Revolade

Eltrombopag olamine

Adult & paed patients ≥6 yr w/ primary immune thrombocytopenia (ITP) lasting ≥6 mth from diagnosis & refractory to other treatments. Chronic HCV infection in adults for thrombocytopenia treatment. In combination w/ standard immunosuppressive therapy for 1st-line treatment of adult & adolescents ≥12 yr w/ severe aplastic anemia (SAA). Acquired SAA in adults either refractory to prior immunosuppressive therapy or heavily pretreated & unsuitable for haematopoietic stem cell transplantation.

Individualised dosage based on patient's platelet count. ITP Adult & paed patient 6-17 yr Initially 50 mg once daily, adjust doses to maintain platelet count ≥50,000/microliter. Max: 75 mg daily. HCV-associated thrombocytopenia Adult Initially 25 mg once daily, adjust dose in 25-mg increments every 2 wk. Max: 100 mg daily. 1st-line SAA Adult & adolescent ≥12 yr Initially 150 mg once daily for 6 mth. Refractory SAA Adult Initially 50 mg once daily, adjust dose in 50-mg increments every 2 wk. Max: 150 mg daily. ITP patient w/ hepatic impairment Initially 25 mg once daily w/ 3 wk interval before increasing dose. Chronic HCV & refractory SAA patient w/ hepatic impairment; ITP, chronic HCV, & refractory SAA of East-/Southeast-Asian ancestry Initially 25 mg once daily. 1st-line SAA of East-/Southeast-Asian ancestry or w/ mild, moderate or severe hepatic impairment Initially 75 mg once daily for 6 mth.

Should be taken on an empty stomach: Take at least 2 hr before or 4 hr after antacids, dairy products or other Ca-containing food products or polyvalent cations-containing mineral supplements.

Hypersensitivity.

Discontinue use if ALT ≥3 x ULN, is progressive or persistent ≥4 wk, or accompanied by increased direct bilirubin, clinical symptoms of liver injury or evidence for hepatic decompensation; new or worsening morphological abnormalities or cytopenia develops. Not indicated for thrombocytopenia in patients w/ chronic liver disease undergoing invasive procedures. Increased risk of fatal hepatic decompensation & thromboembolic events in thrombocytopenic HCV patients w/ advanced chronic hepatic disease using α-interferon therapy. Advanced age, patients w/ prolonged periods of immobilisation, malignancies, contraceptives & HRT, surgery/trauma, obesity, smoking, factor V Leiden, ATIII deficiency & antiphospholipid syndrome. Increased risk for development or progression of bone marrow reticulin fibres; cytogenic abnormalities & progression in SAA patients; progression of existing haematological malignancies eg, myelodysplastic syndrome. QTc interval prolongation in patients w/ ITP & thrombocytopenic patients w/ HCV. Monitor serum ALT, AST, bilirubin prior to, every 2 wk then mthly; platelet counts wkly for 4 wk; signs or symptoms of GI bleeding after discontinuation. Examine peripheral blood smear prior to initiation of therapy. Perform FBC w/ WBC count differential mthly; routine monitoring for ocular changes. Serum discolouration & interference w/ total bilirubin & creatinine testing. Combination w/ direct-acting antiviral agents. May affect ability to drive & use machines. Renal impairment. Not to be used in ITP patients w/ hepatic impairment (Child-Pugh score ≥5). Not recommended during pregnancy & in women of childbearing potential not using contraception. Lactation. Not recommended in childn <1 yr w/ ITP; childn & adolescents <18 yr w/ chronic HCV-related thrombocytopenia or SAA. Elderly ≥65 yr w/ ITP; >75 yr w/ HCV & SAA.

ITP, HCV & SAA: Nausea, diarrhoea; cough. ITP & 1st-line SAA: Increased ALT. Paed ITP & SAA: Abdominal pain. HCV & SAA: Headache; fatigue, chills. Paed ITP, HCV & SAA: Pyrexia. ITP: Nasopharyngitis, URTI; back pain. HCV: Anaemia; decreased appetite; pruritus; myalgia, flu-like illness, asthenia. 1st-line SAA: Increased AST & blood bilirubin. SAA: Dizziness; oropharyngeal pain, rhinorrhea; gingival bleeding; increased transaminases; arthralgia, pain in extremity, muscle spasms.

Increased plasma C_max of rosuvastatin & other HMG-CoA reductase inhibitors. Decreased C_max & AUC_0-∞ w/ ciclosporin. Reduced absorption by polyvalent cation-containing antacids. Decreased conc w/ lopinavir/ritonavir, rifampicin. Increased conc w/ fluvoxamine. Reduced plasma AUC_0-∞ & C_max w/ high-Ca, -calorie & -fat meal. Combination w/ drugs for ITP eg, corticosteroids, danazol, azathioprine, IVIg, anti-D Ig. Concomitant use w/ MTX, topotecan; HCV PIs.

Haemostatics

B02BX05 - eltrombopag ; Belongs to the class of other systemic hemostatics. Used in the treatment of hemorrhage.

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