Drug: Effient

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, 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. Prasugrel hydrochloride has the empirical formula C20H20FNO3S •HCl representing a molecular weight of 409.90. The chemical structure of presugrel hydrochloride is: Prasugrel hydrochloride is a white to practically white solid. It is soluble at pH 2, slightly soluble at pH 3 to 4, and practically insoluble at pH 6 to 7.5. It also dissolves freely in methanol and is slightly soluble in 1- and 2-propanol and acetone. It is practically insoluble in diethyl ether and ethyl acetate. Effient is available for oral administration as 5 mg or 10 mg elongated hexagonal, film-coated, non-scored tablets, debossed on each side. Each yellow 5 mg tablet is manufactured with 5.49 mg prasugrel hydrochloride, equivalent to 5 mg prasugrel and each beige 10 mg tablet with 10.98 mg prasugrel hydrochloride, equivalent to 10 mg of prasugrel. Original Formulation During manufacture and storage, partial conversion from prasugrel hydrochloride to prasugrel free base may occur. Other ingredients include mannitol, hypromellose, croscarmellose sodium, microcrystalline cellulose, and vegetable magnesium stearate. The color coatings contain lactose, hypromellose, titanium dioxide, triacetin, iron oxide yellow, and iron oxide red (only in Effient 10 mg tablet). Revised Formulation Other ingredients include mannitol, hypromellose, low-substituted hydroxypropyl cellulose, microcrystalline cellulose, sucrose stearate, and glyceryl behenate. The color coatings contain lactose, hypromellose, titanium dioxide, triacetin, iron oxide yellow, and iron oxide red (only in Effient 10 mg tablet).

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Clinical Trials Experience The following serious adverse reactions are also discussed elsewhere in the labeling:
  • Bleeding [see BOXED WARNING and WARNINGS AND PRECAUTIONS]
  • Thrombotic thrombocytopenic purpura [see WARNINGS AND PRECAUTIONS]
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 a median of 14.5 months (5802 patients were treated for over 6 months; 4136 patients were treated for more than 1 year). The population treated with Effient was 27 to 96 years of age, 25% female, and 92% Caucasian. All patients in the TRITON-TIMI 38 study were to receive aspirin. The dose of clopidogrel in this study was a 300-mg loading dose and 75 mg once daily. Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials cannot be directly compared with the rates observed in other clinical trials of another drug and may not reflect the rates observed in practice. Drug Discontinuation The rate of study drug discontinuation because of adverse reactions was 7.2% for Effient and 6.3% for clopidogrel. Bleeding was the most common adverse reaction leading to study drug discontinuation for both drugs (2.5% for Effient and 1.4% for clopidogrel). Bleeding Bleeding Unrelated to CABG Surgery - In TRITON-TIMI 38, overall rates of TIMI Major or Minor bleeding adverse reactions unrelated to coronary artery bypass graft surgery (CABG) were significantly higher on Effient than on clopidogrel, as shown in Table 1. Table 1: Non-CABG-Related Bleedinga (TRITON-TIMI 38)
  Effient (%) (N=6741) Clopidogrel (%) (N=6716) p-value TIMI Major or Minor bleeding 4.5 3.4 p=0.002 TIMI Major bleedingb 2.2 1.7 p=0.029   Life-threatening 1.3 0.8 p=0.015     Fatal 0.3 0.1       Symptomatic intracranial hemorrhage (ICH) 0.3 0.3       Requiring inotropes 0.3 0.1       Requiring surgical intervention 0.3 0.3       Requiring transfusion ( ≥ 4 units) 0.7 0.5   TIMI Minor bleedingb 2.4 1.9 p=0.022 aPatients may be counted in more than one row.
bSee PRECAUTIONS for definition. Figure 1 demonstrates non-CABG related TIMI Major or Minor bleeding. The bleeding rate is highest initially, as shown in Figure 1 (inset: Days 0 to 7) [see WARNINGS AND PRECAUTIONS]. Bleeding rates in patients with the risk factors of age 75 years and weight < 60 kg are shown in Table 2. Table 2: Bleeding Rates for Non-CABG-Related Bleeding by Weight and Age (TRITON-TIMI 38)
  Major/Minor Fatal Effient (%) Clopidogrel (%) Effient (%) Clopidogrel (%) Weight < 60 kg (N=308 Effient, N=356 clopidogrel) 10.1 6.5 0 0.3 Weight ≥ 60 kg (N=6373 Effient, N=6299 clopidogrel) 4.2 3.3 0.3 0.1 Age < 75 years (N=5850 Effient, N=5822 clopidogrel) 3.8 2.9 0.2 0.1 Age ≥ 75 years (N=891 Effient, N=894 clopidogrel) 9 6.9 1 0.1 Bleeding Related to CABG - In TRITON-TIMI 38, 437 patients who received a thienopyridine underwent CABG during the course of the study. The rate of CABG-related TIMI Major or Minor bleeding was 14.1% for the Effient group and 4.5% in the clopidogrel group (see Table 3). The higher risk for bleeding adverse reactions in patients treated with Effient persisted up to 7 days from the most recent dose of study drug. Table 3: CABG-Related Bleedinga (TRITON-TIMI 38)
  Effient (%)
(N=213) Clopidogrel (%)
(N=224) TIMI Major or Minor bleeding 14.1 4.5 TIMI Major bleeding 11.3 3.6    Fatal 0.9 0    Reoperation 3.8 0.5    Transfusion of ≥ 5 units 6.6 2.2    Intracranial hemorrhage 0 0 TIMI Minor bleeding 2.8 0.9 aPatients may be counted in more than one row. Bleeding Reported as Adverse Reactions - Hemorrhagic events reported as adverse reactions in TRITON-TIMI 38 were, for Effient and clopidogrel, respectively: epistaxis (6.2%, 3.3%), gastrointestinal hemorrhage (1.5%, 1.0%), hemoptysis (0.6%, 0.5%), subcutaneous hematoma (0.5%, 0.2%), post-procedural hemorrhage (0.5%, 0.2%), retroperitoneal hemorrhage (0.3%, 0.2%), pericardial effusion/hemorrhage/tamponade (0.3%, 0.2%), and retinal hemorrhage (0.0%, 0.1%). Malignancies During TRITON-TIMI 38, newly-diagnosed malignancies were reported in 1.6% and 1.2% of patients treated with prasugrel and clopidogrel, respectively. The sites contributing to the differences were primarily colon and lung. It is unclear if these observations are causally-related or are random occurrences. Other Adverse Events In TRITON-TIMI 38, common and other important non-hemorrhagic adverse events were, for Effient and clopidogrel, respectively: severe thrombocytopenia (0.06%, 0.04%), anemia (2.2%, 2.0%), abnormal hepatic function (0.22%, 0.27%), allergic reactions (0.36%, 0.36%), and angioedema (0.06%, 0.04%). Table 4 summarizes the adverse events reported by at least 2.5% of patients. Table 4: Non-Hemorrhagic Treatment Emergent Adverse Events Reported by at Least 2.5% of Patients in Either Group
  Effient (%)
(N=6741) Clopidogrel (%)
(N=6716) Hypertension 7.5 7.1 Hypercholesterolemia/Hyperlipidemia 7 7.4 Headache 5.5 5.3 Back pain 5 4.5 Dyspnea 4.9 4.5 Nausea 4.6 4.3 Dizziness 4.1 4.6 Cough 3.9 4.1 Hypotension 3.9 3.8 Fatigue 3.7 4.8 Non-cardiac chest pain 3.1 3.5 Atrial fibrillation 2.9 3.1 Bradycardia 2.9 2.4 Leukopenia ( < 4 x 109 WBC/L) 2.8 3.5 Rash 2.8 2.4 Pyrexia 2.7 2.2 Peripheral edema 2.7 3 Pain in extremity 2.6 2.6 Diarrhea 2.3 2.6 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 to reliably estimate their frequency or establish a causal relationship to drug exposure. Blood and lymphatic system disorders — Thrombocytopenia, Thrombotic thrombocytopenic purpura (TTP) [see WARNINGS AND PRECAUTIONS and Patient Counseling Information] Immune system disorders — Hypersensitivity reactions including anaphylaxis [see CONTRAINDICATIONS] Read the Effient (prasugrel tablets) Side Effects Center for a complete guide to possible side effectsLearn More »

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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 and CLINICAL PHARMACOLOGY]. Effient may be administered with or without food [see CLINICAL PHARMACOLOGY and Clinical Studies]. Dosing in Low Weight Patients Compared to patients weighing 60 kg, patients weighing < 60 kg have an increased exposure to the active metabolite of prasugrel and an increased risk of bleeding on a 10 mg once daily maintenance dose. Consider lowering the maintenance dose to 5 mg in patients < 60 kg. The effectiveness and safety of the 5 mg dose have not been prospectively studied.

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Warfarin Coadministration of Effient and warfarin increases the risk of bleeding [see WARNINGS AND PRECAUTIONS and CLINICAL PHARMACOLOGY]. Non-Steroidal Anti-Inflammatory Drugs Coadministration of Effient and NSAIDs (used chronically) may increase the risk of bleeding [see WARNINGS AND PRECAUTIONS]. Other Concomitant Medications Effient can be administered with drugs that are inducers or inhibitors of cytochrome P450 enzymes [see CLINICAL PHARMACOLOGY]. Effient can be administered with aspirin (75 mg to 325 mg per day), heparin, GPIIb/IIIa inhibitors, statins, digoxin, and drugs that elevate gastric pH, including proton pump inhibitors and H2 blockers [see CLINICAL PHARMACOLOGY]. Read the Effient Drug Interactions Center for a complete guide to possible interactions Learn More »

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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).
  • Patients with ST-elevation myocardial infarction (STEMI) when managed with primary or delayed PCI.
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]. 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]. 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.

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Active Bleeding Effient is contraindicated in patients with active pathological bleeding such as peptic ulcer or intracranial hemorrhage [see WARNINGS AND PRECAUTIONS and ADVERSE REACTIONS]. Prior Transient Ischemic Attack or Stroke Effient is contraindicated in patients with a history of prior transient ischemic attack (TIA) or stroke. In TRITON-TIMI 38 (TRial to Assess Improvement in Therapeutic Outcomes by Optimizing Platelet InhibitioN with Prasugrel), patients with a history of TIA or ischemic stroke ( > 3 months prior to enrollment) had a higher rate of stroke on Effient (6.5%; of which 4.2% were thrombotic stroke and 2.3% were intracranial hemorrhage [ICH]) than on clopidogrel (1.2%; all thrombotic). In patients without such a history, the incidence of stroke was 0.9% (0.2% ICH) and 1.0% (0.3% ICH) with Effient and clopidogrel, respectively. Patients with a history of ischemic stroke within 3 months of screening and patients with a history of hemorrhagic stroke at any time were excluded from TRITON-TIMI 38. Patients who experience a stroke or TIA while on Effient generally should have therapy discontinued [see ADVERSE REACTIONS and Clinical Studies]. Hypersensitivity Effient is contraindicated in patients with hypersensitivity (e.g., anaphylaxis) to prasugrel or any component of the product [see ADVERSE REACTIONS]. Last reviewed on RxList: 12/14/2012
This monograph has been modified to include the generic and brand name in many instances.

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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 was observed after administration of 2000 mg/kg. Symptoms of acute toxicity in dogs included emesis, increased serum alkaline phosphatase, and hepatocellular atrophy. Symptoms of acute toxicity in rats included mydriasis, irregular respiration, decreased locomotor activity, ptosis, staggering gait, and lacrimation. Recommendations about Specific Treatment Platelet transfusion may restore clotting ability. The prasugrel active metabolite is not likely to be removed by dialysis.

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Dosage Forms And Strengths Effient 5 mg is available as a yellow, elongated hexagonal, film-coated, non-scored tablet:
  • debossed with “5 MG” on one side and “4760” on the other side (original formulation)
    OR
  • debossed with “5121” on one side and 3 parallel arched lines followed by a “5” on the other side (revised formulation)
Effient 10 mg is available as a beige, elongated hexagonal, film-coated, non-scored tablet:
  • debossed with “10 MG” on one side and with “4759” on the other side (original formulation)
    OR
  • debossed with “5123” on one side and 3 parallel arched lines followed by a “10” on the other side (revised formulation)
Storage And Handling 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 yellow beige Formulation Original Revised Original Revised Tablet imprint 5 MG 5 10 MG 10 Tablet imprint 4760 5121 4759 5123 Presentations and NDC Codes Bottles of 7 0002-4760-76 NA NA NA Bottles of 30 0002-4760-30 0002-5121-30 0002-4759-30 0002-5123-30 Blisters ID*24 NA 0002-5121-52 NA NA Blisters ID*90 NA NA 0002-4759-77 0002-5123-77 * Identi Dose®, unit dose medication, Lilly Store at 25°C (77°F); excursions permitted to 15° to 30°C (59° to 86°F) [see USP controlled room temperature]. Dispense and keep product in original container. Keep container closed and do not remove desiccant from bottle. Do not break the tablet. Revised: 11/2012. Manufactured by Eli Lilly and Company, Indianapolis, IN, 46285. Marketed by Daiichi Sankyo, Inc. and Lilly USA, LLC Last reviewed on RxList: 12/14/2012
This monograph has been modified to include the generic and brand name in many instances.

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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 overt bleeding associated with a fall in hemoglobin 5 g/dL, or intracranial hemorrhage) and TIMI Minor (overt bleeding associated with a fall in hemoglobin of 3 g/dL but < 5 g/dL) bleeding events were more common on Effient than on clopidogrel [see ADVERSE REACTIONS]. The bleeding risk is highest initially, as shown in Figure 1 (events through 450 days; inset shows events through 7 days). Figure 1: Non-CABG-Related TIMI Major or Minor Bleeding Events
Suspect bleeding in any patient who is hypotensive and has recently undergone coronary angiography, PCI, CABG, or other surgical procedures even if the patient does not have overt signs of bleeding. Do not use Effient in patients with active bleeding, prior TIA or stroke [see CONTRAINDICATIONS]. Other risk factors for bleeding are:
  • Age 75 years. Because of the risk of bleeding (including fatal bleeding) and uncertain effectiveness in patients 75 years of age, use of Effient is generally not recommended in these patients, except in high-risk situations (patients with diabetes or history of myocardial infarction) where its effect appears to be greater and its use may be considered [see ADVERSE REACTIONS, Use In Specific Populations, CLINICAL PHARMACOLOGY, and Clinical Trials].
  • CABG or other surgical procedure.
  • Body weight < 60 kg. Consider a lower (5 mg) maintenance dose [see DOSAGE AND ADMINISTRATION, ADVERSE REACTIONS, Use In Specific Populations].
  • Propensity to bleed (e.g., recent trauma, recent surgery, recent or recurrent gastrointestinal (GI) bleeding, active peptic ulcer disease, severe hepatic impairment, or moderate to severe renal impairment) [see ADVERSE REACTIONS and Use In Specific Populations].
  • Medications that increase the risk of bleeding (e.g., oral anticoagulants, chronic use of non-steroidal anti-inflammatory drugs [NSAIDs], and fibrinolytic agents). Aspirin and heparin were commonly used in TRITON-TIMI 38 [see DRUG INTERACTIONS, Clinical Studies].
Thienopyridines inhibit platelet aggregation for the lifetime of the platelet (7-10 days), so withholding a dose will not be useful in managing a bleeding event or the risk of bleeding associated with an invasive procedure. Because the half-life of prasugrel's active metabolite is short relative to the lifetime of the platelet, it may be possible to restore hemostasis by administering exogenous platelets; however, platelet transfusions within 6 hours of the loading dose or 4 hours of the maintenance dose may be less effective. Coronary Artery Bypass Graft Surgery-Related Bleeding The risk of bleeding is increased in patients receiving Effient who undergo CABG. If possible, Effient should be discontinued at least 7 days prior to CABG. Of the 437 patients who underwent CABG during TRITON-TIMI 38, the rates of CABG-related TIMI Major or Minor bleeding were 14.1% in the Effient group and 4.5% in the clopidogrel group [see ADVERSE REACTIONS]. The higher risk for bleeding events in patients treated with Effient persisted up to 7 days from the most recent dose of study drug. For patients receiving a thienopyridine within 3 days prior to CABG, the frequencies of TIMI Major or Minor bleeding were 26.7% (12 of 45 patients) in the Effient group, compared with 5.0% (3 of 60 patients) in the clopidogrel group. For patients who received their last dose of thienopyridine within 4 to 7 days prior to CABG, the frequencies decreased to 11.3% (9 of 80 patients) in the prasugrel group and 3.4% (3 of 89 patients) in the clopidogrel group. Do not start Effient in patients likely to undergo urgent CABG. CABG-related bleeding may be treated with transfusion of blood products, including packed red blood cells and platelets; however, platelet transfusions within 6 hours of the loading dose or 4 hours of the maintenance dose may be less effective. Discontinuation of Effient Discontinue thienopyridines, including Effient, for active bleeding, elective surgery, stroke, or TIA. The optimal duration of thienopyridine therapy is unknown. In patients who are managed with PCI and stent placement, premature discontinuation of any antiplatelet medication, including thienopyridines, conveys an increased risk of stent thrombosis, myocardial infarction, and death. Patients who require premature discontinuation of a thienopyridine will be at increased risk for cardiac events. Lapses in therapy should be avoided, and if thienopyridines must be temporarily discontinued because of an adverse event(s), they should be restarted as soon as possible [see CONTRAINDICATIONS]. Thrombotic Thrombocytopenic Purpura Thrombotic thrombocytopenic purpura (TTP) has been reported with the use of Effient. TTP can occur after a brief exposure ( < 2 weeks). TTP is a serious condition that can be fatal and requires urgent treatment, including plasmapheresis (plasma exchange). TTP is characterized by thrombocytopenia, microangiopathic hemolytic anemia (schistocytes [fragment red blood cells] seen on peripheral smear), neurological findings, renal dysfunction, and fever [see ADVERSE REACTIONS]. Hypersensitivity Including Angioedema Hypersensitivity including angioedema has been reported in patients receiving Effient, including patients with a history of hypersensitivity reaction to other thienopyridines [see CONTRAINDICATIONS, ADVERSE REACTIONS]. Patient Counseling Information See Medication Guide Benefits and Risks
  • Summarize the effectiveness features and potential side effects of Effient.
  • Tell patients to take Effient exactly as prescribed.
  • Remind patients not to discontinue Effient without first discussing it with the physician who prescribed Effient.
  • Recommend that patients read the Medication Guide.
Bleeding Inform patients that they:
  • will bruise and bleed more easily.
  • will take longer than usual to stop bleeding.
  • should report any unanticipated, prolonged, or excessive bleeding, or blood in their stool or urine.
Other Signs and Symptoms Requiring Medical Attention
  • Inform patients that TTP is a rare but serious condition that has been reported with Effient.
    • Instruct patients to get prompt medical attention if they experience any of the following symptoms that cannot otherwise be explained: fever, weakness, extreme skin paleness, purple skin patches, yellowing of the skin or eyes, or neurological changes.
  • Inform patients that they may have hypersensitivity reactions including rash, angioedema, anaphylaxis, or other manifestations. Patients who have had hypersensitivity reactions to other thienopyridines may have hypersensitivity reactions to Effient.
Invasive Procedures Instruct patients to:
  • inform physicians and dentists that they are taking Effient before any invasive procedure is scheduled.
  • tell the doctor performing the invasive procedure to talk to the prescribing health care professional before stopping Effient.
Concomitant Medications Ask patients to list all prescription medications, over-the-counter medications, or dietary supplements they are taking or plan to take so the physician knows about other treatments that may affect bleeding risk (e.g., warfarin and NSAIDs). Nonclinical Toxicology 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 exposures to the major circulating human metabolite). There was an increased incidence of tumors (hepatocellular adenomas) in mice exposed for 2 years to high doses ( > 250 times the human metabolite exposure). Mutagenesis Prasugrel was not genotoxic in two in vitro tests (Ames bacterial gene mutation test, clastogenicity assay in Chinese hamster fibroblasts) and in one in vivo test (micronucleus test by intraperitoneal route in mice). Impairment of Fertility Prasugrel had no effect on fertility of male and female rats at oral doses up to 300 mg/kg/day (80 times the human major metabolite exposure at daily dose of 10 mg prasugrel). Use In Specific Populations Pregnancy Pregnancy Category B There are no adequate and well-controlled studies of Effient use in pregnant women. Reproductive and developmental toxicology studies in rats and rabbits at doses of up to 30 times the recommended therapeutic exposures in humans (based on plasma exposures to the major circulating human metabolite) revealed no evidence of fetal harm; however, animal studies are not always predictive of a human response. Effient should be used during pregnancy only if the potential benefit to the mother justifies the potential risk to the fetus. In embryo fetal developmental toxicology studies, pregnant rats and rabbits received prasugrel at maternally toxic oral doses equivalent to more than 40 times the human exposure. A slight decrease in pup body weight was observed; but, there were no structural malformations in either species. In prenatal and postnatal rat studies, maternal treatment with prasugrel had no effect on the behavioral or reproductive development of the offspring at doses greater than 150 times the human exposure [see Nonclinical Toxicology]. Nursing Mothers It is not known whether Effient is excreted in human milk; however, metabolites of Effient were found in rat milk. Because many drugs are excreted in human milk, prasugrel should be used during nursing only if the potential benefit to the mother justifies the potential risk to the nursing infant. Pediatric Use Safety and effectiveness in pediatric patients have not been established [see CLINICAL PHARMACOLOGY]. 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 (Effient compared with clopidogrel) was similar across age groups. Patients 75 years of age who received Effient had an increased risk of fatal bleeding events (1.0%) compared to patients who received clopidogrel (0.1%). In patients 75 years of age, symptomatic intracranial hemorrhage occurred in 7 patients (0.8%) who received Effient and in 3 patients (0.3%) who received clopidogrel. Because of the risk of bleeding, and because effectiveness is uncertain in patients 75 years of age [see Clinical Studies], use of Effient is generally not recommended in these patients, except in high-risk situations (diabetes and past history of myocardial infarction) where its effect appears to be greater and its use may be considered [see WARNINGS AND PRECAUTIONS, CLINICAL PHARMACOLOGY, and Clinical Studies]. 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 active metabolite of prasugrel [see DOSAGE AND ADMINISTRATION, WARNINGS AND PRECAUTIONS, and CLINICAL PHARMACOLOGY]. Consider lowering the maintenance dose to 5 mg in patients < 60 kg. The effectiveness and safety of the 5 mg dose have not been prospectively studied. 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 [see WARNINGS AND PRECAUTIONS and CLINICAL PHARMACOLOGY]. 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 disease have not been studied, but such patients are generally at higher risk of bleeding [see WARNINGS AND PRECAUTIONS and CLINICAL PHARMACOLOGY]. Metabolic Status In healthy subjects, patients with stable atherosclerosis, and patients with ACS receiving prasugrel, there was no relevant effect of genetic variation in CYP2B6, CYP2C9, CYP2C19, or CYP3A5 on the pharmacokinetics of prasugrel's active metabolite or its inhibition of platelet aggregation. Last reviewed on RxList: 12/14/2012
This monograph has been modified to include the generic and brand name in many instances.

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