Prasugrel

Prasugrel
Black Box Warning
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Sheng Shi, M.D. [2]

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Black Box Warning

WARNING: BLEEDING RISK See full prescribing information for complete Boxed Warning. * Effient can cause significant, sometimes fatal, bleeding (5.1, 5.2, 6.1). Do not use Effient in patients with active pathological bleeding or a history of transient ischemic attack or stroke (4.1, 4.2). In patients ≥75 years of age, Effient is generally not recommended, except in high-risk patients (diabetes or prior MI), where its use may be considered (8.5). Do not start Effient in patients likely to undergo urgent coronary artery bypass graft surgery (CABG). When possible, discontinue Effient at least 7 days prior to any surgery (5.2). Additional risk factors for bleeding include: body weight <60 kg; propensity to bleed; concomitant use of medications that increase the risk of bleeding (5.1). Suspect bleeding in any patient who is hypotensive and has recently undergone coronary angiography, percutaneous coronary intervention (PCI), CABG, or other surgical procedures in the setting of Effient (5.1). If possible, manage bleeding without discontinuing Effient. Stopping Effient increases the risk of subsequent cardiovascular events (5.3).

Overview

Prasugrel is a P2Y12 platelet inhibitor, Platelet aggregation inhibitor that is FDA approved for the {{{indicationType}}} of Acute Coronary Syndrome. There is a Black Box Warning for this drug as shown here. Common adverse reactions include hypertension, hyperlipidemia, backache, headache, epistaxis.

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Acute Coronary Syndrome

• Dosing Information

• Initial loading dosage: 60 mg PO
• Maintaining dosage: 10 mg PO qd
• Incombination with: aspirin 75 mg-325 mg

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

Condition 1

• Developed by: (Organization)

• Class of Recommendation: (Class) (Link)

• Strength of Evidence: (Category A/B/C) (Link)

• Dosing Information/Recommendation

• (Dosage)

Non–Guideline-Supported Use

Prophylaxis treatment of Thrombosis of Acute coronary syndrome

• Dosing Information

• Recommended: 10 mg/day

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

Condition 1

• Dosing Information

(Dosage)

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

Condition 1

• Developed by: (Organization)

• Class of Recommendation: (Class) (Link)

• Strength of Evidence: (Category A/B/C) (Link)

• Dosing Information/Recommendation

• (Dosage)

Non–Guideline-Supported Use

Condition 1

• Dosing Information

• There is limited information about Off-Label Non–Guideline-Supported Use of Prasugrel in pediatric patients.

Contraindications

• 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 (6.1)].

• 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 (6.1) and Clinical Studies (14)].

• Hypersensitivity

• Effient is contraindicated in patients with hypersensitivity (e.g., anaphylaxis) to prasugrel or any component of the product [see Adverse Reactions (6.2)].

Warnings

WARNING: BLEEDING RISK See full prescribing information for complete Boxed Warning. * Effient can cause significant, sometimes fatal, bleeding (5.1, 5.2, 6.1). Do not use Effient in patients with active pathological bleeding or a history of transient ischemic attack or stroke (4.1, 4.2). In patients ≥75 years of age, Effient is generally not recommended, except in high-risk patients (diabetes or prior MI), where its use may be considered (8.5). Do not start Effient in patients likely to undergo urgent coronary artery bypass graft surgery (CABG). When possible, discontinue Effient at least 7 days prior to any surgery (5.2). Additional risk factors for bleeding include: body weight <60 kg; propensity to bleed; concomitant use of medications that increase the risk of bleeding (5.1). Suspect bleeding in any patient who is hypotensive and has recently undergone coronary angiography, percutaneous coronary intervention (PCI), CABG, or other surgical procedures in the setting of Effient (5.1). If possible, manage bleeding without discontinuing Effient. Stopping Effient increases the risk of subsequent cardiovascular events (5.3).

General Risk of Bleeding

clopidogrel, 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 (6.1)]. The bleeding risk is highest initially, as shown in Figure 1 (events through 450 days; inset shows events through 7 days).

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 (4.1, 4.2)]. 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 (6.1), Use in Specific Populations (8.5), Clinical Pharmacology (12.3), and Clinical Trials (14)].
• CABG or other surgical procedure [see Warnings and Precautions (5.2)].
• Body weight <60 kg. Consider a lower (5-mg) maintenance dose [see Dosage and Administration (2), Adverse Reactions (6.1), and Use in Specific Populations (8.6)].
• 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 (6.1) and Use in Specific Populations (8.7, 8.8)].
• 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 (7.1, 7.2. 7.3), and Clinical Studies (14)].

clopidogrel 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 (6.1)]. 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 clopidogrel, 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 clopidogrel, 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 clopidogrel must be temporarily discontinued because of an adverse event(s), they should be restarted as soon as possible [see Contraindications (4.1, 4.2) and Warnings and Precautions (5.1)].

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 (6.2)].

Hypersensitivity Including Angioedema

Hypersensitivity including angioedema has been reported in patients receiving Effient, including patients with a history of hypersensitivity reaction to other clopidogrel [see Contraindications (4.3) and Adverse Reactions (6.2)].

Adverse Reactions

Clinical Trials Experience

Central Nervous System

(list/description of adverse reactions)

Cardiovascular

(list/description of adverse reactions)

Respiratory

(list/description of adverse reactions)

Gastrointestinal

(list/description of adverse reactions)

Hypersensitive Reactions

(list/description of adverse reactions)

Miscellaneous

(list/description of adverse reactions)

Postmarketing Experience

Central Nervous System

(list/description of adverse reactions)

Cardiovascular

(list/description of adverse reactions)

Respiratory

(list/description of adverse reactions)

Gastrointestinal

(list/description of adverse reactions)

Hypersensitive Reactions

(list/description of adverse reactions)

Miscellaneous

(list/description of adverse reactions)

Drug Interactions

• (Drug 1)

• (Description)

• (Drug 2)

• (Description)

• (Drug 3)

• (Description)

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA): There is no FDA guidance on usage of Prasugrel in women who are pregnant.
Pregnancy Category (AUS): There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Prasugrel in women who are pregnant.

Labor and Delivery

There is no FDA guidance on use of Prasugrel during labor and delivery.

Nursing Mothers

There is no FDA guidance on the use of Prasugrel in women who are nursing.

Pediatric Use

There is no FDA guidance on the use of Prasugrel in pediatric settings.

Geriatic Use

There is no FDA guidance on the use of Prasugrel in geriatric settings.

Gender

There is no FDA guidance on the use of Prasugrel with respect to specific gender populations.

Race

There is no FDA guidance on the use of Prasugrel with respect to specific racial populations.

Renal Impairment

There is no FDA guidance on the use of Prasugrel in patients with renal impairment.

Hepatic Impairment

There is no FDA guidance on the use of Prasugrel in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Prasugrel in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Prasugrel in patients who are immunocompromised.

Administration and Monitoring

Administration

There is limited information regarding Prasugrel Administration in the drug label.

Monitoring

There is limited information regarding Prasugrel Monitoring in the drug label.

IV Compatibility

There is limited information regarding the compatibility of Prasugrel and IV administrations.

Overdosage

There is limited information regarding Prasugrel overdosage. If you suspect drug poisoning or overdose, please contact the National Poison Help hotline (1-800-222-1222) immediately.

Pharmacology

There is limited information regarding Prasugrel Pharmacology in the drug label.

Mechanism of Action

There is limited information regarding Prasugrel Mechanism of Action in the drug label.

Structure

There is limited information regarding Prasugrel Structure in the drug label.

Pharmacodynamics

There is limited information regarding Prasugrel Pharmacodynamics in the drug label.

Pharmacokinetics

There is limited information regarding Prasugrel Pharmacokinetics in the drug label.

Nonclinical Toxicology

There is limited information regarding Prasugrel Nonclinical Toxicology in the drug label.

Clinical Studies

There is limited information regarding Prasugrel Clinical Studies in the drug label.

How Supplied

There is limited information regarding Prasugrel How Supplied in the drug label.

Storage

There is limited information regarding Prasugrel Storage in the drug label.

Images

Drug Images

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Package and Label Display Panel

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Patient Counseling Information

There is limited information regarding Prasugrel Patient Counseling Information in the drug label.

Precautions with Alcohol

Alcohol-Prasugrel interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

There is limited information regarding Prasugrel Brand Names in the drug label.

Look-Alike Drug Names

There is limited information regarding Prasugrel Look-Alike Drug Names in the drug label.

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.

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Prasugrel
EFFIENT® FDA Package Insert
Indications and Usage
Dosage and Administration
Dosage Forms and Strengths
Contraindications
Warnings and Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Overdosage
Description
Clinical Pharmacology
Nonclinical Toxicology
Clinical Studies
How Supplied/Storage and Handling
Patient Counseling Information
Labels and Packages
Clinical Trials on Prasugrel
ClinicalTrials.gov

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [3]; Associate Editor(s)-in-Chief: Sheng Shi, M.D. [4]

For patient information about Prasugrel, click here

Synonyms / Brand Names: EFFIENT^®

Overview

Prasugrel is a novel platelet inhibitor developed by Daiichi Sankyo Co. and produced by Ube and currently under clinical development in cooperation with Eli Lilly and Company for acute coronary syndromes planned for percutaneous coronary intervention (PCI). Prasugrel is a member of the thienopyridine class of ADP receptor inhibitors, like ticlopidine and clopidogrel (trade name Plavix). These agents are believed to reduce the aggregation ("clumping") of platelets by irreversibly binding to P2Y₁₂ receptors.

Category

Cardiovascular Drugs:Antiplatelet drugs

FDA Package Insert

Indications and Usage | Dosage and Administration | Dosage Forms and Strengths | Contraindications | Warnings and Precautions | Adverse Reactions | Drug Interactions | Use in Specific Populations | Overdosage | Description | Clinical Pharmacology | Nonclinical Toxicology | Clinical Studies | How Supplied/Storage and Handling | Patient Counseling Information | Labels and Packages

WARNING: BLEEDING RISK See full prescribing information for complete boxed warning. Effient can cause significant, sometimes fatal, bleeding. Do not use Effient in patients with active pathological bleeding or a history of transient ischemic attack or stroke. In patients ≥75 years of age, Effient is generally not recommended, except in high-risk patients (diabetes or prior MI), where its use may be considered. Do not start Effient in patients likely to undergo urgent coronary artery bypass graft surgery (CABG). When possible, discontinue Effient at least 7 days prior to any surgery. Additional risk factors for bleeding include: body weight <60 kg; propensity to bleed; concomitant use of medications that increase the risk of bleeding. Suspect bleeding in any patient who is hypotensive and has recently undergone coronary angiography, percutaneous coronary intervention (PCI), CABG, or other surgical procedures in the setting of Effient. If possible, manage bleeding without discontinuing Effient. Stopping Effient increases the risk of subsequent cardiovascular events.

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.