Introduction
Brilinta (ticagrelor) is an oral antiplatelet medication belonging to the class of cyclopentyltriazolopyrimidines. It is a reversibly binding P2Y12 adenosine diphosphate (ADP) receptor antagonist approved by the FDA in 2011. Brilinta is primarily used in combination with aspirin to reduce thrombotic cardiovascular events in patients with acute coronary syndrome (ACS).
Mechanism of Action
Ticagrelor inhibits platelet activation and aggregation by selectively and reversibly antagonizing the ADP receptor P2Y12 on platelets. Unlike thienopyridines (clopidogrel, prasugrel), ticagrelor does not require metabolic activation and provides faster, more consistent platelet inhibition. Its reversible binding allows for more rapid offset of antiplatelet effects compared to irreversible P2Y12 inhibitors.
Indications
- Acute coronary syndrome (unstable angina, non-ST-elevation myocardial infarction, ST-elevation myocardial infarction)
- Reduction of cardiovascular death and myocardial infarction in patients with ACS
- Secondary prevention in patients with history of myocardial infarction (≥1 year prior) with high risk of ischemic events
Dosage and Administration
Standard dosing: 180 mg loading dose followed by 90 mg twice daily Duration: Typically prescribed for at least 12 months in ACS patients Administration: Can be taken with or without food Special populations:- Renal impairment: No dosage adjustment necessary
- Hepatic impairment: Avoid in severe hepatic impairment
- Elderly: No dosage adjustment necessary
- CYP2C19 poor metabolizers: No dosage adjustment required (unlike clopidogrel)
Pharmacokinetics
Absorption: Rapid with bioavailability of approximately 36% Distribution: Volume of distribution 88 L, protein binding >99% Metabolism: Primarily via CYP3A4 with formation of active metabolite AR-C124910XX Elimination: Half-life approximately 7 hours for ticagrelor, 9 hours for active metabolite Excretion: Feces (58%) and urine (26%)Contraindications
- History of intracranial hemorrhage
- Active pathological bleeding
- Severe hepatic impairment
- Hypersensitivity to ticagrelor or any component
- Concurrent use with strong CYP3A4 inhibitors
Warnings and Precautions
Boxed Warning:- Bleeding risk: Can cause significant, sometimes fatal, bleeding
- Aspirin dose: Maintenance dose of aspirin should be 75-100 mg daily
- Dyspnea (usually mild to moderate)
- Bradyarrhythmias including pauses
- Increased serum uric acid
- Increased risk of bleeding in patients undergoing CABG
Drug Interactions
Major interactions:- Strong CYP3A4 inhibitors (ketoconazole, itraconazole, clarithromycin): Contraindicated
- Strong CYP3A4 inducers (rifampin, carbamazepine): Avoid concurrent use
- Aspirin: Doses >100 mg daily reduce effectiveness
- Opioids: May delay and decrease absorption
- Simvastatin, lovastatin: Dose limitation recommended
Adverse Effects
Common (≥10%): Dyspnea (14-21%), bleeding events (12-16%) Less common (1-10%):- Bruising
- Epistaxis
- Gastrointestinal hemorrhage
- Dizziness
- Headache
- Hypotension
- Nausea
- Major bleeding
- Intracranial hemorrhage
- Fatal bleeding
- Acute coronary events after discontinuation
Monitoring Parameters
- Signs and symptoms of bleeding
- Complete blood count (baseline and as clinically indicated)
- Dyspnea assessment
- Cardiac monitoring for bradyarrhythmias
- Serum creatinine and liver function tests (baseline)
- Adherence to therapy
- Aspirin dose verification (maintain 75-100 mg daily)
Patient Education
- Take exactly as prescribed (twice daily)
- Do not discontinue without consulting healthcare provider
- Report any signs of bleeding (unusual bruising, blood in urine/stool)
- Inform all healthcare providers about Brilinta use before any procedures
- Be aware of potential shortness of breath side effect
- Use caution with activities that may cause bleeding or injury
- Maintain aspirin therapy as directed (low dose)
- Store at room temperature
- Seek immediate medical attention for serious bleeding or chest pain
References
1. Wallentin L, Becker RC, Budaj A, et al. Ticagrelor versus clopidogrel in patients with acute coronary syndromes. N Engl J Med. 2009;361(11):1045-1057. 2. FDA Prescribing Information: Brilinta (ticagrelor). Revised 2023. 3. Bonaca MP, Bhatt DL, Cohen M, et al. Long-term use of ticagrelor in patients with prior myocardial infarction. N Engl J Med. 2015;372(19):1791-1800. 4. Storey RF, Becker RC, Harrington RA, et al. Characterization of dyspnoea in PLATO study patients treated with ticagrelor or clopidogrel and its association with clinical outcomes. Eur Heart J. 2011;32(23):2945-2953. 5. Current guidelines: ACC/AHA and ESC guidelines for management of acute coronary syndromes (2021-2023 updates).