1. Introduction
Ticagrelor is a potent oral antiplatelet agent that acts as a P2Y12 receptor antagonist, preventing platelet aggregation and reducing the risk of blood clots. It is primarily used in acute coronary syndromes (ACS) and post-myocardial infarction (MI) prevention.
2. Indications
- Acute Coronary Syndrome (ACS):
- Unstable angina (UA)
- Non-ST elevation myocardial infarction (NSTEMI)
- ST-elevation myocardial infarction (STEMI)
- Prevention of Cardiovascular Events:
- In patients with a history of myocardial infarction (MI).
- Use in Percutaneous Coronary Intervention (PCI):
- Reduces the risk of stent thrombosis in patients undergoing PCI.
3. Dosage
Adults:
- Acute Coronary Syndrome (ACS) / Post-PCI:
- Loading dose: 180 mg once, followed by
- Maintenance dose: 90 mg twice daily for 12 months.
- Long-Term Secondary Prevention (>1 year post-MI):
- 60 mg twice daily (for continued prevention of thrombotic events).
Elderly:
- No dose adjustment required.
Renal Impairment:
- No dose adjustment needed in mild to moderate impairment.
- Use with caution in severe renal impairment (eGFR <15 mL/min).
Hepatic Impairment:
- Avoid in severe hepatic impairment.
- Use cautiously in moderate impairment.
4. Administration
- Take orally, with or without food.
- Swallow whole; do not crush or chew.
- If unable to swallow, the tablet may be crushed and mixed with water.
5. Forms Available
- Tablets: 60 mg, 90 mg
6. Side Effects
6.1 Common Side Effects:
- Dyspnoea (shortness of breath)
- Bleeding (bruising, nosebleeds, gastrointestinal bleeding)
- Headache
6.2 Less Common Side Effects:
- Nausea
- Dizziness
- Increased uric acid levels (risk of gout)
6.3 Rare but Serious Side Effects:
- Major bleeding (intracranial, gastrointestinal, or life-threatening bleeding)
- Bradycardia (slow heart rate)
- Hypersensitivity reactions (rash, angioedema)
7. Warnings
- Increased Risk of Bleeding:
- Avoid in patients with active bleeding or history of intracranial haemorrhage.
- Use with caution in patients with recent surgery, trauma, or high bleeding risk.
- Dyspnoea (Shortness of Breath):
- Common side effect but usually mild and transient.
- Monitor for severe respiratory symptoms.
- Bradycardia and AV Block:
- Avoid in patients with severe conduction abnormalities without a pacemaker.
- Discontinuation Risk:
- Do not stop ticagrelor abruptly, as it may lead to thrombotic events.
8. Precautions
- Avoid concurrent use with other anticoagulants unless strictly necessary.
- Caution in patients with a history of gout due to increased uric acid levels.
- Monitor renal and liver function periodically in high-risk patients.
9. Interactions
- Strong CYP3A4 inhibitors (e.g., ketoconazole, ritonavir, clarithromycin): Increase ticagrelor levels and bleeding risk.
- Strong CYP3A4 inducers (e.g., rifampin, carbamazepine, phenytoin): Decrease ticagrelor effectiveness.
- Aspirin (>100 mg daily): Reduces ticagrelor effectiveness (use aspirin ≤100 mg/day).
- Digoxin: Ticagrelor may increase digoxin levels.
10. Monitoring Parameters
- Signs of bleeding: Bruising, nosebleeds, blood in stool or urine.
- Dyspnoea symptoms: Monitor for worsening respiratory distress.
- Renal function (eGFR): In high-risk patients.
- Liver function: In patients with hepatic impairment.
11. Use in Children
- Not recommended for use in children.
12. Use in Pregnancy
- Category C:
- Use only if the potential benefit justifies the risk.
- Avoid in the third trimester due to bleeding risk during delivery.
13. Use in Elderly
- Safe to use in elderly patients, but monitor for bleeding risk.
14. Use in Kidney Disease
- No dose adjustment in mild to moderate renal impairment.
- Use with caution in severe renal disease (eGFR <15 mL/min).
15. Use in Liver Disease
- Avoid in severe hepatic impairment.
- Use cautiously in moderate impairment.
16. Patient Counselling Points
- Take ticagrelor exactly as prescribed, do not skip doses.
- Do not stop abruptly, as this increases the risk of heart attack or stroke.
- Avoid NSAIDs and high-dose aspirin (>100 mg daily) due to bleeding risk.
- Report any signs of bleeding (e.g., blood in stools, unexplained bruising).
- Shortness of breath may occur, but it is usually mild and temporary.
- Avoid grapefruit juice, as it may increase ticagrelor levels.
17. Table of Brand Names, Manufacturer, and Prices in USD
Brand Name | Manufacturer | Strength/Dosage Form | Price (USD) |
---|---|---|---|
Brilinta | AstraZeneca | 90 mg Tablet | $300 (30 tablets) |
Generic Ticagrelor | Various | 90 mg Tablet | $150 (30 tablets) |
18. 15 FAQs (Frequently Asked Questions)
1. What is Ticagrelor used for?
Ticagrelor prevents blood clots in patients with acute coronary syndromes (ACS) and heart attacks.
2. How does Ticagrelor work?
It inhibits P2Y12 receptors, preventing platelet aggregation and reducing the risk of heart attacks.
3. How long should I take Ticagrelor after a heart attack?
Usually for 12 months, but in some cases, doctors may recommend longer use at a lower dose.
4. Can Ticagrelor cause shortness of breath?
Yes, dyspnoea is a common side effect, but it is usually mild and temporary.
5. Can Ticagrelor cause excessive bleeding?
Yes, major bleeding is a risk; report any unusual bleeding to your doctor immediately.
6. Can Ticagrelor be taken with aspirin?
Yes, but aspirin dose should not exceed 100 mg daily for best efficacy.
7. Does Ticagrelor need blood monitoring?
No routine blood monitoring is required, but watch for signs of bleeding.
8. Can Ticagrelor be crushed?
Yes, it can be crushed and mixed with water if swallowing is difficult.
9. What should I do if I miss a dose?
Take it as soon as you remember. Do not double the next dose.
10. Can I drink alcohol while taking Ticagrelor?
Limit alcohol intake to reduce the risk of stomach bleeding.
11. Can Ticagrelor be used long-term?
Yes, some patients continue ticagrelor at 60 mg twice daily for long-term prevention.
12. Can Ticagrelor be stopped before surgery?
Yes, but consult your doctor; usually stopped 5 days before surgery.