Prasugrel: Superior Platelet Inhibition for ACS and PCI

Prasugrel

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Product dosage: 10 mg
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Synonyms Effient

Prasugrel is a potent, third-generation thienopyridine antiplatelet agent indicated for the reduction of thrombotic cardiovascular events in patients with acute coronary syndromes (ACS) who are to be managed with percutaneous coronary intervention (PCI). It functions as an irreversible antagonist of the P2Y12 adenosine diphosphate (ADP) receptor on platelets, delivering faster, more consistent, and greater platelet inhibition than its predecessors. This profile provides a comprehensive overview of its pharmacology, clinical application, and essential safety information for healthcare professionals managing high-risk cardiac patients.

Features

• Active Ingredient: Prasugrel hydrochloride.
• Pharmacologic Class: Thienopyridine P2Y12 platelet ADP receptor inhibitor.
• Mechanism of Action: Irreversible binding to the P2Y12 component of ADP receptors on platelet surfaces, inhibiting ADP-mediated platelet activation and aggregation.
• Dosage Forms: Film-coated tablets available in 5 mg and 10 mg strengths.
• Rapid Onset: Achieves >50% inhibition of platelet aggregation (IPA) within 30 minutes and peak effect (approximately 80% IPA) within 2-4 hours of a loading dose.
• Consistent Effect: Demonstrates less inter-patient variability in platelet response compared to clopidogrel, partly due to a more efficient metabolic activation process that is less dependent on CYP2C19 genotype.
• Potent Inhibition: Provides a greater degree of platelet inhibition than standard-dose clopidogrel.

Benefits

• Significant Reduction in Ischemic Events: Demonstrated in the TRITON-TIMI 38 trial to significantly reduce the rate of a composite endpoint of cardiovascular death, nonfatal myocardial infarction (MI), or nonfatal stroke compared to clopidogrel in ACS patients undergoing PCI.
• Lower Rate of Stent Thrombosis: Associated with a markedly reduced incidence of both early and late stent thrombosis, a serious complication of PCI.
• Rapid and Predictable Antiplatelet Effect: The swift and reliable onset of action is particularly beneficial in the urgent setting of ACS, ensuring adequate platelet inhibition at the time of PCI.
• Efficacy Irrespective of CYP2C19 Status: Provides effective platelet inhibition in patients who are poor metabolizers via the CYP2C19 pathway, a group at risk for reduced efficacy with clopidogrel.

Common use

Prasugrel is approved for use in combination with aspirin (acetylsalicylic acid) for the prevention of atherothrombotic events in patients with ACS (unstable angina, non-ST-elevation myocardial infarction [NSTEMI], or ST-elevation myocardial infarction [STEMI]) who are to be managed with PCI. This includes patients undergoing coronary stenting (both drug-eluting and bare-metal stents). Its use is targeted at a specific, high-risk population where its potent antiplatelet effect provides a net clinical benefit, outweighing the increased bleeding risk.

Dosage and direction

• Initiation (Loading Dose): A single 60 mg oral loading dose should be given as soon as possible after a decision is made to proceed with PCI.
• Maintenance Therapy: Follow with a 10 mg oral dose once daily. Patients weighing <60 kg should receive a 5 mg once-daily maintenance dose.
• Timing: Can be taken with or without food.
• Duration: Therapy is typically continued for up to 12 months, unless discontinuation is warranted due to bleeding or other concerns. The optimal duration beyond 12 months in patients who have tolerated therapy is an area of ongoing clinical investigation and should be determined on an individual patient basis considering ischemic and bleeding risks.
• Coadministration: Must be administered concomitantly with aspirin (75 mg to 325 mg daily). The aspirin maintenance dose is typically 81 mg daily.

Precautions

• Bleeding Risk: Prasugrel significantly increases the risk of bleeding, including life-threatening and fatal bleeding. It is contraindicated in patients with active pathological bleeding or a history of transient ischemic attack (TIA) or stroke.
• Surgery: If possible, discontinue prasugrel at least 7 days prior to any elective surgery to mitigate bleeding risk, as its antiplatelet effect is irreversible for the life of the platelet (~7-10 days).
• Thrombotic Thrombocytopenic Purpura (TTP): TTP, a rare but serious condition characterized by thrombocytopenia and microangiopathic hemolytic anemia, has been reported with thienopyridines, including prasugrel, sometimes after a short exposure (<2 weeks). Requires prompt diagnosis and treatment, including 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. No dosage adjustment is necessary in patients with mild to moderate hepatic impairment.

Contraindications

• Active pathological bleeding (e.g., peptic ulcer, intracranial hemorrhage).
• History of 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:

• Very Common (>10%): Minor bleeding (e.g., epistaxis, bruising).
• Common (1% to 10%): Hypertension, hypercholesterolemia/hyperlipidemia, headache, dizziness, nausea, back pain, dyspnea, cough, fatigue, non-cardiac chest pain, atrial fibrillation.
• Uncommon (0.1% to 1%): Severe thrombocytopenia, anemia, rash, pruritus, allergic reactions (including angioedema), hypotension, bradycardia, edema peripheral, fever.
• Rare (<0.1%): Thrombotic Thrombocytopenic Purpura (TTP), neutropenia/agranulocytosis, severe hepatic dysfunction, generalized edema, eosinophilic pneumonia.

Drug interaction

• Other Antithrombotic Agents: Concomitant use with warfarin, other oral anticoagulants, fibrinolytic therapy, or chronic NSAIDs increases the risk of bleeding. Use with extreme caution.
• Opioid Agonists: Concurrent use may delay and decrease the absorption of prasugrel due to reduced gastric motility. Consider the use of a parenteral antiplatelet agent in ACS patients requiring coadministration with opioid agonists.
• Proton Pump Inhibitors (PPIs): While some PPIs can reduce the activation of clopidogrel, this is not a concern with prasugrel. PPIs can be coadministered for gastroprotection.
• Strong CYP3A4 Inducers (e.g., rifampin): May decrease exposure to the active metabolite of prasugrel; avoid concomitant use.

Missed dose

Patients should take their next scheduled dose at its regular 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 symptomatic and supportive. Since the drug is not dialyzable, treatment may include transfusion of platelet concentrates to restore hemostatic function, though transfused platelets may also be inhibited by the circulating active metabolite. Bleeding time and other coagulation parameters should be monitored appropriately.

Storage

• Store at room temperature between 20°C to 25°C (68°F to 77°F); excursions permitted between 15°C to 30°C (59°F to 86°F).
• Keep in the original container to protect from moisture and light.
• Keep out of reach of children.

Disclaimer

This information is intended for educational purposes for healthcare professionals and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of a qualified health provider with any questions you may have regarding a medical condition or before making any changes to a treatment plan. The prescribing physician should be thoroughly familiar with the full Prescribing Information, including Boxed Warnings, before initiating therapy with prasugrel.

Reviews

• TRITON-TIMI 38 (Trial to Assess Improvement in Therapeutic Outcomes by Optimizing Platelet Inhibition with Prasugrel–Thrombolysis in Myocardial Infarction 38): This large, phase III, randomized, double-blind trial compared prasugrel (60 mg loading dose, 10 mg maintenance) to clopidogrel (300 mg loading dose, 75 mg maintenance) in 13,608 patients with ACS scheduled for PCI. The primary efficacy endpoint (a composite of death from cardiovascular causes, nonfatal MI, or nonfatal stroke) occurred in 12.1% of patients receiving clopidogrel versus 9.9% of those receiving prasugrel (HR 0.81; 95% CI, 0.73 to 0.90; P<0.001). The key safety endpoint, major bleeding not related to CABG, occurred in 1.8% of the clopidogrel group versus 2.4% of the prasugrel group (HR 1.32; 95% CI, 1.03 to 1.68; P=0.03). The net clinical benefit (combining efficacy and safety endpoints) favored prasugrel. Subgroup analyses identified patients with a history of TIA/stroke and those aged ≥75 years or weighing <60 kg as having less favorable benefit-risk profiles.
• Expert Consensus Guidelines (ACC/AHA): Guidelines for the management of patients with ACS give prasugrel a Class I recommendation (Level of Evidence: B) for use in ACS patients undergoing PCI who are not at high risk of bleeding and who have no contraindications (specifically, no history of TIA or stroke). It is recognized for its superior efficacy in reducing stent thrombosis and composite ischemic events compared to clopidogrel, balanced against a higher risk of major bleeding.