Ticagrelor
Brilinta · Brilique
Cyclopentyltriazolopyrimidine — REVERSIBLE P2Y12 inhibitor
Directly and REVERSIBLY inhibits P2Y12 (not a prodrug, not thienopyridine). Faster onset/offset than clopidogrel.
Indications
- •ACS
- •Post-PCI (DAPT)
- •High-risk CAD
Dosing
| Context | Adult | Pediatric |
|---|---|---|
| Loading | 180 mg PO | — |
| Maintenance | 90 mg PO BID (60 mg BID after 1 y) | — |
Pharmacokinetics
Onset ~30 min–2 h. Reversible, half-life ~7 h → offset ~3–5 days after stopping.
Side effects
- !Bleeding
- !Dyspnea (~15% — adenosine-mediated, usually benign)
- !Bradyarrhythmias
- !↑ with strong CYP3A inhibitors
Contraindications
- ×Active bleeding
- ×History of intracranial hemorrhage
- ×Severe hepatic impairment
Clinical pearls
- ★ASRA neuraxial: hold 5–7 days before neuraxial procedure.
- ★Dyspnea is a classic ticagrelor side effect (adenosine reuptake inhibition) — not heart failure.
- ★BID dosing + reversible — missed doses lose effect faster than clopidogrel.
Other drugs in Antiplatelets
- Aspirin
Irreversibly acetylates COX-1 → blocks thromboxane A2 for the platelet's lifespan (~7–10 days). Antiplatelet effect at low dose; analgesic/anti-inflammatory at high dose.
- Clopidogrel
Prodrug → active metabolite (CYP2C19) irreversibly blocks the platelet P2Y12 ADP receptor for the platelet lifespan.
- Prasugrel
Prodrug → active metabolite irreversibly blocks P2Y12. More potent + more consistent than clopidogrel (not CYP2C19-limited), but more bleeding.
- Ticlopidine
Irreversibly blocks P2Y12. Largely replaced by clopidogrel due to hematologic toxicity.
- Abciximab
Fab fragment that irreversibly blocks the platelet GP IIb/IIIa receptor → prevents fibrinogen cross-linking (final common pathway of aggregation).
- Eptifibatide
Reversibly blocks GP IIb/IIIa (final common pathway of platelet aggregation). Short-acting.
- Dipyridamole
Inhibits platelet PDE (↑ cAMP) and adenosine reuptake (↑ adenosine → vasodilation). Weak antiplatelet; also a coronary vasodilator used in stress testing.
- Cilostazol
Inhibits PDE3 → ↑ cAMP → antiplatelet + arterial vasodilation. Improves claudication walking distance.
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