Ticagrelor

Prescription ·Strong evidence ·Reviewed May 2026

Ticagrelor is a direct-acting, reversible P2Y12 receptor inhibitor that does not require hepatic activation. The PLATO trial demonstrated superiority over clopidogrel in reducing cardiovascular events in ACS patients. Unlike thienopyridines, its binding is reversible, allowing faster recovery of platelet function after discontinuation.

What it's good for
  • Superior to clopidogrel in ACS (PLATO trial)1,3
  • Faster onset and offset than clopidogrel1,3
  • No dependence on CYP2C19 metabolism
  • Reversible binding allows faster platelet recovery
What to watch for
  • Bleeding
  • Dyspnea (dose-related, usually mild and self-limiting)
  • Bradycardia and ventricular pauses (usually asymptomatic)
  • Active pathological bleeding
  • History of intracranial hemorrhage

The bottom line

Evidence rating strong. Most-documented uses: superior to clopidogrel in acs (plato trial), faster onset and offset than clopidogrel, no dependence on cyp2c19 metabolism. 10 sources indexed (2018–2026), with 5 interaction records on file.

The science

How it works, mechanistically.

Core mechanism

Cyclopentyl-triazolopyrimidine that directly and reversibly binds the P2Y12 ADP receptor at a site distinct from the ADP binding site (allosteric inhibition). Does not require metabolic activation, providing faster and more consistent platelet inhibition than clopidogrel. Also inhibits adenosine reuptake via equilibrative nucleoside transporter-1 (ENT-1), which may contribute to vasodilatory and anti-inflammatory effects.

Class
Antiplatelet Agent (P2Y12 Inhibitor)
Dosing

Dosing & protocol.

Common range
180 mg loading dose, then 90 mg twice daily for 12 months (with aspirin 75–100 mg daily) (as prescribed by your physician)
Recommended form
Oral tablet

Can be taken with or without food; tablets can be crushed and mixed with water for NG tube administration8

Safety

Full safety detail.

Side effects

  • Bleeding
  • Dyspnea (dose-related, usually mild and self-limiting)
  • Bradycardia and ventricular pauses (usually asymptomatic)
  • Elevated uric acid and serum creatinine
  • Headache
  • Bruising

Contraindications

  • Active pathological bleeding
  • History of intracranial hemorrhage
  • Severe hepatic impairment
  • Concurrent strong CYP3A4 inhibitors (ketoconazole, itraconazole, clarithromycin)
  • Concurrent strong CYP3A4 inducers (rifampin, phenytoin, carbamazepine)
Interactions

Interaction records.

SeriousConflict

St. John's Wort

Ticagrelor is metabolised by CYP3A4 and is a P-glycoprotein substrate. St. John's wort potently induces both, and the model CYP3A4/P-gp inducer rifampin reduces ticagrelor AUC by 86% and Cmax by 73%, with a measurable loss of platelet inhibition. The same effect is expected with St. John's wort, risking treatment failure (stent thrombosis, MI, stroke).

Recommendation: Avoid St. John's wort while on ticagrelor. If you have been taking both, stop the St. John's wort and tell your prescriber so antiplatelet adequacy can be reassessed (e.g., platelet reactivity testing if available).

SeriousCaution

Ginkgo Biloba

Ginkgo biloba inhibits platelet-activating factor and platelet aggregation. Added to ticagrelor's reversible P2Y12 inhibition, the antiplatelet effect of ginkgo creates an additive bleeding risk, including the spontaneous intracranial and ocular bleeding reported in ginkgo case literature.

Recommendation: Avoid ginkgo biloba while on ticagrelor. If you have been combining them, stop the ginkgo and call your prescriber if you notice unusual bruising, nosebleeds, or any sign of bleeding.

ModerateCaution

Garlic Extract

Concentrated garlic supplements inhibit platelet aggregation. Combined with ticagrelor's P2Y12 inhibition, garlic supplements stack antiplatelet activity and can raise bleeding risk, particularly perioperatively.

Recommendation: Avoid concentrated garlic supplements (aged garlic, allicin capsules) while on ticagrelor, and stop them at least 7 days before any planned surgery. Cooking with garlic is fine.

ModerateCaution

Fish Oil

Fish oil's omega-3 fatty acids reduce platelet thromboxane A2 generation and modestly prolong bleeding time. Added to ticagrelor's P2Y12 inhibition, high-dose fish oil (more than 3 g/day EPA+DHA) can additively raise bleeding risk, particularly around procedures.

Recommendation: Keep fish oil dose modest (≤2 g/day combined EPA+DHA) on ticagrelor and keep the dose constant. Stop fish oil at least 7 days before any planned surgery.

DangerousCaution

Nattokinase

Nattokinase can add fibrinolytic and anticoagulant effects to ticagrelor's potent antiplatelet action. Human studies show nattokinase lowers clotting-related proteins, and a published case report describes cerebellar hemorrhage after nattokinase was combined with aspirin. The combination is especially concerning in anyone with prior stroke, recent PCI, dual antiplatelet therapy, kidney disease, or upcoming procedures.

Recommendation: Avoid nattokinase while taking ticagrelor unless your cardiologist has explicitly approved it. Do not manage this by separating doses because both effects persist beyond the dosing window. Get urgent help for severe headache, one-sided weakness, black stools, vomiting blood, or uncontrolled bleeding.

Sources

Sources, by evidence tier.

Numbered references. Citations throughout the page link here.

Meta-analyses & systematic reviews

5
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Deep dives & adjacent profiles.

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