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How is prasugrel metabolized?

Prasugrel is a prodrug and is rapidly metabolized by carboxylesterase 2 in the intestine and carboxylesterase 1 in the liver to a likewise inactive thiolactone, which is then converted by CYP3A4 and CYP2B6, and to a minor extent by CYP2C9 and CYP2C19, to a pharmacologically active metabolite (R-138727).

How is prasugrel metabolized?

Prasugrel is a prodrug and is rapidly metabolized by carboxylesterase 2 in the intestine and carboxylesterase 1 in the liver to a likewise inactive thiolactone, which is then converted by CYP3A4 and CYP2B6, and to a minor extent by CYP2C9 and CYP2C19, to a pharmacologically active metabolite (R-138727).

How is prasugrel activated?

Prasugrel, along with other antiplatelet agents such as clopidogrel and ticagrelor, inhibits platelet activation by irreversibly binding to the platelet receptor, P2RY12. Prasugrel is metabolized to its active metabolite primarily by CYP3A5 and CYP2B6, and to a lesser extent by CYP2C9 and CYP2C19.

Is prasugrel a thienopyridine?

Prasugrel (CS-747, LY640315) is a novel member of the thienopyridine class of oral antiplatelet agents that includes ticlopidine and clopidogrel. Like other thienopyridines, prasugrel is a prodrug that is inactive in vitro.

What is the difference between Effient and prasugrel?

Prasugrel is a rapidly-acting thienopyridine that works faster than clopidogrel. Dr. Kereiakes said Effient is absorbed by the body more quickly through the intestines and only requires one chemical conversion process in the liver. Plavix requires two chemical reactions to convert it from a prodrug to an active drug.

Who manufactures prasugrel?

Effient (prasugrel) tablets – Lilly Medical.

When do you use prasugrel over clopidogrel?

The 2016 American College of Cardiology/American Heart Association Dual Antiplatelet Therapy update recommends prasugrel over clopidogrel (class IIa recommendations) in patients with acute coronary syndrome (ACS) after percutaneous coronary intervention (PCI) except for those who are at high risk for bleeding (such as …

What is the function of dipyridamole?

Dipyridamole appears to act in vivo by synergistically modifying several biochemical pathways, including: a) inhibition of platelet cAMP-phosphodiesterase; b) potentiation of adenosine inhibition of platelet function by blocking reuptake by vascular and blood cells, and subsequent degradation of adenosine; and possibly …

Why is dipyridamole contraindicated in angina?

Dipyridamole has a vasodilatory effect and should be used with caution in patients with severe coronary artery disease (e.g., unstable angina or recently sustained myocardial infarction). Chest pain may be aggravated in patients with underlying coronary artery disease who are receiving dipyridamole.

What is another name for prasugrel?

Effient (prasugrel) is an antiplatelet medication. It prevents your platelets from clumping together into blood clots.

What is prasugrel used for?

Prasugrel is used to prevent strokes, heart attacks, or other serious problems with your heart or blood vessels. It is given to patients before they have a heart procedure called percutaneous coronary intervention (PCI).

What is the mechanism of action of prasugrel?

Mechanism of action Prasugrel is a member of the thienopyridine class of ADP receptor inhibitors, like ticlopidine (trade name Ticlid) and clopidogrel (trade name Plavix). These agents reduce the aggregation (“clumping”) of platelets by irreversibly binding to P2Y 12 receptors.

How effective is prasugrel at reducing platelet aggregation?

Prasugrel produces inhibition of platelet aggregation to 20 μM or 5 μM ADP, as measured by light transmission aggregometry. Following a 60-mg loading dose of the drug, about 90% of patients had at least 50% inhibition of platelet aggregation by one hour. Maximum platelet inhibition was about 80%.

What are the limitations of prasugrel?

Given the risk of bleeding, prasugrel should not be used in people who are older than 75 years, who have low body weight or a history of transient ischemic attacks or strokes. The initiation of prasugrel before coronary angiography outside the context of primary PCI is not recommended.

What is the difference between prasugrel and clopidogrel?

Compared to clopidogrel, prasugrel inhibits adenosine diphosphate–induced platelet aggregation more rapidly, more consistently, and to a greater extent than do standard and higher doses of clopidogrel in healthy volunteers and in patients with coronary artery disease, including those undergoing PCI.