What is platelet P2Y12?

Antiplatelet drugs work to make your platelets less sticky and thereby help prevent blood clots from forming in your arteries. Aspirin is an antiplatelet drug that may be used. P2Y12 receptor blockers are another group of antiplatelet drugs.

What is P2Y12 inhibitor effect?

The therapeutic effect of all P2Y12 inhibitors is their ability to prevent blood clotting. By this mechanism, they will also increase the risk of unwanted bleeding.

What does the P2Y12 receptor do?

The P2Y12 receptor is a G-inhibitory-protein receptor in the platelet membrane, which is activated by ADP and results in the inhibition of adenylyl cyclase, thereby inducing platelet aggregation [33,34]. Moreover, the activation of P2Y12 receptor hinders the antiplatelet effects of prostacyclin.

What is normal P2Y12?

reference range: 180 – 376 PRU. Values less than 180 PRU may be evidence of a P2Y12 inhibitor effect.

Is dipyridamole a P2Y12 inhibitor?

Platelet inhibitors include thromboxane inhibitors (aspirin); adenosine diphosphate (ADP) receptor antagonists (or P2Y12 inhibitors) such as the thienopyridines (clopidogrel and prasugrel) and the nonthienopyridines (elinogrel, ticagrelor and cangrelor); the glycoprotein IIb/IIIa inhibitors; and medication working …

How do platelet inhibitors work?

Platelet aggregation inhibitors work in different places of the clotting cascade and prevent platelet adhesion, therefore no clot formation. Aspirin, the most commonly used antiplatelet drug changes the balance between prostacyclin (which inhibits platelet aggregation) and thromboxane (that promotes aggregation).

How do P2Y12 inhibitors work?

Thienopyridines inhibit the platelet activation and aggregation by antagonizing the platelet P2Y12 receptor. This prevents the binding of ADP to the receptor which attenuates platelet aggregation and reaction of platelets to stimuli of thrombus aggregation such as thrombin [4].

Which P2Y12 inhibitors are reversible?

Ticagrelor is the first oral reversible ADP (P2Y12) receptor antagonist. As compared to clopidogrel, ticagrelor has rapid onset as well as offset of action because of its reversible binding to P2Y12 receptor.

Does aspirin affect P2Y12?

Aspirin inhibition of platelet function is measured in a third channel on the VerifyNow system. Therefore, aspirin does not interfere with the P2Y12 assay, and its effect can be measured and reported separately for patients on combination aspirin/clopidogrel therapy.

What should I monitor with clopidogrel?

Most clinical studies on clopidogrel rely on standard platelet aggregometry to measure inhibition of ADP-induced aggregation (4)(5). In addition to aggregometry, cytometric determination of surface expression of platelet proteins, in particular P-selectin (CD62P), is commonly used to monitor platelet activation.

What is the most common antiplatelet drug?

Aspirin is the most common antiplatelet. At a low dose, aspirin reduces inflammation in the arteries. You may be put on aspirin to lower your risk of getting heart disease. Other antiplatelets may be prescribed when you’ve had a heart event or your risk of having one is higher.

Is antiplatelet the same as anticoagulant?

There are two main types of blood thinners. Anticoagulants such as heparin or warfarin (also called Coumadin) slow down your body’s process of making clots. Antiplatelet drugs, such as aspirin, prevent blood cells called platelets from clumping together to form a clot.

Which is the best P2Y12 inhibitor for mi?

Among the oral P2Y 12 inhibitors, ticagrelor and prasugrel provide the greatest reductions in risk of recurrent MI and stent thrombosis, while clopidogrel confers the lowest bleeding risk. The greater reduction in CV and all-cause mortality seen with ticagrelor as compared with prasugrel may relate to lower bleeding risk with ticagrelor.

Are there any direct acting inhibitors of the P2Y 12 receptor?

The newer, direct-acting P2Y 12 inhibitors (cangrelor and ticagrelor) change the conformation of the P2Y 12 receptor, resulting in reversible, concentration dependent inhibition of the receptor.

Which is an irreversible platelet inhibitor of P2Y12?

Active metabolites of the thienopyridine prodrugs (ticlopidine, clopidogrel, and prasugrel) covalently bind to the P2Y 12 receptor and are irreversible, indirect platelet inhibitors.

How much thienopyridine is a P2Y12 inhibitor?

Thienopyridine pharmacokinetics P2Y 12 inhibitor subjects . Dose . AUC (ng h/mL) . Cmax (ng/mL) . Tmax (h) . Healthy 600 mg 126 38 1.4 Healthy 300 mg 44 36 NR Healthy 300 mg 185 141 NR