Prasugrel

What it is and how it works

Mechanism of Action Prasugrel is an inhibitor of platelet activation and aggregation through the irreversible binding of its active metabolite to the P2Y 12 class of ADP receptors on platelets.

Indications

Prasugrel tablets are a P2Y 12 platelet inhibitor indicated for the reduction of thrombotic cardiovascular events (including stent thrombosis) in patients with acute coronary syndrome who are to be managed with percutaneous coronary intervention (PCI) as follows: • Patients with unstable angina or non-ST-elevation myocardial infarction (NSTEMI) . • Patients with ST-elevation myocardial infarction (STEMI) when managed with either primary or delayed PCI . Acute Coronary Syndrome Prasugrel tablets are indicated to reduce the rate of thrombotic CV events (including stent thrombosis) in patients with acute coronary syndrome (ACS) who are to be managed with percutaneous coronary intervention (PCI) as follows: • Patients with unstable angina (UA) or non-ST-elevation myocardial infarction (NSTEMI). • Patients with ST-elevation myocardial infarction (STEMI) when managed with primary or delayed PCI. Prasugrel tablets have been shown to reduce the rate of a combined endpoint of cardiovascular death, nonfatal myocardial infarction (MI), or nonfatal stroke compared to clopidogrel.

Dosage and administration (summary)

Initiate prasugrel tablets treatment as a single 60 mg oral loading dose and then continue at 10 mg orally once daily. Patients taking prasugrel tablets should also take aspirin (75 mg to 325 mg) daily . Prasugrel tablets may be administered with or without food . Timing of Loading Dose: In the clinical trial that established the efficacy and safety of prasugrel tablets, the loading dose of prasugrel tablets was not administered until coronary anatomy was established in UA/NSTEMI patients and in STEMI patients presenting more than 12 hours after symptom onset.

Contraindications

• Active pathological bleeding . • Prior transient ischemic attack or stroke . • Hypersensitivity to prasugrel or any component of the product . Active Bleeding Prasugrel tablets are contraindicated in patients with active pathological bleeding such as peptic ulcer or intracranial hemorrhage (ICH) . Prior Transient Ischemic Attack or Stroke Prasugrel tablets are contraindicated in patients with a history of prior transient ischemic attack (TIA) or stroke.

Warnings and precautions

• CABG-related bleeding: Risk increases in patients receiving prasugrel tablets who undergo CABG . • Discontinuation of prasugrel tablets: Premature discontinuation increases risk of stent thrombosis, MI, and death . • Thrombotic thrombocytopenic purpura (TTP): TTP has been reported with prasugrel tablets . • Hypersensitivity: Hypersensitivity including angioedema has been reported with prasugrel tablets including in patients with a history of hypersensitivity reaction to other thienopyridines .

Pregnancy

Pregnancy Risk Summary There are no data with prasugrel tablets use in pregnant women to inform a drug-associated risk. No structural malformations were observed in animal reproductive and developmental toxicology studies when rats and rabbits were administered prasugrel during organogenesis at doses of up to 30 times the recommended therapeutic ex…

Storage and supply

How Supplied Prasugrel Tablets, USP are available containing prasugrel hydrochloride, USP equivalent to 5 mg or 10 mg prasugrel, respectively. The 5 mg tablets are yellow, film-coated, capsule shaped, unscored tablets debossed with M on one side of the tablet and PH1 on the other side.

Source: Prasugrel (Prasugrel) — US FDA prescribing information, 2022-06-29, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.