Adult: In patients with inadequate response to corticosteroids and immunoglobulins or splenectomy: Initially, 50 mg once daily, adjust dose to achieve and maintain ≥50 x 109 cells/L platelet count. Max: 75 mg daily. Dose reduction, dosing interruption, or discontinuation may be required according to platelet response (refer to detailed product guideline). Child: 1-5 years Initially, 25 mg once daily; 6-17 years Same as adult dose.
Oral Aplastic anaemia
Adult: In patients with severe cases, unresponsive to immunosuppressive therapy and unsuitable for haematopoietic stem cell transplantation: Initially, 50 mg once daily, adjust dose in increments of 50 mg every 2 weeks to achieve and maintain ≥50 x 109 cells/L platelet count. Max: 150 mg daily. Dose reduction, dosing interruption, or discontinuation may be required according to platelet response (refer to detailed product guideline). In patients with tri-lineage response for at least 8 weeks transfusion independence, dose may be reduced by 50%.
Oral Thrombocytopenia associated with chronic hepatitis C
Adult: Initially, 25 mg once daily, adjust dose in increments of 25 mg every 2 weeks until adequate response is achieved to initiate antiviral therapy. Max: 100 mg daily. Dose reduction, dosing interruption, or discontinuation may be required according to platelet response (refer to detailed product guideline).
Special Patient Group
Patients of Asian ancestry (e.g. Chinese, Japanese, Taiwanese, Korean, Thai):
Idiopathic thrombocytopenic purpura: Initially, 25 mg once daily. In hepatic impairment: Initially, 12.5 mg once daily.
Aplastic anaemia: Initially, 25 mg once daily.
Hepatic Impairment
Oral Idiopathic thrombocytopenic purpura
Initially, 25 mg once daily, adjust dose at 3 weeks interval.
Aplastic anaemia
Initially, 25 mg once daily, adjust dose at 2 weeks interval.
Special Precautions
Patient with risk factors for thromboembolism (e.g. advanced chronic liver disease, Factor V Leiden, ATIII deficiency, antiphospholipid syndrome, prolonged periods of immobilisation, malignancies, surgery/trauma, contraceptives and hormone replacement therapy, advanced age, smoking, obesity). Patients of Asian ancestry (e.g. Chinese, Koreans, Japanese, Taiwanese, Thai). Renal and hepatic impairment. Children. Pregnancy and lactation. Not intended for use to normalise platelet count.
This drug may cause dizziness and lack of alertness, if affected, do not drive or operate machinery.
Monitoring Parameters
Monitor CBC with differential and platelet count weekly at initiation then monthly thereafter; LFT prior to therapy, every 2 weeks during dose adjustment and monthly thereafter. Perform bone marrow examination with aspirations for cytogenetics in patients with aplastic anaemia prior to therapy then after 3 months and every 6 months thereafter. Obtain eye examination at baseline and during therapy. Monitor for signs and symptoms of cataract formation and thromboembolism.
Overdosage
Symptoms: Increased platelet counts resulting in thrombotic/thromboembolic complications; rash, transient bradycardia, elevated ALT and AST, and fatigue may also occur. Management: Administer metal cation-containing preparations (e.g. Ca, Al, Mg) to limit eltrombopag absorption. Monitor platelet counts closely.
Drug Interactions
Increased risk of hepatic decompensation in patients with chronic hepatitis C who are using or taking interferon and ribavirin. May increase the serum concentrations of HMG CoA reductase inhibitors (e.g. rosuvastatin, simvastatin). Decreased serum concentration with concomitant use of ciclosporin or lopinavir/ritonavir. Reduced absorption with polyvalent cations (e.g. Fe, Ca, Mg, Zn).
Food Interaction
Decreased plasma concentration with meals that have high Ca (e.g. dairy products) or moderate to high calorie or fat content.
Lab Interference
May discolour serum and interfere with certain laboratory tests (e.g. total bilirubin, serum creatinine).
Action
Description: Mechanism of Action: Eltrombopag is a non-peptide thrombopoietin (TPO) receptor agonist. It binds to and activates the human TPO receptor and initiates signal transduction pathways which induces proliferation and differentiation from bone marrow progenitor cells thereby increasing platelet production. Onset: Within 1-2 weeks. Duration: 1-2 weeks after the last dose. Pharmacokinetics: Absorption: Absorbed from the gastrointestinal tract. Bioavailability: ≥52% (increased by 22% for oral susp). Time to peak plasma concentrations: 2-6 hours. Distribution: Plasma protein binding: >99%. Metabolism: Extensively metabolised in the liver by CYP1A2, CYP2C8 via oxidation and UGT1A1, UGT1A3 via glucuronidation. Excretion: Via faeces (approx 59%, approx 20% as unchanged drug); urine (approx 31%, as metabolites). Elimination half-life: Approx 21-32 hours.
Chemical Structure
Eltrombopag Source: National Center for Biotechnology Information. PubChem Database. Eltrombopag, CID=135449332, https://pubchem.ncbi.nlm.nih.gov/compound/Eltrombopag (accessed on Jan. 22, 2020)
B02BX05 - eltrombopag ; Belongs to the class of other systemic hemostatics. Used in the treatment of hemorrhage.
References
Annotation of EMA Label for Eltrombopag and F5, SERPINC1. Pharmacogenomics Knowledgebase (PharmGKB). https://www.pharmgkb.org/. Accessed 07/01/2020.Annotation of FDA Label for Eltrombopag and F5, SERPINC1. Pharmacogenomics Knowledgebase (PharmGKB). https://www.pharmgkb.org/. Accessed 07/01/2020.Annotation of HCSC Label for Eltrombopag and F5, SERPINC1. Pharmacogenomics Knowledgebase (PharmGKB). https://www.pharmgkb.org/. Accessed 07/01/2020.Anon. Eltrombopag. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 07/01/2020.Buckingham R (ed). Eltrombopag. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 07/01/2020.Joint Formulary Committee. Eltrombopag. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 07/01/2020.Promacta Tablet, Powder for Oral Suspension (Novartis Pharmaceuticals Corporation). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 07/01/2020.
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