Prasugrel: Superior Antiplatelet Protection for ACS Patients

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, thereby inhibiting platelet activation and aggregation. This mechanism is critical in preventing the formation of occlusive arterial thrombi, a common complication following coronary stent placement and in the context of ACS. Its clinical profile is characterized by a more rapid, consistent, and potent platelet inhibitory effect compared to earlier agents, making it a cornerstone therapy in modern interventional cardiology for appropriate patient populations.

Features

• Active Ingredient: Prasugrel hydrochloride.
• Pharmacological Class: P2Y12 platelet 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 film-coated tablets (5 mg and 10 mg).
• Rapid Onset: Achieves ≥50% inhibition of platelet aggregation (IPA) within 30 minutes of a loading dose.
• High Bioavailability: Not significantly affected by food intake.
• Prodrug Metabolism: Requires conversion to its active metabolite primarily by cytochrome P450 enzymes, including CYP3A4 and CYP2B6, with minor contributions from CYP2C9 and CYP2C19.

Benefits

• Significant Reduction in Ischemic Events: Demonstrated superior efficacy over clopidogrel in reducing the rate of a combined endpoint of cardiovascular death, nonfatal myocardial infarction (MI), or nonfatal stroke in the TRITON-TIMI 38 trial.
• Decreased Stent Thrombosis: Associated with a markedly lower rate of both early and late stent thrombosis, a serious complication of PCI.
• Rapid and Potent Antiplatelet Effect: Provides consistent and high-level platelet inhibition, which is particularly beneficial in the acute phase of ACS management.
• Reduced Interpatient Variability: Its metabolic pathway is less susceptible to genetic polymorphisms (e.g., CYP2C19 loss-of-function alleles) that can lead to clopidogrel non-responsiveness, offering more predictable pharmacodynamic response.
• Standardized Dosing Regimen: A simple, weight-independent maintenance dose simplifies long-term therapy management for clinicians.

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 [NSTEMI], or ST-elevation myocardial infarction [STEMI]) who are to be managed with percutaneous coronary intervention (PCI). This includes patients undergoing coronary stenting (bare-metal or drug-eluting). Its use is intended as part of a dual antiplatelet therapy (DAPT) regimen, almost always co-administered with aspirin.

Dosage and direction

• Initiation (Loading Dose): A single 60 mg oral loading dose is administered, preferably at the time of PCI.
• Maintenance Therapy: Followed by a 10 mg oral dose once daily.
• Low-Weight Patients: For patients weighing <60 kg, a maintenance dose of 5 mg once daily is recommended due to an observed increase in exposure to the active metabolite and an associated elevated risk of bleeding.
• Timing: Can be taken with or without food.
• Duration: Therapy should be continued for at least 12 months in patients not at high risk of bleeding, unless the risk of bleeding outweighs the benefit of continued therapy. The duration of DAPT is a clinical decision based on individual patient’s ischemic and bleeding risks.

Precautions

• Bleeding Risk: Prasugrel confers a significant risk of serious, sometimes fatal, bleeding. It is contraindicated in patients with active pathological bleeding or a history of transient ischemic attack (TIA) or stroke.
• Surgical Procedures: Discontinuation of prasugrel 7 days prior to any surgery is recommended due to its irreversible antiplatelet effect and prolonged bleeding time.
• Thrombotic Thrombocytopenic Purpura (TTP): TTP, a rare but serious condition, has been reported with thienopyridines, sometimes after a short exposure (<2 weeks). It requires prompt plasmapheresis.
• Hypersensitivity Reactions: Including anaphylaxis, has been reported.
• Hepatic Impairment: Avoid use in patients with severe hepatic disease, as these patients may have bleeding diatheses. No dosage adjustment is needed in 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 non-hemorrhagic side effects may include:

• Very Common (≥1/10): Minor bleeding (e.g., epistaxis, bruising).
• Common (≥1/100 to <1/10): Severe bleeding (e.g., gastrointestinal, retroperitoneal), anemia, dyspnea, hypertension, headache, dizziness, nausea, diarrhea, rash, hypercholesterolemia/hyperlipidemia, fatigue, back pain, hypotension, atrial fibrillation, non-cardiac chest pain, bradycardia, peripheral edema.
• Uncommon (≥1/1,000 to <1/100): Thrombocytopenia, leukopenia, eosinophilia, hypersensitivity reactions (including angioedema), arthralgia, fever, vertigo.
• Rare (<1/1,000): Thrombotic thrombocytopenic purpura (TTP), serious hypersensitivity reactions including anaphylaxis.

Drug interaction

• Other Antithrombotic Agents: Concomitant use with warfarin, other anticoagulants, fibrinolytics, or chronic NSAIDs (e.g., ibuprofen, naproxen) increases the risk of bleeding.
• Opioid Analgesics: May delay and reduce the absorption of prasugrel due to reduced gastric motility. Consider the use of a parenteral antiplatelet in ACS patients requiring co-administration with opioids.
• Proton Pump Inhibitors (PPIs): While some PPIs can interact with clopidogrel, no clinically significant interaction has been demonstrated between prasugrel and PPIs (e.g., pantoprazole).
• Strong CYP3A4 Inducers: Rifampin and other strong inducers may decrease exposure to the active metabolite of prasugrel, potentially reducing its efficacy. Avoid concomitant use.

Missed dose

Patients should take the next scheduled dose at its regular time. They should not take a double dose to make up for the missed one. Maintaining a consistent daily schedule is important for sustained platelet inhibition.

Overdose

There is no known antidote for prasugrel overdose. Overdose is expected to result in profound platelet inhibition and a significant risk of bleeding. Management should be supportive and include close monitoring for hemorrhagic complications. Platelet transfusion may be considered, but the irreversible binding of the active metabolite means that transfused platelets will also be inhibited until new platelets are generated. 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); excursions permitted between 15°C to 30°C (59°F to 86°F).
• Keep the bottle tightly closed and protect from moisture.
• 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 (2007): A landmark phase III trial comparing prasugrel to clopidogrel in 13,608 patients with ACS scheduled for PCI. Prasugrel significantly reduced the primary efficacy endpoint (a composite of cardiovascular death, nonfatal MI, or nonfatal stroke) from 12.1% to 9.9% (HR 0.81; P<0.001). This benefit came at the cost of an increase in major bleeding (2.4% vs. 1.8%; P=0.03) and fatal bleeding.
• Targeted Literature: Subsequent analyses and real-world evidence studies have consistently reinforced its efficacy in reducing ischemic events, particularly stent thrombosis, while confirming the associated bleeding risk. Its role is firmly established in treatment guidelines for ACS patients undergoing PCI who are at low bleeding risk.
• Expert Consensus: Prasugrel is widely regarded by cardiologists as a highly effective antiplatelet agent for appropriate patients (e.g., those without a history of stroke/TIA, not elderly, and not at high bleeding risk) due to its rapid, potent, and consistent platelet inhibition.