EFFIENT Film-coated tablet (2021)

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Eli Lilly and Company

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BOXED WARNING SECTION

WARNING: BLEEDING RISK Effient can cause significant, sometimes fatal, bleeding [see Warnings and Precautions (5.1, 5.2) and Adverse Reactions (6.1)]. Do not use Effient in patients ...

1. Indications and Usage

1.1 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 ...

2. 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 [see Drug Interactions ...

3. Dosage Forms and Strengths

Effient 5-mg is available as a yellow, elongated hexagonal, film-coated, non-scored tablet debossed with 5121 on one side and 3 parallel arched lines followed by a 5 on the other side. Effient 10-mg is ...

4. Contraindications

4.1 Active Bleeding Effient is contraindicated in patients with active pathological bleeding such as peptic ulcer or intracranial hemorrhage [see Warnings and Precautions (5.1) and Adverse Reactions ...

5. Warnings and Precautions

5.1 General Risk of Bleeding Thienopyridines, including Effient, increase the risk of bleeding. With the dosing regimens used in TRITON-TIMI 38, TIMI (Thrombolysis in Myocardial Infarction) Major (clinically ...

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 ...

6.1. Clinical Trials Experience

Safety in patients with ACS undergoing PCI was evaluated in a clopidogrel-controlled study, TRITON-TIMI 38, in which 6741 patients were treated with Effient (60-mg loading dose and 10-mg once daily) for ...

6.2. Postmarketing Experience

The following adverse reactions have been identified during post-approval use of Effient. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible ...

7. Drug Interactions

7.1 Warfarin Coadministration of Effient and warfarin increases the risk of bleeding [see Warnings and Precautions (5.1) and Clinical Pharmacology (12.3)]. 7.2 Non-Steroidal Anti-Inflammatory ...

8. Use in Specific Populations

8.6 Low Body Weight In TRITON-TIMI 38, 4.6% of patients treated with Effient had body weight <60 kg. Individuals with body weight <60 kg had an increased risk of bleeding and an increased exposure to the ...

8.1. Pregnancy

Risk Summary There are no data with Effient use in pregnant women to inform a drug-associated risk. No structural malformations were observed in animal reproductive and developmental toxicology studies ...

8.2. Lactation

Risk Summary There is no information regarding the presence of prasugrel in human milk, the effects on the breastfed infant, or the effects on milk production. Metabolites of prasugrel were found in rat ...

8.4. Pediatric Use

Safety and effectiveness in pediatric patients have not been established. In a randomized, placebo-controlled trial, the primary objective of reducing the rate of vaso-occlusive crisis (painful crisis ...

8.5. Geriatric Use

In TRITON-TIMI 38, 38.5% of patients were ≥65 years of age and 13.2% were ≥75 years of age. The risk of bleeding increased with advancing age in both treatment groups, although the relative risk of bleeding ...

8.7. Renal Impairment

No dosage adjustment is necessary for patients with renal impairment. There is limited experience in patients with end-stage renal disease, but such patients are generally at higher risk of bleeding ...

8.8. Hepatic Impairment

No dosage adjustment is necessary in patients with mild to moderate hepatic impairment (Child-Pugh Class A and B). The pharmacokinetics and pharmacodynamics of prasugrel in patients with severe hepatic ...

10. Overdosage

10.1 Signs and Symptoms Platelet inhibition by prasugrel is rapid and irreversible, lasting for the life of the platelet, and is unlikely to be increased in the event of an overdose. In rats, lethality ...

11. Description

Effient contains prasugrel, a thienopyridine class inhibitor of platelet activation and aggregation mediated by the P2Y12 ADP receptor. Effient is formulated as the hydrochloride salt, a racemate, ...

12.1. 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.

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 Effient, approximately 90% of patients had ...

12.3. Pharmacokinetics

Prasugrel is a prodrug and is rapidly metabolized to a pharmacologically active metabolite and inactive metabolites. The active metabolite has an elimination half-life of about 7 hours (range 2-15 hours). ...

12.5. Pharmacogenomics

There is no relevant effect of genetic variation in CYP2B6, CYP2C9, CYP2C19, or CYP3A5 on the pharmacokinetics of prasugrels active metabolite or its inhibition of platelet aggregation.

13.1. Carcinogenesis, Mutagenesis, Impairment of Fertility

Carcinogenesis No compound-related tumors were observed in a 2-year rat study with prasugrel at oral doses up to 100 mg/kg/day (>100 times the recommended therapeutic exposures in humans [based on plasma ...

14. Clinical Studies

The clinical evidence for the effectiveness of Effient is derived from the TRITON-TIMI 38 (TRial to Assess Improvement in Therapeutic Outcomes by Optimizing Platelet Inhibitio ...

16.1. How Supplied

Effient (prasugrel) is available as elongated hexagonal, film-coated, non-scored tablets in the following strengths, colors, imprints, and presentations: Features Strengths 5-mg 10-mg Tablet color ...

16.2. Storage and Handling

Store at 25°C (77°F); excursions permitted to 15° to 30°C (59° to 86°F) [see USP controlled room temperature]. Keep and dispense only in original container. Keep container closed and do not remove desiccant ...

17. Patient Counseling Information

Advise the patient to read the FDA-approved patient labeling (Medication Guide). Administration Advise patients not to break Effient tablets. Remind patients not to discontinue Effient without first discussing ...