Prasugrel: Superior Antiplatelet Protection for ACS Patients

Prasugrel

Product dosage: 10 mg
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Prasugrel is a potent, third-generation thienopyridine antiplatelet agent specifically designed to inhibit platelet aggregation and reduce thrombotic cardiovascular events. It is indicated for the acute management of patients with acute coronary syndromes (ACS) who are to be managed with percutaneous coronary intervention (PCI). As a prodrug, prasugrel requires hepatic conversion to its active metabolite, which irreversibly binds to the P2Y12 component of adenosine diphosphate (ADP) receptors on platelets, providing rapid, consistent, and potent inhibition. Its clinical profile is characterized by a faster onset of action and greater platelet inhibition compared to earlier agents, making it a critical therapeutic option in high-risk settings where swift and reliable antiplatelet effect is paramount to preventing ischemic complications.

Features

• Chemical name: 5-[(1RS)-2-cyclopropyl-1-(2-fluorophenyl)-2-oxoethyl]-4,5,6,7-tetrahydrothieno[3,2-c]pyridin-2-yl acetate
• Molecular formula: C₂₀H₂₀FNO₃S
• Mechanism: Irreversible P2Y12 ADP receptor antagonist
• Prodrug requiring CYP-mediated conversion to active metabolite R-138727
• Onset of action: Peak platelet inhibition within 30 minutes to 4 hours
• Half-life of active metabolite: Approximately 7 hours (range 2–15 hours)
• Available as 5 mg and 10 mg oral tablets

Benefits

• Provides rapid, potent, and consistent platelet inhibition, reducing the risk of stent thrombosis and recurrent ischemic events
• Superior efficacy compared to clopidogrel in reducing composite endpoints of cardiovascular death, nonfatal MI, and nonfatal stroke in ACS patients undergoing PCI
• Lower interpatient variability in platelet response, minimizing concerns regarding hyporesponsiveness
• Once-daily dosing supports adherence and simplifies treatment regimens in high-risk populations
• Demonstrated net clinical benefit in reducing ischemic events despite increased bleeding risk in appropriately selected patients

Common use

Prasugrel is indicated to reduce the rate of thrombotic cardiovascular events (including stent thrombosis) in patients with acute coronary syndromes (unstable angina, non–ST-elevation myocardial infarction, or ST-elevation myocardial infarction) who are to be managed with percutaneous coronary intervention. It is typically initiated as a loading dose followed by maintenance therapy and is used as part of dual antiplatelet therapy (DAPT) in combination with aspirin. Its use is most supported in patients without prior stroke or transient ischemic attack who are not at high risk of bleeding.

Dosage and direction

Initiate treatment with a single 60 mg loading dose. Follow with a 10 mg once-daily maintenance dose. For patients weighing <60 kg, consider a maintenance dose of 5 mg once daily. Administer with or without food. Tablets should be swallowed whole; do not break or crush. Duration of therapy depends on clinical context, stent type, and bleeding risk, but typically continues for at least 12 months in ACS patients unless contraindicated. Therapy beyond 12 months may be considered in select high-risk patients after reevaluation of ischemic and bleeding risks.

Precautions

Prasugrel significantly increases the risk of bleeding, which can be fatal. Active pathological bleeding (such as peptic ulcer or intracranial hemorrhage) is a contraindication. Use with caution in patients with propensity to bleed (e.g., recent trauma, recent surgery, severe hepatic impairment, concomitant use of anticoagulants or other antiplatelets). Consider discontinuation 7 days prior to elective surgery. Monitor for signs of bleeding including hematoma, epistaxis, gastrointestinal bleeding, or retroperitoneal hemorrhage. Thrombotic thrombocytopenic purpura (TTP) has been reported rarely, requiring prompt evaluation if signs/symptoms occur. Not recommended in patients ≥75 years except in high-risk situations (e.g., diabetes, prior MI) where net benefit may outweigh risk.

Contraindications

• Active pathological bleeding
• History of transient ischemic attack (TIA) or stroke
• Hypersensitivity to prasugrel or any component of the formulation
• Severe hepatic impairment (Child-Pugh class C)
• Coadministration with other potent P2Y12 inhibitors is contraindicated

Possible side effect

• Major bleeding (including fatal bleeding and intracranial hemorrhage)
• Minor bleeding (bruising, epistaxis, hematuria)
• Dyspnea
• Hypertension
• Headache
• Dizziness
• Fatigue
• Nausea
• Diarrhea
• Rash
• Atrial fibrillation
• Edema
• Thrombocytopenia
• Thrombotic thrombocytopenic purpura (rare)
• Hypersensitivity reactions including angioedema (rare)

Drug interaction

• Concomitant use with NSAIDs, warfarin, heparin, fibrinolytic therapy, or other anticoagulants increases bleeding risk
• Opioids may delay and decrease absorption of prasugrel
• Strong CYP3A4 inducers (e.g., rifampin) may decrease exposure to active metabolite
• Proton pump inhibitors may be used concomitantly without significant interaction
• Avoid concomitant use with other P2Y12 inhibitors (e.g., clopidogrel, ticagrelor)

Missed dose

If a dose is missed, take it as soon as remembered unless it is nearly time for the next dose. Do not double the dose to make up for a missed one. Maintain the regular dosing schedule. Consistent adherence is critical for maintaining antiplatelet effect; advise patients on the importance of not missing doses.

Overdose

Overdose may lead to bleeding complications. There is no known antidote for prasugrel. Management should be symptomatic and supportive. Platelet transfusion may be considered but may not be effective in reversing the antiplatelet effect due to irreversible receptor binding. Activated charcoal may be administered if ingestion was recent. Hemodialysis is not expected to enhance elimination.

Storage

Store at 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C and 30°C (59°F and 86°F). Keep in the original container with the lid tightly closed. Protect from moisture and light. Keep out of reach of children and pets.

Disclaimer

This information is intended for healthcare professionals and is not a substitute for clinical judgment. Prescribers should refer to the full prescribing information and consider individual patient factors including bleeding risk, comorbidities, and concomitant medications. Dosage adjustments may be necessary based on clinical status. Patients should be advised to report any signs of bleeding promptly.

Reviews

Clinical trials, notably the TRITON-TIMI 38 study, have established prasugrel’s efficacy in reducing ischemic events in ACS patients managed with PCI, though with an increased risk of major bleeding compared to clopidogrel. Subsequent real-world studies and subanalyses have reinforced its role in specific high-risk subsets, such as patients with diabetes or STEMI. Expert consensus guidelines endorse its use in appropriate patients, emphasizing the importance of careful patient selection to maximize benefit and minimize harm. Ongoing research continues to refine its place in therapy relative to other antiplatelet agents.