eltrombopag

REMS

Promacta or Alvaiz:

Treatment of the following:
- Persistent or chronic immune thrombocytopenia in patients who have had an inadequate response to corticosteroids, immunoglobulins, or splenectomy (should only be used in patients with an ↑ risk of bleeding);
- Thrombocytopenia in patients with chronic hepatitis C to allow the initiation and maintenance of interferon-based therapy;
- Severe aplastic anemia in patients who have had an inadequate response to immunosuppressive therapy.

Promacta:

First-line treatment of severe aplastic anemia (in combination with standard immunosuppressive therapy).

Contraindicated in:

Lactation: Lactation.

Use Cautiously in:

Myelodysplastic syndromes (may ↑ risk of hematologic malignancy)
Hepatic impairment (↓ initial dose)
Patients of East/Southeast Asian ancestry (may require lower doses)
OB: Use during pregnancy only if potential maternal benefit justifies potential fetal risk
Pedi: Safety and effectiveness not estalished in children <6 yr (Alvaiz) or <1 yr (Promacta)
Geri: Older adults may be more sensitive to drug effects; ↑ dose cautiously and consider age-related ↓ in renal and hepatic function, concurrent disease states and drug therapy.

CV: THROMBOEMBOLISM.

EENT: development/worsening of cataracts.

GI: HEPATOTOXICITY.

Drug-Drug:

↓availability and absorption of iron, calcium, aluminum, magnesium, selenium and zinc by chelation; give eltrombopag 2 hr before or 4 hr after medications containing these and other polyvalent cations.
Ribavirin and interferon may ↑ risk of hepatic decompensation

Drug-Food:

↓availability and absorption of iron, calcium, aluminum, magnesium, selenium, and zinc by chelation; do not administer within 4 hr of foods containing these and other polyvalent cations.

(Generic available)

Powder for oral suspension (Promacta): 12.5 mg/pkt; 25 mg/pkt;
Tablets (Promacta): 12.5 mg; 25 mg; 50 mg; 75 mg;
Tablets (Alvaiz): 9 mg; 18 mg; 36 mg; 54 mg;

Promacta and Alvaiz should NOT be substituted for each other.

Persistent or Chronic Immune Thrombocytopenia

PO (Adults and Children 6 yr): Promacta: 50 mg once daily; may ↑ dose to achieve a platelet count of 50 × 10⁹/L (not to exceed 75 mg/day); Alvaiz: 36 mg once daily; may ↑ dose to achieve a platelet count of 50 × 10⁹/L (not to exceed 54 mg/day). Patients of East/Southeast Asian ancestry: Promacta: 25 mg once daily initially; may ↑ dose to achieve a platelet count of 50 × 10⁹/L (not to exceed 75 mg/day); Alvaiz: 18 mg once daily initially; may ↑ dose to achieve a platelet count of 50 × 10⁹/L (not to exceed 54 mg/day).
PO (Children 1–5 yr): Promacta: 25 mg once daily; may ↑ dose to achieve a platelet count of 50 × 10⁹/L (not to exceed 75 mg/day).

Hepatic Impairment

(Adults): Mild, moderate, or severe hepatic impairment: Promacta: 25 mg once daily initially; may ↑ dose to achieve a platelet count of 50 × 10⁹/L (not to exceed 75 mg/day); Alvaiz: 18 mg once daily initially; may ↑ dose to achieve a platelet count of 50 × 10⁹/L (not to exceed 54 mg/day). Patients of East/Southeast Asian ancestry with mild, moderate, or severe hepatic impairment:Promacta: 12.5 mg once daily initially; may ↑ dose to achieve a platelet count of 50 × 10⁹/L (not to exceed 75 mg/day); Alvaiz: 9 mg once daily initially; may ↑ dose to achieve a platelet count of 50 × 10⁹/L (not to exceed 54 mg/day).

Chronic Hepatitis C-Associated Thrombocytopenia

PO (Adults): Promacta: 25 mg once daily; may ↑ dose by 25 mg every 2 wk to achieve the target platelet count required to initiate antiviral therapy; during antiviral therapy, adjust dose to avoid dose ↓ of peginterferon (not to exceed 100 mg/day); Alvaiz: 18 mg once daily; may ↑ by 18 mg every 2 wk to achieve the target platelet count required to initiate antiviral therapy; during antiviral therapy, adjust dose to avoid dose ↓ of peginterferon (not to exceed 72 mg/day).

First-Line Treatment of Severe Aplastic Anemia

PO (Adults and Children 12 yr): Promacta: 150 mg once daily for 6 mo. Patients of East/Southeast Asian ancestry: Promacta: 75 mg once daily for 6 mo.
PO (Children 6–11 yr): Promacta: 75 mg once daily for 6 mo. Patients of East/Southeast Asian ancestry: Promacta: 37.5 mg once daily for 6 mo.
PO (Children 2–5 yr): Promacta: 2.5 mg/kg once daily for 6 mo. Patients of East/Southeast Asian ancestry: Promacta: 1.25 mg/kg once daily for 6 mo.

Hepatic Impairment

PO (Adults and Children 12 yr): Mild, moderate, or severe hepatic impairment: Promacta: 75 mg once daily for 6 mo.

Hepatic Impairment

PO (Adults and Children 6–11 yr): Mild, moderate, or severe hepatic impairment: Promacta: 37.5 mg once daily for 6 mo.

Hepatic Impairment

PO (Adults and Children 2–5 yr): Mild, moderate, or severe hepatic impairment: Promacta: 1.25 mg/kg once daily for 6 mo.

Refractory Severe Aplastic Anemia

PO (Adults): Promacta: 50 mg once daily; may ↑ by 50 mg every 2 wk to achieve a platelet count of 50 × 10⁹/L (not to exceed 150 mg/day); Alvaiz: 36 mg once daily; may ↑ by 36 mg every 2 wk to achieve a platelet count of 50 × 10⁹/L (not to exceed 108 mg/day). Patients of East/Southeast Asian ancestry: Promacta: 25 mg once daily; may ↑ by 50 mg every 2 wk to achieve a platelet count of 50 × 10⁹/L (not to exceed 150 mg/day); Alvaiz: 18 mg once daily; may ↑ by 36 mg every 2 wk to achieve a platelet count of 50 × 10⁹/L (not to exceed 108 mg/day).

Hepatic Impairment

(Adults): Mild, moderate, or severe hepatic impairment: Promacta: 25 mg once daily; may ↑ by 50 mg every 2 wk to achieve a platelet count of 50 × 10⁹/L (not to exceed 150 mg/day); Alvaiz: 18 mg once daily; may ↑ by 36 mg every 2 wk to achieve a platelet count of 50 × 10⁹/L (not to exceed 108 mg/day).

Increases platelet production by initiating proliferation and differentiation of megakaryocytes from bone marrow progenitor cells.

Therapeutic Effects:

Increased blood counts.

Therapeutic Classification: antithrombocytopenics

Pharmacologic Classification:

Absorption: 52% absorbed following oral administration.

Distribution: Unknown.

Protein Binding: >99%.

Metabolism/Excretion: Extensively metabolized; 59% eliminated in feces, 20% as unchanged drug; 31% excreted in urine as metabolites.

Half-life: 21–35 hr.

(effect on platelet count)

ROUTE	ONSET	PEAK	DURATION
PO	1 wk	2 wk	1 wk

Instruct patient to take eltrombopag as directed. Advise patient to read Medication Guide before starting therapy and with each Rx refill in case of changes. Explain purpose, risks, and benefits of therapy to patient. Risks or long term therapy are unknown.
Instruct patient to avoid taking eltrombopag within 4 hr of foods, mineral supplements, and antacids containing iron, calcium, aluminum, magnesium, zinc, and selenium.
Advise patients to avoid activities and medications that may ↑ risk of bleeding.
Advise patient of need for baseline ocular exam before starting therapy and monitoring for signs and symptoms of cataracts during therapy.
Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications.
Instruct patient to notify health care professional if symptoms of liver problems (yellowing of skin or whites of eyes, unusual darkening of urine, unusual tiredness, pain in right upper stomach, confusion, swelling of abdomen) occur.
May cause fetal harm. Advise females of reproductive potential use effective contraception during and for 7 days after therapy ended and to notify health care professional promptly if pregnancy is planned or suspected and to avoid breastfeeding.
Emphasize the importance of routine lab tests to determine effectiveness and monitor for side effects.

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Indications ⬇

Contraind./Precautions ⬆ ⬇

Adv. Reactions/Side Effects ⬆ ⬇

Interactions ⬆ ⬇

Availability ⬆ ⬇

Route/Dosage ⬆ ⬇

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Classifications ⬆ ⬇

Pharmacokinetics ⬆ ⬇

Canadian Brand Names ⬆ ⬇

Time/Action Profile ⬆ ⬇

Patient/Family Teaching ⬆ ⬇

Pronunciation ⬆