atazanavir, telithromycin,) or potent CYP3A inducers (e.g., rifampin, dexamethasone, phenytoin, carbamazepine, phenobarbital): not recommended. Potentiates simvastatin, lovastatin; avoid doses >40 mg/day. Monitor digoxin during ticagrelor initiation and dose adjustments.

Adverse reactions: Bleeding (may be fatal), dyspnea, headache, cough, dizziness, GI upset, atrial fibrillation, hyper- or hypotension, back pain, fatigue and chest pain.

How supplied: Tabs — 60, 180

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