Antiplatelet (reversible P2Y12 inhibitor)
Ticagrelor is an antiplatelet medicine that prevents clot formation, used after a heart attack or acute coronary syndrome and to prevent stroke and heart attack. It reduces platelet stickiness, lowering the risk of further events.
Also known as: Ticagrelor, Brilinta
Ticagrelor + rifampicin: rifampicin reduces ticagrelor plasma concentration (CYP3A4 induction), decreasing the antiplatelet effect (QUADRO 2).
Ticagrelor is metabolised by CYP3A4 and rifampicin is a potent inducer of this enzyme, potentially drastically reducing the antiplatelet concentrations and compromising cardiovascular protection. QUADRO 2 of Annex 7 records this interaction in the ticagrelor section. The loss of antiplatelet efficacy is clinically relevant in patients with acute coronary syndrome or recent stent, increasing thrombotic risk. The combination should be avoided; if rifampicin is essential (e.g. tuberculosis), consider increasing the ticagrelor dose or using an alternative antiplatelet not dependent on CYP3A4 (e.g. prasugrel or clopidogrel according to profile). Monitor for ischaemic events.
Ticagrelor + rifampicin: CYP3A4 induction — marked reduction of ticagrelor and loss of antiplatelet efficacy; avoid or monitor.
Rifampicin induces CYP3A4 which metabolises ticagrelor — reduced plasma concentration and antiplatelet effect (QUADRO 2, Ticagrelor: "Ticagrelor plasma concentration is reduced by: Rifampicin").
Watch for thrombotic events (reinfarction, stent thrombosis).
Thrombotic event in a patient taking ticagrelor + rifampicin.
Avoid the combination; if unavoidable, consider adjustment or an alternative antiplatelet (e.g. clopidogrel with caution).
Prontuário Terapêutico do INFARMED (11th ed., 2012) — Annex 7, QUADRO 2 (Ticagrelor)
Ticagrelor + sertraline: possible increased bleeding risk when ticagrelor is used simultaneously with SSRIs (sertraline) (QUADRO 2).
Sertraline (SSRI) reduces serotonin uptake in platelets, decreasing their aggregation, and ticagrelor inhibits platelet aggregation via P2Y12 — the effect is additive and increases bleeding risk, especially gastrointestinal. QUADRO 2 of Annex 7 records this interaction in the ticagrelor section. The risk is higher in the elderly, history of peptic ulcer, or concomitant NSAIDs or anticoagulants. The combination is common and generally tolerated, but requires surveillance: warn about melena, bruising and haematuria, consider gastric protection and reassess if anaemia or bleeding appears.
Ticagrelor + sertraline: additive bleeding risk (antiplatelet + serotonin reuptake inhibition); watch for bleeding.
SSRIs (sertraline, citalopram, paroxetine) reduce platelet function (serotonin depletion) — additive effect with ticagrelor on the bleeding risk (QUADRO 2, Ticagrelor: "Possible increased bleeding risk when Ticagrelor is used simultaneously with: Citalopram, Paroxetine, Sertraline").
Monitor signs of bleeding (bruising, epistaxis, GI bleeding).
Bleeding in a patient taking ticagrelor + sertraline.
Use with caution; watch for signs of bleeding in the combination with SSRIs.
Prontuário Terapêutico do INFARMED (11th ed., 2012) — Annex 7, QUADRO 2 (Ticagrelor)
No documented food or drink interactions.
FDA label (4.1): contraindicated in patients with a history of intracranial haemorrhage (high risk of recurrent intracranial haemorrhage).
Contraindicated in patients with a history of intracranial haemorrhage.
DailyMed/FDA (NIH/NLM) — Ticagrelor (BRILINTA), 4.1: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=f7b3f443-e83d-4bf2-0e96-023448fed9a8
FDA label (4.2): contraindicated in patients with active pathological bleeding, such as bleeding peptic ulcer or recent intracranial haemorrhage.
Contraindicated in active pathological bleeding.
DailyMed/FDA (NIH/NLM) — Ticagrelor (BRILINTA), 4.2: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=f7b3f443-e83d-4bf2-0e96-023448fed9a8
Avoid in hepatic impairment.
Avoid use in hepatic impairment.
Prontuário Terapêutico do INFARMED (11th ed., 2012) — Annex 3, Drugs and hepatic impairment: Avoid in hepatic impairment.
FDA label (8.1): case report data in pregnant women have not identified a drug-associated risk of major birth defects, miscarriage or adverse maternal/fetal outcomes; in rats and rabbits, ticagrelor caused structural abnormalities in offspring at maternal doses ~5-7× the maximum recommended dose.
Limited data in pregnant women (post-marketing cases without identified risk); use if benefit justifies risk.
No specific breastfeeding data in the label (section 8.2 not detailed in extraction).
Not applicable (no specific contraception requirements in the label).
DailyMed/FDA (NIH/NLM) — approved Ticagrelor label (BRILINTA), section 8.1: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=f7b3f443-e83d-4bf2-0e96-023448fed9a8 ; Prontuário Terapêutico do INFARMED (11th ed., 2012) — Annex 2, Drugs and Breastfeeding: Contraindicated during breastfeeding.
Clinical and educational support tool. The information does not replace a medical prescription or the opinion of a qualified healthcare professional.
Antiplatelet: reversible inhibition of the platelet P2Y12 ADP receptor — prevents platelet activation and aggregation; the active metabolite is approximately equipotent (FDA label 12.1).
Direct and reversible inhibition of the P2Y12 receptor (no metabolic activation required for the antiplatelet effect).
Absorption: median Tmax of 1.5 h (range 1.0-4.0); mean absolute bioavailability of ~36% (range 30-42%); may be taken with or without food (12.3).
Metabolism by CYP3A4/3A5 to the active metabolite AR-C124910XX (equipotent); CYP3A4 substrate and moderate inhibitor (7.1/7.2).
Half-life of ticagrelor of approximately 7 hours; of the active metabolite approximately 9 hours (12.3).
