ETP 25 mg

Uses of ETP: - Low platelet count due to ITP or HCV infection Adult chronic immune (idiopathic) thrombocytopenic purpura (ITP), Hepatitis C Virus (HCV) related, Thrombocytopenia, Aplastic anemia Eltrombopag is contraindicated in patients with severe hepatic impairment and who are hypersensitive to any of its excipients.

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.

How to use Eltrombopag Olamine: Take this medicine in the dose and duration as advised by your doctor. Swallow it as a whole. Do not chew, crush or break it. Eltrombopag Olamine is to be taken empty stomach. 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. Adult Dose: Adult Chronic ITP: Initial dose 50 mg once daily. Adjust to maintain platelet count greater than or equal to 50×109 /L Chronic hepatitis C associated thrombocytopenia: Initial recommended dose is 50 mg once daily and do not exceed a daily dose of 100 mg. Severe aplastic anemia: Initial recommended dose is 50 mg once daily, adjust to maintain platelet count greater or equal 50×109 /L. Do not exceed 150 mg per day 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: Child 6 years or older Chronic ITP: Initial dose 50 mg once daily. Child 1 to 5 year The initial dose is 25 mg once daily. Adjust to maintain platelet count greater than or equal to 50×109 /L Renal Dose: Renal Impairment: No dose adjustment is necessary in ITP patients with renal impairment.

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).

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

Common - Nausea - Diarrhea - Upper respiratory tract infection - Vomiting - Increased liver enzymes - Muscle pain - Urinary tract infection Most common adverse reactions are nausea diarrhea, upper respiratory tract infection, increased ALT, mayalgia, urinanry tract infection, fatigue, headache, Insomnia; headache, paraesthesia; cataract, dry eye; GI & hepatobiliary disorders; rash, pruritus, alopecia; arthralgia, muscle spasm, bone pain; fatigue, peripheral oedema; thromboembolic events.

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.

Precaution: 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.

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

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.

Pregnancy Available data from published case reports and postmarketing experience with use in pregnant women are insufficient to assess any drug-associated risks for major birth defects, miscarriage, or adverse maternal or fetal outcomes Animal data In animal reproduction and developmental toxicity studies, oral administration of eltrombopag to pregnant rats during organogenesis resulted in embryolethality and reduced fetal weights at maternally toxic doses Effects were observed at doses resulting in exposures that were 6 times the human clinical exposure based on AUC in patients with chronic ITP at 75 mg/day, and 3 times the AUC in patients with chronic hepatitis C at 100 mg/day Contraception Based on animal reproduction studies, fetal harm may occur when administered to a pregnant woman Use effective contraception in sexually-active females of reproductive during treatment and for at least 7 days after stopping treatment Lactation No data available regarding presence of eltrombopag or metabolites in human milk, effects on breastfed child, or on milk production However, drug was detected in pups of lactating rats 10 days postpartum suggesting potential for transfer during lactation; due to potential for serious adverse reactions in a breastfed child from drug, breastfeeding is not recommended during treatment