Eltrombopag 75mg 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 available
FDA Approved
Nov 2008
DEA Schedule
Not Controlled
Overview
What is this medicine?
Eltrombopag is a medication used to help 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 types of low platelet counts (ITP) or a serious bone marrow condition called aplastic anemia. It works by mimicking a natural substance in your body that tells your bone marrow to produce more platelets.
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 avoid interactions. To minimize interactions, 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. Also, 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 avoid interactions. To minimize interactions, 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. Also, 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 food, dairy products, calcium-fortified juices, or mineral supplements (e.g., iron, calcium, magnesium, aluminum, selenium, zinc). These can significantly reduce how much of the medicine your body absorbs.
- Do not crush, chew, or break tablets. Swallow them whole.
- Regular blood tests (platelet counts and liver function tests) are crucial to monitor your response and check for side effects. Do not miss your appointments.
- Report any signs of liver problems (e.g., unusual tiredness, yellowing of skin/eyes, dark urine, stomach pain) or blood clots (e.g., swelling/pain in leg, sudden shortness of breath, chest pain) to your doctor immediately.
- Avoid grapefruit and grapefruit juice as they may interact with the medication.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
Dosage varies by indication and patient response. For chronic ITP, initial dose is typically 50 mg once daily; for severe aplastic anemia (SAA), initial dose is 50 mg once daily; for HCV-associated thrombocytopenia, initial dose is 25 mg once daily. The 75 mg dose is a common maintenance dose for ITP or SAA.
Dose Range:
12.5 - 150 mg
Condition-Specific Dosing:
Chronic Immune Thrombocytopenia (ITP):
Initial: 50 mg once daily. Adjust to achieve and maintain platelet count âĨ 50,000/mcL. Max: 150 mg once daily.
Severe Aplastic Anemia (SAA):
Initial: 50 mg once daily. Adjust in 50 mg increments every 2 weeks to achieve target platelet count. Max: 150 mg once daily.
HCV-associated Thrombocytopenia:
Initial: 25 mg once daily. Adjust in 25 mg increments every 2 weeks to achieve target platelet count for antiviral therapy. Max: 100 mg once daily.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
For chronic ITP (âĨ1 year old): Initial 25 mg once daily. Adjust to achieve and maintain platelet count âĨ 50,000/mcL. Max: 150 mg once daily.
Adolescent:
For chronic ITP (âĨ1 year old): Initial 25 mg once daily. Adjust to achieve and maintain platelet count âĨ 50,000/mcL. Max: 150 mg once daily. For SAA (âĨ2 years old): Initial 50 mg once daily. Adjust in 50 mg increments every 2 weeks to achieve target platelet count. Max: 150 mg once daily.
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.
Moderate:
Child-Pugh Class B or C: For chronic ITP or SAA, reduce initial dose to 25 mg once daily. For HCV-associated thrombocytopenia, reduce initial dose to 25 mg every other day. Monitor closely.
Severe:
Child-Pugh Class B or C: For chronic ITP or SAA, reduce initial dose to 25 mg once daily. For HCV-associated thrombocytopenia, reduce initial dose to 25 mg every other 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, thereby increasing platelet production.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 52% (oral solution), 31% (tablet)
Tmax:
2-6 hours
FoodEffect:
Absorption is significantly decreased by food, especially high-fat meals and products containing polyvalent cations (e.g., dairy products, mineral supplements, antacids). Must be taken at least 2 hours before or 4 hours after such products.
Distribution:
Vd:
Approximately 34.6 L
ProteinBinding:
>99.9%
CnssPenetration:
Limited
Elimination:
HalfLife:
21-32 hours
Clearance:
Approximately 0.8 L/hr
ExcretionRoute:
Fecal (approximately 59%), Renal (approximately 31%)
Unchanged:
Approximately 20% (feces), <1% (urine)
Pharmacodynamics
OnsetOfAction:
Platelet count increase typically observed within 1-2 weeks.
PeakEffect:
Peak platelet response typically occurs within 2-4 weeks.
DurationOfAction:
Platelet counts generally return to baseline within 1-2 weeks after discontinuation.
Safety & Warnings
Side Effects
Serious Side Effects: Seek Medical Help Immediately
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you experience any of the following symptoms, contact your doctor or seek medical attention right away:
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), such as:
+ 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, such as:
+ Change in eyesight
+ Eye pain
+ Severe eye irritation
Bleeding or bruising while taking or after stopping the medication
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 may not experience any side effects or may only have mild ones. If you experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor or seek medical attention:
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 is not a comprehensive list of all 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.
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you experience any of the following symptoms, contact your doctor or seek medical attention right away:
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), such as:
+ 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, such as:
+ Change in eyesight
+ Eye pain
+ Severe eye irritation
Bleeding or bruising while taking or after stopping the medication
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 may not experience any side effects or may only have mild ones. If you experience any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor or seek medical attention:
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 is not a comprehensive list of all 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:
- Yellowing of skin or eyes (jaundice)
- Unusual tiredness or weakness
- Nausea, vomiting, or stomach pain
- Dark urine
- Swelling, pain, or redness in an arm or leg (signs of blood clot)
- Sudden shortness of breath or chest pain (signs of blood clot in lungs)
- Sudden numbness or weakness, especially on one side of the body (signs of stroke)
- Sudden vision changes or blurred vision (may indicate cataracts or blood clots in the eye)
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 issues.
* 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.
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 issues.
* 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.
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 this risk and any necessary preventive measures.
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. If MDS transforms into AML, it may reduce your life expectancy. 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 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 this risk and any necessary preventive measures.
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. If MDS transforms into AML, it may reduce your life expectancy. 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 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 (thrombocytosis)
- Increased risk of thrombotic/thromboembolic complications
- Potential for liver enzyme elevations
What to Do:
In case of overdose, platelet counts may become excessively high. Closely monitor platelet counts and liver function. Consider supportive care and symptomatic treatment. Eltrombopag is highly protein bound and not expected to be removed by hemodialysis. Call 1-800-222-1222 (Poison Control).
Drug Interactions
Major Interactions
- Polyvalent cation-containing products (e.g., antacids, dairy products, mineral supplements containing calcium, iron, magnesium, aluminum, selenium, zinc): 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 reducing statin dose and monitor for adverse effects.
Moderate Interactions
- Other OATP1B1 substrates (e.g., Methotrexate, Irinotecan, Lopinavir, Ritonavir): Potential for increased exposure of these drugs. Monitor for toxicity.
- UGT1A1 and UGT1A3 substrates (e.g., Irinotecan, Raltegravir): Eltrombopag is a substrate and inhibitor of UGT1A1 and UGT1A3. Potential for altered metabolism of these drugs.
- CYP2C8 substrates (e.g., Repaglinide): Eltrombopag is a weak inhibitor of CYP2C8. Potential for increased 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
Rationale: To establish baseline liver function, as eltrombopag can cause hepatotoxicity.
Timing: Prior to initiation of therapy.
Routine Monitoring
Complete Blood Count (CBC) with differential and platelet count
Frequency: Weekly for the first 4 weeks, then every 2-4 weeks thereafter, or as clinically indicated, until a stable platelet count (âĨ 50,000/mcL for ITP) is achieved. Once stable, monthly.
Target: Platelet count âĨ 50,000/mcL (for ITP) or as per indication.
Action Threshold: If platelet count exceeds 400,000/mcL, reduce dose or hold therapy. If platelet count falls below target, consider dose increase. If platelet count does not respond after 4 weeks at maximum dose, discontinue.
Liver Function Tests (LFTs) including ALT, AST, bilirubin
Frequency: Every 2 weeks during dose adjustment, then monthly after stable dose is achieved. More frequently if abnormalities are detected.
Target: Within normal limits or stable from baseline.
Action Threshold: If ALT/AST increase to âĨ 3x ULN and < 5x ULN, repeat LFTs within 3-5 days. If confirmed, reduce dose or hold therapy. If ALT/AST increase to âĨ 5x ULN, discontinue eltrombopag and monitor LFTs frequently until resolved or stable.
Symptom Monitoring
- Signs of hepatotoxicity (e.g., fatigue, nausea, vomiting, right upper quadrant pain, dark urine, jaundice)
- Signs of thrombosis/thromboembolism (e.g., pain, swelling, warmth, redness in an arm or leg; sudden shortness of breath; chest pain; sudden numbness or weakness on one side of the body; sudden vision changes)
- Signs of bleeding (e.g., easy bruising, petechiae, purpura, nosebleeds, gum bleeding, blood in urine or stool)
- Symptoms of cataracts (e.g., blurred vision, glare, difficulty with night vision)
Special Patient Groups
Pregnancy
Use during pregnancy is generally not recommended unless the potential benefit justifies the potential risk to the fetus. Animal studies have shown adverse developmental effects. A pregnancy registry is available.
Trimester-Specific Risks:
First Trimester:
Potential for embryo-fetal toxicity based on animal data.
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 unknown if eltrombopag is excreted in human milk. Due to the potential for serious adverse reactions in a breastfed infant, breastfeeding is not recommended during treatment and for at least 3 weeks after the last dose.
Infant Risk:
Risk of serious adverse reactions (e.g., thrombocytopenia, hepatotoxicity) in breastfed infant. L3 (Moderately Safe - limited data, possible risk).
Pediatric Use
Approved for chronic ITP in patients 1 year and older, and for SAA in patients 2 years and older. Dosing is weight-based for younger children. Safety and efficacy not established in children younger than 1 year for ITP or 2 years for SAA.
Geriatric Use
No overall differences in safety or efficacy were observed between elderly (âĨ65 years) and younger patients, but greater sensitivity of some older individuals cannot be ruled out. Use with caution due to potentially higher incidence of comorbidities and concomitant medications.
Clinical Information
Clinical Pearls
- Strict adherence to dosing instructions regarding food and polyvalent cations is critical for optimal absorption and efficacy.
- Regular monitoring of platelet counts and liver function tests is paramount due to the risk of thrombotic events and hepatotoxicity.
- Patients with pre-existing liver impairment require a lower starting dose and closer monitoring.
- Discontinuation of eltrombopag can lead to a rebound thrombocytopenia, requiring careful monitoring of platelet counts for at least 4 weeks after stopping.
- Eltrombopag is a TPO receptor agonist, not a chemotherapy agent, and does not directly suppress the immune system.
Alternative Therapies
- Romiplostim (another TPO receptor agonist, injectable)
- Avatrombopag (another TPO receptor agonist, oral)
- Corticosteroids (e.g., Prednisone, Dexamethasone)
- Intravenous Immunoglobulin (IVIG)
- Anti-D immunoglobulin
- Rituximab
- Splenectomy (for ITP)
- Immunosuppressants (e.g., Cyclosporine, ATG for SAA)
Cost & Coverage
Average Cost:
$10,000 - $15,000+ per 30 tablets (approximate for 50mg or 75mg)
Insurance Coverage:
Specialty Tier (requires prior authorization, often subject to step therapy)
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 valuable resource that provides important information about your treatment. Please read this guide carefully and review it again whenever you refill your prescription. If you have any questions or concerns about your medication, don't hesitate to reach out to your doctor, pharmacist, or healthcare provider for clarification.
In the event of a suspected overdose, it's crucial to seek immediate medical attention. Call your local poison control center or visit the emergency room right away. When seeking help, be prepared to provide detailed information about the overdose, including the name of the medication, the amount taken, and the time it occurred.
This medication is accompanied by a Medication Guide, which is a valuable resource that provides important information about your treatment. Please read this guide carefully and review it again whenever you refill your prescription. If you have any questions or concerns about your medication, don't hesitate to reach out to your doctor, pharmacist, or healthcare provider for clarification.
In the event of a suspected overdose, it's crucial to seek immediate medical attention. Call your local poison control center or visit the emergency room right away. When seeking help, be prepared to provide detailed information about the overdose, including the name of the medication, the amount taken, and the time it occurred.