Ticagrelor (Brilinta, Brilique)

Table 1 provides a summary of the indications, contraindications, dosage, administration, warnings, precautions, and other relevant information for the drug Ticagrelor.

Table 1Summary
IndicationsTicagrelor, in combination with acetylsalicylic acid (ASA), is indicated for the prevention of atherothrombotic events in adult patients with acute coronary syndrome (ACS) or a prior heart attack and a high risk of developing an atherothrombotic event.
Contraindications– Hypersensitivity to the active substance or any excipient.
– Active bleeding.
– Previous intracranial hemorrhage.
– Severe liver impairment.
– Concurrent administration of ticagrelor with strong CYP3A4 inhibitors (e.g., ketoconazole, clarithromycin, nefazodone, ritonavir, and atazanavir) can lead to a significant increase in exposure to ticagrelor.
Dosage: Acute Coronary SyndromesTreatment with Ticagrelor should start with a loading dose of 180 mg (two 90 mg tablets) followed by 90 mg twice daily.
For patients with coronary syndromes, Ticagrelor 90 mg twice daily is recommended for 12 months unless discontinuation is clinically indicated.
Dosage: Prior Myocardial InfarctionTicagrelor 60 mg twice daily is the recommended dose for extended treatment for patients who had a heart attack at least a year ago and are at high risk of a new event. Treatment can be started without interruption as continuation treatment after the initial one-year treatment with Ticagrelor 90 mg or treatment with another adenosine diphosphate (ADP) receptor inhibitor for patients who had coronary syndrome and are at high risk of developing a new event.
AdministrationTicagrelor can be administered with or without food. For patients who cannot swallow the tablets whole, they can be crushed, mixed in half a glass of water, and consumed immediately. The mixture can also be administered via a nasogastric tube.
Warnings and Precautions– Increased risk of bleeding, especially in patients with known elevated bleeding risk.
– Discontinuation of Ticagrelor should be avoided. If a dose is missed, only one tablet should be taken at the next regular time.
– Use with caution in patients with asthma/chronic obstructive pulmonary disease (COPD).
– Dyspnea has been reported in patients treated with ticagrelor.
– Patients with a history of ischemic stroke can be treated with ticagrelor for up to 12 months.
– Use with caution in patients at risk for bradycardia (slow heart rate).
– Central sleep apnea, including Cheyne-Stokes respiration, has been reported in patients taking ticagrelor. If suspected, further clinical evaluation is recommended.
– Creatinine levels may rise during treatment with ticagrelor. The mechanism is unclear. Kidney function should be monitored according to clinical practice. Special attention should be given to patients ≥ 75 years, those with moderate/severe renal impairment, and those concurrently treated with an angiotensin receptor blocker (ARB).
– Hyperuricemia may occur during treatment with ticagrelor. Caution is advised for patients with hyperuricemia or gout. Use of ticagrelor is discouraged in patients with uric acid nephropathy.
– Thrombotic Thrombocytopenic Purpura (TTP): In very rare cases, TTP has been reported with ticagrelor treatment. TTP is characterized by thrombocytopenia and microangiopathic hemolytic anemia associated with neurological findings, renal failure, or fever. It’s a potentially fatal condition that requires prompt treatment, including plasmapheresis.
– Interference with Platelet Function Test for Heparin-Induced Thrombocytopenia (HIT): False-negative results in platelet function tests (including HIPA-test) for HIT have been reported in patients taking ticagrelor. This is related to ticagrelor inhibiting the P2Y12 receptor on healthy donor platelets in the test. Information about concurrent ticagrelor treatment is required for interpreting platelet function tests for HIT.
Other cosiderations– Based on a relationship observed in the PLATO study between the maintenance dose of ASA and the relative effect of ticagrelor compared to clopidogrel, concurrent use of ticagrelor and a high maintenance dose of ASA (> 300 mg) is not recommended.
– Premature discontinuation of antiplatelet treatment, including Ticagrelor, could lead to an increased risk of cardiovascular death, heart attack, or stroke.
– Ticagrelor contains less than 1 mmol (23 mg) sodium per dose unit, making it essentially “sodium-free”.
Updated on 2025-01-18