Ticarel90 mg

Ticarel is an antiplatelet medicine used, in combination with low-dose aspirin, to lower the risk of thrombotic (clot-related) cardiovascular events.

Established / FDA-approved indications

• Acute coronary syndrome (ACS): Ticarel is indicated to reduce the rate of cardiovascular death, myocardial infarction (MI), and stroke in patients with unstable angina, non-ST-elevation MI (NSTEMI), or ST-elevation MI (STEMI), including patients managed medically or with percutaneous coronary intervention (PCI) or coronary artery bypass grafting (CABG). It also reduces the rate of stent thrombosis in patients who have received a coronary stent for ACS.
• History of myocardial infarction: In patients with a history of MI of at least one year, Ticarel reduces the risk of cardiovascular death, MI, and stroke.

Guideline-supported / adjunct use

• Cardiology guidelines support use of Ticarel as part of dual antiplatelet therapy (with aspirin) for secondary prevention after ACS, and in select high-risk patients with established coronary artery disease or peripheral artery disease.

Ticarel must always be used together with a maintenance dose of aspirin, as directed by a physician (see Dosage and Precautions).

Each film-coated tablet contains Ticagrelor 60 mg or 90 mg as the active ingredient, along with standard pharmaceutical excipients.

Ticarel is an oral antiplatelet agent belonging to the cyclopentyltriazolopyrimidine chemical class. Unlike thienopyridine P2Y12 inhibitors (such as clopidogrel), Ticarel reversibly binds to the platelet P2Y12 receptor without requiring metabolic activation, giving it a rapid onset of action and a more predictable antiplatelet effect.

Ticarel is used together with aspirin to reduce the risk of serious cardiovascular events in people with acute coronary syndrome or a prior heart attack.

Ticarel belongs to the antiplatelet drug class, specifically the P2Y12 platelet receptor inhibitors (non-thienopyridine subclass).

Mechanism of action

Ticagrelor and its major active metabolite reversibly interact with the platelet P2Y12 ADP-receptor to prevent ADP-mediated platelet activation and aggregation. Because binding is reversible, platelet function recovers as drug levels decline, without needing new platelet production.

Pharmacokinetics

• Absorption: Rapidly absorbed; median time to peak plasma concentration is about 1.5 hours.
• Metabolism: Extensively metabolized by CYP3A4/CYP3A5 to an active metabolite with similar potency.
• Half-life: Approximately 7 hours for Ticagrelor and 8.5 hours for its active metabolite.
• Excretion: Primarily via the biliary/faecal route; a small fraction is renally excreted.

Ticarel tablets can be taken with or without food. Tablets should be swallowed whole with water. Patients unable to swallow whole tablets may crush the tablet and mix it in water and drink immediately; the crushed tablet may also be given via a nasogastric tube, as directed by a physician. Do not stop taking Ticarel without consulting the prescribing physician, as premature discontinuation increases the risk of cardiovascular events.

Contraindicated / avoid combinations

• Strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, voriconazole, clarithromycin, nefazodone, ritonavir, atazanavir): markedly increase Ticarel exposure and bleeding risk; concurrent use should be avoided.
• Strong CYP3A4 inducers (e.g., rifampin, phenytoin, carbamazepine, St. John's Wort): substantially reduce Ticarel exposure and its antiplatelet effect; concurrent use should be avoided.
• Aspirin maintenance doses above 100 mg/day: reduce the effectiveness of Ticarel; use only low-dose aspirin (75–100 mg/day) with Ticarel.

Use with caution

• Simvastatin or lovastatin at doses above 40 mg: Ticarel increases exposure to these statins, raising the risk of statin-related toxicity; avoid high-dose simvastatin/lovastatin.
• Digoxin: Ticarel increases digoxin plasma concentrations; monitoring of digoxin levels is advised.
• Other anticoagulants, antiplatelet agents, chronic NSAIDs, and SSRIs: may additively increase the risk of bleeding when used with Ticarel.

Most common

• Bleeding (bruising, epistaxis (nosebleed), gastrointestinal bleeding, and other minor or major bleeding) — the most common adverse effect of Ticarel (see Precautions and Warnings).
• Dyspnea (shortness of breath) — a distinctive side effect of Ticarel, usually mild-to-moderate, self-limiting, and occurring early in treatment; it rarely requires stopping therapy.

Less common

• Bradyarrhythmias, including ventricular pauses (mostly detected on cardiac monitoring, usually asymptomatic)
• Elevated blood uric acid levels
• Dizziness, headache
• Nausea, diarrhea
• Elevated serum creatinine

Pregnancy: Data on the use of Ticarel in pregnant women are limited. Ticarel should be used during pregnancy only if clearly needed and if the potential benefit to the mother justifies the potential risk to the fetus. A physician should be consulted before use in pregnancy.

Lactation: It is not known whether Ticarel or its metabolites are excreted in human breast milk. Because many drugs are excreted in breast milk and the potential for adverse effects on the infant is unknown, a decision should be made, in consultation with a physician, whether to discontinue breastfeeding or discontinue Ticarel, taking into account the importance of the medicine to the mother.

Bleeding risk (important warning)

Ticarel, like other antiplatelet agents, can cause significant, and sometimes fatal, bleeding. Do not use Ticarel in patients with active pathological bleeding or a history of intracranial hemorrhage (see Contraindications). Use with caution in patients with an increased risk of bleeding (e.g., recent trauma, recent surgery, recent gastrointestinal bleeding, or coagulation disorders), and in those taking other medications that increase bleeding risk.

Aspirin dose must not exceed 100 mg daily

After any initial loading dose of aspirin, Ticarel must be used with a daily aspirin maintenance dose of 75–100 mg. Maintenance aspirin doses above 100 mg reduce the effectiveness of Ticarel and should be avoided.

Surgery

If possible, Ticarel should be discontinued at least 5 days before elective surgery to reduce the risk of bleeding, unless urgent revascularization is required. Discontinuation should only be done on medical advice, as stopping Ticarel increases the risk of cardiovascular events.

Dyspnea

Dyspnea has been reported with Ticarel; it is usually mild and self-limiting, but other causes of breathlessness should be evaluated if severe or persistent.

Hepatic impairment

Ticarel is not recommended in patients with severe hepatic impairment and should be used with caution in moderate hepatic impairment.

Do not stop taking Ticarel without first talking to the prescribing physician, and always take it exactly as prescribed.

There is no known antidote to reverse the antiplatelet effect of Ticarel. Overdose with Ticarel may increase the risk of bleeding complications. Any suspected overdose of Ticarel should be treated as a medical emergency — seek immediate medical attention or contact the nearest hospital/emergency services. Management is supportive and based on clinical presentation; platelet transfusion may be considered by a physician if clinically significant bleeding occurs, though its benefit may be limited due to circulating active metabolite.

Store at room temperature (below 30°C), away from light and moisture. Keep out of reach of children.

Renal impairment

No dose adjustment of Ticarel is generally required in patients with renal impairment. Limited data are available in patients on dialysis; caution is advised.

Hepatic impairment

Ticarel is contraindicated in severe hepatic impairment and should be used with caution in moderate hepatic impairment; no dose adjustment is needed in mild hepatic impairment.

Elderly

No specific dose adjustment of Ticarel is required based on age alone, though elderly patients may have a higher baseline risk of bleeding.

Pediatric

Safety and efficacy of Ticarel in pediatric patients have not been established.

The duration of treatment with Ticarel depends on the indication and should be determined by the treating physician. In acute coronary syndrome, Ticarel 90 mg twice daily is typically continued for up to 12 months, after which the physician may continue therapy at a reduced dose (60 mg twice daily) for extended secondary prevention. Patients with a history of myocardial infarction may continue 60 mg twice daily long-term as advised by their physician. Ticarel should not be stopped early without medical advice, as this increases the risk of cardiovascular events.

Ticagrelor belongs to the antiplatelet agent class; specifically the P2Y12 platelet receptor inhibitor (cyclopentyltriazolopyrimidine class).

Ticagrelor reversibly binds to and inhibits the platelet P2Y12 ADP-receptor, blocking ADP-induced platelet activation and aggregation, thereby reducing the risk of clot formation in blood vessels.

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The safety and efficacy of Ticarel in pediatric patients (below 18 years) have not been established. Ticarel is therefore not recommended for use in children and adolescents outside of clinical trial settings.