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Eltrombopag is an oral small-molecule thrombopoietin (TPO) receptor agonist. It stimulates the proliferation and differentiation of megakaryocytes in the bone marrow by specifically binding to and activating the TPO receptor (c-Mpl), thereby promoting platelet production.
1. Common name: Eltrombopag (Eltrombopag)
2. Trade name: PROMACTA® (Riverland)
3. English name: b>Eltrombopag Tablets
For the treatment of thrombocytopenia in patients with chronic immune (idiopathic) thrombocytopenic purpura (ITP) who have an inadequate response to corticosteroids, immunoglobulins, or splenectomy. It should only be used in ITP patients with a degree of thrombocytopenia and clinical conditions that increase the risk of bleeding and should not be used to attempt to normalize platelet counts.
25mg tablets, 50mg tablets
1. Active ingredient:Eltrombopag ethanolamine salt (equivalent to 25mg or 50mg eltrombopag free acid).
2. Excipients include: Magnesium stearate, mannitol, microcrystalline cellulose, etc. (tablet core), and hypromellose, polyethylene glycol 400, etc. (coating).
1. Standard dose of :
Most patients: 50mg once a day.
Eastern Asians or patients with moderate to severe liver damage: 25 mg once daily.
2. How to take : Take it on an empty stomach (1 hour before a meal or 2 hours after a meal). Avoid taking it with drugs or food containing multivalent cations (such as iron, calcium, aluminum) (an interval of 4 hours is required).
3. Treatment of missed doses : If it is ≥ 12 hours before the next dose, you can take it again, otherwise skip it. No need to take additional doses after vomiting.
1. Platelet count <50×10⁹/L : Increase the daily dose by 25 mg (maximum 75 mg/day).
2. Platelet count >400×10⁹/L : Stop the drug immediately, and then reduce the dose by 25mg and restart after the count is <150×10⁹/L.
3. Hepatotoxicity : Permanently discontinue the drug when ALT ≥ 3 times the normal value and is progressive, lasting ≥ 4 weeks, directly elevated bilirubin or symptoms of liver damage.
1. Monitoring requirements :
Detect ALT/AST/bilirubin every 2 weeks before treatment and during the dose adjustment period, and once a month after stabilization.
Monitor platelet count weekly until stable and continue monitoring for 4 weeks after discontinuation of medication.
2. Dietary taboos : Avoid grapefruit juice and foods/supplements containing polyvalent cations.
3. Special risks : It may aggravate thrombocytopenia after discontinuation of treatment and increase the risk of thrombosis or myelofibrosis.
1. Pregnant women : Contraindicated, may cause fetal malformation (pregnancy category C).
2. During lactation : Discontinue medication or stop breastfeeding.
3. Children and the elderly : The safety has not been established (children); the elderly need to adjust the dose carefully.
4. Liver injury : The starting dose is halved for moderate to severe patients].
1. Common (>1%): Nausea (6%), vomiting (4%), menorrhagia (4%), myalgia (3%), paresthesias (3%), cataracts (3%), elevated ALT/AST (2%), etc.
2. Serious reactions include: Hepatotoxicity, thrombosis and myelofibrosis [6.1].
There are no clear contraindications.
1. OATP1B1 substrate (such as rosuvastatin):Eltrombopag can increase its exposure, so the dosage needs to be reduced by 50%.
2. Multivalent cation (such as antacids, dairy products): Significantly reduces absorption and requires an interval of 4 hours.
Stored at room temperature 25-30℃, the original bottle should be sealed and moisture-proof.