Eltrombopag (1 brand name, 1 dosage form, 1 route)
Available dosage forms: TABLET.
Routes of administration: ORAL.
Brand Names
- ELTROMBOPAG
Boxed Warning
In patients with chronic hepatitis C, eltrombopag in combination with interferon and ribavirin may increase the risk of hepatic decompensation [see Warnings and Precautions (5.1)]. Eltrombopag tablets may increase the risk of severe and potentially life-threatening hepatotoxicity. Monitor hepatic function and discontinue dosing as recommended [see Warnings and Precautions (5.2)].
Contraindications
None.
Adverse Reactions
The following clinically significant adverse reactions associated with eltrombopag are described in other sections. • Hepatic Decompensation in Patients with Chronic Hepatitis C [see Warnings and Precautions (5.1)] • Hepatotoxicity [see Warnings and Precautions (5.2)] • Increased Risk of Death and Progression of Myelodysplastic Syndromes to Acute Myeloid Leukemia [see Warnings and Precautions (5.3)] • Thrombotic/Thromboembolic Complications [see Warnings and Precautions (5.4)] • Cataracts [see Warnings and Precautions (5.5)]
Mechanism of Action
Eltrombopag is a TPO-receptor agonist that interacts with the transmembrane domain of the human TPO-receptor (also known as cMpl) and initiates signaling cascades that induce proliferation and differentiation of megakaryocytes leading to increased platelet production.
Overdosage
In the event of overdose, platelet counts may increase excessively and result in thrombotic/thromboembolic complications. In one report, a subject who ingested 5000 mg of eltrombopag had a platelet count increase to a maximum of 929 x 10 9/L at 13 days following the ingestion. The patient also experienced rash, bradycardia, ALT/AST elevations, and fatigue. The patient was treated with gastric lavage, oral lactulose, intravenous fluids, omeprazole, atropine, furosemide, calcium, dexamethasone, and plasmapheresis; however, the abnormal platelet count and liver test abnormalities persisted for 3 weeks. After 2 months’ follow-up, all events had resolved without sequelae. In case of an overdose, consider oral administration of a metal cation-containing preparation, such as calcium, aluminum, or magnesium preparations to chelate eltrombopag and thus limit absorption. Closely monitor platelet counts. Reinitiate treatment with eltrombopag in accordance with dosing and administration recommendations [see Dosage and Administration (2.1, 2.2)]. Consider contacting the Poison Help line (1-800-222-1222) or a medical toxicologist for additional overdose management recommendations.