Ticagrelor

Ticagrelor is a prescription medication used to lower your chance of having another heart attack or stroke in adults. Ticagrelor belongs to a group of drugs called antiplatelet medications, which help prevent platelets from forming clots that could lead to heart attacks and strokes.

This medication comes in tablet form and is usually taken twice a day, with or without food, along with a low dose of aspirin.

Some of the common side effects of ticagrelor include bleeding and shortness of breath.

CYP2C19 is an enzyme in the blood that is responsible for breaking down ticagrelor and other drugs in the body. Some patients have less of this protein in their bodies, affecting how much of the drug gets eliminated. Levels of CYP2C19 can vary greatly between individuals, and those having less of this protein are known as "poor metabolizers." 

CYP2C19 testing is done to determine whether you are a poor metabolizer. If you are a poor metabolizer, the levels of ticagrelor in your blood can become too high. As a result you may be at an increased risk of having more side effects from ticagrelor. 

Your doctor may adjust your dose of ticagrelor if you are a poor metabolizer.

Ticagrelor is a prescription medicine used, with aspirin, to prevent heart attacks and strokes in adults. Ticagrelor is used to prevent blood clots and is for people who:

• have had a recent heart attack or severe chest pain that happened because their heart was not getting enough oxygen.
• have had a heart attack or chest pain and are being treated with medicines or with a procedure to open blocked arteries in the heart.

This medication may be prescribed for other uses. Ask your doctor or pharmacist for more information.

Ticagrelor may be found in some form under the following brand names:

• Brilinta

Ticagrelor can cause serious side effects, including:

• Serious bleeding. See “Drug Precautions”

• Shortness of breath. Call your doctor if you have new or unexpected shortness of breath when you are at rest, at night, or when you are doing any activity. Your doctor can decide what treatment is needed.

This is not a complete list of ticagrelor side effects. Ask your doctor or pharmacist for more information.

Tell your doctor if you have any side effect that bothers you or that does not go away.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

Tell your doctor about all the medicines you take, including prescription and non-prescription medicines, vitamins, and herbal supplements. Ticagrelor may affect the way other medicines work, and other medicines may affect how ticagrelor works.

Especially tell your doctor if you take:

• an HIV-AIDS medicine
• medicine for heart conditions or high blood pressure
• medicine for high blood cholesterol levels
• an anti-fungal medicine by mouth
• an anti-seizure medicine
• a blood thinner medicine
• rifampin (Rifater, Rifamate, Rimactane, Rifadin)

This is not a complete list of ticagrelor drug interactions. Ask your doctor or pharmacist for more information.

Ticagrelor can cause bleeding that can be serious and sometimes lead to death. In cases of serious bleeding, such as internal bleeding, the bleeding may result in the need for blood transfusions or surgery. Call your doctor right away if you:

• bruise and bleed more easily
• have nose bleeds
• are having bleeding that is severe or that you cannot control
• have pink, red or brown urine
• are vomiting blood or your vomit looks like “coffee grounds”
• have red or black stools (looks like tar)
• are coughing up blood or blood clots

Do not stop taking ticagrelor without talking to the doctor who prescribes it for you. People who are treated with a stent, and stop taking ticagrelor too soon, have a higher risk of getting a blood clot in the stent, having a heart attack, or dying. If you stop ticagrelor because of bleeding, or for other reasons, your risk of a heart attack or stroke may increase.

When instructed by your doctor, you should stop taking ticagrelor 5 days before you have elective surgery. This will help to decrease your risk of bleeding with your surgery or procedure. Your doctor should tell you when to start taking ticagrelor again, as soon as possible after surgery.

Ticagrelor is taken with aspirin. You should not take a dose of aspirin higher than 100 mg daily because it can affect how well ticagrelor works. Do not take doses of aspirin higher than what your doctor tells you to take.

Do not take ticagrelor if you:

• are bleeding now
• have a history of bleeding in the brain
• have bleeding from your stomach or intestine now (an ulcer)
• have severe liver problems

Grapefruit and grapefruit juice may interact with ticagrelor and lead to potentially dangerous effects. Discuss the use of grapefruit products with your doctor.

Before you take ticagrelor, tell your doctor about all of your medical conditions including if you:

• have had bleeding problems in the past
• have had any recent serious injury or surgery
• plan to have surgery or a dental procedure
• have a history of stomach ulcers or colon polyps
• have lung problems, such as COPD or asthma
• have liver problems
• have a history of stroke
• are pregnant, or are plan to become pregnant
• are breastfeeding

Tell all of your doctors and dentists that you are taking ticagrelor. They should talk to the doctor who prescribed ticagrelor for you before you have any surgery or invasive procedure.

Tell your doctor about all the medicines you take, including prescription and non-prescription medicines, vitamins, and herbal supplements.

Tell your doctor if you are pregnant or plan to become pregnant.

The FDA categorizes medications based on safety for use during pregnancy. Five categories - A, B, C, D, and X, are used to classify the possible risks to an unborn baby when a medication is taken during pregnancy.

This medication falls into category C. In animal studies, pregnant animals were given this medication and had some babies born with problems. No well-controlled studies have been done in humans. Therefore, this medication may be used if the potential benefits to the mother outweigh the potential risks to the unborn child.

Tell your doctor if you are breastfeeding or plan to breastfeed. It is not known if ticagrelor passes into your breast-milk. You and your doctor should decide if you will take ticagrelor or breastfeed. You should not do both without talking with your doctor.

Ticagrelor comes as a tablet to be taken by mouth with or without food. It is usually taken two times a day.

Take your doses of ticagrelor around the same time each day. 

Take ticagrelor with a low dose (not more than 100 mg daily) of aspirin, as directed by your doctor. 

If you forget to take your scheduled dose of ticagrelor, take your next dose at its scheduled time. Do not take two doses at the same time unless your doctor tells you to.

Take ticagrelor exactly as prescribed by your doctor. Follow the directions on your prescription label carefully.

• The recommended loading dose of ticagrelor after an acute coronary syndrome (ACS) event is 180 mg (two 90 mg tablets).
• Following the loading dose, the recommended Brilinta dose is 90 mg twice daily for the first year after an ACS event. 
• After one year, ticagrelor 60 mg twice daily is recommended. 
• After the initial loading dose of aspirin (usually 325 mg), use ticagrelor with a daily maintenance dose of aspirin of 75-100 mg.

Your doctor will determine how long you should continue to take ticagrelor.

If you take too much ticagrelor, call your healthcare provider or local Poison Control Center, or seek emergency medical attention right away.

If ticagrelor is administered by a healthcare provider in a medical setting, it is unlikely that an overdose will occur. However, if overdose is suspected, seek emergency medical attention.

• Store ticagrelor at room temperature between 59°F to 86°F (15°C to 30°C).
• Keep ticagrelor and all medicines out of the reach of children.

WARNING: BLEEDING RISK

Ticagrelor, like other antiplatelet agents, can cause significant, sometimes fatal, bleeding.

Do not use ticagrelor in patients with active pathological bleeding or a history of intracranial hemorrhage.

Do not start ticagrelor in patients planned to undergo urgent coronary artery bypass graft surgery (CABG). When possible, discontinue ticagrelor at least 5 days prior to any surgery.

Suspect bleeding in any patient who is hypotensive and has recently undergone coronary angiography, percutaneous coronary intervention (PCI), CABG, or other surgical procedures in the setting of ticagrelor.

If possible, manage bleeding without discontinuing ticagrelor. Stopping ticagrelor increases the risk of subsequent cardiovascular events.

WARNING: ASPIRIN DOSE AND TICAGRELOR EFFECTIVENESS

Maintenance doses of aspirin above 100 mg reduce the effectiveness of ticagrelor and should be avoided. After any initial dose, use with aspirin 75-100 mg per day.