Promacta (Eltrombopag Tablets) Drug Overview and Uses for Patients and Caregivers at RxList

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May 27, 2012

Promacta

Thrombocytopenia (Low Platelet Count) »

What is thrombocytopenia?

Thrombocytopenia is a lower than normal number of platelets in the blood.

Platelets are one of the components of the blood along with white and red blood cells. Platelets play an important role in clotting and bleeding. Platelets are made in the bone marrow similar to other cells in the blood such as, white blood cells and red blood cells. Platelets originate from megakaryocytes which are large cells found in the bone marrow. The fragments of these megakaryocytes are platelets that are released into the blood stream. The circulating platelets make up about two third of the platelets that are released from the bone marrow. The other one third is typically stored (sequestered) in the spleen.

Platelets, in general, have a brief 7 to 10 days life in the blood, after which they are removed from the blood circulation. The number of platelets in the blood is referred to as the platelet count and is normally betw...

Read the Thrombocytopenia (Low Platelet Count) article »

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Promacta

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PROMACTA®
(eltrombopag)

WARNING

RISK FOR HEPATOTOXICITY

PROMACTA may cause hepatotoxicity:

Measure serum alanine aminotransferase (ALT), aspartate aminotransferase (AST), and bilirubin prior to initiation of PROMACTA, every 2 weeks during the dose adjustment phase, and monthly following establishment of a stable dose. If bilirubin is elevated, perform fractionation.
Evaluate abnormal serum liver tests with repeat testing within 3 to 5 days. If the abnormalities are confirmed, monitor serum liver tests weekly until the abnormality(ies) resolve, stabilize, or return to baseline levels.
Discontinue PROMACTA if ALT levels increase to ≥ 3X the upper limit of normal (ULN) and are:
- progressive, or
- persistent for ≥ 4 weeks, or
- accompanied by increased direct bilirubin, or
- accompanied by clinical symptoms of liver injury or evidence for hepatic
- decompensation.

DRUG DESCRIPTION

PROMACTA (eltrombopag) Tablets contain eltrombopag olamine, a small molecule thrombopoietin (TPO) receptor agonist for oral administration. Eltrombopag interacts with the transmembrane domain of the TPO receptor (also known as cMpl) leading to increased platelet production. Each tablet contains eltrombopag olamine in the amount equivalent to 12.5 mg, 25 mg, 50 mg, or 75 mg of eltrombopag free acid.

Eltrombopag olamine is a biphenyl hydrazone. The chemical name for eltrombopag olamine is 3'-{(2Z)-2-[1-(3,4-dimethylphenyl)-3-methyl-5-oxo-1,5-dihydro-4H-pyrazol-4 ylidene]hydrazino}-2'-hydroxy-3-biphenylcarboxylic acid - 2-aminoethanol (1:2). It has the molecular formula C₂₅H₂₂N₄O₄•2(C₂H₇NO). The molecular weight is 564.65 for eltrombopag olamine and 442.5 for eltrombopag free acid. Eltrombopag olamine has the following structural formula:

PROMACTA® (eltrombopag) Structural Formula Illustration

Eltrombopag olamine is practically insoluble in aqueous buffer across a pH range of 1 to 7.4, and is sparingly soluble in water.

The inactive ingredients of PROMACTA are: Tablet Core: magnesium stearate, mannitol, microcrystalline cellulose, povidone, and sodium starch glycolate. Coating: hypromellose, polyethylene glycol 400, titanium dioxide, polysorbate 80 (12.5 mg tablet), FD&C Yellow No. 6 aluminum lake (25 mg tablet), FD&C Blue No. 2 aluminum lake (50 mg tablet), or Iron Oxide Red and Iron Oxide Black (75 mg tablet).

Last reviewed on RxList: 12/28/2011
This monograph has been modified to include the generic and brand name in many instances.