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eltrombopag (Rx)Brand and Other Names:Promacta

 
 
 

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 12.5mg
  • 25mg
  • 50mg
  • 75mg
  • 100mg
more...

Chronic Immune Thrombocytopenia (ITP)

Indicated for treatment of thrombocytopenia in adults and pediatric patients ≥6 yr with chronic immune (idiopathic) thrombocytopenia (ITP) with insufficient response to corticosteroids, immunoglobulins, or splenectomy

Initial: 50 mg PO qDay

Maintenance: Adjust dose to achieve and maintain platelet count (Plt) >50 x 10^9/L to reduce risk of bleeding; not to exceed 75 mg/day

Dosing considerations

  • Should be used only in patients with ITP whose degree of thrombocytopenia and clinical condition increase the risk for bleeding
  • Use the lowest dose to achieve and maintain a platelet count >50 x 10^9/L as necessary to reduce the risk for bleeding
  • Dose adjustment based upon the platelet count response; do not use to normalize platelet counts
  • Monitor LFTs and CBC prior to initiation, and throughout therapy

Dosage Modifications (ITP)

East Asian ancestry: Decrease initial dose to 25 mg PO qDay

Hepatic impairment

  • Mild-to-severe (Child-Pugh A, B, or C): Decrease initial dose to 25 mg PO qDay
  • East Asian ancestry with hepatic impairment: Decrease initial dose to 12.5 mg PO qDay

Adjust dose according to platelets

  • Plt <50 x 10^9/L; after at least 2 weeks: Increase daily dose by 25 mg; not to exceed 75 mg/day
  • Plt 200-400 x 10^9/L: Decrease daily dose by 25 mg; assess after 2 weeks
  • Plt >400 x 10^9/L: Discontinue and monitor platelet 2x/week; once platelet <150 x 10^9/L; restart therapy with 25 mg reduction in daily dose
  • Plt >400 x 10^9/L; after 2 weeks of therapy at lowest dose: Discontinue permanently

Discontinue if

  • No improvement after 4 weeks at maximum dose, OR
  • Abnormal LFTs or excessive Plt responses

Chronic Hepatitis C-Associated Thrombocytopenia

Indicated for treatment of thrombocytopenia in patients with chronic hepatitis C to allow the initiation and maintenance of interferon-based therapy

Initial: 25 mg PO qDay

Adjust dose in 25 mg increments q2weeks PRN to achieve the target platelet count required to initiate antiviral therapy; not to exceed 100 mg/day

During antiviral therapy, adjust dose to avoid dose reductions of peginterferon

Dosage considerations

  • Should be used only in patients with chronic hepatitis C whose degree of thrombocytopenia prevents the initiation of interferon-based therapy or limits the ability to maintain interferon-based therapy
  • Prior to starting antiviral therapy: Monitor platelet counts qWeek
  • During antiviral therapy: Monitor CBCs with differentials (including platelet counts) qWeek until a stable platelet count achieved, then monitor platelet counts monthly thereafter
  • Safety and efficacy have not been established in combination with direct-acting antiviral agents used without interferon for treatment of chronic hepatitis C infection

Dosage Modifications (CHC)

Hepatic impairment: No dosage adjustment required

Adjust dose according to platelets

  • Plt <50 x 10^9/L after at least 2 weeks: Increase daily dose by 25 mg; not to exceed 100 mg/day
  • Plt 200-400 x 10^9/L: Decrease daily dose by 25 mg; assess after 2 weeks
  • Plt >400 x 10^9/L: Discontinue and monitor Plt 2x/week; once Plt <150 x 10^9/L, restart therapy with 25 mg reduction in daily dose
  • Plt >400 x 10^9/L after 2 weeks of therapy at lowest dose: Discontinue permanently

Discontinue if

  • Antiviral therapy is discontinued
  • Abnormal LFTs or excessive Plt responses

Aplastic Anemia

Indicated for severe aplastic anemia (SAA) in patients who fail to respond adequately to at least 1 prior immunosuppressive therapy

Initial dose: 50 mg PO qDay

Adjust dose q2wk as needed to maintain platelet count ≥50 x 10^9/L; not to exceed 150 mg qDay

May take for up to 16 wk after initiating

Dosage Modifications (SAA)

East Asian ancestry: Decrease initial dose to 25 mg/day

Hepatic impairment (Child-Pugh Class A, B, or C): Decrease initial dose to 25 mg/day

Adjust dose according to platelets

  • <50 x 10^9/L following at least 2 wk after initiating: Increase by 50 mg/day to a maximum of 150 mg/day; if taking 25 mg/day, increase dose to 50 mg daily before increasing by 50 mg/day
  • ≥200 x 10^9/L to ≤400 x 10^9/L at any time: Decrease by 50 mg/day, wait 2 wk to assess effects and the need for any subsequent dose adjustments
  • >400 x 10^9/L: Stop for 1 wk, when platelet count <150 x 10^9/L, reinitiate at dose reduced by 50 mg/day
  • >400 x 10^9/L after 2 wk of therapy at lowest dose: Discontinue

Tri-lineage response (including transfusion independence ≥8 wk)

  • Reduce dose by 50%
  • If counts remain stable after 8 weeks at the reduced dose, then discontinue eltrombopag and monitor blood counts
  • If platelet counts drop to <30 x 10^9/L, hemoglobin <9 g/dL, or ANC <0.5 x 10^9/L: May reinitiated at the previous effective dose

Discontinue if

  • No hematologic response after 16 wk
  • New cytogenetic abnormalities observed, consider discontinuation
  • Excessive platelet count responses (see Dosage Modifications above) or important liver test abnormalities occur

Dosage Forms & Strengths

tablet

  • 12.5mg
  • 25mg
  • 50mg
  • 75mg
  • 100mg

powder for oral suspension

  • 25mg/unit dose (30-day supply kit)
more...

Chronic Immune Thrombocytopenia (ITP)

Indicated for treatment of thrombocytopenia in adults and pediatric patients ≥1 yr with chronic immune (idiopathic) thrombocytopenia (ITP) with insufficient response to corticosteroids, immunoglobulins, or splenectomy

<1 year: Safety and efficacy not established

1-5 years (initial dose): 25 mg PO qDay (use oral suspension)

≥6 years (initial dose): 50 mg PO qDay

Maintenance: Adjust dose to achieve and maintain platelet count (Plt) >50 x 10^9/L to reduce risk of bleeding; not to exceed 75 mg/day

Dosing considerations

  • Should be used only in patients with ITP whose degree of thrombocytopenia and clinical condition increase the risk for bleeding
  • Use the lowest dose to achieve and maintain a platelet count >50 x 10^9/L as necessary to reduce the risk for bleeding
  • Dose adjustment based upon the platelet count response; do not use to normalize platelet counts
  • Monitor LFTs and CBC prior to initiation, and throughout therapy
  • When switching between the oral suspension and tablet, assess platelet counts weekly for 2 weeks, and then follow standard monthly monitoring

Dosage Modifications (ITP)

East Asian ancestry: Decrease initial dose to 25 mg PO qDay

Hepatic impairment

  • Mild-to-severe (Child-Pugh A, B, or C): Decrease initial dose to 25 mg PO qDay
  • East Asian ancestry with hepatic impairment: Decrease initial dose to 12.5 mg PO qDay

Adjust dose according to platelets

  • Plt <50 x 10^9/L; after at least 2 weeks: Increase daily dose by 25 mg; not to exceed 75 mg/day
  • Plt 200-400 x 10^9/L: Decrease daily dose by 25 mg; assess after 2 weeks
  • Plt >400 x 10^9/L: Discontinue and monitor platelet 2x/week; once platelet <150 x 10^9/L; restart therapy with 25 mg reduction in daily dose
  • Plt >400 x 10^9/L; after 2 weeks of therapy at lowest dose: Discontinue permanently

Discontinue if

  • No improvement after 4 weeks at maximum dose, OR
  • Abnormal LFTs or excessive Plt responses
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Interactions

Interaction Checker

eltrombopag and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

            Sort by :  
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            Adverse Effects

            >10%

            Influenza-like symptoms (26-35%)

            Headache (10-36%)

            Rigor (6-32%)

            Fatigue (3-29%)

            Nausea (4-21%)

            Arthralgia (3-21%)

            Myalgia (3-21%)

            Depression (5-17%)

            Upper abdominal pain (11-14%)

            Xerostomia (9-14%)

            1-10%

            Abnormal LFT's (10%)

            Thrombocytopenia (2%)

            Frequency Not Defined

            Paresthesias

            Vomiting

            Dyspepsia

            Thrombotic or thromboembolic complications

            Hemorrhage

            Conjunctival hemorrhage

            Ecchymosis

            Menorrhagia

            Cataract

            Postmarketing Reports

            Thrombotic microangiopathy with acute renal failure

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            Warnings

            Black Box Warnings

            May cause hepatotoxicity; in combination with interferon and ribavirin in patients with chronic hepatitis C, may increase the risk of hepatic decompensation

            Measure ALT, AST, and bilirubin level prior to initiation, q2 weeks during the dose adjustment phase, and monthly following establishment of a stable dose

            If bilirubin level is elevated, perform fractionation

            If serum liver test results are abnormal, repeat tests within 3-5 days; if the abnormalities are confirmed, obtain serum liver tests weekly until the abnormalities resolve, stabilize, or return to baseline

            Discontinue if ALT levels increase to ≥3xULN in patients with normal liver function or ≥3x baseline in patients with pretreatment elevation in transaminases and are progressive, persistent for >4 wk, accompanied by increased direct bilirubin, or accompanied by clinical symptoms of liver injury or evidence for hepatic decompensation

            Contraindications

            None reported

            Cautions

            Risk of hepatotoxicity (see Black Box Warnings)

            Chronic hepatitis C with cirrhosis may increase risk of hepatic decompensation and death when treated with alfa interferons

            Thrombotic/thromboembolic complications reported (rare)

            Risk of thrombocytopenia and hemorrhage after discontinuation

            May develop or worsen cataracts; screen before administering and during treatment

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            Pregnancy & Lactation

            Pregnancy Category: C

            Lactation: excretion in milk unknown/not recommended

            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.

            more...
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            Pharmacology

            Mechanism of Action

            Small-molecule thrombopoietin (TPO)-receptor agonist that interacts with human TPO receptor transmembrane domain of human TPO-receptor & initiates signaling cascades that induce proliferation & differentiation of megakaryocytes from bone marrow progenitor cells

            Absorption

            Bioavailability: 52%+

            Peak Plasma Time: 2-6 hr

            Peak plasma concentration: 8.-1-12.7 mcg/mL

            AUC: 108-168 mcg·hr/mL

            Distribution

            Concentration in blood cells is ~50-79% of plasma concentrations

            Metabolism

            Extensively metabolized predominantly through pathways including cleavage, oxidation, and conjugation with glucuronic acid, glutathione, or cysteine

            In vitro studies suggest that CYP1A2 and CYP2C8 are responsible for the oxidative metabolism

            UGT1A1 and UGT1A3 are responsible for the glucuronidation

            Elimination

            Half-life: 26-35 hr (in patients with ITP)

            Excretion: Feces 59%; urine 31%

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            Administration

            Instructions

            Take on empty stomach 1 hr before or 2 hr after food

            Allow 4-hr interval when taking foods/medication, calcium-rich foods, or supplements containing polyvalent cations (eg, calcium, iron, zinc, magnesium)

            Do NOT administer more than 1 dose within a 24-hr period

            Oral Suspension Preparation

            Prior to use of the oral suspension, ensure patients or caregivers receive training on proper dosing, preparation, and administration of oral suspension

            Prepare the suspension with cool or cold water only

            NOTE: Do not use hot water to prepare the suspension

            Measure 20 mL of drinking water in reusable oral syringe, empty water into mixing bottle provided in 30-day supply kit

            Take only the prescribed number of packets for one dose out of the kit

            Tap the top of each packet to make sure the contents fall to the bottom, and then cut off the top of the packet with scissors and empty the entire contents of the packet into the mixing bottle

            Make sure not to spill the powder outside the mixing bottle

            Screw the lid tightly onto the bottle and the cap is pushed onto the lid

            Gently and slowly shake the bottle back and forth for a least 20 seconds to mix thoroughly without foaming (ie, do not shake the bottle hard)

            The liquid will be dark brown in color

            Pull cap off the mixing bottle lid and insert the syringe tip into the hole in the lid

            Transfer the mixture into the oral syringe by turning the mixing bottle upside down along with the syringe

            Measure prescribed dose into syringe (see full instructions within the Prescribing Information)

            Oral Suspension Administration

            Place the tip of the oral syringe into the inside of the child’s cheek

            Slowly push the plunger all the way down to give the entire dose

            Make sure the child has time to swallow the medicine

            Storage

            Powder for oral suspension or tablets: Store at room temperature between 68-77°F (20-25°C)

            Reconstituted oral suspension

            • After mixing, should be taken right away but may be stored for up to 30 minutes at room temperature between 68-77°F (20-25°C)
            • Discard the mixture in trash if not used within 30 minutes; do not throw down the drain
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            Images

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            Formulary

            FormularyPatient Discounts

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

            Adding plans allows you to:

            • View the formulary and any restrictions for each plan.
            • Manage and view all your plans together – even plans in different states.
            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            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.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
            Add or Remove Plans
            Plans for
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            Select a box to add or remove a plan.

            Select a class to view formulary status for similar drugs

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