Effient (prasugrel hydrochloride) is a type of anti-clotting medicine that helps prevent harmful blood clots from forming. It is prescribed to people who have recently experienced a heart attack or severe chest pain and are undergoing a procedure to open blocked heart arteries (called PCI), to reduce their risk of future heart problems like another heart attack or stroke..
Typical Cost
$200-$500/month
Status
Rx
Generic
Brand Only
Clopidogrel bisulfate is the lowest-cost Antiplatelet Agents at $4-$25/month/month
Uses & Indications
Effient is 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 . 1.1 Acute Coronary Syndrome Effient ® is 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. 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 ] .
Dosage & 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 and Clinical Pharmacology ] . Effient may be administered with or without food [see Clinical Pharmacology and Clinical Studies ] . Initiate treatment with a single 60 mg oral loading dose . Continue at 10 mg once daily with or without food. Consider 5 mg once daily for patients <60 kg . Patients should also take aspirin (75 mg to 325 mg) daily . Timing of Loading Dose In the clinical trial that established the efficacy and safety of Effient, the loading dose of Effient was not administered until coronary anatomy was established in UA/NSTEMI patients and in STEMI patients presenting more than 12 hours after symptom onset. In STEMI patients presenting within 12 hours of symptom onset, the loading dose of Effient was administered at the time of diagnosis, although most received Effient at the time of PCI [see Clinical Studies ] . For the small fraction of patients that required urgent CABG after treatment with Effient, the risk of significant bleeding was substantial. Although 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 a trial of 4033 NSTEMI patients, no clear benefit was observed when Effient loading dose was administered prior to diagnostic coronary angiography compared to at the time of PCI; however, risk of bleeding was increased with early administration in patients undergoing PCI or early CABG. 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 [see Warnings and Precautions , Adverse Reactions , and Clinical Pharmacology ] .
How It Works
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.
Side Effects
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 ] Hypersensitivity Including Angioedema [see Warnings and Precautions ] Bleeding, including life-threatening and fatal bleeding, is the most commonly reported adverse reaction . To report SUSPECTED ADVERSE REACTIONS, contact Cosette Pharmaceuticals, Inc. at 1-800-922-1038 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 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 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 of a drug 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 Bleeding Patients may be counted in more than one row. (TRITON-TIMI 38) Effient (%) (N=6741) Clopidogrel (%) (N=6716) TIMI Major or Minor bleeding 4.5
TIMI Major bleeding See 5.1 for definition. 2.2
Life-threatening 1.3
Fatal 0.3
Symptomatic intracranial hemorrhage (ICH) 0.3
Requiring inotropes 0.3
Requiring surgical intervention 0.3
Requiring transfusion (≥4 units) 0.7
TIMI Minor bleeding 2.4
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 by Weight and Age In TRITON-TIMI 38, non-CABG-related TIMI Major or Minor 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 10 mg Effient maintenance dose (%) Clopidogrel 75 mg clopidogrel maintenance dose (%) Effient (%) Clopidogrel (%) Weight <60 kg (N=308 Effient, N=356 clopidogrel) 10.1 6.5 0.0
Weight ≥60 kg (N=6373 Effient, N=6299 clopidogrel) 4.2 3.3 0.3
Age <75 years (N=5850 Effient, N=5822 clopidogrel) 3.8 2.9 0.2
Age ≥75 years (N=891 Effient, N=894 clopidogrel) 9.0 6.9 1.0
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 Bleeding Patients may be counted in more than one row. (TRITON-TIMI 38) Effient (%) (N=213) Clopidogrel (%) (N=224) TIMI Major or Minor bleeding 14.1
TIMI Major bleeding 11.3
Fatal 0.9 0 Reoperation 3.8
Transfusion of ≥5 units 6.6
Intracranial hemorrhage 0
0 TIMI Minor bleeding 2.8 0.9 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. In another Phase 3 clinical study of ACS patients not undergoing PCI, in which data for malignancies were prospectively collected, newly diagnosed malignancies were reported in 1.8% and 1.7% of patients treated with prasugrel and clopidogrel, respectively. The site of malignancies was balanced between treatment groups except for colorectal malignancies. The rates of colorectal malignancies were 0.3% prasugrel, 0.1% clopidogrel and most were detected during investigation of GI bleed or anemia. It is unclear if these observations are causally related, are the result of increased detection because of bleeding, or are random occurrences. Other Adverse Events In TRITON-TIMI 38, common and other important nonhemorrhagic 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
Hypercholesterolemia/Hyperlipidemia 7.0
Headache 5.5
Back pain 5.0
Dyspnea 4.9
Nausea 4.6
Dizziness 4.1
Cough 3.9
Hypotension 3.9
Fatigue 3.7
Noncardiac chest pain 3.1
Atrial fibrillation 2.9
Bradycardia 2.9
Leukopenia (<4 × 10
9 WBC WBC = white blood cell /L) 2.8
Rash 2.8
Pyrexia 2.7
Peripheral edema 2.7
Pain in extremity 2.6
Diarrhea 2.3 2.6
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 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 ]
Warnings & Precautions
5 WARNINGS AND PRECAUTIONS CABG-related bleeding: Risk increases in patients receiving Effient who undergo CABG . Discontinuation of Effient: Premature discontinuation increases risk of stent thrombosis, MI, and death . Thrombotic thrombocytopenic purpura (TTP): TTP has been reported with Effient . Hypersensitivity: Hypersensitivity including angioedema has been reported with Effient including in patients with a history of hypersensitivity reaction to other thienopyridines . 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 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 Studies ] . CABG or other surgical procedure [see Warnings and Precautions ] . Body weight <60 kg. Consider a lower (5 mg) maintenance dose [see Dosage and Administration , Adverse Reactions , and 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 nonsteroidal anti-inflammatory drugs [NSAIDs], and fibrinolytic agents). Aspirin and heparin were commonly used in TRITON-TIMI 38 [see Drug Interactions and 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. Figure 1 5.2 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. 5.3 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 and Warnings and Precautions ] . 5.4 Thrombotic Thrombocytopenic Purpura (TTP) 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 ] . 5.5 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 and Adverse Reactions ] .
Contraindications
Active pathological bleeding Prior transient ischemic attack or stroke Hypersensitivity to prasugrel or any component of the product 4.1 Active Bleeding Effient is contraindicated in patients with active pathological bleeding such as peptic ulcer or intracranial hemorrhage (ICH) [see Warnings and Precautions and Adverse Reactions ] . 4.2 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 ( TR ial to Assess I mprovement in T herapeutic Outcomes by O ptimizing Platelet Inhibitio N 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 ] . 4.3 Hypersensitivity Effient is contraindicated in patients with hypersensitivity (e.g., anaphylaxis) to prasugrel or any component of the product [see Adverse Reactions ] .
Drug Interactions
Opioids: Decreased exposure to prasugrel. Consider use of parenteral antiplatelet agent . 7.1 Warfarin Coadministration of Effient and warfarin increases the risk of bleeding [see Warnings and Precautions and Clinical Pharmacology ] . 7.2 Nonsteroidal Anti-Inflammatory Drugs Coadministration of Effient and NSAIDs (used chronically) may increase the risk of bleeding [see Warnings and Precautions ] . 7.3 Opioids As with other oral P2Y 12 inhibitors, coadministration of opioid agonists delay and reduce the absorption of prasugrel's active metabolite presumably because of slowed gastric emptying [see Clinical Pharmacology ] . Consider the use of a parenteral anti-platelet agent in acute coronary syndrome patients requiring coadministration of morphine or other opioid agonists. 7.4 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 H 2 blockers [see Clinical Pharmacology ] .
Use in Specific Populations
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 when rats and rabbits were administered prasugrel during organogenesis at doses of up to 30 times the recommended therapeutic exposures in humans [see Data ]. Due to the mechanism of action of Effient, and the associated identified risk of bleeding, consider the benefits and risks of Effient and possible risks to the fetus when prescribing Effient to a pregnant woman [see Boxed Warning and Warnings and Precautions ] . The background risk of major birth defects and miscarriage for the indicated population is unknown. The background risk in the U.S. general population of major birth defects is 2-4% and of miscarriage is 15-20% of clinically recognized pregnancies. Data Animal Data 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 fetal 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. 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 milk [see Data ] . The developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for Effient and any potential adverse effects on the breastfed child from Effient or from the underlying maternal condition. Data Animal Data Following a 5 mg/kg oral dose of [ 14 C]-prasugrel to lactating rats, metabolites of prasugrel were detected in the maternal milk and blood. 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 or acute chest syndrome) in pediatric patients, aged 2 to less than 18 years, with sickle cell anemia was not met. 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 (Effient compared with clopidogrel) was similar across age groups. Patients ≥75 years of age who received Effient 10 mg 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 ] . 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 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 [see Dosage and Administration and Clinical Pharmacology ] . 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 [see Warnings and Precautions and Clinical Pharmacology ] . 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 disease have not been studied, but such patients are generally at higher risk of bleeding [see Warnings and Precautions and Clinical Pharmacology ] . 8.9 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.
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 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. 10.2 Recommendations about Specific Treatment Platelet transfusion may restore clotting ability. The prasugrel active metabolite is not likely to be removed by dialysis.
Frequently Asked Questions
What is PRASUGREL HYDROCHLORIDE used for?
1 INDICATIONS AND USAGE Effient is 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 ). 1.1 Acute Coronary Syndrome Effient ® is indicated to reduce the rate of thrombotic CV events (including stent…
What is the recommended dosage for PRASUGREL HYDROCHLORIDE?
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 (7.4) and Clinical Pharmacology (12.3) ] . Effient may be administered with or without food [see Clinical Pharmacology (12.3) and Clinical Studies (14) ] . Initiate treatment with a single 60 mg oral loading dose ( 2 ). Continue at 10 mg once daily with or without food. Consider 5 mg once daily for patients <60 kg ( 2 ). Patients should also take aspirin (75 mg to…
How does PRASUGREL HYDROCHLORIDE work?
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.
Who should not take PRASUGREL HYDROCHLORIDE?
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 Effient is 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 Effient is contraindicated in patients with a history of prior transient ischemic attack (TIA) or stroke. In TRITON-TIMI 38 ( TR ial to Assess I mprovement in T…
What are the side effects of PRASUGREL HYDROCHLORIDE?
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 Cosette Pharmaceuticals, Inc. at 1-800-922-1038 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical…
What drugs interact with PRASUGREL HYDROCHLORIDE?
7 DRUG INTERACTIONS Opioids: Decreased exposure to prasugrel. Consider use of parenteral antiplatelet agent ( 7.3 ). 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 Nonsteroidal Anti-Inflammatory Drugs Coadministration of Effient and NSAIDs (used chronically) may increase the risk of bleeding [see Warnings and Precautions (5.1) ] . 7.3 Opioids As with other oral P2Y 12 inhibitors, coadministration of opioid agonists delay and reduce the absorption of prasugrel's active metabolite…
What are the important warnings for PRASUGREL HYDROCHLORIDE?
5 WARNINGS AND PRECAUTIONS CABG-related bleeding: Risk increases in patients receiving Effient who undergo CABG ( 5.2 ). Discontinuation of Effient: Premature discontinuation increases risk of stent thrombosis, MI, and death ( 5.3 ). Thrombotic thrombocytopenic purpura (TTP): TTP has been reported with Effient ( 5.4 ). Hypersensitivity: Hypersensitivity including angioedema has been reported with Effient including in patients with a history of hypersensitivity reaction to other thienopyridines ( 5.5 ). 5.1 General Risk of Bleeding Thienopyridines, including Effient, increase the risk of…
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