Formulary
Eltrombopag: Indications, Dosing, Side Effects and Interactions
Eltrombopag is a thrombopoietin receptor agonist that binds to and activates the thrombopoietin (TPO) receptor, thereby increasing platelet production.
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Eltrombopag: Indications, Dosing, Side Effects and Interactions
Eltrombopag is a thrombopoietin receptor agonist that binds to and activates the thrombopoietin (TPO) receptor, thereby increasing platelet production.
Drug action
Eltrombopag is a thrombopoietin receptor agonist that binds to and activates the thrombopoietin (TPO) receptor, thereby increasing platelet production.
Indications and dose
**Chronic immune (idiopathic) thrombocytopenic purpura in patients of East or Southeast Asian origin refractory to other treatments (such as corticosteroids or immunoglobulins) (under expert supervision)**
- **Adult** (By Mouth): Initially 25 mg once daily, dose to be adjusted to achieve a platelet count of 50x10 9 /litre or more-consult product literature for dose adjustments, dose can be increased if necessary up to maximum 75 mg per day, discontinue if inadequate response after 4 weeks treatment at maximum dose.
**Chronic immune (idiopathic) thrombocytopenic purpura in patients refractory to other treatments (such as corticosteroids or immunoglobulins) (under expert supervision)**
- **Adult** (By Mouth): Initially 50 mg once daily, dose to be adjusted to achieve a platelet count of 50x10 9 /litre or more-consult product literature for dose adjustments, dose can be increased if necessary up to maximum 75 mg per day, discontinue if inadequate response after 4 weeks treatment at maximum dose.
**Treatment of thrombocytopenia associated with chronic hepatitis C infection, where the degree of thrombocytopenia is the main factor preventing the initiation or limiting the ability to maintain optimal interferon-based therapy (under expert supervision)**
- **Adult** (By Mouth): Initially 25 mg once daily, dose to be adjusted to achieve a platelet count sufficient to initiate antiviral therapy then a platelet count of 50-75x10 9 /litre during antiviral therapy-consult product literature for dose adjustments, dose can be increased if necessary up to maximum 100 mg per day, discontinue if inadequate response after 2 weeks treatment at maximum dose.
**Acquired severe aplastic anaemia in patients of East or Southeast Asian origin either refractory to or heavily pretreated with prior immunosuppressive therapy and are unsuitable**
- **Adult** (By Mouth): for haematopoietic stem cell transplantation (under expert supervision) Initially 25 mg once daily, dose to be adjusted to achieve a platelet count of 50x10 9 /litre or more-consult product literature for dose adjustments, dose can be increased if necessary up to maximum 150 mg per day, discontinue if no haematological response after 16 weeks treatment.
**Acquired severe aplastic anaemia in patients either refractory to or heavily pretreated with prior immunosuppressive therapy and are unsuitable**
- **Adult** (By Mouth): for haematopoietic stem cell transplantation (under expert supervision) Initially 50 mg once daily, dose to be adjusted to achieve a platelet count of 50x10 9 /litre or more-consult product literature for dose adjustments, dose can be increased if necessary up to maximum 150 mg per day, discontinue if no haematological response after 16 weeks treatment.
**Chronic immune (idiopathic) thrombocytopenic purpura in patients of East or Southeast Asian origin refractory to other treatments (such as corticosteroids or immunoglobulins) (under expert supervision) for eltrombopag**
- **Child 1-17 years** (By mouth): Initially 25 mg once daily, dose to be adjusted to achieve a platelet count of 50x109/litre or more-consult product literature for dose adjustments, dose can be increased if necessary up to maximum 75 mg per day, discontinue if inadequate response after 4 weeks treatment at maximum dose.
**Chronic immune (idiopathic) thrombocytopenic purpura in patients refractory to other treatments (such as corticosteroids or immunoglobulins) (under expert supervision) for eltrombopag**
- **Child 1-5 years** (By mouth): Initially 25 mg once daily, dose to be adjusted to achieve a platelet count of 50x109/litre or more-consult product literature for dose adjustments, dose can be increased if necessary up to maximum 75 mg per day, discontinue if inadequate response after 4 weeks treatment at maximum dose.
- **Child 6-17 years** (By mouth): Initially 50 mg once daily, dose to be adjusted to achieve a platelet count of 50x109/litre or more-consult product literature for dose adjustments, dose can be increased if necessary up to maximum 75 mg per day, discontinue if inadequate response after 4 weeks treatment at maximum dose.
Cautions
Patients of East or Southeast Asian origin; risk factors for thromboembolism
Side effects
Common or very common Abnormal loss of weight; alopecia; anaemia; anxiety; appetite abnormal; arthralgia; asthenia; cataract; chest discomfort; chills; concentration impaired; constipation; cough; depression; diarrhoea; dizziness; drowsiness; dry eye; dry mouth; dysphagia; dyspnoea; ear pain; electrolyte imbalance; embolism and thrombosis; eosinophilia; eye disorders; eye pain; fever; gastrointestinal discomfort; gastrointestinal disorders; haemorrhage; headaches; hepatic disorders; hyperbilirubinaemia; hyperglycaemia; hypoglycaemia; increased leucocytes; increased risk of infection; influenza like illness; iron overload; lymphopenia; malaise; memory impairment; menorrhagia; mood altered; muscle complaints; nasal complaints; nausea; neutropenia; oedema; oral disorders; oropharyngeal complaints; pain; palpitations; renal impairment; renal thrombotic microangiopathy; sensation abnormal; skin reactions; sleep disorder; splenic infarction; sweat changes; syncope; taste altered; urine abnormalities; urine discolouration; vasodilation; vertigo; vision disorders; vomiting; weight decreased Uncommon Anisocytosis; arrhythmias; balance impaired; cardiovascular disorder; confusion; cyanosis; eye inflammation; feeling hot; feeling jittery; food poisoning; gout; haemolytic anaemia; hemiparesis; lens opacity; muscle weakness; myocardial infarction; nephritis lupus; nerve disorders; QT interval prolongation; rectosigmoid cancer; retinal pigment epitheliopathy; sinus disorder; sleep apnoea; speech disorder; sunburn; tremor; urinary disorders; wound inflammation Frequency not known Cerebral infarction; sepsis
Interactions
**Severe interactions:**
- No clinically significant interactions are expected when eltrombopag and CYP450 substrates are co-administered (see section 5.2).
- Eltrombopag should be taken at least two hours before or four hours after any products such as antacids, dairy products or mineral supplements containing polyvalent cations to avoid significant...
- Medicinal products that inhibit or induce a single enzyme are unlikely to significantly affect plasma eltrombopag concentrations, whereas medicinal products that inhibit or induce multiple enzymes...
- HCV protease inhibitors Results of a drug-drug pharmacokinetic (PK) interaction study show that co-administration of repeat doses of boceprevir 800 mg every 8 hours or telaprevir 750 mg every 8...
- Food interaction The administration of eltrombopag tablet or powder for oral suspension formulations with a high- calcium meal (e.g.
- In contrast, the administration of eltrombopag 2 hours before or 4 hours after a high- calcium meal or with low-calcium food [< 50 mg calcium] did not alter plasma eltrombopag exposure to a...
- Food low in calcium (< 50 mg calcium), including fruit, lean ham, beef and unfortified (no added calcium, magnesium or iron) fruit juice, unfortified soya milk and unfortified grain, did not...
**Other interactions (27):**
- Effects of eltrombopag on other medicinal products HMG CoA reductase inhibitors Administration of eltrombopag 75 mg once daily for 5 days with a single 10 mg dose of the OATP1B1 and BCRP substrate...
- Interactions are also expected with other HMG-CoA reductase inhibitors, including atorvastatin, fluvastatin, lovastatin, pravastatin and simvastatin.
- When co-administered with eltrombopag, a reduced dose of statins should be considered and careful monitoring for statin adverse reactions should be undertaken (see section 5.2).
- OATP1B1 and BCRP substrates Concomitant administration of eltrombopag and OATP1B1 (e.g.
- Cytochrome P450 substrates In studies utilising human liver microsomes, eltrombopag (up to 100 M) showed no in vitro inhibition of the CYP450 enzymes 1A2, 2A6, 2C19, 2D6, 2E1, 3A4/5, and 4A9/11 and...
- Administration of eltrombopag 75 mg once daily for 7 days to 24 healthy male subjects did not inhibit or induce the metabolism of probe substrates for 1A2 (caffeine), 2C19 (omeprazole), 2C9...
Pregnancy
Avoid-toxicity in animal studies.
Breast feeding
Manufacturer advises avoid.
Hepatic impairment
When used for Idiopathic thrombocytopenic purpura: Manufacturer advises consider avoiding. When used for Severe aplastic anaemia: Manufacturer advises caution. When used for Thrombocytopenia associated with chronic hepatitis C infection: Manufacturer advises caution (increased risk of hepatic decompensation and thromboembolic events). Dose adjustments When used for Idiopathic thrombocytopenic purpura: Manufacturer advises initial dose reduction to 25 mg once daily and wait at least 3 weeks before upwards titration of dose. When used for Severe aplastic anaemia: Manufacturer advises initial dose reduction to 25 mg once daily and wait at least 2 weeks before upwards titration of dose. When used for Thrombocytopenia associated with chronic hepatitis C infection: Manufacturer advises initial dose reduction to 25 mg once daily in moderate to severe impairment and wait at least 2 weeks before upwards titration of dose.
Renal impairment
Use with caution. M
Medicinal forms
Tablet,Suspension
Clinical governance
**Author:** MedNext Clinical Team. **Clinical reviewer:** Dr Shameer Deen, MBBS, MS, MRCS. **Sources:** BNF, Indian Pharmacopoeia, CIMS India. **Correction:** Report errors at support@mednext.academy.
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