Avatrombopag, also known as Doptelet, is a thrombopoietin receptor agonist (TPO-RA) that is mainly used to treat thrombocytopenia in patients with chronic immune thrombocytopenia (ITP) who have not responded well to prior treatments and in patients with chronic liver disease (CLD) undergoing medical procedures. By increasing platelet production, this drug lowers the chance of bleeding problems in those who take it.

Pharmacological Classification

• Generic Name: Avatrombopag
• Brand Name: Doptelet
• INN (International Nonproprietary Name): Avatrombopag
• Drug Class: Thrombopoietin Receptor Agonist (TPO-RA)
• Formulation: Oral Tablets
• Strength: 20 mg

Mechanism of Action

By activating the thrombopoietin (TPO) receptor on bone marrow megakaryocytes, the small-molecule thrombopoietin receptor agonist avatrombopag promotes platelet formation. In contrast to recombinant TPOs, Avatrombopag increases platelet synthesis by binding to and activating the transmembrane region of the TPO receptor (c-Mpl). Avatrombopag is a safer option for long-term treatment because it does not cause neutralizing antibodies or compete with natural thrombopoietin.

Indications and Uses

1. Thrombocytopenia in Chronic Liver Disease (CLD)

Avatrombopag with chronic liver disease who need medical or surgical treatments and have low platelet counts should take Avatrombopag. In order to reduce the danger of bleeding issues, the medication raises platelet levels prior to treatments.

2. Chronic Immune Thrombocytopenia (ITP)

Adult patients with chronic immunological thrombocytopenia who have not responded well to corticosteroids, immunoglobulins, or splenectomy can take avatrombopag. It offers a non-immunosuppressive method for preserving sufficient platelet levels.

Dosage and Administration

For Chronic Immune Thrombocytopenia (ITP):

• Initial Dose: 20 mg once daily
• Dose Adjustment: Based on platelet response, up to a maximum of 40 mg daily

Tablets should be taken with food to enhance absorption.

Pharmacokinetics

• Absorption: Well absorbed orally, with peak plasma concentrations achieved in 6-8 hours.
• Bioavailability: Increased with food.
• Metabolism: Primarily metabolized by the CYP2C9 and CYP3A4 enzymes in the liver.
• Elimination: Excreted mainly through feces (88%) and urine (6%).
• Half-life: Approximately 19 hours.

Side Effects and Adverse Reactions

While generally well tolerated, Avatrombopag can cause mild to moderate side effects, including:

• Common Side Effects:
  • Headache
  • Fatigue
  • Nausea
  • Diarrhea
  • Abdominal pain
• Serious Side Effects:
  • Thromboembolic Events (e.g., deep vein thrombosis, pulmonary embolism)
  • Hepatic Dysfunction
  • Allergic Reactions (rash, itching, swelling)

Patients with a history of thrombosis should be closely monitored, as Avatrombopag may increase the risk of clotting complications.

Contraindications and Warnings

Contraindications:

• Known hypersensitivity to Avatrombopag or any excipient in the formulation.

Warnings and Precautions:

Thrombosis Risk: Patients with underlying prothrombotic disorders are particularly at risk for clotting complications due to elevated platelet levels. Hepatic Impairment: Individuals who suffer from severe liver disease need to be closely watched. Drug Interactions: Since CYP enzymes are responsible for the metabolism of avatrombopag, interactions with potent CYP3A4/CYP2C9 inducers or inhibitors (such as rifampin or ketoconazole) should be taken into account.

Drug Interactions

• Strong CYP3A4/CYP2C9 Inhibitors (e.g., Fluconazole, Clarithromycin): May increase Avatrombopag levels, leading to excessive platelet production.
• CYP3A4/CYP2C9 Inducers (e.g., Rifampin, Carbamazepine): May decrease Avatrombopag levels, reducing efficacy.
• Anticoagulants & Antiplatelet Drugs: Use with caution as Avatrombopag alters platelet function and may affect bleeding/clotting risks.

Advantages of Avatrombopag (Doptelet)

• Oral administration (unlike injectable thrombopoietin receptor agonists such as romiplostim).
• No immunogenicity issues (does not cause neutralizing antibodies).
• Flexible dosing regimen for chronic ITP and pre-procedural platelet elevation.
• Food enhances absorption rather than interfering with it.

Conclusion

Patients with immunological thrombocytopenia and chronic liver illness can safely enhance their platelet production with Avatrombopag (Doptelet), a very efficient thrombopoietin receptor agonist. Because of its oral formulation, consistent pharmacokinetics, and lack of immunogenicity, it is a better option than conventional TPO-RAs. However, to prevent excessive thrombosis risks, doctors should routinely check platelet counts.

Order Now At Mdx Pharma bd….

To order from MDX Pharma BD, visit their website at https://mdxpharmabd.com, where you can browse products and place orders online. For inquiries or orders via email, contact emedicarepharma@gmail.com. Alternatively, call (+88) 01929123476. Their address is 29, Abdullahpur, Uttara, Dhaka-1230, Bangladesh.

Q. What is the avatrombopag maleate drug class?
Thrombopoietin (TPO) receptor agonists are the class of drugs that includes avatrombopag. It functions by increasing platelet production in the body.

Q. Is ITP a long-term illness?
ITP can occur abruptly and resolve in roughly six months (acute). Or it could be chronic, meaning it lasts for years.