Prasurel

• Acute Coronary Syndrome (ACS):
  Indicated to reduce thrombotic cardiovascular events, including stent thrombosis, in patients with unstable angina, non–ST-segment elevation myocardial infarction (NSTEMI), or ST-segment elevation myocardial infarction (STEMI) undergoing percutaneous coronary intervention (PCI).
• Off-label uses:
  Occasionally used in other thrombotic disorders requiring potent platelet inhibition, although not officially approved for these indications.

• Adults:
• Loading dose: 60 mg orally once, administered at least 1 hour before PCI or immediately after PCI if not given before.
• Maintenance dose: 10 mg orally once daily starting 24 hours after the loading dose.
• For patients weighing less than 60 kg, a reduced maintenance dose of 5 mg once daily is recommended.
• Elderly (>75 years):
  Generally not recommended unless high-risk features are present; if used, consider 5 mg maintenance dose.
• Renal impairment:
  No dose adjustment required.
• Hepatic impairment:
  Use with caution in severe hepatic impairment; no specific dose adjustment available.
• Route: Oral.
• Administration: Tablets may be taken with or without food.

Prasugrel is an irreversible inhibitor of the platelet P2Y12 ADP receptor. It blocks ADP-mediated activation of the glycoprotein GPIIb/IIIa complex on platelets, preventing platelet aggregation. This action reduces the formation of blood clots within coronary arteries, thus lowering the risk of ischemic events in patients with ACS undergoing PCI.

• Absorption: Rapid and nearly complete after oral administration.
• Bioavailability: High due to rapid conversion from prodrug to active metabolite.
• Distribution: Approximately 98% plasma protein binding.
• Metabolism: Extensive hepatic metabolism primarily via CYP3A4 and CYP2B6 enzymes to the active metabolite.
• Elimination: Mainly excreted in urine (~68%) and feces (~27%).
• Half-life: Active metabolite half-life approximately 7 hours.
• Onset of action: Platelet inhibition begins within 30 minutes to 1 hour post-dose.

• Pregnancy: Category B. Animal studies have shown no harm to the fetus; however, controlled human studies are lacking. Use only if clearly needed and after risk-benefit evaluation.
• Lactation: Unknown if excreted in breast milk. Use caution when administering to breastfeeding women.

• Antiplatelet agent
• Thienopyridine class P2Y12 receptor antagonist

• Known hypersensitivity to prasugrel or any component of the formulation.
• Active pathological bleeding (e.g., peptic ulcer, intracranial hemorrhage).
• History of transient ischemic attack (TIA) or stroke.
• Severe hepatic impairment.

• Increased risk of bleeding, including life-threatening and fatal hemorrhage. Use caution in patients at risk for bleeding.
• Not recommended in patients with prior stroke or TIA due to increased risk of intracranial hemorrhage.
• Discontinue prasugrel at least 7 days before elective surgery to reduce bleeding risk.
• Monitor for signs of bleeding during treatment.
• Use with caution in elderly patients and those with low body weight (<60 kg).
• Rare cases of thrombotic thrombocytopenic purpura (TTP) have been reported.

• Common: Bleeding (gastrointestinal, genitourinary), bruising, nausea, headache.
• Serious: Major bleeding (intracranial, gastrointestinal), hypersensitivity reactions, thrombotic thrombocytopenic purpura, thrombocytopenia.
• Side effects are dose- and duration-dependent.

• Increased bleeding risk with concomitant use of anticoagulants, other antiplatelet agents, NSAIDs, SSRIs, and SNRIs.
• Metabolized by CYP3A4 and CYP2B6; inhibitors or inducers of these enzymes may affect drug levels.
• No significant interaction with proton pump inhibitors has been reported.

• Guidelines recommend prasugrel for ACS patients undergoing PCI with high ischemic risk and low bleeding risk.
• Dose adjustments for body weight and age emphasized in recent recommendations.
• Enhanced warnings about bleeding risk and contraindications have been highlighted by regulatory authorities.

• Store at 20°C to 25°C (68°F to 77°F).
• Protect from moisture and light.
• Keep container tightly closed.
• Do not freeze.