Clopidogrel resistance
Clopidogrel resistance occurs when the antiplatelet drug clopidogrel is less effective than normal, increasing the risk of blood clots in certain patients.
Overview
Clopidogrel resistance is a condition where the drug clopidogrel (Plavix) does not work as effectively as expected. Clopidogrel is an antiplatelet drug used to prevent blood clots in individuals with a history of heart attack, stroke, deep vein thrombosis, or those who have received a stent to open blood vessels.
Risks and Complications
Patients with this resistance are at risk for serious complications because the drug fails to adequately prevent platelet aggregation. This can lead to:
- Recurrent heart attacks or strokes
- Thrombosis (blood clots) within stents, which impedes blood flow
Patients are categorized as intermediate metabolizers (receiving partial benefit) or poor metabolizers (receiving very limited benefit).
Causes
The condition is primarily linked to variations (polymorphisms) in the CYP2C19 gene. This gene provides instructions for an enzyme in the liver that converts clopidogrel into its active form. When the enzyme is nonfunctional—often due to the CYP2C19*2 or CYP2C19*3 polymorphisms—the drug cannot be activated to inhibit the P2RY12 receptor on platelets, allowing blood clots to form.
Inheritance
Clopidogrel resistance is inherited in a codominant manner. This means that both versions of the CYP2C19 gene are expressed and influence the trait. Individuals with one altered copy are typically intermediate metabolizers, while those with two altered copies are poor metabolizers. Not every individual with these gene variants will experience clinical resistance to the drug.