SUPAGREL TABLETS

Indications

• Acute coronary syndrome (ACS)
• Unstable angina
• Myocardial infarction (MI)
• Percutaneous coronary intervention (PCI)
• Secondary prevention of cardiovascular events

Dosage

Children: There is no established

Adults: Refer to the BNF for specific dosing guidelines based on clinical indications and individual patient factors.

Mechanism of action

Ticagrelor acts as a selective and reversible antagonist of the P2Y12 receptor, which is a subtype of the purinergic receptor involved in platelet activation and aggregation. By inhibiting the binding of adenosine diphosphate (ADP) to the P2Y12 receptor, ticagrelor prevents the activation of the glycoprotein IIb/IIIa complex, thereby inhibiting platelet aggregation and thrombus formation.

Pharmacodynamics

The pharmacodynamic effects of ticagrelor are characterized by a rapid and consistent antiplatelet effect, which is dose-dependent. Ticagrelor leads to a significant reduction in platelet aggregation, which is observed within 30 minutes of administration. This effect is sustained over the dosing interval, contributing to a decrease in the risk of cardiovascular events such as heart attacks and strokes.

Pharmacokinetics

Ticagrelor is rapidly absorbed after oral administration, with peak plasma concentrations occurring within 1-3 hours. It undergoes extensive hepatic metabolism, primarily via the cytochrome P450 isoenzyme CYP3A4, resulting in active metabolites. The half-life of ticagrelor is approximately 7 hours, but its antiplatelet effects can persist longer due to the irreversible nature of platelet inhibition. Ticagrelor is eliminated primarily through the urine, with around 60% of the dose excreted as metabolites.

Contra-indications

• Active bleeding
• History of intracranial hemorrhage
• Severe hepatic impairment
• Hypersensitivity to ticagrelor or any of its components

Adverse effects

• Bleeding
• Dyspnea
• Bradycardia
• Gastrointestinal disturbances
• Elevated uric acid levels
• Rash

Interactions

• Increased risk of bleeding with other antiplatelet agents
• CYP3A4 inhibitors (e.g., ketoconazole, ritonavir) may increase ticagrelor levels
• CYP3A4 inducers (e.g., rifampicin, carbamazepine) may decrease ticagrelor levels
• Aspirin doses above 100 mg may reduce the effectiveness of ticagrelor

Precautions

• Monitor for signs of bleeding
• Use with caution in patients with a history of gastrointestinal bleeding
• Caution in patients with renal impairment
• Discontinue prior to surgery to reduce risk of bleeding

Pregnancy

There are limited data on the use of ticagrelor in pregnancy. Use only if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

Ticagrelor is excreted in human milk. Caution should be exercised when administering to nursing mothers.

Storage

Store at room temperature, away from moisture and heat. Keep out of reach of children.

Formulations

• Tablets: 90 mg, 60 mg