| These highlights do not include all the information needed to use Effient safely and effectively. See full prescribing information for Effient.
EFFIENT (prasugrel) tablets
Initial U.S. Approval: 2009
| CLINICAL PHARMACOLOGY
Mechanism of Action
Prasugrel is an inhibitor of platelet activation and aggregation through the irreversible binding of its active metabolite to the P2Y12 class of ADP receptors on platelets.
Platelet aggregation gradually returns to baseline values over 5-9 days after discontinuation of prasugrel, this time course being a reflection of new platelet production rather than pharmacokinetics of prasugrel. Discontinuing clopidogrel 75 mg and initiating prasugrel 10 mg with the next dose resulted in increased inhibition of platelet aggregation, but not greater than that typically produced by a 10 mg maintenance dose of prasugrel alone. The relationship between inhibition of platelet aggregation and clinical activity has not been established.
| INDICATIONS AND USAGE
Acute Coronary Syndrome
Effient™ is indicated to reduce the rate of thrombotic cardiovascular (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).
Effient has been shown to reduce the rate of a combined endpoint of cardiovascular death, nonfatal myocardial infarction (MI), or nonfatal stroke compared to clopidogrel. The difference between treatments was driven predominantly by MI, with no difference on strokes and little difference on CV death [see Clinical Studies (14)].
It is generally recommended that antiplatelet therapy be administered promptly in the management of ACS because many cardiovascular events occur within hours of initial presentation. In the clinical trial that established the efficacy of Effient, Effient and the control drug were not administered to UA/NSTEMI patients until coronary anatomy was established. For the small fraction of patients that required urgent CABG after treatment with Effient, the risk of significant bleeding was substantial [see Warnings and Precautions (5.2)]. Because the large majority of patients are managed without CABG, however, treatment can be considered before determining coronary anatomy if need for CABG is considered unlikely. The advantages of earlier treatment with Effient must then be balanced against the increased rate of bleeding in patients who do need to undergo urgent CABG.
-- Active pathological bleeding
| WARNINGS AND PRECAUTIONS
--CABG-related bleeding: Risk increases in patients receiving Effient who undergo CABG.
| ADVERSE REACTIONS
Bleeding, including life-threatening and fatal bleeding, is the most commonly reported adverse reaction.
| DOSAGE AND ADMINISTRATION
Initiate Effient treatment as a single 60 mg oral loading dose and then continue at 10 mg orally once daily. Patients taking Effient should also take aspirin (75 mg to 325 mg) daily. Effient may be administered with or without food].
Dosing in Low Weight Patients
| HOW SUPPLIED/STORAGE AND HANDLING
Effient (prasugrel) 5 mg is supplied as a yellow, elongated hexagonal, film-coated, non-scored tablet debossed with "5 MG" on one side and with "4760" on the other side.
5 mg tablets are supplied as follows:
Effient (prasugrel) 10 mg is supplied as a beige, elongated hexagonal, film-coated, non-scored tablet debossed with "10 MG" on one side and "4759" on the other side.
10 mg tablets are supplied as follows:
(*Identi Dose®, unit dose medication, Lilly)
Dispense and keep product in original container. Keep container closed and do not remove desiccant from bottle. Do not break the tablet.
National Institutes of Health, U.S. National Library of Medicine, DailyMed Database.
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