Prasugrel: Superior Antiplatelet Protection for ACS Patients
| Product dosage: 10 mg | |||
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Synonyms | |||
Prasugrel is a potent, third-generation thienopyridine antiplatelet agent specifically designed to inhibit platelet aggregation and reduce the incidence of thrombotic cardiovascular events in high-risk patients. It achieves rapid and consistent platelet inhibition through irreversible binding to the P2Y12 ADP receptor, offering a significant therapeutic advantage in acute coronary syndrome (ACS) management, particularly for those undergoing percutaneous coronary intervention (PCI). Its optimized metabolic pathway ensures reliable bioavailability and predictable pharmacodynamic response, making it a cornerstone therapy in modern cardiology for preventing stent thrombosis and recurrent ischemic events.
Features
- Irreversible P2Y12 ADP receptor antagonist with potent antiplatelet effects
- Prodrug requiring hepatic cytochrome P450-mediated conversion to active metabolite
- Rapid onset of action, achieving >50% inhibition of platelet aggregation within 30 minutes
- Consistent platelet inhibition with low interpatient variability
- Once-daily oral dosing regimen for maintenance therapy
- Available in 5 mg and 10 mg film-coated tablets
Benefits
- Significantly reduces rates of stent thrombosis compared to clopidogrel
- Lowers incidence of cardiovascular death, myocardial infarction, and stroke in ACS patients
- Provides more predictable antiplatelet response, minimizing treatment failure risk
- Rapid therapeutic effect benefits urgent PCI scenarios
- Maintains efficacy across various genetic metabolizer profiles
- Supports long-term secondary prevention in high-risk cardiovascular patients
Common use
Prasugrel is indicated for the reduction of thrombotic cardiovascular events in patients with acute coronary syndrome (unstable angina, non-ST-elevation myocardial infarction, or ST-elevation myocardial infarction) who are to be managed with percutaneous coronary intervention. This includes patients requiring stent placement to maintain coronary artery patency and those at high risk for subsequent ischemic events. It is typically administered as part of dual antiplatelet therapy (DAPT) alongside aspirin, following current ACC/AHA guideline recommendations for ACS management.
Dosage and direction
Initiate treatment with a 60 mg loading dose followed by 10 mg once daily maintenance dosing. For patients weighing <60 kg, consider 5 mg once daily maintenance dose. Administer with or without food. Swallow tablet whole; do not crush or break. Continue therapy for at least 12 months unless contraindicated by bleeding risk or other clinical considerations. For patients undergoing PCI, administer loading dose at time of diagnosis or immediately prior to procedure. Do not initiate prasugrel in patients likely to undergo coronary artery bypass graft surgery.
Precautions
Monitor for signs of bleeding throughout treatment period. Assess bleeding risk using standardized scoring systems before initiation. Use caution in patients with propensity to bleed (e.g., recent trauma, surgery, peptic ulcer disease, or hemorrhagic disorders). Consider shorter duration of therapy (3-6 months) in patients with high bleeding risk. Regularly evaluate hemoglobin and hematocrit levels. Discontinue至少 7 days prior to elective surgery if possible. Use caution in patients with severe hepatic impairment (avoid in patients with active pathological bleeding). Educate patients about bleeding risk and need to report unusual bruising or bleeding promptly.
Contraindications
Active pathological bleeding; history of transient ischemic attack or stroke; severe hepatic impairment; hypersensitivity to prasugrel or any component of the formulation; concomitant use with other potent P2Y12 inhibitors; planned coronary artery bypass graft surgery. Not recommended for patients ≥75 years except in high-risk situations where benefit outweighs risk. Contraindicated in patients with prior intracranial hemorrhage or structural intracranial abnormalities.
Possible side effects
- Bleeding (major and minor bleeding events including fatal bleeding)
- Thrombotic thrombocytopenic purpura (TTP)
- Hypersensitivity reactions including anaphylaxis
- Hematological abnormalities (thrombocytopenia, neutropenia)
- Gastrointestinal hemorrhage
- Epistaxis
- Hematuria
- Bruising
- Dyspnea
- Atrial fibrillation
- Hypertension
- Headache
- Back pain
- Fatigue
- Rash
Drug interaction
Strong CYP3A inhibitors (ketoconazole): May decrease active metabolite exposure Rifampin: May decrease prasugrel exposure Other anticoagulants/antiplatelets (warfarin, heparin): Increased bleeding risk NSAIDs: Increased gastrointestinal bleeding risk SSRIs/SNRIs: Potential increased bleeding risk Proton pump inhibitors: No clinically significant interaction Opioids: Delayed absorption and reduced exposure
Missed dose
If a dose is missed, take the next dose at its scheduled time. Do not take a double dose to make up for the missed dose. Maintain regular dosing schedule to ensure consistent platelet inhibition. If multiple doses are missed, consult healthcare provider regarding need for reloading dose or therapy adjustment.
Overdose
Overdose may lead to bleeding complications. There is no specific antidote for prasugrel overdose. Management should focus on symptomatic treatment and supportive care. Platelet transfusion may be considered but effectiveness may be limited due to irreversible platelet inhibition. Activated charcoal may be administered if ingestion was recent. Monitor hematological parameters and provide appropriate hemodynamic support. Dialysis is not expected to enhance elimination.
Storage
Store at 20-25°C (68-77°F); excursions permitted to 15-30°C (59-86°F). Keep in original container with desiccant to protect from moisture. Keep tightly closed and out of reach of children. Do not transfer to other containers. Discard any unused medication after expiration date. Protect from light and excessive humidity.
Disclaimer
This information is for educational purposes only and does not constitute medical advice. Always consult with a qualified healthcare professional before starting or changing any medication regimen. Treatment decisions should be based on individual patient characteristics and current clinical guidelines. The prescribing physician should be aware of all contraindications, warnings, and precautions associated with prasugrel therapy.
Reviews
Clinical trials demonstrate prasugrel’s superior efficacy compared to clopidogrel in reducing ischemic events, though with increased bleeding risk. The TRITON-TIMI 38 trial showed significant reduction in primary efficacy endpoint (CV death, MI, stroke) with prasugrel versus clopidogrel (9.9% vs 12.1%; HR 0.81; P<0.001) but higher rate of major bleeding (2.4% vs 1.8%; P=0.03). Subsequent real-world studies confirm these findings while emphasizing appropriate patient selection. Current guidelines recommend prasugrel as a first-line option for DAPT in ACS patients undergoing PCI, particularly those at high ischemic risk without elevated bleeding risk.