Eltrombopag 50mg Tablets
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
Thrombopoietin receptor agonist
Pregnancy Category
Not applicable (FDA no longer uses categories, but risk of fetal harm)
FDA Approved
Nov 2008
DEA Schedule
Not Controlled
Overview
What is this medicine?
Eltrombopag is a medication that helps your body make more platelets, which are tiny blood cells that help stop bleeding. It's used to treat conditions where you have too few platelets, such as immune thrombocytopenia (ITP), severe aplastic anemia, and low platelets due to chronic hepatitis C.
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 either on an empty stomach or with a meal that is low in calcium.
If you are taking other medications, you may need to take this medication at a different time. To ensure proper absorption, take your medication at least 2 hours before or 4 hours after consuming foods or drinks that are high in calcium, such as dairy products, certain fruits, vegetables, and juices. Additionally, avoid taking your medication at the same time as antacids or products that contain calcium, iron, aluminum, magnesium, selenium, or zinc.
Important Administration Instructions
Swallow your medication whole; do not chew, break, or crush it.
Do not mix your medication with food or drinks.
Storing and Disposing of Your Medication
Store your medication in its original container at room temperature, in a dry place. Avoid storing it in a bathroom.
What to Do If You Miss a Dose
If you miss a dose, skip it and take your next dose at the usual time. 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 either on an empty stomach or with a meal that is low in calcium.
If you are taking other medications, you may need to take this medication at a different time. To ensure proper absorption, take your medication at least 2 hours before or 4 hours after consuming foods or drinks that are high in calcium, such as dairy products, certain fruits, vegetables, and juices. Additionally, avoid taking your medication at the same time as antacids or products that contain calcium, iron, aluminum, magnesium, selenium, or zinc.
Important Administration Instructions
Swallow your medication whole; do not chew, break, or crush it.
Do not mix your medication with food or drinks.
Storing and Disposing of Your Medication
Store your medication in its original container at room temperature, in a dry place. Avoid storing it in a bathroom.
What to Do If You Miss a Dose
If you miss a dose, skip it and take your next dose at the usual time. Do not take two doses at the same time or take extra doses to make up for the missed dose.
Lifestyle & Tips
- Take eltrombopag on an empty stomach, at least 2 hours before or 4 hours after any foods, drinks, or supplements that contain polyvalent cations (e.g., calcium, iron, magnesium, aluminum, selenium, zinc). This includes dairy products (milk, cheese, yogurt), calcium-fortified juices, antacids, and mineral supplements.
- Swallow tablets whole; do not crush, chew, or break them.
- Do not stop taking eltrombopag without talking to your doctor, as your platelet count may drop significantly.
- Avoid activities that increase your risk of bleeding or injury, especially when your platelet count is low.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
Varies by indication and patient factors. Initial doses typically 25 mg or 50 mg once daily.
Dose Range:
25 - 150 mg
Condition-Specific Dosing:
Chronic Immune Thrombocytopenia (ITP):
Initial 50 mg once daily (25 mg for patients of East Asian descent). Titrate to achieve platelet count âĨ50 x 10^9/L. Max 75 mg/day.
Severe Aplastic Anemia (SAA):
Initial 50 mg once daily. Titrate up to 150 mg/day.
Thrombocytopenia in Chronic Hepatitis C (HCV):
Initial 25 mg once daily. Titrate up to 100 mg/day.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established for <1 year
Child:
ITP (âĨ1 year): Initial 25 mg once daily. SAA (âĨ2 years): Initial 25 mg once daily. Titrate as per adult guidelines.
Adolescent:
ITP (âĨ1 year): Initial 25 mg once daily. SAA (âĨ2 years): Initial 25 mg once daily. Titrate as per adult guidelines.
Dose Adjustments
Renal Impairment:
Mild:
No dose adjustment needed.
Moderate:
No dose adjustment needed.
Severe:
No dose adjustment needed.
Dialysis:
No specific recommendations; use with caution and monitor.
Hepatic Impairment:
Mild:
No dose adjustment needed for SAA. For ITP/HCV-ITP, consider starting at 25 mg once daily.
Moderate:
For ITP/HCV-ITP, reduce initial dose to 25 mg once daily. For SAA, reduce initial dose to 25 mg once daily.
Severe:
For ITP/HCV-ITP, reduce initial dose to 25 mg once daily. For SAA, reduce initial dose to 25 mg once daily. Use with caution and monitor closely.
Pharmacology
Mechanism of Action
Eltrombopag is an orally bioavailable, small-molecule thrombopoietin (TPO) receptor agonist that interacts with the transmembrane domain of the human TPO receptor. It initiates signaling cascades that lead to proliferation and differentiation of megakaryocytes from bone marrow progenitor cells, resulting in an increased production of platelets.
Pharmacokinetics
Absorption:
Bioavailability:
Variable (e.g., 52% for oral solution, but significantly affected by food/cations)
Tmax:
2-6 hours
FoodEffect:
Polyvalent cations (e.g., calcium, iron, magnesium, aluminum, selenium, zinc) significantly decrease absorption. Must be taken at least 2 hours before or 4 hours after products containing polyvalent cations. High-fat, high-calorie meal decreases AUC by 59%.
Distribution:
Vd:
11.6 L
ProteinBinding:
>99%
CnssPenetration:
Limited (P-glycoprotein substrate)
Elimination:
HalfLife:
21-32 hours
Clearance:
0.8 L/hr
ExcretionRoute:
Feces (59%), Urine (31%)
Unchanged:
20% (feces), 5% (urine)
Pharmacodynamics
OnsetOfAction:
Within 1-2 weeks (platelet count increase)
PeakEffect:
Approximately 2-3 weeks (platelet count increase)
DurationOfAction:
Platelet counts typically return to baseline within 1-2 weeks after discontinuation.
Safety & Warnings
BLACK BOX WARNING
Risk of Hepatotoxicity: Promacta can cause severe and potentially fatal hepatotoxicity. Monitor liver function tests (ALT, AST, bilirubin) prior to initiation, every 2 weeks during dose adjustment, and monthly after stable dose. Interrupt or discontinue Promacta if liver enzyme elevations are progressive or clinically significant.
Risk of Myelodysplastic Syndromes (MDS) and Acute Myeloid Leukemia (AML) in Patients with Severe Aplastic Anemia (SAA): In patients with SAA, there is an increased risk of progression to MDS/AML. Perform bone marrow examination with cytogenetics prior to and during treatment with Promacta.
Risk of Myelodysplastic Syndromes (MDS) and Acute Myeloid Leukemia (AML) in Patients with Severe Aplastic Anemia (SAA): In patients with SAA, there is an increased risk of progression to MDS/AML. Perform bone marrow examination with cytogenetics prior to and during treatment with Promacta.
Side Effects
Serious Side Effects: Seek Medical Help Right Away
Although rare, some people may experience severe and potentially life-threatening side effects while 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
Bleeding or bruising 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
Most people experience few or no side effects while taking this medication. However, some individuals may encounter mild to moderate side effects. If you experience any of the following symptoms, contact your doctor if they bother you or do not go away:
Headache
Diarrhea
Stomach pain
Upset stomach
Vomiting
Dizziness
Fatigue
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 list is not exhaustive, and you may experience other side effects not mentioned here. If you have questions or concerns about side effects, consult your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, some people may experience severe and potentially life-threatening side effects while 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
Bleeding or bruising 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
Most people experience few or no side effects while taking this medication. However, some individuals may encounter mild to moderate side effects. If you experience any of the following symptoms, contact your doctor if they bother you or do not go away:
Headache
Diarrhea
Stomach pain
Upset stomach
Vomiting
Dizziness
Fatigue
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 list is not exhaustive, and you may experience other side effects not mentioned here. If you have questions or concerns about side effects, consult 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:
- Signs of liver problems: yellowing of your skin or the whites of your eyes (jaundice), dark urine, unusual tiredness, nausea, vomiting, or pain in the upper right side of your stomach area.
- Signs of blood clots: sudden pain, swelling, warmth, or redness in an arm or leg; sudden shortness of breath, chest pain, or rapid breathing; sudden numbness or weakness on one side of your body; sudden vision changes, confusion, or trouble speaking.
- Signs of bleeding: easy bruising, nosebleeds, bleeding gums, prolonged bleeding from cuts, heavy menstrual bleeding, blood in your urine or stools (black or tarry stools).
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 allergic reaction you experienced, including any symptoms that occurred.
A low platelet count caused by other 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 (including prescription, over-the-counter, natural products, and vitamins) and health problems with your doctor and pharmacist. They will help determine if it is safe to take this medication with your other medications and health conditions.
Remember, do not start, stop, or change the dose of any medication without first consulting your doctor to ensure your safety.
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 allergic reaction you experienced, including any symptoms that occurred.
A low platelet count caused by other 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 (including prescription, over-the-counter, natural products, and vitamins) and health problems with your doctor and pharmacist. They will help determine if it is safe to take this medication with your other medications and health conditions.
Remember, do not start, stop, or change the dose of any medication without first consulting your doctor to ensure your safety.
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, consult with your doctor to determine the best course of action.
This medication may exacerbate existing cataracts or increase the risk of developing new cataracts. Consult with your doctor about this potential risk and schedule an eye exam as recommended by your doctor.
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. To minimize this risk, take precautions to prevent injuries and avoid falls or accidents. Consult with 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 that can be fatal. If you have MDS, consult with your doctor to discuss alternative treatment options.
Additionally, this medication may cause harm to an unborn baby if taken during pregnancy. If you are pregnant or may become pregnant, it is crucial to use effective birth control while taking this medication and for a specified period after the last dose. Consult with 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, consult with your doctor to determine the best course of action.
This medication may exacerbate existing cataracts or increase the risk of developing new cataracts. Consult with your doctor about this potential risk and schedule an eye exam as recommended by your doctor.
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. To minimize this risk, take precautions to prevent injuries and avoid falls or accidents. Consult with 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 that can be fatal. If you have MDS, consult with your doctor to discuss alternative treatment options.
Additionally, this medication may cause harm to an unborn baby if taken during pregnancy. If you are pregnant or may become pregnant, it is crucial to use effective birth control while taking this medication and for a specified period after the last dose. Consult with 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 counts (potentially leading to thrombotic events)
- Exaggerated liver enzyme elevations
- Other adverse effects seen at therapeutic doses
What to Do:
There is no specific antidote. In case of overdose, monitor platelet counts closely and manage any adverse reactions symptomatically. Consider oral administration of a polyvalent cation-containing product (e.g., calcium-containing antacid) to chelate eltrombopag and limit absorption if overdose is recent. Call 1-800-222-1222 (Poison Control Center) for further guidance.
Drug Interactions
Major Interactions
- Polyvalent cation-containing products (e.g., antacids, dairy products, mineral supplements): Significantly reduce eltrombopag absorption. Administer eltrombopag at least 2 hours before or 4 hours after these products.
- Statins (e.g., rosuvastatin, atorvastatin): Eltrombopag is an OATP1B1 inhibitor, increasing statin exposure. Consider statin dose reduction and monitor for adverse effects.
- Lopinavir/Ritonavir: May decrease eltrombopag exposure. Monitor platelet counts and adjust eltrombopag dose as needed.
Moderate Interactions
- Other OATP1B1 substrates (e.g., methotrexate, topotecan): Increased exposure of these drugs possible. Monitor and adjust dose.
- UGT1A1 and UGT1A3 substrates (e.g., irinotecan, SN-38): Increased exposure of these drugs possible. Monitor and adjust dose.
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 (ALT, AST, total bilirubin)
Rationale: To establish baseline liver function due to risk of hepatotoxicity.
Timing: Prior to initiation of therapy.
Renal Function Tests (Creatinine, BUN)
Rationale: To assess baseline renal function.
Timing: Prior to initiation of therapy.
Routine Monitoring
Platelet count
Frequency: Weekly until stable platelet count (âĨ50 x 10^9/L) is achieved, then monthly.
Target: Maintain platelet count âĨ50 x 10^9/L to reduce bleeding risk. Avoid platelet counts >200-400 x 10^9/L to reduce thrombotic risk.
Action Threshold: If platelet count >400 x 10^9/L, reduce or interrupt dose. If platelet count <50 x 10^9/L, increase dose (if tolerated and no other cause).
Liver Function Tests (ALT, AST, total bilirubin)
Frequency: Every 2 weeks during dose adjustment, then monthly after stable dose is achieved.
Target: Within normal limits or stable baseline.
Action Threshold: Interrupt or discontinue if ALT/AST increase to >3x ULN and are progressive, or >5x ULN. Re-evaluate if bilirubin increases.
Signs and symptoms of thrombosis
Frequency: Regularly throughout therapy.
Target: Absence of thrombotic events.
Action Threshold: Promptly evaluate any signs/symptoms of thrombosis (e.g., pain, swelling, redness in limb, shortness of breath, chest pain, vision changes).
Symptom Monitoring
- Signs of liver injury: unusual fatigue, nausea, vomiting, right upper quadrant abdominal pain, dark urine, jaundice (yellowing of skin or eyes).
- Signs of blood clots: sudden pain, swelling, warmth, or redness in an arm or leg; sudden shortness of breath, chest pain, or rapid breathing; sudden numbness or weakness on one side of the body; sudden vision changes, confusion, or trouble speaking.
- Signs of bleeding: easy bruising, nosebleeds, bleeding gums, prolonged bleeding from cuts, heavy menstrual bleeding, blood in urine or stools (black or tarry stools).
Special Patient Groups
Pregnancy
Eltrombopag can cause fetal harm when administered to a pregnant woman based on findings from animal reproduction studies and its mechanism of action. Advise pregnant women of the potential risk to a fetus.
Trimester-Specific Risks:
First Trimester:
Potential for fetal harm due to mechanism of action.
Second Trimester:
Potential for fetal harm due to mechanism of action.
Third Trimester:
Potential for fetal harm due to mechanism of action.
Lactation
There are no data on the presence of eltrombopag in human milk, the effects on the breastfed child, or the effects on milk production. Due to the potential for serious adverse reactions in a breastfed child, advise women not to breastfeed during treatment with eltrombopag and for at least 21 days after the last dose.
Infant Risk:
Potentially hazardous (L4)
Pediatric Use
Approved for chronic ITP in patients 1 year and older, and for SAA in patients 2 years and older. Dosing is age- and weight-dependent. Safety and efficacy have not been established in younger pediatric populations.
Geriatric Use
No overall differences in safety or effectiveness were observed between elderly (âĨ65 years) and younger patients. However, greater sensitivity of some older individuals cannot be ruled out. Use with caution due to higher incidence of comorbidities and concomitant medications in this population.
Clinical Information
Clinical Pearls
- Strict adherence to administration instructions regarding food and polyvalent cations is crucial for optimal absorption and efficacy. Patients must take eltrombopag at least 2 hours before or 4 hours after any food, drink, or supplement containing polyvalent cations.
- Regular and diligent monitoring of platelet counts and liver function tests is essential to ensure efficacy, prevent excessive platelet counts (which increase thrombotic risk), and detect hepatotoxicity early.
- Patients should be educated on the signs and symptoms of both bleeding and thrombotic events, and instructed to seek immediate medical attention if these occur.
- Upon discontinuation of eltrombopag, platelet counts may drop below baseline levels, increasing the risk of bleeding. Close monitoring of platelet counts is required for at least 4 weeks after stopping treatment.
- Eltrombopag is a specialty medication often requiring prior authorization and patient assistance programs due to its high cost.
Alternative Therapies
- Other Thrombopoietin Receptor Agonists (TPO-RAs): Romiplostim (Nplate), Avatrombopag (Doptelet).
- For ITP: Corticosteroids (e.g., prednisone, dexamethasone), Intravenous Immunoglobulin (IVIG), Anti-D immunoglobulin, Rituximab, Splenectomy, Fostamatinib.
- For Severe Aplastic Anemia (SAA): Immunosuppressive therapy (e.g., anti-thymocyte globulin (ATG) + cyclosporine), Allogeneic hematopoietic stem cell transplantation.
- For HCV-associated Thrombocytopenia: Other antiviral therapies, platelet transfusions (for acute bleeding).
Cost & Coverage
Average Cost:
$10,000 - $20,000+ per 30 tablets (approximate, highly variable)
Insurance Coverage:
Specialty Tier (requires prior authorization, may have high co-pays/coinsurance)
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 provides crucial information about its use. Please read this guide carefully and review it again whenever you receive a refill. If you have any questions or concerns about this medication, don't hesitate to consult 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 taken, the amount consumed, and the time it occurred.
This medication is accompanied by a Medication Guide, which provides crucial information about its use. Please read this guide carefully and review it again whenever you receive a refill. If you have any questions or concerns about this medication, don't hesitate to consult 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 taken, the amount consumed, and the time it occurred.