What is the mechanism of action of prasugrel?

Prasugrel is a prodrug that is converted to an active and inactive metabolite by the hepatic CYP system. The active component (R- 138727) of the metabolites irreversibly blocks P2Y12 at ADP receptors, preventing GPIIb/IIIa receptor complex activation, thus reducing platelet aggregation and activation.

Is prasugrel an antiplatelet?

Prasugrel, trade name Effient, is an investigational new antiplatelet drug currently under review for clinical use by the Food and Drug Administration. It is a thienopyridine analog with a structure similar to that of clopidogrel and ticlopidine.

What enzyme activates prasugrel?

It belongs to the thienopyridine class, which also includes clopidogrel and ticlopidine. Like other drugs in its class, prasugrel requires hepatic conversion by cytochrome P-450 enzymes (CYP) into an active metabolite that binds irreversibly to the P2Y12 receptor.

Is prasugrel better than clopidogrel?

In clinical studies, prasugrel has consistently demonstrated greater and more rapid platelet inhibition than clopidogrel in healthy subjects, patients with stable coronary artery disease (CAD) and acute coronary syndromes, and those undergoing PCI.

What time of day should prasugrel be taken?

Prasugrel comes as a tablet to take by mouth. It is usually taken once a day with or without food. Take prasugrel at around the same time every day. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand.

What is another name for prasugrel?

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

What time of day should you take prasugrel?

Is prasugrel a blood thinner?

Effient (prasugrel) is a blood thinner that prevents heart attacks after a stent is placed in the heart.

What are the side effects of prasugrel?

Common side effects of Prasugrel include:

  • Bleeding.
  • Anemia.
  • Atrial fibrillation.
  • Back pain.
  • Slow heart rate.
  • Dizziness.
  • Shortness of breath.
  • Headache.

When should I stop prasugrel?

Prasugrel should also be avoided with concomitant use of medications that increase bleeding risk (i.e. warfarin) and should be used with caution in patients with low body weight (less than 60 kg).

What are side effects of prasugrel?

How long do you take prasugrel?

After getting a stent in the heart, most people need to take Effient (prasugrel) for at least 12 months. Depending on your other medical problems, you may need to take Effient (prasugrel) for a shorter or longer period of time.

What is the maximum platelet aggregation inhibition of prasugrel?

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 Effient, approximately 90% of patients had at least 50% inhibition of platelet aggregation by 1 hour. Maximum platelet inhibition was about 80% (see Figure 2).

What is the chemical structure of prasugrel hydrochloride?

The chemical structure of prasugrel hydrochloride is: Prasugrel hydrochloride is a white to practically white solid. It is soluble at pH 2, slightly soluble at pH 3 to 4, and practically insoluble at pH 6 to 7.5. It also dissolves freely in methanol and is slightly soluble in 1- and 2- propanol and acetone.

Are there any side effects to taking prasugrel?

Compared to patients weighing ≥60 kg, patients weighing <60 kg have an increased exposure to the active metabolite of prasugrel and an increased risk of bleeding on a 10 mg once daily maintenance dose. Consider lowering the maintenance dose to 5 mg in patients <60 kg.

When to lower the dose of prasugrel for bleeding?

Dosing In Low Weight Patients Compared to patients weighing ≥60 kg, patients weighing <60 kg have an increased exposure to the active metabolite of prasugrel and an increased risk of bleeding on a 10-mg once daily maintenance dose. Consider lowering the maintenance dose to 5-mg in patients <60 kg.

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