Eltrombopag Olamine

Indications

Eltrombopag Olamine is used for: Adult chronic immune (idiopathic) thrombocytopenic purpura (ITP), Hepatitis C Virus (HCV) related Thrombocytopenia.

Adult Dose

Adult Initially 50 mg once daily. East Asian patient 25 mg once daily. Then, adjust dose to maintain platelet count >50,000/microliter. Max: 75 mg daily. After adjustment, platelet counts should be monitored at least weekly for 2-3 weeks. Wait for at least 2 weeks to see the effect of any dose adjustment on the patient’s platelet response prior to considering another dose adjustment. Hepatic Impairment: Should not be used in ITP patients with liver cirrhosis (hepatic impairment unless the expected benefit outweighs the identified risk of portal venous thrombosis.

Child Dose

Renal Dose

Renal Impairment: No dose adjustment is necessary in ITP patients with renal impairment.

Administration

Should be taken on an empty stomach: Take at least 4 hr before or after antacids, dairy products or other Ca-containing food products or mineral supplements containing polyvalent cations.

Contra Indications

Eltrombopag is contraindicated in patients with severe hepatic impairment and who are hypersensitive to any of its excipients.

Precautions

Not established for use in other thrombocytopenic conditions. Regularly monitor clinical haematology, platelet counts & serum liver test throughout therapy. Renal & hepatic impairment; hepatic disease. Thrombotic/thromboembolic complications. Increased risk of bleeding upon discontinuation of treatment. Bone marrow reticulin formation & risk of bone marrow fibrosis. Malignancies & progression of malignancies. Pregnancy & lactation. Childn <18 yr, elderly.

Pregnancy-Lactation

Interactions

Increased plasma Cmax & AUC of HMG-CoA reductase inhibitors. Caution w/ methotrexate, topotecan. Increased conc w/ fluvoxamine; decreased conc w/ rifampicin & lopinavir/ritonavir. Reduced absorption by antacids, dairy products & other products containing polyvalent cations (eg Fe, Ca, Mg, Al, Se, Zn). Reduced plasma AUC & Cmax w/ high-calorie & -fat meal. Monitor platelet counts when used in combination w/ lopinavir/ritonavir & other drugs for treatment of idiopathic thrombocytopenic purpura (ITP).

Adverse Effects

Side effects of Eltrombopag Olamine : Insomnia; headache, paraesthesia; cataract, dry eye; nausea; GI & hepatobiliary disorders; rash, pruritus, alopecia; arthralgia, myalgia, muscle spasm, bone pain; fatigue, peripheral oedema; thromboembolic events.

Mechanism of Action

Small-molecule thrombopoietin (TPO)-receptor agonist that interacts with human TPO receptor transmembrane domain of human TPO-receptor & initiates signaling cascades that induce proliferation & differentiation of megakaryocytes from bone marrow progenitor cells.