P2Y12 ADP Receptor Inhibitors

P2Y12 ADP receptor inhibitors are used for the treatment of MI and the prevention of stroke.  These medications prevent ADP from binding to P2Y12 receptors, which results in decreased clot formation inhibiting platelet-platelet and platelet fibrinogen binding by decreasing expression of the active GP IIb/IIIa receptors on platelets.  Obviously, these medications can result in bleeding, which can be life threatening.  

Class Drugs

• Ticlopidine

• Clopidogrel

• Prasugrel

• Ticagrelor

Class Mechanism of Action

Inhibits binding of ADP to P2Y12 receptors on platelets, which decreases expression of active GP IIb/IIIa on platelets. 

• Results in decreased platelet-platelet binding and platelet-fibrinogen binding

ADP activates P2Y12 ADP receptors, which in turn stimulate release of calcium ions to the cytoplasm, which triggers activation of GP IIb/IIIa receptors. GP IIb/IIIa receptors bind fibrinogen, which allows for platelet aggregation.

Class Applications

Generally used for prevention of strokes and/or treatment/prevention of acute MI

See individual drugs for indications

Class Adverse Effects

Bleeding, can be life threatening

See individual drugs

Drug Table

Drug Name	Application	Comments	Image
Ticlopidine	Prevention of subsequent TIA/stroke	Mechanism of Action; Irreversible P2Y12 ADP receptor binding; Adverse Effects ; Severe hematologic reactions, limiting use; Agranulocytosis; TTP; Aplastic Anemia	"Tie" "Cupid" "Dining"
Clopidogrel	Prevention of subsequent TIA/stroke; Prevention of subsequent MI; Treatment of PAD (peripheral artery disease); Prevention of thrombotic events associated with percutaneous coronary intervention; Thrombotic prophylaxis in acute coronary syndrome (ACS)	Mechanism of Action; Irreversible P2Y12 ADP receptor binding; Adverse Effects; Hematologic reactions are present but less prominent than with Ticlopidine:; -Neutropenia; -TTP; Genetic variances in the CYP2C19 lead to decreased metabolism to active metabolite	"Claw" "Doe" "Grill"
Prasugrel	Prevention of thrombotic events associated with percutaneous coronary intervention; Thrombotic prophylaxis in acute coronary syndrome (ACS)	Mechanism of Action; Irreversible P2Y12 ADP receptor binding; Adverse Effects; Hematologic reactions are present but less prominent than with Ticlopidine:; -TTP; Black box warning for bleeding risk	"Praying" "Sue" "Grill"
Ticagrelor	Prevention of thrombotic events associated with percutaneous coronary intervention; Thrombotic prophylaxis in acute coronary syndrome (ACS)	Mechanism of Action; Reversible P2Y12 ADP receptor binding; Adverse Effects; Black box warning for bleeding; Black box warning for decreased effectiveness with concomitant use of greater than 100 mg of aspirin	"Tic Tac" "Grill"