Eltrombopag Olamine is indicated in Chronic Immune (Idiopathic) Thrombocytopenia, Chronic Hepatitis C-associated Thrombocytopenia, Severe Aplastic Anemia.

Haemostatic drugs

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. It should be noted that when given to patients with aplastic anemia, other lineages besides platelet count were increased, suggesting that either eltrombopag enhanced the effect of TPO in vivo; or there is a yet uncovered mechanism of action at work.

Chronic Immune (Idiopathic) Thrombocytopenia- Adult and Pediatric Patients 6 Years and Older with ITP: Initiate Eltrombopag at a dose of 50 mg once daily, except in patients who are of East Asian ancestry (such as Chinese, Japanese, Taiwanese or Korean) or who have mild to severe hepatic impairment (Child-Pugh Class A,B,C). For patients of East Asian ancestry with ITP, initiate Eltrombopag at a reduced dose of 25 mg once daily. For patients with ITP and mild, moderate or severe hepatic impairment (Child-Pugh Class A,B,C), initiate Eltrombopag at a reduced dose of 25 mg once daily. For patients of East Asian ancestry with ITP and hepatic impairment (Child-Pugh Class A,B,C), consider initiating Eltrombopag at a reduced dose of 12.5 mg once daily. Pediatric Patients with ITP Aged 1 to 5 Years: Initiate Eltrombopag at a dose of 25 mg once daily. Chronic Hepatitis C-associated Thrombocytopenia- Initiate Eltrombopag at a dose of 25 mg once daily. Monitoring and Dose Adjustment: Adjust the dose of Eltrombopag in 25-mg increments every 2 weeks as necessary to achieve the target platelet count required to initiate antiviral therapy. Monitor platelet counts every week prior to starting antiviral therapy. During antiviral therapy, adjust the dose of Eltrombopag to avoid dose reductions of Peginterferon. Monitor CBCs with differentials, including platelet counts, weekly during antiviral therapy until a stable platelet count is achieved. Monitor platelet counts monthly thereafter. Do not exceed a dose of 100 mg daily. Monitor clinical hematology and liver tests regularly throughout therapy with Eltrombopag. Severe Aplastic Anemia- Initiate Eltrombopag at a dose of 50 mg once daily. For patients with severe aplastic anemia of East Asian ancestry or those with mild, moderate or severe hepatic impairment (Child-Pugh Class A,B,C), initiate Eltrombopag at a reduced dose of 25 mg once daily.

Take Eltrombopag at least 2 hours before or 4 hours after any medications or products containing polyvalent cations such as antacids, calcium-rich foods and mineral supplements.

There are no contraindications for Eltrombopag

The most common side effects of Eltrombopag in adults when used to treat chronic ITP are: In adult patients with ITP, the most common adverse reactions (greater than or equal to 5% and greater than placebo) were: nausea, diarrhea, upper respiratory tract infection, vomiting, increased ALT, myalgia and urinary tract infection. In pediatric patients age 1 year and older with ITP, the most common adverse reactions (greater than or equal to 10% and greater than placebo) were upper respiratory tract infection and nasopharyngitis.In patients with chronic hepatitis C-associated thrombocytopenia, the most common adverse reactions (greater than or equal to 10% and greater than placebo) were: anemia, pyrexia, fatigue, headache, nausea, diarrhea, decreased appetite, influenza-like illness, asthenia, insomnia, cough, pruritus, chills, myalgia, alopecia and peripheral edema. In patients with severe aplastic anemia, the most common adverse reactions (greater than or equal to 20%) were: nausea, fatigue, cough, diarrhea and headache.

Pregnancy Category C. There are no adequate and well controlled studies of Eltrombopag usein pregnancy. In animal reproduction and developmental toxicity studies, there was evidence ofembryolethality and reduced fetal weights at maternally toxic doses. Eltrombopag should beused in pregnancy only if the potential benefit to the mother justifies the potential risk to thefetus.Nursing Mothers: It is not known whether Eltrombopag is excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants from Eltrombopag, a decision should be made whether to discontinue nursing or to discontinue Eltrombopag taking into account the importance of Eltrombopag to the mother.

Hepatotoxicity: Monitor liver function before and during therapy. Thrombotic or Thromboembolic Complications: Portal vein thrombosis has been reported in patients with chronic liver disease receiving Eltrombopag. Monitor platelet counts regularly.

In the event of overdose, platelet counts may increase excessively and result in thrombotic/thromboembolic complications.In one report, a subject who ingested 5,000 mg of Eltrombopag had a platelet count increase to a maximum of 929 x 109/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, andPlasmapheresis; 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.

Store in a cool and dry place, away from light and moisture. Keep out of the reach of children.

Haemostatic drugs

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. It should be noted that when given to patients with aplastic anemia, other lineages besides platelet count were increased, suggesting that either eltrombopag enhanced the effect of TPO in vivo; or there is a yet uncovered mechanism of action at work.

Pregnancy Category C. There are no adequate and well controlled studies of Eltrombopag usein pregnancy. In animal reproduction and developmental toxicity studies, there was evidence ofembryolethality and reduced fetal weights at maternally toxic doses. Eltrombopag should beused in pregnancy only if the potential benefit to the mother justifies the potential risk to thefetus.Nursing Mothers: It is not known whether Eltrombopag is excreted in human milk. Because many drugs are excreted in human milk and because of the potential for serious adverse reactions in nursing infants from Eltrombopag, a decision should be made whether to discontinue nursing or to discontinue Eltrombopag taking into account the importance of Eltrombopag to the mother.