Prasugrel

From Drugs Prescribing Information
(Redirected from Efient)
Jump to: navigation, search
Click on "►" to expand:

Contents

[edit] BRAND NAMES

[edit] STRUCTURE

Prasugrel.jpg

[edit] MECHANISM OF ACTION

Prasugrel is an inhibitor of platelet activation and aggregation. This means that it helps to prevent blood clots from forming. When the blood clots, this is due to special cells in the blood, the platelets, sticking together (aggregating).

Prasugrel is a prodrug, its active metabolite acts as an irreversible antagonist of the adenosine diphosphate (ADP) P2Y12 receptor. it binds to the platelet P2Y12 receptors and prevents ADP-mediated platelet activation of the glycoprotein GPIIb/IIIa complex. As the glycoprotein GPIIb/IIIa complex is the major receptor for fibrinogen, its impaired activation prevents fibrinogen binding to platelets and inhibits platelet aggregation.

Inhibition of platelet function reduces the risk of a blood clot forming and the rate of cardiovascular events such as death, myocardial infarction, or stroke.

[edit] INDICATIONS

Prasugrel is taken together with aspirin to prevent thrombotic cardiovascular events (including stent thrombosis) in patients with acute coronary syndrome who are to be managed with percutaneous coronary intervention (an operation used to unblock narrowed coronary arteries), as follows:

  • Patients with unstable angina or, non-ST-elevation myocardial infarction (NSTEMI)
  • Patients with ST-elevation myocardial infarction (STEMI) when managed with either primary or delayed PCI.

[edit] DOSAGE

Initiate treatment with a single 60-mg oral loading dose. Continue at 10 mg once daily with or without food. Consider 5 mg once daily for patients <60 kg. Patients should also take aspirin (75 mg to 325 mg) daily

Prasugrel treatment starts with one 60 mg loading dose, followed by 10 mg takenonce daily with or without food, except in patients weighing less than 60 kg, who should take 5 mg once a day. Patients taking prasugrel should also take aspirin (75 mg to 325 mg) daily. It is recommended that treatment with prasugrel and aspirin continue for up to a year.

[edit] CONTRAINDICATIONS

  • Active pathological bleeding
  • Prior transient ischemic attack (a temporary reduction in the blood supply to part of the brain) or stroke.
  • Hypersensitivity to Prasugrel or any component of the product
  • In patients ≥75 years of age, Prasugrel is generally not recommended because of the increased risk of fatal and intracranial bleeding and uncertain benefit, except in high-risk patients (diabetes or prior MI), where its effect appears to be greater and its use may be considered. In this case, the 5 mg daily dose should be used following a 60 mg starting dose.
  • Severe liver problems

[edit] WARNINGS AND PRECAUTIONS

  • Coronary artery bypass graft surgery (CABG)-related bleeding: Risk increases in patients receiving Prasugrel who undergo CABG. Do not start this drug in patients likely to undergo urgent CABG. When possible, discontinue Prasugrel at least 7 days prior to any surgery.
  • Discontinuations: Premature discontinuation increases risk of stent thrombosis, MI, and death. Premature discontinuation of treatment should be avoided.
  • Thrombotic thrombocytopenic purpura (TTP): TTP has been reported with Prasugrel.
  • Hypersensitivity: Hypersensitivity including angioedema has been reported with Prasugrel including in patients with a history of hypersensitivity reaction to other thienopyridines (Ticlopidine and Clopidogrel)
  • Prasugrel can cause significant, sometimes fatal, bleeding

[edit] INTERACTIONS

  • Nonsteroidal anti-inflammatory drugs (NSAIDs): Combination use increases risk of gastrointestinal bleeding.
  • Warfarin: Combination use increases risk of bleeding

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category B (US). There are no adequate and well-controlled studies of Prasugrel use in pregnant women. Prasugrel should be used during pregnancy only if the potential benefit to the mother justifies the potential risk to the fetus.
  • Nursing Mothers: It is not known whether Prasugrel is excreted in human milk; however, metabolites of Prasugrel were found in rat milk. Because many drugs are excreted in human milk, prasugrel should be used during nursing only if the potential benefit to the mother justifies the potential risk to the nursing infant.

[edit] SIDE EFFECTS

The most common side effects include, anemia, hematoma, epistaxis (nosebleeds), gastrointestinal hemorrhage, rash, hematuria (blood in the urine) and bleeding at puncture sites and bruising.

[edit] RELATED LINKS

[edit] BIBLIOGRAPHY

[edit] REFERENCES