Eltrombopag 12.5mg Pow Oral Sus Kt
WARNING: Severe and sometimes deadly liver problems have happened with this drug. Call your doctor right away if you have signs of liver problems like dark urine, tiredness, decreased appetite, upset stomach or stomach pain, light-colored stools, throwing up, or yellow skin or eyes.This drug may raise the risk of liver failure when taken with interferon and ribavirin in patients with hepatitis C. If your doctor tells you to stop taking interferon and ribavirin, you will also need to stop taking this drug. @ COMMON USES: It is used to raise platelet counts.It is used to treat immune thrombocytopenia (ITP).It is used to treat aplastic anemia.
Drug Class
Thrombopoietin Receptor Agonist
Pharmacologic Class
Hematopoietic Agent; Platelet Stimulator
Pregnancy Category
Category C
FDA Approved
Nov 2008
DEA Schedule
Not Controlled
Overview
What is this medicine?
Eltrombopag is a medicine that helps your body make more platelets, which are tiny blood cells that help your blood clot. It's used for conditions where your body doesn't make enough platelets, like certain bleeding disorders or a serious bone marrow condition.
How to Use This Medicine
Taking Your Medication Correctly
To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided to you and follow the instructions closely.
Take your medication with or without food, but avoid taking it with meals high in calcium.
If you take other medications, you may need to take this medication at a different time. Be sure to take it at least 2 hours before or 4 hours after consuming foods or drinks high in calcium, antacids, or products containing calcium, iron, aluminum, magnesium, selenium, or zinc. Examples of foods and drinks high in calcium include dairy products, certain fruits, vegetables, and juices.
Preparing Your Dose
Before taking your medication, make sure you understand how to mix and measure the correct dose. If you're unsure, consult with your doctor or pharmacist.
This medication comes with single-use oral dosing syringes. Use each syringe only once and discard it after use.
Mix the powder with water only, as instructed by your doctor or pharmacist. Avoid using hot water to mix the medication.
Take your dose within 30 minutes of mixing the medication. Discard any unused portion within 30 minutes of mixing.
Storing and Disposing of Your Medication
Store your medication in its original container at room temperature.
Keep it in a dry place, away from the bathroom.
What to Do If You Miss a Dose
If you miss a dose, skip it and return to your regular dosing schedule.
* Do not take two doses at the same time or take extra doses to make up for the missed dose.
To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided to you and follow the instructions closely.
Take your medication with or without food, but avoid taking it with meals high in calcium.
If you take other medications, you may need to take this medication at a different time. Be sure to take it at least 2 hours before or 4 hours after consuming foods or drinks high in calcium, antacids, or products containing calcium, iron, aluminum, magnesium, selenium, or zinc. Examples of foods and drinks high in calcium include dairy products, certain fruits, vegetables, and juices.
Preparing Your Dose
Before taking your medication, make sure you understand how to mix and measure the correct dose. If you're unsure, consult with your doctor or pharmacist.
This medication comes with single-use oral dosing syringes. Use each syringe only once and discard it after use.
Mix the powder with water only, as instructed by your doctor or pharmacist. Avoid using hot water to mix the medication.
Take your dose within 30 minutes of mixing the medication. Discard any unused portion within 30 minutes of mixing.
Storing and Disposing of Your Medication
Store your medication in its original container at room temperature.
Keep it in a dry place, away from the bathroom.
What to Do If You Miss a Dose
If you miss a dose, skip it and return to your regular dosing schedule.
* Do not take two doses at the same time or take extra doses to make up for the missed dose.
Lifestyle & Tips
- Take this medicine on an empty stomach, at least 1 hour before or 2 hours after any food, dairy products, or mineral supplements (like iron, calcium, magnesium, aluminum, selenium, zinc).
- Mix the powder for oral suspension exactly as directed by your pharmacist or doctor. Do not chew or crush the tablets if you are prescribed the tablet form.
- Do not stop taking this medicine without talking to your doctor, as your platelet count may drop significantly.
- Avoid activities that could cause injury or bleeding, especially when your platelet count is low.
- Report any signs of bleeding, liver problems, or blood clots to your doctor immediately.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
Varies by indication
Dose Range:
12.5 - 150 mg
Condition-Specific Dosing:
Chronic Immune Thrombocytopenia (ITP):
50 mg orally once daily; adjust dose to achieve and maintain platelet count âĨ50,000/mcL. Max 75 mg/day.
Severe Aplastic Anemia (SAA) - Refractory:
50 mg orally once daily for 2 weeks; increase to 150 mg/day if no response. Max 150 mg/day.
Severe Aplastic Anemia (SAA) - First-line (in combination with standard immunosuppressive therapy):
150 mg orally once daily for 6 months.
Chronic Hepatitis C-associated Thrombocytopenia:
25 mg orally once daily; adjust dose to achieve platelet count âĨ50,000/mcL. Max 100 mg/day.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
ITP: 25 mg orally once daily for patients 1 to 5 years old; 50 mg orally once daily for patients 6 to 17 years old. Adjust dose to achieve and maintain platelet count âĨ50,000/mcL. Max 75 mg/day.
Adolescent:
ITP: 50 mg orally once daily for patients 6 to 17 years old. Adjust dose to achieve and maintain platelet count âĨ50,000/mcL. Max 75 mg/day. SAA: 75 mg orally once daily for patients 12 years and older with refractory SAA; increase to 150 mg/day if no response. Max 150 mg/day.
Dose Adjustments
Renal Impairment:
Mild:
No dose adjustment required.
Moderate:
No dose adjustment required.
Severe:
No dose adjustment required.
Dialysis:
No dose adjustment required; Eltrombopag is highly protein bound and not expected to be removed by dialysis.
Hepatic Impairment:
Mild:
Child-Pugh Class A: No dose adjustment required for ITP/HCV. For SAA, start at 75 mg/day.
Moderate:
Child-Pugh Class B: For ITP/HCV, start at 25 mg/day. For SAA, start at 75 mg/day.
Severe:
Child-Pugh Class C: For ITP/HCV, start at 25 mg/day. For SAA, start at 75 mg/day. Monitor closely.
Pharmacology
Mechanism of Action
Eltrombopag is an orally bioavailable, small-molecule thrombopoietin (TPO) receptor agonist. It interacts with the transmembrane domain of the human TPO receptor and initiates signaling cascades that lead to the proliferation and differentiation of megakaryocytes from bone marrow progenitor cells, resulting in an increase in platelet production.
Pharmacokinetics
Absorption:
Bioavailability:
Not available (variable, influenced by food/cations)
Tmax:
2-6 hours
FoodEffect:
Absorption is significantly decreased by food, especially high-fat meals and products containing polyvalent cations (e.g., dairy products, antacids, mineral supplements). Administer at least 1 hour before or 2 hours after a meal or other products containing polyvalent cations.
Distribution:
Vd:
Approximately 10 L (oral suspension)
ProteinBinding:
Greater than 99% (primarily to albumin)
CnssPenetration:
Limited
Elimination:
HalfLife:
21-32 hours (oral suspension)
Clearance:
Not available
ExcretionRoute:
Approximately 52% in feces (unchanged drug), 31% in urine (metabolites).
Unchanged:
Approximately 20% in feces
Pharmacodynamics
OnsetOfAction:
Within 1-2 weeks (platelet count increase)
PeakEffect:
Approximately 2-3 weeks (platelet count peak)
DurationOfAction:
Platelet counts typically return to baseline within 1-2 weeks after discontinuation.
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
While rare, some people may experience severe and potentially life-threatening side effects when taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical attention immediately:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of a urinary tract infection (UTI), including:
+ Blood in the urine
+ Burning or pain when passing urine
+ Frequent or urgent need to urinate
+ Fever
+ Lower stomach pain
+ Pelvic pain
Neurological symptoms, such as:
+ Weakness on one side of the body
+ Trouble speaking or thinking
+ Change in balance
+ Drooping on one side of the face
+ Blurred eyesight
Eye problems, including:
+ Change in eyesight
+ Eye pain
+ Severe eye irritation
Unusual bruising or bleeding while taking this medication or after stopping it
Confusion
Swelling of the abdomen
Swelling in the arms or legs
Fever or chills
Signs of a blood clot, such as:
+ Chest pain or pressure
+ Coughing up blood
+ Shortness of breath
+ Swelling, warmth, numbness, change of color, or pain in a leg or arm
+ Trouble speaking or swallowing
Other Possible Side Effects
Like all medications, this drug can cause side effects. Many people experience no side effects or only mild ones. If you notice any of the following side effects or any other unusual symptoms, contact your doctor or seek medical attention if they bother you or do not go away:
Headache
Diarrhea
Stomach pain
Upset stomach
Nausea or vomiting
Dizziness
Fatigue or weakness
Cough
Muscle or joint pain
Signs of a common cold
Muscle spasm
Nose or throat irritation
Mouth pain
Tooth pain
Change in skin color
Pain in arms or legs
Reporting Side Effects
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
While rare, some people may experience severe and potentially life-threatening side effects when taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical attention immediately:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of a urinary tract infection (UTI), including:
+ Blood in the urine
+ Burning or pain when passing urine
+ Frequent or urgent need to urinate
+ Fever
+ Lower stomach pain
+ Pelvic pain
Neurological symptoms, such as:
+ Weakness on one side of the body
+ Trouble speaking or thinking
+ Change in balance
+ Drooping on one side of the face
+ Blurred eyesight
Eye problems, including:
+ Change in eyesight
+ Eye pain
+ Severe eye irritation
Unusual bruising or bleeding while taking this medication or after stopping it
Confusion
Swelling of the abdomen
Swelling in the arms or legs
Fever or chills
Signs of a blood clot, such as:
+ Chest pain or pressure
+ Coughing up blood
+ Shortness of breath
+ Swelling, warmth, numbness, change of color, or pain in a leg or arm
+ Trouble speaking or swallowing
Other Possible Side Effects
Like all medications, this drug can cause side effects. Many people experience no side effects or only mild ones. If you notice any of the following side effects or any other unusual symptoms, contact your doctor or seek medical attention if they bother you or do not go away:
Headache
Diarrhea
Stomach pain
Upset stomach
Nausea or vomiting
Dizziness
Fatigue or weakness
Cough
Muscle or joint pain
Signs of a common cold
Muscle spasm
Nose or throat irritation
Mouth pain
Tooth pain
Change in skin color
Pain in arms or legs
Reporting Side Effects
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Unusual bleeding or bruising (e.g., nosebleeds, bleeding gums, red/purple spots on skin, blood in urine/stools)
- Yellowing of skin or eyes (jaundice)
- Dark urine, pale stools
- Severe nausea, vomiting, or stomach pain (especially upper right side)
- Unusual tiredness or weakness
- Swelling, pain, or redness in an arm or leg (signs of a blood clot)
- Sudden shortness of breath, chest pain, or rapid heartbeat (signs of a blood clot in the lung)
- Sudden numbness or weakness on one side of the body, sudden vision changes, or severe headache (signs of a stroke)
- Blurred vision or changes in eyesight (potential cataracts)
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
A low platelet count caused by underlying health conditions.
* If you are breastfeeding, as you should not breastfeed while taking this medication.
This list is not exhaustive, and it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health problems with your doctor and pharmacist. They will help you determine if it is safe to take this medication with your existing treatments and health conditions. Never start, stop, or adjust the dosage of any medication without consulting your doctor first.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
A low platelet count caused by underlying health conditions.
* If you are breastfeeding, as you should not breastfeed while taking this medication.
This list is not exhaustive, and it is crucial to discuss all your medications (prescription, over-the-counter, natural products, and vitamins) and health problems with your doctor and pharmacist. They will help you determine if it is safe to take this medication with your existing treatments and health conditions. Never start, stop, or adjust the dosage of any medication without consulting your doctor first.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. Regular blood tests will be necessary, as directed by your doctor, to monitor your condition. Discuss any concerns or questions you have with your doctor.
Do not discontinue this medication without consulting your doctor first, as this may increase your risk of developing severe thrombocytopenia (very low platelet count) and bleeding. If you need to stop taking this drug, talk to your doctor to determine the best course of action.
This medication may exacerbate existing cataracts or increase the risk of developing new cataracts. Consult your doctor and follow their recommendations for regular eye exams to monitor your eye health.
If you are of East or Southeast Asian descent, discuss your treatment options with your doctor, as you may require a lower initial dose of this medication.
Be aware that this medication has been associated with an increased risk of blood clots, which can be life-threatening and may lead to heart attack or stroke. Take precautions to prevent injuries and avoid falls or accidents. Consult your doctor to discuss any concerns you may have.
This medication is contraindicated in individuals with myelodysplastic syndrome (MDS), a specific bone marrow disorder. If you have MDS and take this medication, your condition may worsen and potentially progress to acute myelogenous leukemia (AML), a type of blood cancer. This can significantly reduce your life expectancy. If you have MDS, consult your doctor to discuss alternative treatment options.
Additionally, this medication may harm an unborn baby if taken during pregnancy. If you are pregnant or planning to become pregnant, you must use effective birth control while taking this medication and for a specified period after the last dose. Consult your doctor to determine the recommended duration of birth control use. If you become pregnant while taking this medication, notify your doctor immediately.
Do not discontinue this medication without consulting your doctor first, as this may increase your risk of developing severe thrombocytopenia (very low platelet count) and bleeding. If you need to stop taking this drug, talk to your doctor to determine the best course of action.
This medication may exacerbate existing cataracts or increase the risk of developing new cataracts. Consult your doctor and follow their recommendations for regular eye exams to monitor your eye health.
If you are of East or Southeast Asian descent, discuss your treatment options with your doctor, as you may require a lower initial dose of this medication.
Be aware that this medication has been associated with an increased risk of blood clots, which can be life-threatening and may lead to heart attack or stroke. Take precautions to prevent injuries and avoid falls or accidents. Consult your doctor to discuss any concerns you may have.
This medication is contraindicated in individuals with myelodysplastic syndrome (MDS), a specific bone marrow disorder. If you have MDS and take this medication, your condition may worsen and potentially progress to acute myelogenous leukemia (AML), a type of blood cancer. This can significantly reduce your life expectancy. If you have MDS, consult your doctor to discuss alternative treatment options.
Additionally, this medication may harm an unborn baby if taken during pregnancy. If you are pregnant or planning to become pregnant, you must use effective birth control while taking this medication and for a specified period after the last dose. Consult your doctor to determine the recommended duration of birth control use. If you become pregnant while taking this medication, notify your doctor immediately.
Overdose Information
Overdose Symptoms:
- Excessive platelet count (thrombocytosis), which may increase risk of thromboembolic events
- Liver enzyme elevations
What to Do:
There is no specific antidote. In case of overdose, monitor platelet counts and liver function closely. Provide supportive care. Consider oral administration of a polyvalent cation-containing product (e.g., calcium-containing antacid) to limit absorption if overdose is recent. Call 1-800-222-1222 (Poison Control Center).
Drug Interactions
Major Interactions
- Polyvalent cation-containing products (e.g., antacids, dairy products, mineral supplements containing iron, calcium, magnesium, aluminum, selenium, zinc): Significantly reduce eltrombopag absorption. Administer eltrombopag at least 1 hour before or 2 hours after these products.
- Statins (e.g., Rosuvastatin, Atorvastatin): Eltrombopag is an OATP1B1 and BCRP inhibitor, increasing statin exposure. Reduce statin dose and monitor.
Moderate Interactions
- UGT1A1 and UGT1A3 substrates (e.g., Irinotecan, Raltegravir): Eltrombopag is a UGT1A1 and UGT1A3 inhibitor, potentially increasing exposure of these drugs.
- BCRP substrates (e.g., Methotrexate, Topotecan): Eltrombopag is a BCRP inhibitor, potentially increasing exposure of these drugs.
- OATP1B1 substrates (e.g., Valsartan, Glibenclamide): Eltrombopag is an OATP1B1 inhibitor, potentially increasing exposure of these drugs.
Monitoring
Baseline Monitoring
Complete Blood Count (CBC) with differential and platelet count
Rationale: To establish baseline platelet count and assess overall hematologic status.
Timing: Prior to initiation of therapy.
Liver Function Tests (LFTs) including ALT, AST, bilirubin (total and direct)
Rationale: Eltrombopag can cause hepatotoxicity.
Timing: Prior to initiation of therapy.
Serum Creatinine and BUN
Rationale: To assess renal function.
Timing: Prior to initiation of therapy.
Ophthalmologic examination
Rationale: To assess for cataracts, which have been reported.
Timing: Prior to initiation of therapy.
Routine Monitoring
CBC with platelet count
Frequency: Weekly until stable platelet count (âĨ50,000/mcL for ITP/HCV, or target for SAA) for at least 4 weeks, then monthly.
Target: Platelet count âĨ50,000/mcL (ITP/HCV); individualized for SAA.
Action Threshold: If platelet count >400,000/mcL, reduce dose or hold therapy. If <50,000/mcL, consider dose increase (after 2 weeks at current dose).
Liver Function Tests (ALT, AST, bilirubin)
Frequency: Every 2 weeks during dose adjustment, then monthly after stable dose for 3 months, then every 3 months.
Target: Within normal limits or baseline.
Action Threshold: If ALT/AST >3x ULN and total bilirubin >2x ULN, or if ALT/AST >5x ULN, hold therapy and monitor. Re-initiate at lower dose if LFTs return to baseline.
Signs/symptoms of thromboembolic events
Frequency: Regularly throughout therapy.
Target: Absence of symptoms.
Action Threshold: Prompt evaluation if symptoms occur.
Signs/symptoms of bone marrow reticulin formation/fibrosis
Frequency: Periodically, especially in SAA patients.
Target: Absence of symptoms.
Action Threshold: Consider bone marrow biopsy if clinically indicated (e.g., new cytopenias, abnormal peripheral blood smear).
Ophthalmologic examination
Frequency: Annually.
Target: No new cataracts or worsening.
Action Threshold: If cataracts develop or worsen, consider ophthalmology referral.
Symptom Monitoring
- Unusual bleeding or bruising (e.g., petechiae, purpura, epistaxis, gingival bleeding)
- Signs of liver problems (e.g., yellowing of skin/eyes, dark urine, unusual tiredness, right upper quadrant pain, nausea, vomiting)
- Signs of blood clots (e.g., swelling, pain, redness in a limb; sudden shortness of breath, chest pain, rapid heart rate; sudden numbness/weakness, vision changes, severe headache)
- Vision changes or blurred vision (potential cataracts)
- New or worsening fatigue, bone pain, or abnormal blood counts (potential bone marrow changes)
Special Patient Groups
Pregnancy
Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. Based on animal studies, eltrombopag may cause fetal harm.
Trimester-Specific Risks:
First Trimester:
Potential for embryo-fetal toxicity based on animal data (e.g., reduced fetal weight, delayed ossification).
Second Trimester:
Potential for embryo-fetal toxicity based on animal data.
Third Trimester:
Potential for embryo-fetal toxicity based on animal data.
Lactation
It is not known if eltrombopag is excreted in human milk. Due to the potential for serious adverse reactions in a breastfed infant, advise women not to breastfeed during treatment with eltrombopag and for at least 21 days after the last dose.
Infant Risk:
L3 - Moderate risk. Potential for serious adverse reactions in breastfed infant.
Pediatric Use
Approved for chronic ITP in patients 1 year and older, and for refractory SAA in patients 12 years and older. Dosing is weight-based or age-based depending on indication. Close monitoring of LFTs and platelet counts is crucial.
Geriatric Use
No overall differences in safety or effectiveness were observed between elderly and younger patients. However, greater sensitivity of some older individuals cannot be ruled out. Dose adjustments for age alone are not typically required, but consider age-related decreases in hepatic, renal, or cardiac function and concomitant disease or other drug therapy.
Clinical Information
Clinical Pearls
- Strict adherence to administration instructions (empty stomach, away from polyvalent cations) is critical for optimal absorption and efficacy.
- The oral suspension formulation is particularly sensitive to proper mixing and administration. Ensure caregivers/patients are thoroughly educated.
- Patients with Asian ancestry may require a lower starting dose due to higher plasma concentrations observed in this population.
- Regular monitoring of liver function tests is paramount due to the risk of hepatotoxicity. Dose adjustments or discontinuation may be necessary.
- Be vigilant for signs and symptoms of thromboembolic events, especially in patients with risk factors or those with high platelet counts.
- Eltrombopag is a long-term treatment for many indications; patient education on adherence and monitoring is key for safety and efficacy.
Alternative Therapies
- Romiplostim (another TPO-RA)
- Avatrombopag (another TPO-RA)
- Fostamatinib (Syk inhibitor for ITP)
- Rituximab (anti-CD20 antibody for ITP)
- Corticosteroids (e.g., Prednisone for ITP, SAA)
- Immunosuppressants (e.g., Cyclosporine, ATG for SAA)
- Splenectomy (for ITP)
Cost & Coverage
Average Cost:
Price varies significantly by dosage and kit size (e.g., 12.5mg, 25mg, 50mg, 75mg). Typically several thousand USD. per kit/bottle
Insurance Coverage:
Specialty Tier (requires prior authorization, often subject to co-pay assistance programs)
General Drug Facts
If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication.
This medication is accompanied by a Medication Guide, which is a patient fact sheet that provides important information. Please read this guide carefully and review it again whenever you receive a refill of this medication. If you have any questions or concerns about this medication, don't hesitate to discuss them with your doctor, pharmacist, or other healthcare provider.
In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When reporting the incident, be prepared to provide details about the medication, including the amount taken and the time it occurred, to help healthcare professionals provide the best possible care.
This medication is accompanied by a Medication Guide, which is a patient fact sheet that provides important information. Please read this guide carefully and review it again whenever you receive a refill of this medication. If you have any questions or concerns about this medication, don't hesitate to discuss them with your doctor, pharmacist, or other healthcare provider.
In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When reporting the incident, be prepared to provide details about the medication, including the amount taken and the time it occurred, to help healthcare professionals provide the best possible care.