Prasugrel

Brand Names: Prasugrel

Drug Class: General Prescription

Overview

11 DESCRIPTION Prasugrel tablets USP contain prasugrel, a thienopyridine class inhibitor of platelet activation and aggregation mediated by the P2Y 12 ADP receptor. Prasugrel is formulated as the hydrochloride salt, a racemate, which is chemically designated as 5-[(1RS)-2-cyclopropyl-1-(2-fluorophenyl)-2-oxoethyl]-4,5,6,7-tetrahydrothieno[3,2-c]pyridin-2-yl acetate hydrochloride.

Mechanism of Action

12 CLINICAL PHARMACOLOGY 12.1 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. 12.2 Pharmacodynamics Prasugrel produces inhibition of platelet aggregation to 20 μM or 5 μM ADP, as measured by light transmission aggregometry. Following a 60 mg loading dose of prasugrel, approximately 90% of patients had at least 50% inhibition of platelet aggregation by 1 hour. Maximum platelet inhibition was about 80% (see Figure 2). Mean steady-state inhibition of platelet aggregation was about 70% following 3 to 5 days of dosing at 10 mg daily after a 60 mg loading dose of prasugrel.

Indications

  • 1 INDICATIONS AND USAGE 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) (1.1) . Patients with ST-elevation myocardial infarction (STEMI) when managed with either primary or delayed PCI (1.1) . 1.

Common Doses

  • 60 mg
  • 10 mg
  • 75 mg
  • 325 mg

Dosage

2 DOSAGE AND ADMINISTRATION 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 [see Drug Interactions (7.4) and Clinical Pharmacology (12.3) ] . Prasugrel tablets may be administered with or without food [see Clinical Pharmacology (12.3) and Clinical Studies (14) ] . 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...

Black Box Warning

WARNING: BLEEDING RISK Prasugrel can cause significant, sometimes fatal, bleeding [see Warnings and Precautions (5.1 , 5.2) and Adverse Reactions (6.1) ] . Do not use prasugrel in patients with active pathological bleeding or a history of transient ischemic attack (TIA) or stroke [see Contraindications (4.1 , 4.2) ] . In patients ≥75 years of age, prasugrel is generally not recommended, because of the increased risk of fatal and intracranial bleeding and uncertain benefit, except in high-risk situations (patients with diabetes or a history of prior myocardial infarction [MI]) where its effect...

Contraindications

  • 4 CONTRAINDICATIONS Active pathological bleeding (4.1) Prior transient ischemic attack or stroke (4.2) Hypersensitivity to prasugrel or any component of the product (4.3) 4.1 Active Bleeding Prasugrel tablets are contraindicated in patients with active pathological bleeding such as peptic ulcer or intracranial hemorrhage (ICH) [see Warnings and Precautions (5.1) and Adverse Reactions (6.1) ] . 4.2 Prior Transient Ischemic Attack or Stroke Prasugrel tablets are contraindicated in patients with a history of prior transient ischemic attack (TIA) or stroke.

Side Effects

  • 6 ADVERSE REACTIONS The following serious adverse reactions are also discussed elsewhere in the labeling: Bleeding [see Boxed Warning and Warnings and Precautions (5.1 , 5.2) ] Thrombotic Thrombocytopenic Purpura [see Warnings and Precautions (5.4) ] Hypersensitivity Including Angioedema [see Warnings and Precautions (5.5) ] Bleeding, including life-threatening and fatal bleeding, is the most commonly reported adverse reaction (6.1) . To report SUSPECTED ADVERSE REACTIONS, contact Aurobindo Pharma USA, Inc. at 1-866-850-2876 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.

Interactions

  • 7 DRUG INTERACTIONS Opioids: Decreased exposure to prasugrel. Consider use of parenteral antiplatelet agent (7.3). 7.1 Warfarin Coadministration of prasugrel and warfarin increases the risk of bleeding [see Warnings and Precautions (5.1) and Clinical Pharmacology (12.3) ] . 7.2 Nonsteroidal Anti-Inflammatory Drugs Coadministration of prasugrel and NSAIDs (used chronically) may increase the risk of bleeding [see Warnings and Precautions (5.1) ] . 7.