Tienopyridines

Tienopyridines are a class of thienopyridine antiplatelet drugs. These medications work by irreversibly inhibiting the P2Y12 subtype of ADP receptors on the surface of platelets. By blocking these receptors, they prevent adenosine diphosphate (ADP) from binding, which is a key step in platelet activation and aggregation. This inhibition ultimately reduces the formation of blood clots.

The primary therapeutic use of tienopyridines is in the prevention of thrombotic events, such as heart attacks and strokes, particularly in patients with acute coronary syndrome or those who have undergone percutaneous coronary intervention (PCI) with stent placement. They are often used in combination with aspirin, forming dual antiplatelet therapy (DAPT).

Commonly known tienopyridines include clopidogrel, prasugrel, and ticagrelor, although ticagrelor is technically a cyclopentyltriazolopyrimidine, it is often grouped with tienopyridines due to its similar mechanism of action and clinical use. These drugs are prodrugs, meaning they require metabolic activation in the liver to become effective. The metabolism and effectiveness can vary among individuals due to genetic factors affecting the enzymes involved in their activation.

Potential side effects include bleeding, which is a direct consequence of their antiplatelet activity. Other side effects can include gastrointestinal issues, rash, and, in rare cases, more serious adverse reactions. Dosage and duration of treatment are carefully managed by healthcare professionals to balance the benefits of clot prevention against the risk of bleeding.