Ticagrelor Intas: Uses, Dosage & Side Effects

What Is Ticagrelor Intas and What Is It Used For?

Ticagrelor Intas is a generic antiplatelet medicine containing ticagrelor 60 mg. It is prescribed together with low-dose aspirin to reduce the risk of atherothrombotic events (heart attack, stroke and cardiovascular death) in adult patients who had a myocardial infarction at least one year previously and remain at high risk of further events.

Ticagrelor Intas is a generic version of ticagrelor manufactured by Intas Pharmaceuticals. The original brand-name product is known as Brilique in Europe and Brilinta in the United States, developed by AstraZeneca. Generic ticagrelor contains exactly the same active ingredient, at the same strength, and must meet strict bioequivalence requirements set by the European Medicines Agency (EMA), U.S. Food and Drug Administration (FDA) and other regulatory authorities before it can be marketed.

Ticagrelor belongs to a class of medicines called antiplatelet agents, and more specifically to the subgroup of P2Y12 receptor antagonists. Platelets are small cells circulating in the blood that play a central role in blood clotting. When a blood vessel is damaged – such as when an atherosclerotic plaque ruptures inside a coronary artery – platelets are activated and clump together (aggregate) to form a clot. In people with cardiovascular disease, this clotting process can block an artery and cause a heart attack or stroke. Antiplatelet medicines reduce the tendency of platelets to clump, making dangerous blood clots less likely.

Ticagrelor is chemically classified as a cyclopentyltriazolopyrimidine (CPTP), distinct from the older thienopyridine class that includes clopidogrel and prasugrel. It has two important pharmacological features that set it apart from other P2Y12 inhibitors. First, it is a direct-acting drug: unlike clopidogrel, ticagrelor does not need to be converted into an active form by liver enzymes. This means its effect is more predictable, faster in onset, and less affected by genetic variation in the CYP2C19 enzyme. Second, ticagrelor binds reversibly to the P2Y12 receptor. When ticagrelor is stopped, platelet function recovers within 3–5 days, compared with 7–10 days for clopidogrel and prasugrel, which bind irreversibly.

Approved indications

Ticagrelor is approved for two main cardiovascular indications, distinguished by the strength used:

• Acute coronary syndrome (ACS) – 90 mg strength: For the first 12 months after a heart attack or unstable angina, given as a 180 mg loading dose followed by 90 mg twice daily together with low-dose aspirin. This indication is not served by the 60 mg Ticagrelor Intas tablets.
• Long-term secondary prevention – 60 mg strength (the focus of this article): In adults with a history of myocardial infarction of at least one year and a high risk of atherothrombotic events, ticagrelor 60 mg twice daily is given together with low-dose aspirin to reduce the risk of cardiovascular death, myocardial infarction or stroke.

High-risk features that support the use of long-term ticagrelor 60 mg include age 65 years or older, diabetes requiring medication, a second prior spontaneous myocardial infarction, multivessel coronary artery disease and chronic non-end-stage kidney dysfunction. The balance of benefits and bleeding risk must be assessed for each patient individually by the treating cardiologist or internist.

Ticagrelor is also used off-label or in specific regional approvals for secondary stroke prevention in selected patients, for example in combination with aspirin for short-term dual antiplatelet therapy after a minor ischaemic stroke or transient ischaemic attack (TIA) of atherosclerotic origin, based on the THALES trial. However, the 60 mg strength is not typically used for these indications.

Mechanism of action in detail

To understand why ticagrelor is effective, it helps to know how platelets are activated. When a blood vessel is injured, a molecule called adenosine diphosphate (ADP) is released. ADP binds to a specific receptor on the platelet surface called the P2Y12 receptor, which triggers a cascade of events that lead to platelet activation, shape change and aggregation. Ticagrelor blocks this process by binding to a site on the P2Y12 receptor that is distinct from where ADP normally binds. This is called allosteric inhibition, and it prevents the receptor from responding to ADP even when ADP is present in high concentrations.

An interesting secondary property of ticagrelor is that it also inhibits the cellular reuptake of adenosine. This increases adenosine levels in the blood and may contribute to some of ticagrelor's distinctive effects, including its rapid vasodilation, the common side effect of dyspnoea (shortness of breath), and possibly some of its protective cardiovascular effects beyond platelet inhibition. This adenosine-mediated effect is not seen with clopidogrel or prasugrel and is one reason why ticagrelor has a somewhat different side-effect profile.

What Should You Know Before Taking Ticagrelor Intas?

Before starting Ticagrelor Intas, tell your doctor about any history of bleeding, intracranial haemorrhage, liver disease, severe asthma or COPD, gout, bradyarrhythmias, or planned surgery. Ticagrelor must not be used in patients with active bleeding, a history of brain haemorrhage or severe hepatic impairment.

It is essential to discuss your full medical history and all medicines you take with your doctor before starting Ticagrelor Intas. Several conditions can alter the balance between the benefits of treatment (prevention of heart attacks and strokes) and the risks (mainly bleeding). The information below is a guide, but every decision should be individualised between you and your healthcare provider.

Contraindications

You must not take Ticagrelor Intas if:

• You are allergic to ticagrelor or to any of the other ingredients in the tablets (listed in the “Contents” section)
• You have an active pathological bleeding, such as a bleeding stomach or duodenal ulcer
• You have ever had a bleeding stroke (intracranial haemorrhage)
• You have severe liver disease (Child-Pugh class C or severe hepatic impairment)
• You are taking a strong CYP3A4 inhibitor such as ketoconazole, itraconazole, voriconazole, clarithromycin, nefazodone or ritonavir, because these drugs substantially increase ticagrelor blood levels and bleeding risk

If any of these apply to you, tell your doctor or pharmacist immediately and do not take Ticagrelor Intas.

Warnings and precautions

Speak with your doctor or pharmacist before taking Ticagrelor Intas if any of the following situations apply to you:

• You have an increased risk of bleeding, for example recent trauma or surgery, a bleeding disorder, active or recent gastrointestinal bleeding, or very low body weight (below 60 kg)
• You are scheduled for surgery or dental procedures. Ticagrelor should normally be stopped at least 5 days before elective major surgery to reduce bleeding complications
• You have had a previous ischaemic stroke. In patients with a history of stroke who did not have a recent heart attack, ticagrelor is generally not recommended
• You have moderate liver disease. Ticagrelor is not recommended in severe hepatic impairment and should be used with caution in moderate impairment; no dose adjustment is required in mild hepatic impairment
• You have slow heart rate problems (bradyarrhythmias). Ticagrelor can cause transient ventricular pauses, particularly in patients with sick sinus syndrome, second- or third-degree atrioventricular (AV) block, or previous syncope attributed to bradycardia who do not have a pacemaker
• You have asthma or chronic obstructive pulmonary disease (COPD). Ticagrelor can worsen shortness of breath; inform your doctor so lung function can be assessed if needed
• You have gout or elevated uric acid levels. Ticagrelor can increase serum uric acid levels and may precipitate gout attacks in predisposed patients
• You have kidney problems. Although no dose adjustment is needed, rare cases of creatinine increase have been reported in patients with severe renal impairment, particularly those over 75 years of age or with comorbid diabetes

Because ticagrelor increases bleeding risk, cuts and injuries may bleed longer than usual. Carry a wallet card or medical alert identification stating that you take an antiplatelet medicine, so that in an emergency (road accident, sudden collapse, etc.) the treating team is aware immediately. Always inform all healthcare providers – including dentists and alternative-medicine practitioners – that you take ticagrelor before any procedure.

Pregnancy and breastfeeding

Ticagrelor Intas is not recommended during pregnancy. Adequate and well-controlled studies in pregnant women have not been conducted, and animal studies have shown reproductive toxicity at high doses. Women of childbearing potential should use effective contraception while taking ticagrelor. If you become pregnant or suspect you may be pregnant while on treatment, contact your doctor immediately for advice on whether to continue, switch or stop the medicine.

It is not recommended to breastfeed while taking ticagrelor. Available animal data suggest that ticagrelor and its active metabolite are excreted in breast milk. A decision should be made whether to discontinue breastfeeding or to discontinue or avoid the drug, considering the importance of the medicine for the mother.

Children and adolescents

The safety and efficacy of ticagrelor in children and adolescents under 18 years of age have not been established. Ticagrelor Intas is not approved for paediatric use. The HESTIA 3 trial in paediatric sickle cell disease did not demonstrate efficacy, and the drug is not recommended in this population.

Elderly patients

No dose adjustment is required for elderly patients (65 years and older). However, older adults may have a higher risk of bleeding, falls and drug interactions, and should be monitored more closely. The need for long-term 60 mg dual antiplatelet therapy should be re-evaluated regularly, balancing ongoing ischaemic risk against bleeding risk.

Driving and using machines

Ticagrelor has negligible effects on the ability to drive and use machines. Some patients report dizziness or confusion during treatment; if you experience these, do not drive or operate machinery until the symptoms resolve.

Excipients

Ticagrelor Intas tablets may contain excipients such as mannitol. Patients with rare hereditary problems of fructose intolerance should not take this medicine. Always check the specific product information provided with your pack, as formulations can vary slightly between manufacturers.

How Does Ticagrelor Intas Interact with Other Drugs?

Ticagrelor is metabolised mainly by CYP3A4 and interacts with numerous medicines. Strong CYP3A inhibitors (ketoconazole, clarithromycin, ritonavir) are contraindicated. Strong CYP3A inducers (rifampicin, phenytoin, carbamazepine) should be avoided. Care is needed with simvastatin, digoxin, opioids, anticoagulants and NSAIDs.

Tell your doctor or pharmacist about all medicines you take, have recently taken or might take – including over-the-counter medicines, herbal products and supplements. Some interactions can substantially affect the safety or effectiveness of Ticagrelor Intas. Understanding these interactions is critical for safe long-term use.

Major interactions (contraindicated or requiring avoidance)

The following interactions are the most clinically important and usually mean that the combination should be avoided:

Other notable interactions

The following interactions are generally of lower clinical significance or only apply in specific situations, but are still worth noting:

• Selective serotonin reuptake inhibitors (SSRIs) such as fluoxetine, sertraline and paroxetine: These drugs impair platelet function and may increase bleeding risk when combined with ticagrelor. Monitor for bleeding signs and consider alternatives where appropriate.
• Moderate CYP3A inhibitors such as diltiazem, verapamil, erythromycin and fluconazole: These may moderately increase ticagrelor exposure. Use with caution but do not usually require a dose change.
• Moderate CYP3A inducers such as efavirenz, bosentan and modafinil: May reduce ticagrelor effectiveness. Consider alternatives or closer clinical monitoring.
• Tacrolimus, ciclosporin and sirolimus: Ticagrelor may increase plasma levels of these immunosuppressants via P-gp inhibition. Monitor trough levels and adjust doses accordingly.
• Heparin and low-molecular-weight heparins: Additive bleeding effect. Required in some clinical settings (e.g. post-PCI), but requires careful monitoring.
• Fibrinolytic agents (alteplase, tenecteplase): Significantly increased bleeding risk, particularly intracranial haemorrhage. Decisions about timing and combination are made by specialist teams in acute stroke or STEMI care.
• SGLT2 inhibitors, DPP-4 inhibitors, metformin, insulin: No significant pharmacokinetic interactions. Ticagrelor is safe and routinely co-prescribed in patients with type 2 diabetes.

Food and lifestyle

Ticagrelor Intas can be taken with or without food, as food does not significantly affect its absorption. However, regular consumption of grapefruit or grapefruit juice should be avoided because of moderate CYP3A inhibition. Alcohol in moderation is generally acceptable, but heavy alcohol use increases the risk of gastrointestinal bleeding and should be discussed with your doctor. Smoking cessation is strongly recommended in all patients with cardiovascular disease, as ongoing smoking greatly reduces the benefits of any antiplatelet therapy.

What Is the Correct Dosage of Ticagrelor Intas?

The approved dose of Ticagrelor Intas 60 mg is one tablet twice daily (every 12 hours), taken with or without food, together with low-dose aspirin (75–100 mg daily). Treatment is started at least 12 months after a heart attack and continued long-term while the benefit-risk balance remains favourable.

Always take Ticagrelor Intas exactly as your doctor has prescribed. If you are unsure, check with your doctor or pharmacist. Do not stop taking this medicine without medical advice, even if you feel well.

Adults

Take Ticagrelor Intas at approximately the same times each day, about 12 hours apart (for example, one tablet at 8 a.m. and one at 8 p.m.). You can take the tablet with or without food, and with a glass of water. If you have difficulty swallowing tablets whole, they may be crushed and mixed in water or dispersed in water to drink immediately, or given through a nasogastric tube for hospitalised patients; ask your pharmacist for details.

Patients with renal impairment

No dose adjustment is required in patients with renal impairment. Ticagrelor is not removed by haemodialysis. However, patients with severe renal impairment or end-stage renal disease may be at higher risk of bleeding and should be monitored closely.

Patients with hepatic impairment

No dose adjustment is needed in mild hepatic impairment. In moderate hepatic impairment, use with caution and weigh the benefit-risk balance. Ticagrelor is contraindicated in severe hepatic impairment (Child-Pugh class C).

Children

Ticagrelor Intas is not approved for use in children and adolescents under 18 years of age. Do not give this medicine to children.

Elderly

No specific dose adjustment is required for elderly patients (65 years and older), but bleeding risk may be higher, and regular review of the need for continued treatment is recommended.

Missed dose

If you forget to take a dose of Ticagrelor Intas:

• Do not take a double dose to make up for a missed tablet
• Take the next tablet at the regular scheduled time
• If more than a few doses are missed in a row, contact your doctor – prolonged interruption increases cardiovascular risk

To help remember, set an alarm on your phone or use a pill organiser. Because the antiplatelet effect wears off within a few hours of a missed dose, regular timing is important to maintain protection.

Overdose

If you take too much Ticagrelor Intas, contact your doctor, pharmacist or nearest emergency department immediately. Overdose primarily causes an increased risk of bleeding and may also cause nausea, vomiting and diarrhoea, as well as possible breathlessness or ventricular pauses.

There is no specific antidote for ticagrelor. Ticagrelor is not removed by dialysis. Management is supportive. In cases of serious bleeding, platelet transfusion may be considered, although the effectiveness of transfusion in reversing the antiplatelet effect is limited because ticagrelor circulating in the blood can inhibit transfused platelets as well. An investigational reversal agent (bentracimab) has shown promising results in clinical trials but is not yet universally available.

What Are the Side Effects of Ticagrelor Intas?

The most common side effects of Ticagrelor Intas are bleeding (bruising, nosebleeds, heavy menstrual bleeding, GI bleeding) and dyspnoea (shortness of breath). Other common effects include headache, dizziness, gout, raised creatinine and rash. Serious but rare effects include intracranial haemorrhage, severe bradycardia, and angioedema.

Like all medicines, ticagrelor can cause side effects, although not everyone gets them. The two most characteristic side effects of ticagrelor are bleeding and dyspnoea (shortness of breath). Most side effects are mild and transient, but some require prompt medical evaluation.

Bleeding

As with any antiplatelet medicine, the most common side effect of ticagrelor is bleeding. Most bleeding events are minor and include easy bruising, nosebleeds, bleeding gums after brushing teeth, longer bleeding from small cuts, small amounts of blood in the urine, or heavier or prolonged menstrual periods in women.

Major bleeding is less common but serious. This includes gastrointestinal bleeding (black, tarry stools or bright red blood in stools, vomiting blood or coffee-ground material), intracranial haemorrhage (sudden severe headache, visual or neurological symptoms) and bleeding into the eye, joints or retroperitoneum. Any unusual or heavy bleeding should prompt immediate medical evaluation.

Older patients, those weighing less than 60 kg, patients with prior bleeding, and those taking anticoagulants or NSAIDs are at higher risk of bleeding. Do not use over-the-counter NSAIDs such as ibuprofen or aspirin (beyond the prescribed low-dose cardiac aspirin) without talking to your doctor.

Dyspnoea (shortness of breath)

Approximately 1 in 7 patients taking ticagrelor experience dyspnoea, most often early in treatment. It is usually mild to moderate, transient and does not progress. The mechanism is thought to involve increased adenosine levels, which can stimulate airway sensory nerves. If you develop new shortness of breath, tell your doctor so that they can exclude more serious causes such as heart failure, angina, anaemia or pulmonary embolism. In most cases, no specific treatment is needed and the dyspnoea resolves without stopping the medicine.

Side effects by frequency

The following list is based on EMA and FDA approved labelling and large clinical trials (PLATO, PEGASUS-TIMI 54, THEMIS, THALES). Frequencies apply to ticagrelor as a class, including the 60 mg and 90 mg strengths.

Laboratory changes

Your doctor may detect laboratory changes during monitoring, including:

• Raised serum uric acid (up to 15% on average, with about 0.5–2% developing clinical gout)
• Raised serum creatinine (usually mild and reversible)
• Mildly increased liver enzymes

These changes are usually clinically insignificant but may prompt dose review in certain patients (for example, those with pre-existing gout or renal impairment).

How Should You Store Ticagrelor Intas?

Store Ticagrelor Intas in its original packaging at room temperature (below 30°C), out of the sight and reach of children. Do not use after the expiry date printed on the carton. Dispose of unused tablets at a pharmacy; do not flush them down the toilet or throw them in household waste.

Correct storage keeps Ticagrelor Intas effective throughout its shelf life and prevents accidental ingestion by children. Follow these guidelines:

• Keep out of the sight and reach of children at all times. Accidental ingestion by a child can cause serious bleeding and requires urgent medical attention
• Store below 30°C unless the manufacturer's leaflet specifies otherwise
• Keep tablets in their original blister pack until you are ready to take them, to protect them from moisture and light
• Do not use Ticagrelor Intas after the expiry date printed on the carton and blister after “EXP”. The expiry date refers to the last day of the month shown
• Do not use tablets that look damaged, discoloured, broken or that have an unusual smell
• Do not dispose of medicines in wastewater or household waste. Return unused or expired tablets to your local pharmacy for safe destruction. This helps protect the environment from pharmaceutical contamination

If you are travelling, keep a copy of your prescription and the patient information leaflet with you, store the medicine in your carry-on luggage (not the hold) to avoid temperature extremes, and bring enough for the whole trip plus a few extra days in case of delays.

What Does Ticagrelor Intas Contain?

Each Ticagrelor Intas 60 mg film-coated tablet contains 60 mg of ticagrelor as the active ingredient. Inactive excipients typically include mannitol, dibasic calcium phosphate, sodium starch glycolate, hydroxypropylcellulose, magnesium stearate and a film coating containing hypromellose, titanium dioxide, macrogol and iron oxides.

Active ingredient

Each film-coated tablet contains 60 mg of ticagrelor, a direct-acting, reversible P2Y12 receptor antagonist belonging to the cyclopentyltriazolopyrimidine (CPTP) class.

Inactive ingredients (excipients)

The inactive ingredients in Ticagrelor Intas 60 mg film-coated tablets typically include:

• Tablet core: Mannitol (E421), dibasic calcium phosphate, sodium starch glycolate type A, hydroxypropylcellulose and magnesium stearate
• Film coating: Hypromellose (E464), titanium dioxide (E171), macrogol 400, and iron oxides (E172) – typically black and red to give the 60 mg tablet its characteristic pink colour

The exact excipient composition may vary slightly between batches and between different generic ticagrelor manufacturers. If you have a known allergy or intolerance to a specific excipient (for example, fructose intolerance can be relevant for mannitol-containing tablets), ask your pharmacist to check the most recent patient information leaflet for the specific product you receive.

Appearance and packaging

Ticagrelor 60 mg film-coated tablets are usually round or oval, biconvex and pink, with embossed markings that vary by manufacturer. Ticagrelor Intas tablets are typically supplied in blister strips (often 10 or 14 tablets per strip), packaged in cartons containing multiples of 14, 28, 56, 84 or 100 tablets. Not all pack sizes may be available in every country.

Generic equivalents of ticagrelor are manufactured by several companies worldwide, including Intas Pharmaceuticals (Ticagrelor Intas), Krka, Mylan, Teva, Hetero, Aurobindo and others. All generic versions must demonstrate bioequivalence to the original Brilique / Brilinta before regulatory approval.

Frequently Asked Questions About Ticagrelor Intas