Prasugrel: Superior Antiplatelet Protection in ACS

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 rapid, consistent, and potent inhibition of platelet aggregation. This profile is engineered for high-risk scenarios where robust platelet suppression is critical to prevent stent thrombosis and recurrent ischemic events. Its clinical utility is firmly established in large-scale outcomes trials, positioning it as a cornerstone therapy in modern interventional cardiology.

Features

• Active Ingredient: Prasugrel hydrochloride.
• Pharmacological Class: P2Y12 ADP receptor inhibitor; thienopyridine.
• Mechanism of Action: Irreversible binding to the P2Y12 receptor on platelet cell membranes, inhibiting ADP-mediated platelet activation and aggregation.
• Dosage Forms: Film-coated tablets (5 mg and 10 mg).
• Onset of Action: Rapid; achieves >50% inhibition of platelet aggregation within 30 minutes of a loading dose.
• 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 median half-life of approximately 7 hours (range 2–15 hours).
• Excretion: Approximately 68% in urine and 27% in feces as inactive metabolites.

Benefits

• Rapid and Potent Platelet Inhibition: Achieves a higher level of platelet inhibition more quickly than clopidogrel, which is crucial in the acute phase of ACS to prevent ongoing thrombosis.
• Reduced Incidence of Stent Thrombosis: Demonstrated a significant relative risk reduction in both definite and definite/probable stent thrombosis compared to standard clopidogrel therapy.
• Superior Efficacy in Reducing Ischemic Events: Proven to significantly reduce the composite endpoint of cardiovascular death, nonfatal myocardial infarction (MI), or nonfatal stroke in a defined patient population.
• Consistent Pharmacodynamic Response: Exhibits less inter-patient variability in platelet inhibition due to a more efficient metabolic activation process, minimizing the concern for non- or low-response.
• Established Mortality Benefit in High-Risk Subgroups: Shows particular benefit in reducing cardiovascular mortality in patients with diabetes mellitus or a history of prior MI.

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). This includes patients undergoing coronary stenting (both drug-eluting and bare-metal stents). Its use is predicated on the decision to proceed with an invasive strategy. It is not indicated for use in patients managed medically without PCI.

Dosage and direction

• Initiation: Treatment should be initiated as a single 60 mg loading dose.
• Maintenance Dose: Followed by a once-daily 10 mg maintenance dose.
• Timing: The loading dose is typically administered at the time of PCI. Patients taking prasugrel should also take aspirin (75 mg to 325 mg daily) unless contraindicated.
• Duration: Therapy is recommended for up to 12 months in patients not at high risk of bleeding. Duration may be shorter or longer based on individual patient assessment (ischemic vs. bleeding risk).
• Low-Body-Weight Patients: For patients weighing <60 kg, consider a maintenance dose of 5 mg once daily, though the effectiveness of this dose is uncertain.

Precautions

• Bleeding Risk: Prasugrel increases the risk of bleeding, including life-threatening and fatal bleeding. Active pathological bleeding (e.g., peptic ulcer, intracranial hemorrhage) is a contraindication.
• Risk Assessment: Carefully consider the patient’s inherent bleeding risk (e.g., age, weight, history of bleeding disorders, concomitant medications, recent surgery) before initiating therapy.
• Surgery: If possible, discontinue prasugrel at least 7 days prior to any elective surgery to mitigate bleeding risk.
• Thrombotic Thrombocytopenic Purpura (TTP): TTP, a potentially fatal condition characterized by thrombocytopenia and microangiopathic hemolytic anemia, has been reported rarely with thienopyridine use. It requires prompt plasmapheresis.
• Hypersensitivity: Hypersensitivity reactions including anaphylaxis have been reported.

Contraindications

• Active pathological bleeding (e.g., peptic ulcer, intracranial hemorrhage).
• History of transient ischemic attack (TIA) or stroke.
• Severe hepatic impairment (Child-Pugh Class C), as the impact on drug metabolism and bleeding risk is unknown.
• Hypersensitivity to prasugrel or any component of the product.

Possible side effect

The most common adverse reaction is bleeding. Other important side effects include:

• Major bleeding (e.g., fatal bleeding, intracranial hemorrhage, requiring transfusion).
• Minor bleeding (e.g., epistaxis, bruising, gingival bleeding).
• Thrombocytopenia (including severe cases).
• Leukopenia (including severe cases).
• Anemia.
• Rash.
• Hypertension.
• Hypercholesterolemia/Hyperlipidemia.
• Headache.
• Dizziness.
• Back pain.
• Dyspnea.
• Atrial fibrillation.
• Fatigue.
• Non-cardiac chest pain.
• Hypertensive crisis.

Drug interaction

• Other Antithrombotics: 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 reduce the absorption and peak concentration of prasugrel due to reduced gastric motility. Consider the use of a parenteral antiplatelet agent in ACS patients requiring opioid agonists.
• Proton Pump Inhibitors (PPIs): Unlike clopidogrel, prasugrel’s activation is not dependent on CYP2C19; therefore, it can be co-administered with PPIs (e.g., omeprazole) without a anticipated reduction in efficacy.

Missed dose

Patients should take the 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. Platelet transfusion may be considered, but restoration of hemostasis may not be immediate due to the irreversible nature of the drug’s binding.

Storage

• Store at room temperature, 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 to protect from moisture and light.
• Keep out of reach of children and pets.

Disclaimer

This information is for educational and informational purposes only and does not constitute medical advice. It is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition or before starting or stopping any medication. Never disregard professional medical advice or delay in seeking it because of something you have read here.

Reviews

• TRITON-TIMI 38 Trial (New England Journal of Medicine, 2007): The pivotal trial demonstrated that in patients with ACS with scheduled PCI, prasugrel therapy was associated with a significant 19% reduction in the primary efficacy endpoint (a composite of death from cardiovascular causes, nonfatal MI, or nonfatal stroke) compared to clopidogrel. This came at the cost of a significant 32% increase in major bleeding, including fatal bleeding. The net clinical benefit was favorable except in specific subgroups (prior stroke/TIA, age ≥75 years, weight <60 kg).
• Expert Consensus (Journal of the American College of Cardiology, various): Prasugrel is consistently given a Class I recommendation in U.S. and European guidelines for P2Y12 inhibitor therapy in ACS patients undergoing PCI, particularly for those at high ischemic risk without high bleeding risk (e.g., diabetics, those with stent thrombosis on clopidogrel).
• Real-World Evidence Studies: Numerous registry-based studies have confirmed the efficacy and safety profile of prasugrel observed in the clinical trial, supporting its use in contemporary practice with appropriate patient selection to maximize benefit and minimize harm.