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 specifically 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 characteristics, clinical utility, and essential safety information for healthcare professionals managing high-risk cardiovascular patients.

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 platelet surfaces, 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 loading dose.
• High Bioavailability: Not significantly affected by food; demonstrates minimal inter-patient variability in platelet response.
• Prodrug Metabolism: Requires conversion to its active metabolite (R-138727) primarily by 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 composite endpoint of cardiovascular death, nonfatal myocardial infarction (MI), or nonfatal stroke in the pivotal TRITON-TIMI 38 trial.
• Decreased Stent Thrombosis Risk: Provides a markedly lower incidence of both early and late stent thrombosis, a critical concern in PCI.
• Rapid and Predictable Antiplatelet Effect: Offers a more consistent pharmacodynamic response compared to other agents, minimizing the prevalence of high on-treatment platelet reactivity (HPR), which is associated with adverse ischemic outcomes.
• Standardized Dosing Regimen: Simplifies treatment initiation and maintenance without the need for routine platelet function testing for dose adjustment in the vast majority of 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 [NSTEMI], or ST-elevation myocardial infarction [STEMI]) who are to be managed with percutaneous coronary intervention (PCI). Its use is predicated on the significant ischemic benefit outweighing the inherent increase in bleeding risk. It is not indicated for the management of patients with ACS who are managed medically without coronary intervention.

Dosage and direction

• Initiation: Treatment should be initiated as a single 60 mg loading dose.
• Maintenance: Followed by a once-daily 10 mg maintenance dose.
• Patient Weight <60 kg: For patients weighing less than 60 kg, consider a maintenance dose of 5 mg once daily, though the effectiveness and safety of this dose are not fully established.
• Timing: Administer with or without food. The loading dose should be given promptly and generally prior to, or at the time of, PCI.
• Duration: Therapy is recommended for up to 12 months in patients not at high risk of bleeding, unless discontinuation is clinically warranted. The optimal duration beyond 12 months has not been established.

Precautions

• Bleeding Risk: Prasugrel increases the risk of significant, sometimes fatal, bleeding. It is contraindicated in patients with active pathological bleeding or a history of transient ischemic attack (TIA) or stroke.
• Surgical Discontinuation: If possible, discontinue prasugrel at least 7 days prior to any surgery, including coronary artery bypass graft (CABG) 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 and requires prompt treatment.
• 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 (due to lack of clinical data and potential for increased bleeding risk).
• Hypersensitivity to prasugrel or any component of the product.

Possible side effect

The most common and serious adverse reaction is bleeding. Other reported side effects include:

• Very Common (≥1/10): Minor bleeding (e.g., epistaxis, bruising).
• Common (≥1/100 to <1/10): Hypertension, hypercholesterolemia/hyperlipidemia, headache, dizziness, nausea, back pain, dyspnea, cough, fever.
• Uncommon (≥1/1,000 to <1/100): Severe thrombocytopenia, anemia, rash, pruritus, hypertension crisis, atrial fibrillation, bradycardia, hypotension, peripheral edema.
• Rare (<1/1,000): Thrombotic thrombocytopenic purpura (TTP), hypersensitivity reactions including angioedema, leukopenia, eosinophilia, hepatic function abnormalities.

Drug interaction

• Other Antithrombotics: Coadministration with warfarin, other oral anticoagulants, fibrinolytics, or chronic NSAIDs increases the risk of bleeding. Avoid concomitant use with other P2Y12 inhibitors (e.g., clopidogrel, ticagrelor).
• Proton Pump Inhibitors (PPIs): Unlike clopidogrel, prasugrel’s metabolism is not significantly affected by PPIs (e.g., omeprazole); coadministration is acceptable.
• CYP3A4 Inducers/Inhibitors: Prasugrel is metabolized to its active form by CYP3A4. Strong inhibitors (e.g., ketoconazole) may decrease active metabolite exposure, while inducers (e.g., rifampin) may increase it. However, dose adjustment is not recommended.

Missed dose

Patients should be instructed to 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. It may include appropriate transfusion of blood products and monitoring of vital signs. Platelet transfusion is unlikely to be effective due to the irreversible binding of the active metabolite to platelets; however, it may be considered in life-threatening situations.

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. The prescribing physician should be thoroughly familiar with the full Prescribing Information, including the Boxed Warning regarding bleeding risk, before initiating therapy with prasugrel. Always consider the individual patient’s clinical status, bleeding risk, and concomitant medications.

Reviews

(Compilation of expert consensus and clinical trial data summaries)

• TRITON-TIMI 38 Trial (2007): The landmark trial that established prasugrel’s superior efficacy over clopidogrel in reducing ischemic events in ACS patients undergoing PCI (12.1% vs. 9.9%, HR 0.81; P<0.001), albeit with an increased risk of major bleeding (2.4% vs. 1.8%, P=0.03) and fatal bleeding.
• 2011 ACCF/AHA Focused Update: Incorporated prasugrel as a Class I recommendation (Level of Evidence: B) for antiplatelet therapy in UA/NSTEMI patients undergoing PCI.
• Real-World Evidence: Subsequent registry studies and meta-analyses have generally confirmed the efficacy and safety profile observed in the pivotal trial, reinforcing its role in contemporary PCI practice for appropriate, low-bleeding-risk patients.
• Expert Consensus: Widely regarded as a first-line option for P2Y12 inhibition in ACS-PCI patients who are not at high risk for bleeding and without a history of stroke/TIA, valued for its rapid onset and predictable effect.