ticagrelor

Brand: Brilinta

⚠ BBW Prototype: clopidogrel

Drug Class: antiplatelet

Drug Family: antiplatelet

Subclass: P2Y12 ADP receptor antagonist (direct-acting)

Organ Systems: cardiovascular

Mechanism of Action

Direct-acting, reversible P2Y12 antagonist; not a prodrug (no CYP activation required); faster onset and more consistent antiplatelet effect than clopidogrel.

P2Y12 ADP receptor

Indications

ACS (NSTEMI, STEMI) — PLATO trial preference over clopidogrel
stroke/TIA prevention (SOCRATES)
secondary prevention in CAD

Contraindications

active pathological bleeding
intracranial hemorrhage history
severe hepatic impairment
concomitant simvastatin >40 mg

Adverse Effects

Common

dyspnea (dose-dependent — bradykinin/adenosine mechanism)
bleeding
bradycardia

Serious

major hemorrhage
serious dyspnea requiring discontinuation

Pharmacokinetics (ADME)

Absorption	36% oral bioavailability
Distribution	reversible platelet binding
Metabolism	hepatic CYP3A4 to active metabolite
Excretion	biliary and renal
Half-life	7-8.5 hours
Onset	2-4 hours
Peak	2-4 hours
Duration	12 hours
Protein Binding	99.7%
Vd	87.5 L

Drug Interactions

Drug / Agent	Mechanism	Severity
strong CYP3A4 inhibitors	increase ticagrelor and active metabolite levels	major
strong CYP3A4 inducers (rifampin)	reduce ticagrelor levels — avoid	major
aspirin >100 mg	reduces ticagrelor efficacy — use only low-dose aspirin	major

Nursing Considerations

PLATO trial: ticagrelor superior to clopidogrel for ACS outcomes including CV mortality
Dyspnea in ~14%: adenosine-mediated (reversible); reassure patient and monitor
Aspirin dose: use ONLY low-dose aspirin (81 mg) — high-dose aspirin reduces ticagrelor efficacy
Twice-daily dosing (90 mg BID for ACS; 60 mg BID for chronic CAD)
Reversible binding: platelet function recovers 3-5 days after stopping (vs 7-10 for clopidogrel)

Clinical Pearls

PLATO trial: 16% relative risk reduction in CV death/MI/stroke vs clopidogrel in ACS
Dyspnea mechanism: ticagrelor inhibits adenosine cellular uptake causing transient bronchospasm
Direct-acting: no CYP2C19 activation needed — consistent efficacy regardless of metabolizer status

Safety Profile

Pregnancy avoid

Lactation avoid

Renal Adjustment Not required

Hepatic Adjustment Required

TDM Not required

Guideline Update pending

Concordance Terms

Cross-referenced clinical concepts — click any term to see all content where it appears.

ACS (NSTEMI, STEMI) — PLATO Trial Preference Over Clopidogrel Antiplatelet Secondary Prevention In CAD Stroke/TIA Prevention (SOCRATES)

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