Ticagrelor

Products

Ticagrelor is commercially available in the form of film-coated tablets (Brilique). The active ingredient was approved in many countries in 2011. In 2018, additional meltable tablets were registered.

Structure and properties

Ticagrelor (C23H28F2N6O4S, Mr = 522.6 g/mol) is a cyclopentyltriazolopyrimidine without a thienopyridine structure. Ticagrelor is directly active. It has an active metabolite but, unlike clopidogrel and prasugrel, does not require metabolic activation.

Effects

Ticagrelor (ATC B01AC24) has antiplatelet properties with a rapid onset of action. It is a reversible antagonist of adenosine diphosphate (ADP) at the P2Y12 ADP receptor on platelets. This receptor plays a central role in platelet activation and aggregation. Clopidogrel and prasugrel also bind to this receptor, but result in irreversible inhibition, resulting in a prolonged effect after discontinuation (during the life of the platelet). This is disadvantageous when rapid discontinuation is required, such as during surgery.

Indications

In combination with acetylsalicylic acid to prevent atherothrombotic events such as myocardial infarction or stroke in high-risk patients.

Dosage

According to the SmPC. Started by taking 180 mg at one time. Subsequently, 90 mg is taken twice daily due to the medium-long half-life of 7 hours. The intake is independent of meals. Therapy is continued for up to one year.

Contraindications

  • Hypersensitivity
  • Active pathological bleeding
  • History of intracranial hemorrhage
  • Liver dysfunction
  • Combination with strong CYP3A4 inhibitors.

Full precautions can be found in the drug label.

Interactions

Ticagrelor is metabolized primarily by CYP3A4 to the major active metabolite AR-C124910XX. It is a substrate and mild inhibitor of P-glycoprotein. Appropriate drug-drug interactions must be considered.

Adverse effects

The most common potential adverse effects include difficulty breathing (dyspnea), nosebleeds, bleeding in the digestive tract, bleeding in the skin and under the skin, and bleeding at the procedure site.