Ticagrelor

Ticagrelor tablets are approved for several heart and blood vessel conditions across multiple products.

• Reduces the risk of cardiovascular death, heart attack (myocardial infarction), and stroke in people with acute coronary syndrome (ACS) or a prior heart attack — Brilinta is noted to be superior to clopidogrel for at least the first 12 months after ACS
• Reduces the risk of stent thrombosis (blood clots in a coronary stent) in people stented for ACS treatment
• Reduces the risk of a first heart attack or stroke in people with coronary artery disease (CAD) at high risk — efficacy was established in a population with type 2 diabetes mellitus, though use is not limited to that group
• Brilinta (ticagrelor) tablets are approved to reduce the risk of stroke in adults with a mild acute ischemic stroke (low stroke severity score) or a high-risk transient ischemic attack (TIA)

Ticagrelor works by attaching to and blocking the P2Y12 receptor — a docking site on platelets (tiny blood cells that form clots). When this receptor is blocked, platelets cannot receive the chemical signal that tells them to clump together. This reversible blockade reduces the formation of dangerous clots in narrowed or stented arteries. Both ticagrelor and its active metabolite contribute equally to this effect.

Unlike some other antiplatelet drugs, ticagrelor's effect is reversible, meaning platelet function gradually returns after the medication is stopped — typically within a few days of the last dose.

Ticagrelor tablets are taken by mouth, typically twice a day, and can be taken with or without food. The dosing schedule and duration depend on what the medication is being used for — for example, ACS treatment involves a higher starting frequency that may change after the first year, while use for coronary artery disease without a prior stroke or heart attack uses a twice-daily schedule throughout. For mild acute ischemic stroke or TIA, treatment is generally continued for up to 30 days.

• Tablets may be crushed and mixed with water if swallowing whole is difficult — the mixture can also be given through a nasogastric tube
• If you miss a dose, take your next dose at its normally scheduled time — do not double up
• Do not combine with another oral P2Y12 platelet inhibitor

The most common side effects of ticagrelor tablets are bleeding and shortness of breath (dyspnea). Here is what to expect:

Seek emergency care for heavy or uncontrolled bleeding, signs of a stroke, or a severe allergic reaction (swelling of the face, lips, or throat). In rare cases, a serious blood disorder called Thrombotic Thrombocytopenic Purpura (TTP) has been reported — symptoms include unusual bruising, confusion, fever, and extreme fatigue.

• Serious bleeding risk: Ticagrelor can cause life-threatening bleeding. Never stop it suddenly without your doctor's okay — stopping increases the risk of heart attack, stroke, and death in people being treated for coronary artery disease. If bleeding occurs, doctors prefer to manage it without stopping the drug.
• Surgery precaution: If you need elective surgery with a major bleeding risk, your doctor will typically pause ticagrelor about five days beforehand and restart it as soon as it is safe to do so.
• Shortness of breath: About 14–21% of patients in clinical trials developed dyspnea (shortness of breath). It is usually mild, does not reflect a lung problem, and often eases over time. Tell your doctor if it becomes intolerable.
• Slow heart rate (bradyarrhythmia): Ticagrelor can cause ventricular pauses — brief moments where the heart skips a beat. People with certain pre-existing heart rhythm conditions not managed by a pacemaker may be at greater risk.
• Severe liver disease: Avoid ticagrelor in severe hepatic (liver) impairment, as it greatly increases drug exposure and bleeding risk.
• Central sleep apnea: Reported in post-marketing experience — tell your doctor if you or a partner notices breathing pauses during sleep.
• Lab test interference: Ticagrelor can cause false-negative results on certain platelet function tests used to diagnose a condition called Heparin-Induced Thrombocytopenia (HIT). Always tell your lab team you are on this medication.

Ticagrelor has several important drug interactions that can affect how well it works or raise your risk of side effects:

• Strong CYP3A inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, ritonavir) — greatly raise ticagrelor blood levels, increasing bleeding risk; avoid these combinations
• Strong CYP3A inducers (e.g., rifampin, phenytoin, carbamazepine, phenobarbital) — greatly lower ticagrelor levels, reducing its effectiveness; avoid these combinations
• Opioids (e.g., morphine, fentanyl) — slow ticagrelor absorption, which can delay its clot-preventing effect; your doctor may consider an injectable antiplatelet agent in ACS patients needing opioids
• Simvastatin and lovastatin — ticagrelor raises their blood levels by blocking the same enzyme; higher doses of these statins should be avoided to lower the risk of muscle damage (rhabdomyolysis)
• Rosuvastatin — ticagrelor raises rosuvastatin levels through a different mechanism; doses above a certain threshold should be avoided, especially in people already at higher risk for muscle injury
• Digoxin — ticagrelor can increase digoxin levels in the blood; your doctor should monitor digoxin closely when ticagrelor is started or the dose changes
• High-dose aspirin — doses of aspirin above the recommended maintenance range may reduce ticagrelor's effectiveness; stick to the low-dose aspirin your doctor recommends

Not a complete list. The label covers the interactions the manufacturer studied or reported, and our own interaction database does not cover every medicine either. Bring your full medication list, including vitamins and herbal products, to your pharmacist.

• History of intracranial hemorrhage (bleed inside the skull) — do not take ticagrelor; the risk of a repeat bleed is too high
• Active serious internal bleeding (such as a bleeding stomach ulcer or brain bleed) — do not take ticagrelor until the bleeding is resolved
• Allergy to ticagrelor or any component of the tablet — do not take it; severe allergic reactions including angioedema (dangerous swelling) have been reported
• Upcoming urgent coronary artery bypass graft (CABG) surgery — do not start ticagrelor; it should be paused for significant surgeries with major bleeding risk
• Severe liver (hepatic) impairment — avoid ticagrelor; the drug builds up to unsafe levels
• Moderate liver impairment — talk to your doctor; risks and benefits need to be weighed carefully
• Pregnancy — limited human data; animal studies showed potential harm at high doses; discuss risks with your doctor
• Breastfeeding — not recommended; it is unknown whether ticagrelor passes into human breast milk
• Children and adolescents — safety and effectiveness have not been established in pediatric patients
• Older adults (≥65) — no overall difference in safety or effectiveness was observed in clinical trials, but older patients should still be monitored carefully given bleeding risk
• End-stage renal disease on dialysis — ticagrelor is not removed by dialysis; drug levels are modestly higher, though platelet inhibition appears similar to people with normal kidney function

There is no known antidote for ticagrelor overdose, and the drug cannot be removed by dialysis. The main expected effect of too much ticagrelor is bleeding; if this occurs, supportive medical care should be given right away. Platelet transfusions are unlikely to help reverse ticagrelor's antiplatelet effect. An overdose may also cause nausea, vomiting, diarrhea, or irregular heart pauses, so heart monitoring (ECG) is recommended.

Ticagrelor inhibits the clumping of platelets by blocking the P2Y12 receptor. Its effect starts quickly — peak platelet inhibition is reached within about 2 hours of a dose and is maintained for at least 8 hours. Studies show that ticagrelor produces stronger and more consistent platelet inhibition compared to clopidogrel. After stopping ticagrelor, platelet function gradually returns over about 5 days. Switching from clopidogrel to ticagrelor can be done without a gap in antiplatelet protection.

Ticagrelor is absorbed from the gut within about 1.5 hours of swallowing a tablet, and can be taken with or without food — a high-fat meal has little meaningful effect on how much drug enters the bloodstream. The liver (mainly an enzyme called CYP3A4) breaks ticagrelor down into an active metabolite that contributes to its platelet-blocking effects. Ticagrelor has a half-life of about 7 hours (meaning the body clears half of it every 7 hours), and the active metabolite has a half-life of about 9 hours. Most of the drug leaves the body through the feces, with very little exiting in the urine — and it cannot be removed by dialysis.

Store at 20° to 25°C (68° to 77°F). Dispense in a tight container as defined in the USP using a child-resistant closure.