Ticagrelor: 7 things you should know

Medically reviewed by Carmen Pope, BPharm. Last updated on May 20, 2024.

1. How it works

• Ticagrelor is an antiplatelet agent that may be given together with aspirin to people who have had a heart attack or to those with acute coronary syndrome (ACS) to reduce their risk of having a stroke or other heart problems. Ticagrelor is available as a generic and the brand name drug Brilinta.
• Ticagrelor works differently from other antiplatelet agents, such as aspirin, clopidogrel, and prasugrel. Although it still blocks a substance called ADP (adenosine-5-diphosphate) which plays a crucial role in blood clotting, it does it by reversibly binding to a receptor called P2Y12 on the platelet surface. Reversible binding means platelet activity is restored once concentrations of Ticagrelor decrease below a certain level, in contrast to other antiplatelet agents such as clopidogrel and prasugrel which bind irreversibly for the life of the platelet.
• Ticagrelor prevents platelets in your blood from sticking together to form an unwanted blood clot that could block an artery. Platelets are tiny blood cells that clump and stick together to repair a damaged blood vessel. Ticagrelor keeps blood flowing smoothly.
• Ticagrelor belongs to the class of medicines known as platelet aggregation inhibitors. It may also be called a P2Y12 inhibitor or an antiplatelet agent.

2. Upsides

• Ticagrelor may be given together with aspirin to people who have had a heart attack or with acute coronary syndrome (ACS), to reduce their risk of having a stroke or other heart problems.
• Ticagrelor may also be given to people who have had a stent inserted to reduce the rate of stent thrombosis (a blood clot forming and blocking an area near a stent).
• Ticagrelor may also be given to some people with other heart conditions who are intolerant to aspirin.
• Ticagrelor works more quickly than clopidogrel (Plavix). Within 30 minutes, a 180mg loading dose of Ticagrelor inhibited 41% of platelets. It takes almost 8 hours for clopidogrel 600mg to achieve this same effect.
• Crushing tablets and then administering them appears to make ticagrelor work more quickly.
• Ticagrelor is not a prodrug. This means it does not require metabolism to be active, unlike clopidogrel and prasugrel. Because clopidogrel is a prodrug and requires conversion in the liver to its active version, clinical response to clopidogrel is variable with 20–40% of patients being classified as non-responders, poor responders, or resistant to clopidogrel.
• Ticagrelor has an active metabolite that is equally as potent and active as the parent drug, ticagrelor. This increases how long it works.
• Ticagrelor is an oral medication that is usually taken twice a day.
• Ticagrelor is currently recommended over clopidogrel by current guidelines for people with ACS or following a myocardial infarction (heart attack). Trials have found ticagrelor is more effective than clopidogrel at reducing the percentage of CV death, MI, or stroke in the first year of treatment in people taking low-dose aspirin. Apart from genetics (including variations in CYP2C19), other factors that affect the response to clopidogrel include age, diabetes, renal failure, and cardiac failure.
• Ticagrelor is more potent than clopidogrel. Side effects, such as bleeding and bruising are similar although ticagrelor is more likely to cause shortness of breath.
• A dosage adjustment is needed in people with mild liver disease or kidney disease. Avoid ticagrelor in people with severe liver disease; there is limited experience in those with moderate liver disease.
• Ticagrelor is available as a generic and as the brand name drug Brilinta.

3. Downsides

If you are between the ages of 18 and 60, take no other medication or have no other medical conditions, side effects you are more likely to experience include:

• Bleeding, shortness of breath (dyspnea), dizziness, and nausea are the most common side effects reported with ticagrelor.
• Ticagrelor carries a Boxed Warning on its label about bleeding risks because, like other antiplatelet agents, ticagrelor can cause significant, sometimes fatal bleeding. If possible, manage bleeding without discontinuing ticagrelor, because stopping it increases the risk of subsequent cardiovascular events. Do not use ticagrelor in patients with active pathological bleeding or a history of intracranial (within the skull) hemorrhage. Do not start it in patients undergoing urgent coronary artery bypass graft surgery (CABG).
• If ticagrelor is discontinued too soon, it can increase a person's risk of a heart attack, stroke, or death. However, ticagrelor may be temporarily discontinued five days before surgery.
• Although ticagrelor is usually given with aspirin to people who have had a heart attack or who have a condition called acute coronary syndrome (ACS), to reduce their risk of having a stroke or other heart problems, dosages of aspirin greater than 100mg/day should NOT be given because this will reduce the effectiveness of ticagrelor.
• Ticagrelor should not be used in people with an active peptic ulcer, following an intracranial hemorrhage, or who have active bleeding conditions. There is limited experience in using ticagrelor in people with moderate to severe liver disease. Avoid in severe liver disease.
• Although case reports have not shown an increase in major birth defects with ticagrelor, animal studies, using more than the maximum recommended dose of ticagrelor, have shown an increased risk of structural abnormalities, pup death, and growth delays. Advise women to use adequate contraception to ensure they do not become pregnant while taking ticagrelor and to tell their doctor immediately if they become pregnant inadvertently. Breastfeeding is not recommended during treatment with ticagrelor.

Note: In general, seniors or children, people with certain medical conditions (such as liver or kidney problems, heart disease, diabetes, seizures) or people who take other medications are more at risk of developing a wider range of side effects. View complete list of side effects

4. Bottom Line

Ticagrelor blocks a substance called ADP (adenosine-5-diphosphate) which plays a crucial role in blood clotting and may be given together with aspirin to people who have had a heart attack or with acute coronary syndrome (ACS) to reduce their risk of having a stroke or other heart problems. Bleeding, shortness of breath (dyspnea), dizziness, and nausea are the most common side effects reported with ticagrelor. Studies report ticagrelor to be more effective than clopidogrel (Plavix) at reducing the risk of CV death, MI, or stroke in the first year of treatment.

5. Tips

• Ticagrelor is an oral tablet that is usually taken twice a day, in the morning and the evening. Ticagrelor can be taken with or without food and is usually given with a daily maintenance dose of aspirin. The first dose of ticagrelor may be higher than subsequent doses. This is called a loading dose and it helps ticagrelor to reach effective levels faster.
• Do not stop ticagrelor suddenly without talking to your cardiologist first. If ticagrelor is discontinued too soon, it can increase a person's risk of a heart attack, stroke, or death. However, if you are having surgery, your doctor may instruct you to stop taking ticagrelor 5 days before your procedure. This will help to lower the chance of bleeding. Follow your doctor’s directions on when to stop and start taking ticagrelor again.
• Do not drink grapefruit juice while taking ticagrelor. Grapefruit juice can inhibit (block) one of the enzymes (3A4) needed to break down ticagrelor for excretion from the body. Theoretically, drinking grapefruit juice with ticagrelor may increase the antiplatelet effect of your medicine and increase the risk of bleeding. Ask your doctor about this possible drug-food interaction.
• Ticagrelor does not have the same dietary restrictions as warfarin has, and you do not need to worry about eating green leafy vegetables like spinach, broccoli, kale, or other vitamin K-rich foods with ticagrelor.
• Drinking alcohol with ticagrelor is not recommended because you will also be taking aspirin. Combining aspirin with alcohol can lead to stomach bleeding and ulcers. Tell your healthcare provider if you have a history of stomach ulcers or digestive tract bleeding. Call your doctor at once if you have symptoms of bleeding in your stomach or intestines. This includes black, bloody, or tarry stools, or coughing up blood or vomit that looks like coffee grounds.
• Do not take any other medications, including those brought from a supermarket or drug store, without talking to your doctor or a pharmacist first. If you need a mild pain reliever, it is safe to take acetaminophen (Tylenol) with ticagrelor. Many nonprescription, over-the-counter (OTC) products contain aspirin, ibuprofen (Advil, Motrin), or naproxen (Aleve) which are not suitable for use with ticagrelor. These ingredients can also be found in combination products used for cold or flu symptoms or sleep. Be sure to check the labels for these ingredients. Ask your pharmacist if you are not sure.
• You may notice that you bruise or bleed more easily and it will take longer to stop bleeding while you are taking ticagrelor. This shows that ticagrelor is working. However, if bleeding is excessive, or prolonged, or you notice blood in your urine or stool, seek urgent medical advice.
• Seek prompt medical attention if you develop a fever, weakness, yellowing of the skin or eyes, feel confused, or your skin looks extremely pale.
• Tell your dentist and other health professionals that you are taking ticagrelor before an invasive procedure is scheduled.
• Although an increased risk of major birth defects has not been reported in case studies investigating ticagrelor use during pregnancy, animal studies using more than the maximum recommended dose did show an increased risk of structural abnormalities, pup death, and growth delays. If you are taking ticagrelor you should tell your doctor if you are planning a pregnancy before conceiving or if you become pregnant inadvertently. Breastfeeding is not recommended during treatment with ticagrelor.

6. Response and effectiveness

• Ticagrelor works more quickly than clopidogrel (Plavix). Within 30 minutes, a 180mg loading dose of ticagrelor inhibited 41% of platelets. It takes almost 8 hours for clopidogrel 600mg to achieve this same effect.
• Maximum platelet inhibition (88% inhibition) was reached two hours after a dose of ticagrelor. Crushing tablets and then administering them appears to hasten the time to peak concentrations. Maximum platelet inhibition lasts for another six hours (eight hours total). 24 hours after a dose of ticagrelor, platelet inhibition is still 58%. It takes 56 hours (over 2 days) for platelet inhibition to drop to 56% and 110 hours (over 4 days) for platelet inhibition to drop to 10%.
• Ticagrelor is typically used for 6 to 12 months, or longer, after a stent or heart attack. It is given with low-dose aspirin to help prevent blood clots. Based on the use, ticagrelor may be given for different amounts of time.
• For at least one year after ACS, ticagrelor has been found in studies to be better than the use of another antiplatelet drug known as clopidogrel (Plavix).
• In studies of high-risk patients with coronary artery disease (CAD) and type-2 diabetes, at 36 months, the combined use of aspirin plus ticagrelor 60 mg was significantly more effective at preventing a major event such as heart attack or stroke when compared to taking aspirin alone.
• In studies, ticagrelor or a placebo was given to patients with an acute ischemic stroke or TIA within 24 hours of onset. Treatment was continued for a median of 30 days. ticagrelor was found to be superior to a placebo in reducing the rate of a composite of stroke and death (the primary endpoint). The manufacturer suggests treatment be continued for up to 30 days. The treatment effect accrued early in the course of therapy
• Depending on the use, the first dose of ticagrelor may be given as a loading dose which is a higher dose to help achieve therapeutic levels more quickly. The manufacturer has shown that ticagrelor typically works to inhibit platelets within 30 minutes of taking this loading dose (two 90 mg tablets). However, one small, open-label study demonstrated that despite giving a ticagrelor loading dose, it can take from 2 to 11 hours to reach adequate platelet inhibition in patients who have had a heart attack and are receiving a stent.
• Responses can be different for different patients, and some patients may need additional antiplatelet therapy when undergoing a stent placement after a heart attack to prevent stent thrombosis.
• Using PLATO clinical trial figures ticagrelor appears to be more effective than Plavix at reducing the risk of CV death, MI, or stroke in the first year of treatment.

7. Interactions

Medicines that interact with ticagrelor may either decrease its effect, affect how long it works, increase side effects, or have less of an effect when taken with ticagrelor. An interaction between two medications does not always mean that you must stop taking one of the medications; however, sometimes it does. Speak to your doctor about how drug interactions should be managed.

There are over 400 medications that interact with ticagrelor. Common medications that may interact with ticagrelor include:

• aspirin (dosages greater than 100mg)
• amiodarone
• apalutamide
• apixaban
• aprepitant
• bismuth subsalicylate
• calcium channel blockers such as diltiazem or verapamil
• cholesterol-lowering agents, such as simvastatin or lovastatin
• cobicistat
• dabigatran
• dalteparin
• digoxin
• erythromycin
• fluconazole, ketoconazole, or voriconazole
• grapefruit juice
• herbals, such as Dong Quai or echinacea
• mifepristone
• NSAIDs, such as celecoxib, ibuprofen, diclofenac, etodolac, and naproxen
• opioids, such as methadone, morphine, or oxycodone (can delay and reduce the absorption of ticagrelor and its active metabolite possibly due to slowed gastric emptying)
• repaglinide
• steroids such as dexamethasone
• strong CYP3A inducers such as rifampin, phenytoin, carbamazepine, and phenobarbital (substantially reduce the efficacy of ticagrelor). Avoid
• strong CYP3A inhibitors such as itraconazole, ketoconazole, voriconazole, clarithromycin, nefazodone, atazanavir, indinavir, nelfinavir, ritonavir, saquinavir, and telithromycin (substantially increase the risk of side effects such as dyspnea or bleeding). Avoid
• ticlopidine
• tinzaparin
• tramadol
• warfarin and other anticoagulants.

In general, any medicine that can increase the risk of bleeding (such as aspirin, corticosteroids, SSRI antidepressants [eg, citalopram, duloxetine, fluoxetine, venlafaxine], enoxaparin, fish oils) may interact with ticagrelor.

Note that this list is not all-inclusive and includes only common medications that may interact with ticagrelor You should refer to the prescribing information for ticagrelor for a complete list of interactions.

References

Ticagrelor. Updated 01/2023. Amneal Pharmaceuticals NY LLC https://www.drugs.com/pro/ticagrelor.html

Further information

Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use ticagrelor only for the indication prescribed.

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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