Eltrombopag (Eltrombopag) Instructions, Indications, Usage and Dosage, Side Effects

Eltrombopag ethanolamine is an oral, small molecule thrombopoietin receptor agonist. Eltrombopag interacts with the transmembrane domain of the thrombopoietin receptor (also known as cMpl), resulting in increased platelet production. Eltrombopagis particularly indicated for the treatment of thrombocytopenia in patients with chronic immune (idiopathic) thrombocytopenic purpura (ITP) who have had an inadequate response to corticosteroids, immunoglobulins, or splenectomy.

Eltrombopag should not be used in people who: have a precancerous condition called myelodysplastic syndrome (MDS); people who have low levels of platelets in their blood (caused by certain other medical conditions or diseases); or people who need platelet levels to return to normal. Your doctor will determine if you can take eltrombopag.

Mechanism of Action: Eltrombopag is an orally bioavailable small molecule TPO receptor agonist that interacts with the transmembrane domain of the human TPO receptor. Eltrombopag is a stimulator of STAT and JAK phosphorylation. Unlike recombinant TPO or romiplostim, eltrombopag does not activate the AKT pathway in any way. Of note, all lineages except platelet counts increased when given to patients with aplastic anemia, suggesting that eltrombopag potentiates the effects of TPO in vivo; or that an as-yet-undiscovered mechanism of action is at work.

Dosage: Eltrombopag is available as an oral tablet. Except in patients of East Asian ancestry (e.g., Chinese, Japanese, Korean) or with moderate to severe hepatic impairment, the recommended initial dose of eltrombopag is 25 mg once daily, except in such patients, the recommended initial dose of eltrombopag is 50 mg once daily. Eltrombopag should be adjusted as needed to achieve and maintain a platelet count of 50 x 109/L to reduce the risk of bleeding. The dose of eltrombopag should not exceed 75 mg daily.

SIDE EFFECTS: Get emergency medical help if you have signs of an allergic reaction: hives, difficulty breathing, swelling of face, lips, tongue, or throat.

You may develop blood clots while using eltrombopag. Contact your doctor or get emergency medical help if you have: signs of a stroke - sudden numbness or weakness, severe headache, slurred speech, vision or balance problems; signs of a blood clot in the lungs - chest pain, sudden cough or shortness of breath, dizziness, coughing up blood; signs of a blood clot deep in the body - pain, swelling, or warmth in one leg; or signs of a blood clot in the stomach - severe stomach pain, vomiting, diarrhea.

If you have any other side effects, even if they occur after treatment has ended, contact your doctor immediately.

Easy bruising, unusual bleeding, pinpoint purple or red spots under the skin; blurred or cloudy vision, seeing halos around lights, changes in vision; low red blood cells (anemia)—pale skin, tiredness, dizziness or shortness of breath, cold hands and feet; or liver problems—confusion, tiredness, pain in the right upper quadrant, swelling around the abdomen, dark urine, jaundice (yellowing of the skin or eyes). If you develop certain side effects, your treatment may be stopped permanently.

Common side effects of eltrombopag may include: nausea, diarrhea; fever; cough; headache, tiredness; low red blood cells (anemia); or abnormal bone marrow or liver function tests. This is not a complete list of side effects, and other side effects may occur.

NOTE: Contact your doctor right away if you have signs of liver problems: nausea, upper abdominal pain, confusion, feeling tired, loss of appetite, dark urine, clay-colored stools, or yellowing of the skin or eyes.

Before taking this medication, tell your doctor if you have or have had any of the following conditions: blood pooling; a precancerous condition called myelodysplastic syndrome (MDS) or blood cancer; a bleeding or clotting disorder; cataracts; surgery to remove the spleen; if you are of East Asian or Southeast Asian ancestry; using any medicine to treat hepatitis C; or liver disease.

It is not known whether eltrombopag will harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant. You should still use effective birth control while using eltrombopag and for at least 7 days after your last dose. Do not breastfeed while using eltrombopag.

Storage: Store at room temperature, away from moisture and heat. Store tablets in their original containers.