avatrombopag

Action and Spectrum

Actions and Spectrum:

The action of avatrombopag is to stimulate the production of platelets by binding to and activating the TPO receptor on megakaryocytes. It leads to increase of circulating platelets, which can help to prevent or reduce the risk of bleeding in patients with thrombocytopenia.

Drug Interaction

Adverse Reaction

>10%:

Headache (31%)

Pyrexia (8-11%)

Epistaxis (19%)

Fatigue (28%)

Arthralgia (13%)

Upper respiratory tract infection (15%)

Contusion (26%)

Petechiae (11%)

Gingival bleeding (13%)

1-10%:

Nausea (6-7%)

Abdominal pain (6-7%)

Peripheral edema (2-4%)

Fatigue (3-4%)

<1%:

Anemia (0.4%)

Myalgia (0.4%)

Pyrexia (0.4%)

Frequency not defined:

Hyponatremia

Black Box Warning

Contraindication / Caution

Contraindication/Caution:

Contraindications:

• Active severe bleeding or a history of bleeding disorders
• Thrombotic or thromboembolic disorders
• Uncontrolled hypertension
• Known hypersensitivity to avatrombopag or any of its components

Caution:

• Patients with a history of hepatic impairment or hepatic disease, as the drug is primarily eliminated via the liver
• Patients with a history of stroke, as an increased risk of thrombotic events, have been observed in clinical trials
• Patients with a history of cardiovascular disease, as avatrombopag has not been studied in this patient population

Pregnancy / Lactation

Pregnancy consideration:

The drug should not be used in pregnancy as it may cause harm to the fetus.

Breastfeeding warnings:

The excretion of the drug in breast milk is unknown.

Pregnancy category:

Category A: well-controlled and Satisfactory studies do not show risk to the fetus in the first/later trimester.

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.

Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.

Category N: No data is available for the drug under this category.

Pharmacology

Pharmacology

avatrombopag is a small molecule drug that belongs to the class of thrombopoietin (TPO) receptor agonists. It works by binding to and activating the TPO receptor on megakaryocytes, the cells in the bone marrow that produce platelets. This activation stimulates the proliferation and differentiation of megakaryocytes and increases their production and release of platelets into the bloodstream, leading to an increase in the number of circulating platelets.

Pharmacodynamics:

avatrombopag works by binding to and activating the TPO receptor on megakaryocytes, the cells in the bone marrow that produce platelets. This stimulation leads to an increase in the production and release of platelets, which results in increasing the platelets.Bottom of Form

Pharmacokinetics:

Absorption

Peak plasma time is 5-6 hours

Peak plasma concentration is 166 ng/mL

The area under the curve: 4198 ng•hr/mL

Distribution

Protein Bound: >96%

The volume of distribution: 180 L

Metabolism

The drug is basically metabolized by CYP2C9 and CYP3A4

Elimination

Half-life is 19 hours

The renal clearance rate is 6.9 L/hr

The drug is excreted 88% in feces and 6% in urine

Adminstartion

Administration:

avatrombopag is taken orally as a tablet with the food.

In case of chronic liver disease, take the drug for 5 days. Do not miss the dose. If a dose is missed, take the dose as soon as possible. Do not take the two doses at the same time.

Store the medication at room temperature.

Patient Information Leaflet

Patient information leaflet

Generic Name: avatrombopag

Pronounced: a-va-trom-boe-pag

Why do we use avatrombopag?

avatrombopag is used to increase platelet count in patients with thrombocytopenia. avatrombopag is used in a variety of patient populations, including those with chronic liver disease, myelodysplastic syndrome, and others.