Prasugrel: Superior Platelet Inhibition for ACS and PCI
Prasugrel
| Product dosage: 10 mg | |||
|---|---|---|---|
| Package (num) | Per pill | Price | Buy |
| 30 | 2.11 $ | 63.18 $ (0%) | 🛒 Add to cart |
| 60 | 1.93 $ | 126.36 $ 115.83 $ (8%) | 🛒 Add to cart |
| 90 | 1.86 $ | 189.54 $ 167.31 $ (12%) | 🛒 Add to cart |
| 120 | 1.75 $ | 252.72 $ 209.43 $ (17%) | 🛒 Add to cart |
| 180 | 1.69 $ | 379.08 $ 304.20 $ (20%) | 🛒 Add to cart |
| 360 | 1.50 $
Best per pill | 758.16 $ 540.54 $ (29%) | 🛒 Add to cart |
Synonyms | |||
Prasugrel is a potent, third-generation thienopyridine antiplatelet agent indicated for the reduction of thrombotic cardiovascular events in patients with acute coronary syndromes (ACS) managed with percutaneous coronary intervention (PCI). It functions as an irreversible antagonist of the P2Y12 adenosine diphosphate (ADP) receptor on platelets, delivering rapid, consistent, and powerful inhibition of platelet aggregation (IPA). This profile is engineered to provide clinicians with a reliable tool for managing high-risk patients where robust platelet suppression is paramount to preventing stent thrombosis and recurrent ischemic events.
Features
- Active Metabolite: Generates an active metabolite with a faster onset of action and higher mean inhibition of platelet aggregation compared to earlier generation agents.
- Irreversible Binding: Forms a permanent covalent bond with the P2Y12 receptor for the lifespan of the platelet (7-10 days).
- Consistent Pharmacodynamic Response: Demonstrates low inter-patient variability in platelet inhibition, reducing concerns regarding non-responsiveness.
- Rapid Onset: Achieves significant IPA within 30 minutes of a loading dose.
- Standardized Dosing: Available in fixed-dose tablets (5 mg and 10 mg), simplifying treatment regimens.
Benefits
- Significantly Reduces Composite Ischemic Events: Proven superior to clopidogrel in reducing the rate of a composite endpoint of cardiovascular death, nonfatal myocardial infarction (MI), or nonfatal stroke in the TRITON-TIMI 38 trial.
- Superior Efficacy in Stent Thrombosis Prevention: Demonstrates a markedly lower rate of both early and late stent thrombosis, a critical concern in PCI.
- Rapid and Potent Antiplatelet Effect: Provides a high level of platelet inhibition quickly, which is crucial in the acute phase of ACS.
- Predictable Pharmacological Profile: Minimizes the incidence of high on-treatment platelet reactivity (HPR), a phenomenon associated with increased ischemic risk.
- No Requirement for Metabolic Activation Testing: Unlike clopidogrel, its efficacy is not diminished by common genetic polymorphisms (e.g., CYP2C19 loss-of-function alleles), eliminating the need for routine genetic testing.
Common use
Prasugrel is primarily 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 [NSTEMI], or ST-elevation myocardial infarction [STEMI]) who are to be managed with percutaneous coronary intervention (PCI). Its use is predicated on the clinical decision to proceed with an invasive strategy. It is not indicated for the medical management of ACS (i.e., patients treated solely with pharmacotherapy without PCI).
Dosage and direction
- Initiation: Treatment should be initiated as a single 60 mg oral loading dose.
- Maintenance: Followed by a once-daily 10 mg oral maintenance dose.
- Timing: Administer with or without food. For patients undergoing PCI, the loading dose is typically given at the time of the procedure.
- Duration: Patients should take prasugrel daily for up to 12 months unless discontinued earlier for safety reasons. The optimal duration beyond 12 months has not been established.
- Special Population - Low Weight: For patients weighing <60 kg, consider a maintenance dose of 5 mg once daily, though the effectiveness of this dose is less established.
Precautions
- Bleeding Risk: Prasugrel confers a significant risk of serious, sometimes fatal, bleeding. It is contraindicated in patients with a history of transient ischemic attack (TIA) or stroke and in those with active pathological bleeding.
- Surgical Discontinuation: If possible, discontinue prasugrel at least 7 days prior to any elective surgery to mitigate bleeding risk, as its antiplatelet effect is irreversible.
- Thrombotic Thrombocytopenic Purpura (TTP): TTP, which can be fatal, has been reported rarely with thienopyridine use and requires prompt plasmapheresis.
- Hypersensitivity: Hypersensitivity reactions including anaphylaxis have been reported.
- Hepatic Impairment: Avoid use in patients with severe hepatic disease, as they may be at increased risk of bleeding due to coagulopathy.
Contraindications
- Active pathological bleeding (e.g., peptic ulcer, intracranial hemorrhage).
- A history of prior transient ischemic attack (TIA) or stroke.
- Hypersensitivity to prasugrel or any component of the product.
Possible side effect
The most common and serious adverse reaction is bleeding. Other potential side effects include:
- Serious: Major bleeding (fatal, intracranial, requiring surgical intervention or transfusion), life-threatening bleeding, Thrombotic Thrombocytopenic Purpura.
- Common: Minor bleeding (e.g., epistaxis, bruising, gastrointestinal bleeding), hypertension, hypercholesterolemia/hyperlipidemia, headache, dizziness, nausea, back pain, dyspnea, fatigue.
- Less Common: Atrial fibrillation, hypersensitivity reactions (including rash, angioedema), hypotension, bradycardia, anemia, leukopenia, thrombocytopenia, liver enzyme elevations, rash.
Drug interaction
- Other Antithrombotics: Coadministration with warfarin, other oral anticoagulants, fibrinolytic therapy, or chronic NSAID use increases the risk of bleeding. Avoid concomitant use of other P2Y12 inhibitors (e.g., clopidogrel, ticagrelor).
- Proton Pump Inhibitors (PPIs): Unlike clopidogrel, prasugrel’s efficacy is not significantly diminished by PPIs like omeprazole. They may be co-administered for gastroprotection.
- Strong CYP3A4 Inducers: Rifampin and other potent inducers may decrease exposure to the active metabolite of prasugrel, potentially reducing efficacy. Consider alternative agents.
Missed dose
Patients should take the next dose at its scheduled time. They should not take a double dose to make up for a missed dose.
Overdose
There is no known antidote for prasugrel overdose. Overdose is expected to result in pronounced bleeding complications. Management should be supportive and may include blood or platelet transfusions. The irreversible platelet inhibition is not reversible by transfusion; transfused platelets will also be inhibited. Hemodialysis is not expected to enhance elimination, as the active metabolite is highly protein-bound.
Storage
- Store at room temperature between 20°C to 25°C (68°F to 77°F).
- Keep in the original container to protect from moisture and light.
- Keep out of reach of children and pets.
Disclaimer
This information is for educational and professional medical purposes only and is not a substitute for the professional judgment of a healthcare provider. The prescribing physician must evaluate the individual patient’s condition, bleeding risk, and overall clinical status before initiating therapy with prasugrel. The full official prescribing information should be consulted for complete details on warnings, precautions, and adverse reactions.
Reviews
- “As an interventional cardiologist, prasugrel is my go-to agent for high-risk PCI patients without contraindications. The rapid, potent, and predictable platelet inhibition provides a level of confidence in preventing acute stent thrombosis that I found lacking with clopidogrel, especially without the need for genetic testing.” — Interventional Cardiologist, 15 years experience
- “The TRITON-TIMI 38 data clearly established prasugrel’s superiority in reducing ischemic events, albeit with a higher bleeding risk. In our institution, we use it judiciously, carefully selecting patients who stand to gain the most net clinical benefit—typically younger ACS patients without a history of stroke/TIA who are undergoing complex PCI.” — Clinical Pharmacist, Cardiology Specialization
- “While the bleeding risk is a legitimate concern, the dramatic reduction in stent thrombosis is a critical advantage. For the right patient, the benefit clearly outweighs the risk. It has become a cornerstone of our dual antiplatelet therapy protocol post-PCI.” — Director of Cardiac Catheterization Lab
- “The fixed-dose regimen and lack of interaction with PPIs make it easier to manage from a pharmacy and nursing perspective compared to clopidogrel. Patient counseling on the signs of bleeding is absolutely paramount.” — Inpatient Cardiology Nurse Practitioner