Ticagrelor

What is Ticagrelor?

• Ticagrelor (Brilinta) is a P2Y12 platelet inhibitor used for the prevention of stroke, heart attack and other events in people with acute coronary syndrome, meaning problems with blood supply in the coronary arteries.

Ticagrelor structure

Ticagrelor3

Ticagrelor ball-and-stick animation

What are the uses of this medicine?

Ticagrelor (Brilinta) is a prescription medicine used to:

• decrease your risk of death, heart attack, and stroke in people with a blockage of blood flow to the heart (acute coronary syndrome or ACS) or a history of a heart attack. Brilinta can also decrease your risk of blood clots in your stent in people who have received stents for the treatment of ACS.
• decrease your risk of a first heart attack or stroke in people who have a condition where the blood flow to the heart is decreased (coronary artery disease or CAD) who are at high risk for having a heart attack or stroke.
• decrease your risk of stroke in people who are having a stroke (acute ischemic stroke) or mini-stroke (transient ischemic attack or TIA).

How does this medicine work?

• Ticagrelor (tye ka' grel or) is a non-thienopyridine, reversible inhibitor of adenosine diphosphate (ADP) receptors (P2Y 12) on platelets and is used to decrease the risk of recurrent coronary thromboses in patients who undergo interventions during an acute coronary syndrome.
• Activated platelets release ADP which binds to ADP platelet receptors, causing activation of intracellular glycoprotein IIb/IIIA complex which triggers platelet adherence and aggregation.
• The aggregation of platelets plays an important role in the growth of atheromatous plaques, which can lead to coronary, cerebral and peripheral arterial occlusions.
• In clinical trials, ticagrelor therapy during acute coronary events (unstable angina and myocardial infarction) has been shown to decrease the frequency of recurrence of myocardial infarction and stent thrombosis.

Who Should Not Use this medicine ?

This medicine cannot be used in patients who:

• have a history of bleeding in the brain
• are bleeding now
• are allergic to ticagrelor or any of the ingredients in Brilinta.

What drug interactions can this medicine cause?

• Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements.

Be sure to mention any of the following:

• anticoagulants (blood thinners) such as warfarin (Coumadin, Jantoven)
• heparin
• Other medications to treat or prevent blood clots; or regular use of non-steroidal anti-inflammatory medications such as ibuprofen (Advil, Motrin) and naproxen (Aleve)
• antibiotics such as clarithromycin (Biaxin, in PrevPak) and telithromycin (Ketek)
• antifungal medications such as itraconazole (Onmel, Sporanox), ketoconazole (Nizoral), and voriconazole (Vfend)
• cholesterol-lowering medications such as lovastatin (Altoprev, in Advicor) and simvastatin (Zocor, in Simcor, in Vytorin)
• digoxin (Lanoxin)
• medications for high blood pressure
• medications for human immunodeficiency virus (HIV) such as atazanavir (Reyataz, in Evotaz), indinavir (Crixivan), nelfinavir (Viracept), ritonavir (Norvir, in Kaletra, in Viekira Pak), and saquinavir (Invirase)
• medications for seizures such as carbamazepine (Carbatrol, Equetro, Tegretol, others), phenobarbital, and phenytoin (Dilantin)
• nefazodone
• opioid (narcotic) medications for pain such as hydrocodone (in Hydrocet, in Vicodin, others), morphine (Avinza, Kadian, MSIR, others), or oxycodone (OxyContin, in Percocet, in Roxicet, others)
• rifampin (Rifadin, Rimactane, in Rifamate, in Rifater)

Is this medicine FDA approved?

• Ticagrelor was approved for use in the United States in 2011 and has been used in limited numbers of patients for a limited time only.
• Current indications are reduction of recurrent cardiovascular events in patients with acute coronary syndromes.

How should this medicine be used?

Recommended dosage: For Acute Coronary Syndrome or a History of Myocardial Infarction:

• Initiate treatment with 180 mg oral loading dose of Brilinta.
• Then administer 90 mg twice daily during the first year.
• After one year, administer 60 mg twice daily.

For Coronary Artery Disease but No Prior Stroke or Myocardial Infarction:

• Administer 60 mg Brilinta twice daily.

For Acute Ischemic Stroke or Transient Ischemic Attack (TIA):

• Initiate treatment with a 180 mg loading dose of Brilinta then continue with 90 mg twice daily for up to 30 days.

Administration:

• Ticagrelor comes as a tablet to take by mouth.
• Take Brilinta exactly as prescribed by your doctor.
• Your doctor will tell you how many Brilinta tablets to take and when to take them.
• Take Brilinta with aspirin as directed by your doctor.
• You may take Brilinta with or without food.
• Take your doses of Brilinta around the same time every day.
• If you forget to take your scheduled dose of Brilinta, take your next dose at its scheduled time. Do not take 2 doses at the same time unless your doctor tells you to.
• If you take too much Brilinta or overdose, call your doctor or poison control center right away, or go to the nearest emergency room.
• If you are unable to swallow the tablet whole, you may crush the Brilinta tablet and mix it with water. Drink all the water right away. Refill the glass with water, stir, and drink all the water.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As 60 mg and 90 mg tablets

This medicine is available in fallowing brand namesː

• Brilinta

What side effects can this medication cause?

The most common side effects of this medicine include:

• bleeding, dyspnea, headaches, nausea, diarrhea, hypotension and hypersensitivity reactions

Brilinta can cause serious side effects, including:

• bleeding that can be serious and sometimes lead to death
• Shortness of breath
• Irregular breathing

What special precautions should I follow?

• Drugs that inhibit platelet function including Brilinta increase the risk of bleeding.
• Advise patients daily doses of aspirin should not exceed 100 mg and to avoid taking any other medications that contain aspirin.
• Patients treated with Brilinta developed dyspnea. If a patient develops new, prolonged, or worsened dyspnea that is determined to be related to Brilinta, no specific treatment is required; continue Brilinta without interruption if possible. In the case of intolerable dyspnea requiring discontinuation of Brilinta, consider prescribing another antiplatelet agent.
• Discontinuation of Brilinta will increase the risk of myocardial infarction, stroke, and death in patients being treated for coronary artery disease. If Brilinta must be temporarily discontinued (e.g., to treat bleeding or for significant surgery), restart it as soon as possible. When possible, interrupt therapy with Brilinta for five days prior to surgery that has a major risk of bleeding.
• Brilinta can cause ventricular pauses. Bradyarrhythmias including AV block have been reported.
• Avoid use of Brilinta in patients with severe hepatic impairment. Severe hepatic impairment is likely to increase serum concentration of ticagrelor.
• Central sleep apnea (CSA) including Cheyne-Stokes respiration (CSR) has been reported. If central sleep apnea is suspected, consider further clinical assessment.
• Brilinta has been reported to cause false negative results in platelet functional tests for patients with Heparin Induced Thrombocytopenia (HIT).

Advise patients that they:

• Will bleed and bruise more easily
• Will take longer than usual to stop bleeding
• Should report any unanticipated, prolonged or excessive bleeding, or blood in their stool or urine.

• Advise patients to contact their doctor if they experience unexpected shortness of breath, especially if severe.
• Advise patients to inform physicians and dentists that they are taking Brilinta before any surgery or dental procedure.
• Advise women that breastfeeding is not recommended during treatment with Brilinta.
• Ticagrelor has been linked to rare instances of hypersensitivity reactions accompanied by mild liver injury.

What to do in case of emergency/overdose?

Symptoms of overdose may include:

• Bleeding is the expected pharmacologic effect of overdosing.
• Other effects of overdose may include gastrointestinal effects (nausea, vomiting, diarrhea) or ventricular pauses.

Management of overdosage:

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.
• There is currently no known treatment to reverse the effects of Brilinta, and ticagrelor is not dialyzable.
• Treatment of overdose should follow local standard medical practice.
• If bleeding occurs, appropriate supportive measures should be taken.
• Platelet transfusion did not reverse the antiplatelet effect of Brilinta in healthy volunteers and is unlikely to be of clinical benefit in patients with bleeding.
• Monitor the ECG.

Can this medicine be used in pregnancy?

• Available data from case reports with Brilinta use in pregnant women have not identified a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes.
• It is not known if Brilinta will harm your unborn baby. You and your doctor should decide if you will take Brilinta.

Can this medicine be used in children?

• The safety and effectiveness of Brilinta have not been established in pediatric patients.

What are the active and inactive ingredients in this medicine?

• Active ingredient: ticagrelor.

90 mg tablets:

• Inactive ingredients: mannitol, dibasic calcium phosphate, sodium starch glycolate, hydroxypropyl cellulose, magnesium stearate, hydroxypropyl methylcellulose, titanium dioxide, talc, polyethylene glycol 400, and ferric oxide yellow.

60 mg tablets:

• Inactive ingredients: mannitol, dibasic calcium phosphate, sodium starch glycolate, hydroxypropyl cellulose, magnesium stearate, hydroxypropyl methylcellulose, titanium dioxide, polyethylene glycol 400, ferric oxide black and ferric oxide red.

Who manufactures and distributes this medicine?

Distributed by:

• AstraZeneca Pharmaceuticals LP, Wilmington, DE

What should I know about storage and disposal of this medication?

• Store Brilinta at room temperature between 68°F to 77°F (20°C to 25°C).

• Dailymed label info on Ticagrelor
• FDA Ticagrelor

Ticagrelor Resources
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