Generic Name

Ticagrelor

Mechanism

• Reversible binding to the P2Y12 receptor on platelets → blocks ADP‑induced phosphorylation of the receptor.
• Prevents ADP from activating the GPIIb/IIIa inside‑out signaling cascade → reduces fibrinogen cross‑linking and platelet aggregation.
• Short half‑life (~7 h) allows rapid reversal of platelet inhibition when needed.

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Pharmacokinetics

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Indications

• Acute coronary syndrome (unstable angina, NSTEMI, STEMI) – *dual antiplatelet therapy* (DAPT) with aspirin.
• Post‑PCI – maintenance antiplatelet for ≥12 months.
• Atrial fibrillation – not indicated; use with caution when combined with anticoagulants.

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Contraindications

• Contraindicated in patients with:
• Known hypersensitivity to ticagrelor or excipients.
• Concomitant use of strong CYP3A4 inhibitors (e.g., ketoconazole).
• Warnings
• Bleeding risk: evaluate for active bleeding, gastric ulcers, recent surgery.
• Heart failure: may cause dyspnea.
• Severe hepatic impairment: avoid due to increased exposure.

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Dosing

• Initial loading dose: 180 mg orally (2 × 90 mg) in ACS.
• Maintenance: 90 mg orally twice daily (every 12 h) for routine DAPT.
• Perioperative management – hold 24 h before elective surgery; resume 24 h post‑operatively if hemostasis secured.
• Switching from clopidogrel: give 180 mg loading, then 90 mg BID; avoid overlap of >7 days.

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Adverse Effects

• Common:
• Dyspnea (up to 8 %).
• Hypotension, headache.
• Serious:
• Major bleeding (intracranial, GI, genitourinary).
• Thrombocytopenia.
• Bradyarrhythmias (rare).

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Monitoring

• Baseline: CBC, platelet count, liver function tests, renal function.
• Ongoing:
• Watch for signs of bleeding (bruising, hematemesis).
• Monitor pulse and blood pressure for dyspnea or hypotension.
• Platelet function tests – not routinely required but useful in refractory cases.

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Clinical Pearls

• Dual‑Drug Timing: Give ticagrelor within 1 h of ACS presentation; loading dose improves platelet inhibition 2–3 hours faster than clopidogrel.
• No Food Restriction: Unlike clopidogrel, ticagrelor’s absorption is unaffected by food.
• Bleeding Risk Management: Co‑administration of PPIs is acceptable; avoid NSAIDs unless necessary.
• Drug Interaction “Red‑Flag” Chart:
• *High‑risk inhibitors* → Contraindicated (ketoconazole, itraconazole).
• *Moderate* → Dose adjustment/adult monitoring (amiodarone, erythromycin).
• *Low* → Standard dosing.
• Post‑PCI Durability: If early discontinuation is required (e.g., due to bleeding), switch to clopidogrel with a 180 mg loading dose to maintain platelet coverage.
• Reversal Strategy: Platelet transfusion can restore function; no specific antidote, but hold ticagrelor and plan emergent surgery if bleeding.

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• Key Takeaway: Ticagrelor offers rapid, potent, and reversible platelet inhibition, making it the preferred P2Y12 inhibitor in high‑risk ACS and post‑PCI settings, provided bleeding risks are closely monitored and drug–drug interactions are managed.