Ticagrelor (Brilinta)
Noncompetitive, direct-acting P2Y12 receptor antagonist; does not require metabolic activation (unlike thienopyridines). Binds reversibly to P2Y12, causing rapid onset (30 min) and offset (2-3 days) of antiplatelet effect. Rapidly absorbed (tmax 1.5-2h); moderate oral bioavailability (36%). Extensively hepatically metabolized by CYP3A4 to AR-C124910XX, an active metabolite with ~40% the potency of parent drug. Combined parent + metabolite effect provides sustained P2Y12 inhibition. Approved for acute coronary syndromes at 180 mg loading dose, 60-90 mg maintenance. May cause bradycardia and AV block via adenosine pathway. More potent platelet inhibition vs. clopidogrel. Drug interactions with CYP3A4 inducers/inhibitors.
Projected serum levels — 90 mg, once daily
Maintenance schedule: 90 mg once daily (oral).
Modeled steady state after ~1 days: peak ≈ 30.0 mg, trough ≈ 2.6 mg body load. Population-based estimate over 15 days for a 90 mg dose at a 70 kg reference body mass — the interactive app scales curves to your doses, timing, and body mass.
Key facts
- Category
- Antiplatelet
- Route modeled
- Oral
- Model confidence
- inferred
- Half-life
- 7 h
- Common dose
- 90 mg
- Suggested maximum
- 180 mg/day
- Reference dose range
- 45–180 mg (single dose)
- Suggested cadence
- once daily
- Validated against
- 180 mg oral — Cmax 1.4 mg/L at 1.5 h
Documented interactions
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contraindicated
Clarithromycin (Biaxin) + Ticagrelor (Brilinta)
Clarithromycin (Biaxin) mechanism_based of CYP3A4 predicted to change Ticagrelor (Brilinta) AUC by ~6.90x
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contraindicated
Diltiazem + Ticagrelor (Brilinta)
Diltiazem mechanism_based of CYP3A4 predicted to change Ticagrelor (Brilinta) AUC by ~6.90x
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contraindicated
Efavirenz (Sustiva) + Ticagrelor (Brilinta)
Efavirenz (Sustiva) inducer of CYP3A4 predicted to change Ticagrelor (Brilinta) AUC by ~0.13x
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contraindicated
Grapefruit (whole fruit) + Ticagrelor (Brilinta)
Grapefruit (whole fruit) mechanism_based of CYP3A4 predicted to change Ticagrelor (Brilinta) AUC by ~6.90x
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contraindicated
Grapefruit Juice + Ticagrelor (Brilinta)
Grapefruit Juice mechanism_based of CYP3A4 predicted to change Ticagrelor (Brilinta) AUC by ~6.90x
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contraindicated
Paxlovid (Nirmatrelvir/Ritonavir) + Ticagrelor (Brilinta)
Paxlovid (Nirmatrelvir/Ritonavir) mechanism_based of CYP3A4 predicted to change Ticagrelor (Brilinta) AUC by ~6.90x
Serum checks 298 modeled interaction pairings for ticagrelor (brilinta) across your whole stack — absorption conflicts, enzyme inhibition, and nutrient depletion included.
Research behind this entry
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Ticagrelor: Pharmacokinetics, Pharmacodynamics, Clinical Efficacy, and Safety
Comprehensive review of ticagrelor PK (tmax 2h, bioavailability 36%), active metabolite AR-C124910XX, faster onset than clopidogrel, and clinical efficacy in acute coronary syndromes.
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Pharmacokinetics and Bioequivalence of a Generic Ticagrelor 90-mg Formulation Versus the Innovator Product in Healthy White Subjects Under Fasting Conditions
Pharmacodynamic and kinetic study demonstrating ticagrelor faster P2Y12 inhibition onset and greater platelet inhibition than clopidogrel at same time points.
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Simultaneous quantification of ticagrelor and its active metabolite, AR-C124910XX, in human plasma by liquid chromatography-tandem mass spectrometry
Analytical method development showing AR-C124910XX is major circulating metabolite with ~40% parent drug potency, resulting in sustained antiplatelet effect.
3 published studies referenced in the app, each with a plain-language summary.