Brilinta (Ticagrelor) Side Effects
Brilinta's most significant adverse effects include increased bleeding risk, dyspnea (occurring in 14-21% of patients), bradyarrhythmias with ventricular pauses, and minor bleeding events, though major bleeding rates are comparable to clopidogrel. 1
Major Adverse Effects
Bleeding Complications
- Major bleeding risk: Similar to clopidogrel overall, but non-CABG-related major bleeding is increased (4.5% vs 3.8% with clopidogrel) 2, 3
- Intracranial hemorrhage (ICH): Ticagrelor increases fatal ICH risk compared to clopidogrel and should be avoided in patients with prior ICH 4, 1
- Gastrointestinal bleeding: Increased risk, particularly in older adults (≥75 years) 5
- Major or minor bleeding combined: Significantly higher with ticagrelor (OR: 1.40) 6
Critical contraindication: History of intracranial hemorrhage is an absolute contraindication 1
Dyspnea
- Incidence: 14-21% of patients develop dyspnea, making it the most common non-bleeding adverse effect 1, 7, 8
- Characteristics: Usually mild to moderate intensity, often self-limiting and resolves with continued treatment 1, 8
- Discontinuation rates: 0.9-6.9% in clinical trials, but real-world data shows higher rates (2-9%) 9
- Mechanism: Likely related to ticagrelor's inhibition of adenosine reuptake by erythrocytes, increasing circulating adenosine levels 10
- Management: No specific treatment required; encourage continuation as symptoms typically resolve. Only discontinue if intolerable 1
Cardiac Arrhythmias
- Ventricular pauses: Can cause pauses ≥3 seconds (5.8% vs 3.6% with clopidogrel in first week) 2, 1
- Bradyarrhythmias: Including AV block reported in post-marketing surveillance 1, 11
- Syncope: Case reports of syncope from long ventricular pauses following loading doses 11
- High-risk patients: Those with sick sinus syndrome, 2nd or 3rd degree AV block, or bradycardia-related syncope without pacemaker protection are at increased risk 1
Additional Adverse Effects
Metabolic and Renal
- Uric acid elevation: Modest increases reported, potential gout risk 10, 7
- Creatinine elevation: Mild increases in serum creatinine 2
- Kidney damage: Reported in clinical use 7
Respiratory
- Central sleep apnea (CSA): Including Cheyne-Stokes respiration reported post-marketing, with potential recurrence or worsening upon rechallenge 1
Hematologic
- Thrombotic thrombocytopenic purpura (TTP): Rare but serious complication 7
Other
- Gastrointestinal effects: Nausea, vomiting, diarrhea (particularly with overdose) 1
- Drug discontinuation: Overall discontinuation due to adverse events occurs more frequently than with clopidogrel (7.4% vs 6.0%) 2
Special Population Considerations
Elderly Patients (≥75 years)
- Increased bleeding risk, particularly gastrointestinal and intracranial 5
- No dosage adjustment needed, but heightened vigilance required 1
Patients with Prior Stroke/TIA
- Weigh risks carefully: Increased risk of intracranial bleeding when adding ticagrelor to aspirin 4, 12
- Consider alternative antiplatelet strategies in this population 2
Hepatic Impairment
- Avoid in severe hepatic impairment: Likely increases serum concentrations significantly 1
- Limited data in moderate impairment; consider risk-benefit carefully 1
Critical Safety Warnings
Avoid ticagrelor in patients with:
- History of intracranial hemorrhage (absolute contraindication) 1
- Active pathological bleeding 1
- Severe hepatic impairment 1
- Concomitant use with other oral P2Y12 inhibitors 1
- Within 24 hours of thrombolytic therapy 9
Monitor for:
- Signs and symptoms of bleeding 5
- New or worsening dyspnea 1
- Bradycardia or syncope, especially in first week 1
- Central sleep apnea symptoms 1
Surgical considerations: Discontinue at least 5 days before surgery with major bleeding risk; resume as soon as hemostasis achieved 4, 1