BRILINTA Dosage & Rx Info | Uses, Side Effects

Brilinta Generic Name & Formulations

Legal Class

General Description

Ticagrelor 60mg, 90mg; tabs.

Pharmacological Class

P2Y₁₂ platelet inhibitor (cyclopentyltriazolopyrimidine).

How Supplied

Tabs—60

Manufacturer

AstraZeneca Pharmaceuticals

Generic Availability

Mechanism of Action

Ticagrelor and its major metabolite reversibly interact with the platelet P2Y₁₂ ADP-receptor to prevent signal transduction and platelet activation.

Brilinta Indications

Indications

To reduce the risk of cardiovascular death, MI, and stroke in patients with acute coronary syndrome (ACS) or history of MI. To reduce the risk of stent thrombosis in patients who have been stented for ACS. To reduce the risk of a first MI or stroke in patients with coronary artery disease (CAD) at high risk for such events. To reduce the risk of stroke in patients with acute ischemic stroke (NIH Stroke Scale score ≤5) or high-risk transient ischemic attack (TIA).

Brilinta Dosage and Administration

Adult

Swallow whole; if unable to swallow, may crush tabs, then mix with water and drink or give via NG tube (CH8 or greater). ACS or history of MI: initially 180mg loading dose, then give first 90mg maintenance dose 6–12hrs after the loading dose and continue with 90mg twice daily during the first year; after one year, give 60mg twice daily. CAD (no prior stroke or MI): 60mg twice daily. ACS, history of MI, or CAD: use with maintenance dose of aspirin 75–100mg daily; consider single antiplatelet therapy for ACS or history of MI in patients who underwent percutaneous coronary intervention (PCI). Acute ischemic stroke or TIA: initially 180mg loading dose, then give first 90mg maintenance dose 6–12hrs after the loading dose and continue with 90mg twice daily for up to 30 days; use with a loading dose of aspirin (300–325mg), then maintenance dose of aspirin 75–100mg daily.

Children

Not established.

Brilinta Contraindications

Contraindications

History of intracranial hemorrhage. Active pathological bleeding (eg, peptic ulcer, intracranial hemorrhage).

Brilinta Boxed Warnings

Boxed Warning

Bleeding risk.

Brilinta Warnings/Precautions

Warnings/Precautions

Increased risk of bleeding. Do not start in patients undergoing urgent CABG. For acute ischemic stroke or TIA: not recommended if NIHSS >5 or receiving thrombolysis. Discontinuation increases risk for CV events (eg, MI, stroke, death) in those treated for CAD. If temporarily discontinued, restart as soon as possible. When possible, interrupt therapy for 5 days prior to surgery (those with major bleeding risk); resume upon hemostasis. History of sick sinus syndrome, 2^nd or 3^rd-degree AV block or bradycardia-related syncope without a pacemaker: increased risk of bradyarrhythmias. Evaluate if central sleep apnea is suspected. Moderate hepatic impairment. Severe hepatic impairment: avoid. Pregnancy. Nursing mothers: not recommended.

Brilinta Pharmacokinetics

Absorption

Median time to maximum concentration: 1.5 hours. Mean absolute bioavailability: ~36%.

Distribution

Steady state volume of distribution: 88 L. >99% plasma protein bound.

Metabolism

Hepatic (CYP3A4).

Elimination

Fecal (58%), renal (26%). Half-life: ~7 hours.

Brilinta Interactions

Interactions

For ACS: effectiveness reduced with aspirin maintenance dose >100mg; avoid. Concomitant other oral P2Y₁₂ platelet inhibitor: not recommended. Avoid concomitant strong CYP3A inhibitors (eg, ketoconazole, itraconazole, voriconazole, clarithromycin, nefazodone, ritonavir, saquinavir, nelfinavir, indinavir, atazanavir, telithromycin) or potent CYP3A inducers (eg, rifampin, phenytoin, carbamazepine, phenobarbital). Antagonized by opioid agonists (eg, morphine, others); consider using IV anti-platelet agent instead. Potentiates simvastatin, lovastatin; avoid >40mg/day doses. Monitor digoxin during ticagrelor initiation and dose adjustments. May cause false negative platelet function tests for HIT.

Brilinta Adverse Reactions

Adverse Reactions

Bleeding (may be fatal), dyspnea (consider other alternatives if intolerable), dizziness, nausea, diarrhea; ventricular pauses.

Brilinta Clinical Trials

See Literature

Brilinta Note

Not Applicable

Brilinta Patient Counseling