Composition

Elbonix 50 tablet: Each coated tablet contains Eltrombopag Olamine INN, equivalent to Eltrombopag 50 mg.

Therapeutic Classification

Blood Formation Agent

Pharmacological Profile

Mechanism of Action

Eltrombopag is an orally bioavailable TPO-receptor agonist that binds to the transmembrane domain of the TPO-receptor, triggering signaling pathways that promote the growth and maturation of bone marrow progenitor cells.

Pharmacokinetics

Absorption: Eltrombopag’s peak concentration occurs 2-6 hours post-administration. Its oral absorption, inferred from urinary and fecal excretion studies, is estimated to be at least 52% following a single 75-mg dose.
Distribution: Eltrombopag’s concentration in blood cells is roughly 50% to 79% of that in plasma. It binds extensively to human plasma proteins (over 99%) and is a substrate of BCRP but not P-gp or OATP1B1.
Metabolism: Eltrombopag is extensively metabolized, mainly through cleavage, oxidation, and conjugation with Glucuronic acid, Glutathione, or Cysteine. CYP1A2 and CYP2C8 are the primary enzymes for oxidative metabolism, with UGT1A1 and UGT1A3 handling glucuronidation.
Elimination: Feces (59%) and urine (31%) are the main excretion routes, with approximately 20% of the dose excreted unchanged in feces. Eltrombopag’s plasma elimination half-life is about 21 to 32 hours in healthy individuals and 26 to 35 hours in ITP patients.

Dosage and Administration

For Chronic Immune (Idiopathic) Thrombocytopenia (ITP) and other conditions, the starting dose is typically 50 mg once daily, adjusted based on platelet count response and specific patient factors like ethnicity and liver function. Detailed monitoring and dosage adjustments are essential for maintaining platelet counts and managing potential side effects.

Use in Specific Populations

Pregnancy: Category C. Consider the benefits and risks.
Nursing Mothers: Weigh the necessity of Eltrombopag against the potential risk to the infant.Pediatric Use:Efficacy and safety have been established in pediatric patients over 1 year of age for chronic ITP.
Geriatric Use: No significant differences in safety or efficacy observed between older and younger patients, though sensitivity in some older individuals can’t be ruled out.
Hepatic and Renal Impairment:Adjustments are necessary for hepatic impairment; no initial dose adjustment is needed for renal impairment.

Warnings and Precautions:

Monitor liver function and platelet counts due to risks of hepatotoxicity and thrombotic/thromboembolic complications.

Side Effects:

Common adverse effects for Eltrombopag 50 mg may include nausea, diarrhea, respiratory infections, and increased liver enzymes, among others.

Contraindications:

No known contraindications.

Drug Interactions:

Should be taken 2 hours before or 4 hours after any products containing polyvalent cations.

Overdose Management:

In case of overdose, excessive platelet counts and related complications may occur. Treatment involves the use of chelating agents and close monitoring of platelet counts.

Pharmaceutical Information:

Storage:

Store in a cool, dry place, protected from light and moisture. Keep out of children’s reach.

Packaging:

Elbonix 50 tablets are packaged in 28-tablet Alu-Alu blister packs.