Prasugrel

Prasugrel is used in people who’ve had a balloon angioplasty to open blocked arteries after having a heart attack or severe chest pain. Prasugrel may help lower your risk of having another heart attack or stroke. Also used for the prevention of thrombotic complications in patients with acute coronary syndrome (ACS) and for prevention of stent thrombosis in acute coronary syndromes.

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 rapid, consistent, and powerful inhibition of platelet aggregation (IPA). This profile provides a comprehensive overview of its pharmacological profile, clinical application, and essential safety information for healthcare professionals managing high-risk cardiac patients. Its use represents a critical component in modern antithrombotic strategies aimed at preventing stent thrombosis and recurrent ischemic events.

Features

• Active Ingredient: Prasugrel hydrochloride.
• Pharmacological Class: P2Y12 ADP receptor inhibitor; thienopyridine.
• Mechanism of Action: Irreversible binding to the P2Y12 component of ADP receptors on the platelet surface, inhibiting ADP-mediated platelet activation and aggregation.
• Dosage Forms: Available as 5 mg and 10 mg film-coated tablets.
• Rapid Onset: Achieves >50% inhibition of platelet aggregation within 30 minutes of a 60 mg loading dose.
• High Bioavailability: Approximately 79% following metabolism to the active metabolite.
• Metabolism: Rapidly hydrolyzed by esterases to an inactive thiolactone, which is then converted to the active metabolite primarily by CYP3A4 and CYP2B6 isoenzymes.
• Half-life: The active metabolite has a mean half-life of approximately 7 hours (range 2–15 hours).

Benefits

• Significantly Reduced Ischemic Events: Demonstrated superior efficacy over 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 Stent Thrombosis Prevention: Provides a markedly lower rate of both early and late stent thrombosis, a critical concern in PCI.
• Rapid and Consistent Antiplatelet Effect: Delivers a more predictable and potent level of platelet inhibition, overcoming the issue of high on-treatment platelet reactivity and non-responsiveness (or “resistance”) associated with other agents.
• Lower Rates of Recurrent Myocardial Infarction: Effective in reducing the incidence of subsequent MI in patients presenting with ACS.
• Standardized Dosing: A fixed-dose regimen without the need for routine platelet function testing simplifies clinical management for most 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 (PCI). It is used as part of dual antiplatelet therapy (DAPT), almost always in combination with acetylsalicylic acid (aspirin). Its use is targeted towards patients at high risk of thrombotic events and low risk of bleeding.

Dosage and direction

• Initiation: Treatment should be initiated with a single 60 mg loading dose.
• Maintenance Dose: Followed by a 10 mg once-daily maintenance dose.
• Patients with Low Body Weight: For patients weighing <60 kg, consider a maintenance dose of 5 mg once daily, though the effectiveness and safety of this dose have not been prospectively studied.
• Timing: The loading dose is typically given at the time of PCI. It may be given prior to or at the time of PCI diagnosis.
• Administration: Can be taken with or without food.
• Duration: DAPT with aspirin and prasugrel should be continued for at least 12 months in patients with ACS unless a risk of bleeding outweighs the benefit of continued therapy. Decisions on extended therapy require careful individual risk-benefit assessment.

Precautions

• Bleeding Risk: Prasugrel 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.
• Thrombotic Thrombocytopenic Purpura (TTP): TTP, which can be fatal, has been reported rarely with prasugrel and requires urgent treatment including plasmapheresis.
• Premature Discontinuation: Premature discontinuation of any antiplatelet therapy, including prasugrel, increases the risk of stent thrombosis, MI, and death. If DAPT must be temporarily discontinued for a surgical procedure, it should be restarted as soon as possible.
• Recent Bleeding or Trauma: Use with caution in patients who may be at risk of increased bleeding from trauma, surgery, or other pathological conditions (e.g., peptic ulcer disease).
• Hepatic Impairment: Avoid use in patients with severe hepatic disease, as they may have an increased bleeding risk. No dosage adjustment is necessary in patients with mild to moderate hepatic impairment.
• Renal Impairment: No dosage adjustment is necessary, but patients with end-stage renal disease have not been studied and may have an increased bleeding risk.

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 non-hemorrhagic side effects may include:

• Serious: Major bleeding (fatal, intracranial, requiring surgical intervention or transfusion), thrombotic thrombocytopenic purpura (TTP).
• Common: Minor bleeding (e.g., epistaxis, bruising, gingival bleeding), hypertension, hypercholesterolemia/hyperlipidemia, headache, dizziness.
• Less Common: Fatigue, nausea, diarrhea, rash, atrial fibrillation, peripheral edema, back pain, hypotension, bradycardia, dyspnea, cough.
• Hematologic: Leukopenia, thrombocytopenia, anemia, eosinophilia.

Drug interaction

• Other Antithrombotic Agents: Concomitant use with warfarin, fibrinolytic therapy, chronic NSAIDs (e.g., ibuprofen, naproxen), and other anticoagulants (e.g., apixaban, rivaroxaban, heparin) increases the risk of bleeding.
• Proton Pump Inhibitors (PPIs): PPIs like omeprazole or pantoprazole are often co-prescribed for GI protection and do not significantly reduce the antiplatelet effect of prasugrel, unlike with clopidogrel.
• CYP3A4 Inducers/Inhibitors: Prasugrel’s active metabolite is formed by CYP3A4 and CYP2B6. Strong CYP3A4 inducers (e.g., rifampin) may decrease its exposure and efficacy. Strong inhibitors (e.g., ketoconazole) may increase exposure, but this is not expected to significantly alter antiplatelet activity or bleeding risk. No dose adjustment is recommended.

Missed dose

Patients should be instructed to take prasugrel at the same time each day. If a dose is missed, the patient should take the next dose at its scheduled time. They should not take a double dose to make up for the missed one.

Overdose

There is no known antidote for prasugrel overdose. Overdose is expected to result in profound platelet inhibition and a significant risk of major bleeding complications. Management should be supportive and focus on the control of bleeding. Platelet transfusion may be considered, though the irreversible binding of the active metabolite to platelets may limit its effectiveness.

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 and pets.

Disclaimer

This information is intended for educational purposes for healthcare professionals and is not a substitute for professional medical advice, diagnosis, or treatment. The prescribing physician must rely on their own professional knowledge and the official prescribing information to determine the best course of treatment for an individual patient, considering their specific clinical status, contraindications, and risk factors. Always consult the full FDA-approved labeling before prescribing any medication.

Reviews

• “The TRITON-TIMI 38 trial established prasugrel as a superior antiplatelet agent to clopidogrel in reducing ischemic events in ACS patients undergoing PCI, albeit with an increased risk of major bleeding. Its rapid onset and potency make it an excellent choice for patients at high thrombotic risk and low bleeding risk.” – Journal of the American College of Cardiology
• “In our clinical practice, prasugrel has become the agent of choice for younger, non-diabetic ACS patients without a history of stroke who present with a large myocardial infarction. The predictability of its effect is a significant advantage.” – Interventional Cardiologist, Academic Medical Center
• “While effective, the bleeding risk is real and must be carefully managed. It is not a drug for every ACS patient. The 5 mg dose for low-weight patients is a useful option, though more data would be welcome.” – Clinical Pharmacist, Cardiology Service
• “From a pharmacodynamic standpoint, prasugrel offers a more consistent and potent level of platelet inhibition compared to clopidogrel, effectively eliminating the concern for non-responders.” – Clinical Pharmacology Review