prasugrel (Rx)

Brand and Other Names:Effient
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Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

tablet

  • 5mg
  • 10mg

Acute Coronary Syndrome

Reduction of thrombotic cardiovascular events (including stent thrombosis) in patients with acute coronary syndrome (ACS) managed by means of percutaneous coronary intervention (PCI) who have either (a) unstable angina or non-ST-elevation MI (NSTEMI) or (b) ST-elevation MI (STEMI) when managed with primary or delayed PCI

60 mg PO once as loading dose, then 10 mg/day PO in combination with aspirin 81-325 mg/day; if patient <60 kg, consider 5 mg/day PO because of potentially increased bleeding risk (efficacy and safety not established)

Dosing Modifications

Renal impairment

  • No dosage adjustment necessary
  • End-stage renal disease: Limited experience; these patients are generally at higher risk of bleeding

Hepatic impairment

  • Mild-to-moderate (Child-Pugh Class A or B): No dosage adjustment necessary
  • Severe (Child-Pugh Class C): Not studied

Dosing in low weight patients

  • Patients (<60 kg) had an increased exposure to active metabolite of prasugrel and an increased risk of bleeding on a 10-mg daily maintenance dose
  • Consider lowering the maintenance dose to 5-mg in patients <60 kg

Sickle Cell Disease (Orphan)

Orphan designation for treatment of sickle cell disease

Sponsor

  • Eli Lilly; Lilly Corporate Center; Indianapolis, IN 46285

Not recommended

Acute Coronary Syndrome

<75 years

  • 60 mg PO once as loading dose, then 10 mg/day PO in combination with aspirin 81-325 mg/day
  • Weight <60 kg: consider 5 mg/day because of potentially increased bleeding risk (efficacy and safety not established)

≥75 years

  • Generally not recommended, because of increased risk of fatal and intracranial bleeding and uncertain benefit, except in high-risk patients (diabetes or prior MI), for whom effect appears to be greater and use may be considered
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Interactions

Interaction Checker

and prasugrel

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    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

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            Adverse Effects

            1-10%

            Hypertension (7.5%)

            Hypercholesterolemia/hyperlipidemia (7%)

            Headache (5.5%)

            Back pain (5%)

            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 x 10^9 WBC/L) (2.8%)

            Rash (2.8%)

            Pyrexia (2.7%)

            Peripheral edema (2.7%)

            Pain in extremity (2.6%)

            Diarrhea (2.3%)

            <1%

            Thrombotic thrombocytopenic purpura

            Abnormal hepatic function

            Angioedema

            Hematoma

            Hemolysis

            Hemorrhage

            Abnormal liver function

            Postmarketing Reports

            Blood and lymphatic system disorders: Thrombocytopenia, thrombotic thrombocytopenic purpura (TTP)

            Immune system disorders: Hypersensitivity reactions (eg, anaphylaxis)

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            Warnings

            Black Box Warnings

            Potential for significant, sometimes fatal, bleeding

            • Prasugrel can cause significant, sometimes fatal, bleeding
            • Do not use in patients with active pathological bleeding or a history of transient ischemic attack or stroke
            • In patients ≥75 years of age, use is generally not recommended, owing to increased risk of fatal and intracranial bleeding and uncertain benefit, except in high-risk situations (eg, diabetes or prior MI)
            • Do not start in patients likely to undergo urgent coronary artery bypass graft surgery (CABG); when possible, discontinue prasugrel at least 7 days prior to any surgery
            • If possible, manage bleeding without discontinuing (risk of subsequent cardiovascular events is increased if prasugrel stopped, particularly in first few weeks after ACS)
            • Suspect bleeding in any patient who is hypotensive and has recently undergone invasive or surgical procedures

            Additional risk factors for bleeding

            • Weight <60 kg increases risk of bleeding
            • Propensity to bleed (eg, recent trauma, recent surgery, recent or recurrent GI bleeding, active peptic ulcer disease, severe hepatic impairment, or moderate-to-severe renal impairment)
            • Concomitant use of other drugs that increase bleeding risk

            Contraindications

            Hypersensitivity

            Active pathologic bleeding (eg, peptic ulcer, intracranial hemorrhage)

            Prior TIA or stroke

            Cautions

            Hypersensitivity with angioedema reported

            Bleeding diathesis

            Thrombocytopenic purpura occurring within 2 weeks of initiation of therapy reported

            Discontinue treatment for active bleeding, elective surgery, stroke, or TIA; premature discontinuation of any antiplatelet medication 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; avoid lapses in therapy, and if thienopyridines must be temporarily discontinued because of an adverse event(s), restart as soon as possible

            Risk increases in patients receiving drug who undergo CABG

            Premature discontinuation increases risk of stent thrombosis, MI, and death

            See Black Box Warnings

            Drug interactions overview

            • Coadministration with warfarin or nonsteroidal anti-inflammatory drugs (NSAIDs) (used chronically) increases the risk of bleeding
            • Coadministration of opioid agonists delay and reduce the absorption of prasugrel’s active metabolite presumably because of slowed gastric emptying
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            Pregnancy & Lactation

            Pregnancy

            There are no data with prasugrel use in pregnant women to inform a drug-associated risk

            Due to the mechanism of action, and the associated identified risk of bleeding, consider the benefits and possible risks to the fetus when prescribing prasugrel to a pregnant woman

            Lactation

            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

            Consider the developmental and health benefits of breastfeeding along with the mother’s clinical need for prasugrel and any potential adverse effects on the breastfed child from prasugrel or from the underlying maternal condition

            Pregnancy Categories

            A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA: Information not available.

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            Pharmacology

            Mechanism of Action

            A prodrug, a thienopyridine that inhibits platelet activation and aggregation through irreversible binding of active metabolite to adenosine phosphate (ADP) platelet receptors (specifically, P2Y12 receptor)

            Absorption

            Bioavailability: >78%

            Peak plasma time: 30 min

            Absorption: >79%

            With high fat, high calorie meal, peak plasma concentration decreased by 49% and peak plasma time increased from 0.5-1.5 hr

            Distribution

            Protein bound: 98% (active metabolite)

            Vd: 44-68 L (active metabolite)

            Metabolism

            Rapidly hydrolyzed in intestine to active metabolite via CYP3A4 and CYP2B6

            Elimination

            Half-life: 7 hr (range, 2-15 hr)

            Clearance: 112-166 L/hr

            Excretion: Urine (68%), feces (27%)

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            Administration

            Oral Administration

            Take with or without food

            Storage

            Tablets: Store at 25°C (77°F); excursions permitted to 15-30°C (59-86°F); dispense and keep product in original container; keep container closed and do not remove desiccant from bottle

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            Formulary

            FormularyPatient Discounts

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            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
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            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.