ELBONIX 50 TABLET

Indications

• Chronic immune thrombocytopenic purpura (ITP) in adults refractory to other treatments
• Immune thrombocytopenia in pediatric patients who are refractory to other treatments

Dosage

Children: Refer to the BNF for Children for specific dosing information, as pediatric doses may vary based on age and weight.

Adults: Initially 50 mg once daily, adjusted to achieve a platelet count of 50 x 10^9/litre or more. If the platelet count is not adequate after 4 weeks, treatment should be discontinued.

Mechanism of action

Eltrombopag works by binding to the thrombopoietin receptor, which activates intracellular signaling pathways that lead to increased megakaryocyte proliferation and differentiation. This results in enhanced platelet production in the bone marrow.

Pharmacodynamics

By activating the thrombopoietin receptor, eltrombopag increases platelet counts in patients with low platelet counts due to various conditions, particularly immune thrombocytopenia. The efficacy of the drug is monitored by measuring platelet counts, and dosage adjustments are made based on these counts.

Pharmacokinetics

Eltrombopag is well absorbed after oral administration, with peak plasma concentrations occurring within 2 hours. It has a half-life of approximately 5 to 9 hours and is primarily metabolized by the liver via cytochrome P450 enzymes, notably CYP1A2. Eltrombopag is excreted mainly in the feces, with a small percentage eliminated in urine. The presence of food, particularly high-calcium meals, can reduce its absorption.

Contra-indications

• Hypersensitivity to eltrombopag or any of its components
• Severe hepatic impairment

Adverse effects

• Alopecia
• Anaemia
• Appetite decrease
• Asthenia
• Cough
• Depression
• Diarrhoea
• Dry mouth
• Fever
• Gastrointestinal discomfort
• Haemolytic anaemia
• Hepatic disorders
• Hyperbilirubinaemia
• Increased risk of infection
• Malaise
• Menorrhagia
• Muscle complaints
• Nausea
• Oral disorders
• Peripheral oedema
• QT interval prolongation
• Sleep disorders
• Sweat changes
• Vertigo
• Vision disorders
• Vomiting

Interactions

• Eltrombopag and cladribine: Moderate (increases exposure)
• Eltrombopag and statins: Moderate (increases exposure)
• Eltrombopag and alpelisib: Unknown (increases exposure)
• Eltrombopag and berotralstat: Unknown (increases exposure)
• Eltrombopag and larotrectinib: Unknown (increases exposure)
• Eltrombopag and letermovir: Unknown (increases concentration)
• Eltrombopag and methotrexate: Unknown (increases concentration)
• Oral selenium and eltrombopag: Unknown (decreases absorption)
• SSRIs and eltrombopag: Unknown (increases exposure)
• Eltrombopag and talazoparib: Unknown (increases exposure)

Precautions

• Monitor full blood count, platelet count, and liver function regularly during treatment.
• Monitor serum creatinine, urea, and electrolytes (including potassium, magnesium, and calcium) before and during treatment.
• Consider stopping treatment if there is inadequate response after 3 months.
• Caution in patients with mild to moderate hepatic impairment.

Pregnancy

Manufacturer advises avoiding use due to potential toxicity based on animal studies.

Breast-feeding

Present in milk in animal studies; caution

Dosage

Children: Refer to specific product guidelines or clinical protocols for appropriate dosing.

Adults: Refer to specific product guidelines or clinical protocols for appropriate dosing.

Mechanism of action

Olamine is implicated in the phospholipid biosynthesis pathway. It contributes to the formation of phospholipids that are essential for membrane structure and function. By participating in the biosynthesis pathways, olamine aids in the maintenance and repair of cellular membranes, influencing cellular signaling and integrity.

Pharmacodynamics

Olamine influences the lipid composition of cell membranes, which can affect membrane fluidity and the activity of membrane-bound proteins. This modulation can lead to alterations in cell signaling pathways and cellular responses to external stimuli.

Pharmacokinetics

The pharmacokinetics of olamine, including its absorption, distribution, metabolism, and excretion, are not well-documented in the available literature. Further studies are needed to elucidate these parameters and to understand the bioavailability and systemic effects of olamine in humans.

Pregnancy

There is insufficient data on the use of olamine in pregnant women. It is recommended to weigh the potential benefits against the potential risks before prescribing.

Breast-feeding

There is limited information on the excretion of olamine in human milk. Caution should be exercised when administering to nursing mothers.

Storage

Store at room temperature, away from light and moisture. Keep out of reach of children.