Reversible P2Y12 receptor inhibitor
Brand names: Brilinta, Brilique, Possia
Updated · Methodology
First line
First-line in dual antiplatelet therapy for acute coronary syndrome (NSTEMI, STEMI, unstable angina) per 2023 alongside prasugrel. Compared with clopidogrel, PLATO showed 16% reduction in cardiovascular death, MI, and stroke (NNT 53) without an increase in non-CABG major bleeding. Loading dose 180 mg; maintenance 90 mg twice daily for 12 months with aspirin 75–100 mg once daily.
Sources
ICD-10: I20-I22 · ICD-11: BA4Z
The drug is promoted for these uses outside international guidelines. Each entry below is analyzed against AEMPS, FDA, EMA, Cochrane and major RCTs.
Not recommended
Ticagrelor is an antiplatelet drug, a reversible P2Y12 receptor inhibitor. It is prescribed for acute coronary syndrome and for secondary prevention after myocardial infarction ( 2024, 2017). In biohacker and longevity circles, ticagrelor is occasionally promoted for primary CV prevention as a more modern alternative to aspirin. In people without confirmed coronary disease, stroke, or other high CV risk, no clinical studies of primary prevention with ticagrelor exist, and such prescription is dangerous. The drug has serious risks: severe bleeding (including life-threatening intracranial), dyspnea (common, in 14% of patients), bradycardia with syncope risk, and hyperuricemia. If ticagrelor was prescribed without confirmed ACS or post-MI, consider seeking a second opinion.
A direct reversible antagonist of platelet P2Y12 receptors. Unlike clopidogrel, no bioactivation is needed – effect within 30 minutes of the first dose, independent of CYP2C19 polymorphism. Effect is stronger and more predictable than clopidogrel. Half-life 7–9 hours; twice-daily dosing. After stopping, antiplatelet activity recovers within 5 days.
Boxed warning
FDA boxed warning: severe and fatal bleeding; not used in active bleeding or recent intracranial hemorrhage. Maximum aspirin dose 100 mg/day – higher doses reduce ticagrelor efficacy.
Limited pregnancy data. Use in pregnancy is not recommended.
No data. Not used during lactation.
Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.
Large amounts of grapefruit juice (three 200 ml glasses a day) doubled ticagrelor exposure in the study cited in the Brilique SmPC. The SmPC itself does not expect this rise to be clinically relevant for most patients. With heavy daily intake it makes sense to watch for bleeding, bruising after minor knocks and breathlessness, the typical adverse effects of ticagrelor.
Source: EMA: Ficha técnica de Brilique 90 mg comprimidos recubiertos con película (ticagrelor) (2026)
13 pairs found. Sorted from critical to minor.
Mechanism
CYP3A4 clears ticagrelor, and atazanavir inhibits this enzyme (atazanavir SmPC, , section 4.5). The ticagrelor SmPC classes atazanavir as a strong CYP3A4 inhibitor and expects the same effect as with ketoconazole. With ketoconazole, ticagrelor Cmax rose 2.4-fold and AUC 7.3-fold, while the active metabolite fell by 89% (Cmax) and 56% (AUC) (Brilique SmPC, EMA, section 4.5). Ticagrelor acts on platelets on its own, without the metabolite, so the antiplatelet effect and its adverse reactions rise with its concentration. The labels describe no effect of ticagrelor on atazanavir. When atazanavir is boosted with ritonavir, the booster is itself a strong CYP3A4 inhibitor and also appears in the ticagrelor contraindications (Brilique SmPC, EMA, section 4.3).
Symptoms
The main risk is bleeding: bruising, nosebleeds, blood in urine or stool, gastrointestinal bleeding and, at worst, intracranial bleeding. The second typical sign of excess ticagrelor is dyspnea: the ticagrelor label links strong CYP3A4 inhibitors directly to a higher risk of dyspnea, bleeding and other adverse events (section 7.1). The atazanavir SmPC () warns of a possible increase in the antiplatelet activity of ticagrelor (section 4.5).
Management
The combination is contraindicated: the ticagrelor SmPC bars it with strong CYP3A4 inhibitors and names atazanavir explicitly (Brilique SmPC, , sections 4.3 and 4.5). The atazanavir labels are softer: "not recommended" because of a possible increase in antiplatelet activity (atazanavir SmPC, EMA, section 4.5; Reyataz prescribing information, , section 7). The FDA ticagrelor label says to avoid strong CYP3A4 inhibitors including atazanavir (section 7.1). The strictest document wins, and in Spain the ban applies. For a patient on atazanavir who needs a P2Y12 inhibitor after an acute coronary syndrome, choose a different drug. Clopidogrel with atazanavir is also not recommended because its effect may weaken, while prasugrel needs no dose adjustment according to the atazanavir label (atazanavir SmPC, EMA, section 4.5; FDA, section 7). Whether prasugrel suits the individual patient is a question for its own label. If the patient is already taking both, do not drop ticagrelor without a replacement: stopping an antiplatelet drug in coronary artery disease raises the risk of myocardial infarction, stroke and death (Brilinta prescribing information, FDA, section 5.2). Plan the switch at once, and until then keep the higher risk of bleeding and dyspnea in mind (Brilinta, FDA, section 7.1). Investigate new, prolonged or worsening dyspnea on ticagrelor, and if the patient cannot tolerate it, stop ticagrelor (Brilique SmPC, EMA, section 4.4).
Sources
Mechanism
Clarithromycin is a strong CYP3A4 inhibitor. Ticagrelor rises 5-fold.
Symptoms
Bleeding.
Management
Combination contraindicated. Alternative – azithromycin (no CYP3A4 inhibition).
Sources
Mechanism
Strong CYP3A4 inhibitor – ticagrelor rises 5-7 fold. Section 4.3.
Symptoms
Bleeding.
Management
Combination contraindicated.
Sources
Mechanism
Ketoconazole inhibits CYP3A4. Ticagrelor rises 7-fold – severe bleeding risk. Brilinta Section 4.3 strict contraindication.
Symptoms
Spontaneous bleeding, including intracranial.
Management
Combination contraindicated.
Sources
Mechanism
Strongest CYP3A4 inhibitor. Ticagrelor rises 10+ fold.
Symptoms
Severe bleeding.
Management
Combination contraindicated.
Sources
Mechanism
Strong CYP3A4 inhibitor. Section 4.3.
Symptoms
Bleeding.
Management
Combination contraindicated.
Sources
Mechanism
Clopidogrel and ticagrelor block the same platelet receptor, P2Y12. Clopidogrel acts through an active metabolite and binds irreversibly, so affected platelets stay switched off for 7-10 days; ticagrelor binds reversibly and needs no bioactivation. The pair adds no benefit: after a loading dose ticagrelor already suppresses aggregation almost fully, and no trial has tested two oral P2Y12 inhibitors together. 2023 dual antiplatelet therapy is aspirin plus one P2Y12 inhibitor. Bleeding risk, meanwhile, is additive, as both product labels state.
Symptoms
Gum bleeding, epistaxis, bruising and haematomas after minor trauma, melaena, haematuria, a haemoglobin drop with no obvious source. Dyspnoea on ticagrelor is a drug effect of its own and usually has nothing to do with blood loss.
Management
Keep one P2Y12 inhibitor and stop the other the same day. Spacing the doses or halving both makes no sense. For acute-phase escalation, start ticagrelor with a 180 mg loading dose and drop clopidogrel at that moment, the way the 2017 international switching consensus describes it. For an elective switch outside the acute setting the Brilique SmPC gives a different anchor: the first dose 24 hours after the last dose of the other antiplatelet. On ticagrelor keep aspirin maintenance at or below 100 mg daily. Never stop both at once: premature withdrawal of antiplatelet therapy after an acute coronary syndrome raises the risk of infarction and death. After stopping the extra drug watch for bleeding over the next few days, and note that both labels require a 5-day pause before high-bleeding-risk procedures.
Sources
Mechanism
Ticagrelor inhibits P-glycoprotein, which clears digoxin. Digoxin peak concentration rises by 75%, AUC by 28% and trough levels by about 30%, doubling in some individuals.
Symptoms
Nausea, yellow vision, bradycardia.
Management
Measure serum digoxin before starting ticagrelor. Then reduce the digoxin dose by about 15–30% or give it less often, and keep monitoring levels ( digoxin label). Check digoxin levels when ticagrelor is started and after any change in its dose (FDA ticagrelor label). The ticagrelor label also requires appropriate clinical and laboratory monitoring with this combination. Ticagrelor itself can cause ventricular pauses and bradycardia, so use it with caution with drugs that slow the heart rate (EMA ticagrelor label). Take blood for digoxin just before the next dose or at least 6 hours after the last one (FDA digoxin label).
Sources
Mechanism
Enoxaparin blocks factor Xa and ticagrelor blocks platelet aggregation, so two separate points of haemostasis are hit at once. The enoxaparin label asks for medical supervision and laboratory monitoring when it is combined with antiplatelets, anti-inflammatory doses of salicylates and NSAIDs, and it also names thrombolytics and other anticoagulants.
Symptoms
Extensive bruising at injection sites, gum and nose bleeding, black stools, pink urine, unexplained back or abdominal pain that may indicate internal bleeding. Progressive anaemia shows as fatigue and pallor.
Management
The combination exists in hospital protocols for acute coronary syndrome, with defined doses, duration and monitoring. Outside that setting they are not stacked on personal initiative, still less with an NSAID on top. Monitor haemoglobin, platelets and renal function, since enoxaparin accumulates when filtration falls.
Sources
Mechanism
Strong CYP3A4 inducer – ticagrelor falls 86%. Antiplatelet effect lost – stent thrombosis risk.
Symptoms
Stent thrombosis, MI.
Management
Combination contraindicated. Alternative – clopidogrel or prasugrel.
Sources
Mechanism
Ticagrelor inhibits P-glycoprotein. Simvastatin rises 1.5-fold. Brilinta caps simvastatin at 40 mg/day.
Symptoms
Myalgia, rising CK.
Management
Cap simvastatin at 40 mg/day.
Sources
Mechanism
Aspirin irreversibly blocks platelet cyclooxygenase and ticagrelor reversibly blocks the P2Y12 receptor, so their antiplatelet effects add up. This is standard dual antiplatelet therapy after an acute coronary syndrome, and the ticagrelor label pairs it with a low daily dose of aspirin. The risk depends on the aspirin dose. In an exploratory analysis of the PLATO trial, ticagrelor's advantage over clopidogrel shrank as the aspirin dose rose. The Spanish label (AEMPS) therefore does not recommend maintenance aspirin doses above 300 mg, and the US label () advises keeping daily aspirin at 100 mg or less.
Symptoms
Bleeding risk adds up: bruising, gum bleeding, nosebleeds, black stools, blood in urine. Ticagrelor dyspnoea appears in the first weeks and does not by itself require stopping. High aspirin doses also add gastric discomfort.
Management
Aspirin stays at a low dose, usually 75–100 mg daily ( label, guidelines), and is not raised to analgesic regimens while ticagrelor lasts. For pain or fever use paracetamol rather than raising the aspirin dose or adding another NSAID. Dual antiplatelet therapy is not interrupted on personal initiative.
Sources
Mechanism
Ticagrelor acts directly on the P2Y12 receptor and needs no CYP2C19 activation, so the classic clopidogrel-omeprazole problem does not carry over to this pair. The ticagrelor label focuses its warnings on bleeding risk and on aspirin maintenance doses, not on proton pump inhibitors.
Symptoms
No symptoms attributable to the pairing. Ticagrelor's own continue: bruising, gum or nose bleeding, dyspnoea appearing in the first weeks and usually mild. Black stools or coffee-ground vomit remain alarm signs.
Management
Omeprazole can stay alongside ticagrelor when there is a gastric indication. What does not change is bleeding surveillance and the rule against stopping the antiplatelet on your own, since early withdrawal raises cardiovascular risk.
Sources
Verbatim lines from the interaction sections, in the language of the label
«La administración concomitante de ticagrelor con inhibidores potentes del CYP3A4 (p. ej., ketoconazol, claritromicina, nefazodona, ritonavir y atazanavir), ya que la administración concomitante puede…»AEMPS, section 4.3 · Open on CIMA
«La administración concomitante de ticagrelor con inhibidores potentes del CYP3A4 (p. ej., ketoconazol, claritromicina, nefazodona, ritonavir y atazanavir), ya que la administración concomitante puede…»AEMPS, section 4.3 · Open on CIMA
«La administración concomitante de ticagrelor con inhibidores potentes del CYP3A4 (p. ej., ketoconazol, claritromicina, nefazodona, ritonavir y atazanavir), ya que la administración concomitante puede…»AEMPS, section 4.3 · Open on CIMA
«La administración concomitante de ticagrelor con inhibidores potentes del CYP3A4 (p. ej., ketoconazol, claritromicina, nefazodona, ritonavir y atazanavir), ya que la administración concomitante puede…»AEMPS, section 4.3 · Open on CIMA
«Strong CYP3A Inhibitors: Strong CYP3A inhibitors substantially increase ticagrelor exposure and so increase the risk of dyspnea, bleeding, and other adverse events. Avoid use of strong inhibitors of…»FDA, section 7 · Open on DailyMed
«Inductores del CYP3A: La administración concomitante de rifampicina y ticagrelor redujo la C max y el AUC de ticagrelor en un 73% y un 86%, respectivamente. La C max del metabolito activo no varió y…»AEMPS, section 4.5 · Open on CIMA
«Strong CYP3A Inducers: Strong CYP3A inducers substantially reduce ticagrelor exposure and so decrease the efficacy of ticagrelor. Avoid use with strong inducers of CYP3A (e.g., rifampin, phenytoin…»FDA, section 7 · Open on DailyMed
«Medicamentos metabolizados por CYP3A4: Ticagrelor es un inhibidor leve del CYP3A4. No se recomienda la administración concomitante de ticagrelor con sustratos del CYP3A4 con índices terapéuticos…»AEMPS, section 4.5 · Open on CIMA
«Strong CYP3A Inhibitors: Strong CYP3A inhibitors substantially increase ticagrelor exposure and so increase the risk of dyspnea, bleeding, and other adverse events. Avoid use of strong inhibitors of…»FDA, section 7 · Open on DailyMed
«DRUG INTERACTIONS: Avoid use with strong CYP3A inhibitors or CYP3A inducers. ( 7.1 , 7.2 )»FDA, section 7 · Open on DailyMed
«Strong CYP3A Inhibitors: Strong CYP3A inhibitors substantially increase ticagrelor exposure and so increase the risk of dyspnea, bleeding, and other adverse events. Avoid use of strong inhibitors of…»FDA, section 7 · Open on DailyMed
«Strong CYP3A Inhibitors: Strong CYP3A inhibitors substantially increase ticagrelor exposure and so increase the risk of dyspnea, bleeding, and other adverse events. Avoid use of strong inhibitors of…»FDA, section 7 · Open on DailyMed
«Medicamentos metabolizados por CYP3A4: Simvastatina: la administración concomitante de ticagrelor y simvastatina aumentó la C max de la simvastatina en un 81% y el AUC en un 56%, y también aumentó la…»AEMPS, section 4.5 · Open on CIMA
«Simvastatin, Lovastatin, Rosuvastatin: Ticagrelor increases serum concentrations of simvastatin and lovastatin because these drugs are metabolized by CYP3A4. Avoid simvastatin and lovastatin doses…»FDA, section 7 · Open on DailyMed
«Inductores del CYP3A: La administración concomitante de rifampicina y ticagrelor redujo la C max y el AUC de ticagrelor en un 73% y un 86%, respectivamente. La C max del metabolito activo no varió y…»AEMPS, section 4.5 · Open on CIMA
«Strong CYP3A Inducers: Strong CYP3A inducers substantially reduce ticagrelor exposure and so decrease the efficacy of ticagrelor. Avoid use with strong inducers of CYP3A (e.g., rifampin, phenytoin…»FDA, section 7 · Open on DailyMed
«Inductores del CYP3A: La administración concomitante de rifampicina y ticagrelor redujo la C max y el AUC de ticagrelor en un 73% y un 86%, respectivamente. La C max del metabolito activo no varió y…»AEMPS, section 4.5 · Open on CIMA
«Strong CYP3A Inducers: Strong CYP3A inducers substantially reduce ticagrelor exposure and so decrease the efficacy of ticagrelor. Avoid use with strong inducers of CYP3A (e.g., rifampin, phenytoin…»FDA, section 7 · Open on DailyMed
«Ciclosporina (inhibidor de la P-gp y el CYP3A): No hay datos disponibles sobre el uso concomitante de ticagrelor con otros principios activos que también son inhibidores potentes de la P-gp e…»AEMPS, section 4.5 · Open on CIMA
«Inductores del CYP3A: La administración concomitante de rifampicina y ticagrelor redujo la C max y el AUC de ticagrelor en un 73% y un 86%, respectivamente. La C max del metabolito activo no varió y…»AEMPS, section 4.5 · Open on CIMA
«Strong CYP3A Inhibitors: Strong CYP3A inhibitors substantially increase ticagrelor exposure and so increase the risk of dyspnea, bleeding, and other adverse events. Avoid use of strong inhibitors of…»FDA, section 7 · Open on DailyMed
«Simvastatin, Lovastatin, Rosuvastatin: Ticagrelor increases serum concentrations of simvastatin and lovastatin because these drugs are metabolized by CYP3A4. Avoid simvastatin and lovastatin doses…»FDA, section 7 · Open on DailyMed
«Medicamentos metabolizados por CYP3A4: Simvastatina: la administración concomitante de ticagrelor y simvastatina aumentó la C max de la simvastatina en un 81% y el AUC en un 56%, y también aumentó la…»AEMPS, section 4.5 · Open on CIMA
«Simvastatin, Lovastatin, Rosuvastatin: Ticagrelor increases serum concentrations of simvastatin and lovastatin because these drugs are metabolized by CYP3A4. Avoid simvastatin and lovastatin doses…»FDA, section 7 · Open on DailyMed
«Ciclosporina (inhibidor de la P-gp y el CYP3A): No hay datos disponibles sobre el uso concomitante de ticagrelor con otros principios activos que también son inhibidores potentes de la P-gp e…»AEMPS, section 4.5 · Open on CIMA
«Strong CYP3A Inhibitors: Strong CYP3A inhibitors substantially increase ticagrelor exposure and so increase the risk of dyspnea, bleeding, and other adverse events. Avoid use of strong inhibitors of…»FDA, section 7 · Open on DailyMed
«Medicamentos conocidos por inducir bradicardia: Debido a las observaciones de pausas ventriculares, en su mayoría asintomáticas, y bradicardia, se debe tener precaución cuando se administre…»AEMPS, section 4.5 · Open on CIMA
«Medicamentos conocidos por inducir bradicardia: Debido a las observaciones de pausas ventriculares, en su mayoría asintomáticas, y bradicardia, se debe tener precaución cuando se administre…»AEMPS, section 4.5 · Open on CIMA
«Ciclosporina (inhibidor de la P-gp y el CYP3A): No hay datos disponibles sobre el uso concomitante de ticagrelor con otros principios activos que también son inhibidores potentes de la P-gp e…»AEMPS, section 4.5 · Open on CIMA
«Otros tratamientos concomitantes: Debido a las notificaciones de anomalías hemorrágicas cutáneas con ISRS (por ejemplo, paroxetina, sertralina y citalopram) se recomienda precaución al administrar…»AEMPS, section 4.5 · Open on CIMA
«DRUG INTERACTIONS: Avoid use with strong CYP3A inhibitors or CYP3A inducers. ( 7.1 , 7.2 )»FDA, section 7 · Open on DailyMed
«Medicamentos conocidos por inducir bradicardia: Debido a las observaciones de pausas ventriculares, en su mayoría asintomáticas, y bradicardia, se debe tener precaución cuando se administre…»AEMPS, section 4.5 · Open on CIMA
«DRUG INTERACTIONS: Monitor digoxin levels with initiation of or any change in ticagrelor. ( 7.5 )»FDA, section 7 · Open on DailyMed
«La administración concomitante con ticagrelor, ivabradina o ranolazina está contraindicada.»AEMPS, section 4.3 · Open on CIMA
«ANTICOAGULANTES /AEMPS, section 4.5 · Open on CIMA
«Agentes antitrombóticos: Ticagrelor»AEMPS, section 4.3 · Open on CIMA
«Established and Other Potentially Significant Drug Interactions: Antiplatelets ticagrelor clopidogrel ↑ ticagrelor ↓ clopidogrel active metabolite Coadministration with ticagrelor is not recommended…»FDA, section 7 · Open on DailyMed
«Established and Other Potentially Significant Interactions: ticagrelor ↑ ticagrelor Coadministration with ticagrelor is not recommended.»FDA, section 7 · Open on DailyMed
«Anticoagulantes y medicamentos antiagregantes plaquetarios: No hay experiencia o esta es limitada con los siguientes tratamientos que pueden aumentar el riesgo de sangrado cuando se utilicen de forma…»AEMPS, section 4.5 · Open on CIMA
«Ticagrelor: La coadministración de ticagrelor con simvastatina aumentó un 81% la C máx y un 56% el AUC de simvastatina y aumentó un 64% la C máx y un 52% el AUC de simvastatina ácida, con algunos…»AEMPS, section 4.5 · Open on CIMA
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Ticagrelor is evaluated for the following indications with varying evidence strength: Acute coronary syndrome (evidence tier A), Primary cardiovascular disease prevention (evidence tier F). See the full indication matrix with dosing and citations above on this page.
Common side effects of Ticagrelor (≥ 1 in 100): Dyspnea (15%, without organic cause, usually mild), Bleeding (epistaxis, gingival, hematoma), Headache, Gout flares (uric acid rise), Bradycardia (sinoatrial pauses). See the Safety section for uncommon and serious reactions.
Limited pregnancy data. Use in pregnancy is not recommended.
No data. Not used during lactation.
Ticagrelor is contraindicated in: Ticagrelor hypersensitivity; Active clinically significant bleeding; History of intracranial hemorrhage; Severe hepatic impairment; Concomitant strong CYP3A4 inhibitors. Full list in the Safety section.
FDA boxed warning: severe and fatal bleeding; not used in active bleeding or recent intracranial hemorrhage. Maximum aspirin dose 100 mg/day – higher doses reduce ticagrelor efficacy.
Direct links to regulator labels. Open in a new tab.
Acetylsalicylic acid, Apixaban, Clopidogrel, Dabigatran, Enoxaparin sodium, Nattokinase (serine protease from fermented soybean natto, Bacillus subtilis var. natto), Rivaroxaban, Warfarin