Drug Information: Eptifibatide
Eptifibatide is a synthetic cyclic heptapeptide used as an antiplatelet agent. It belongs to the class of glycoprotein IIb/IIIa inhibitors, which are crucial in preventing platelet aggregation. Eptifibatide is primarily used in acute coronary syndromes and during percutaneous coronary intervention (PCI) to reduce the risk of thrombotic events. Its relatively short half-life allows for rapid reversibility upon discontinuation, making it a valuable tool in managing acute cardiovascular conditions.
Category
Antiplatelet
Mechanism of Action
Eptifibatide acts as a reversible antagonist of the glycoprotein (GP) IIb/IIIa receptor, a critical integrin found on the surface of platelets. This receptor is the primary mediator of platelet aggregation. Upon activation, platelets undergo conformational changes that expose the GP IIb/IIIa receptors. These receptors then bind to fibrinogen, von Willebrand factor, and other adhesive ligands, forming cross-links between platelets and initiating clot formation. Eptifibatide binds to the GP IIb/IIIa receptor, preventing the binding of these ligands. By blocking this interaction, Eptifibatide effectively inhibits platelet aggregation, thus reducing the risk of thrombus formation in patients undergoing percutaneous coronary intervention (PCI) or experiencing acute coronary syndromes. The drug’s relatively short half-life allows platelet function to recover within a few hours after discontinuation, minimizing the risk of prolonged bleeding.
Clinical Uses
Eptifibatide is primarily used in the management of acute coronary syndromes (ACS), including unstable angina and non-ST-segment elevation myocardial infarction (NSTEMI), as well as in patients undergoing percutaneous coronary intervention (PCI). In ACS, it is used in conjunction with aspirin and heparin to prevent thrombus formation and reduce the risk of myocardial infarction. During PCI, Eptifibatide helps to prevent acute ischemic complications such as abrupt vessel closure and stent thrombosis. Studies have shown that Eptifibatide significantly reduces the incidence of death, myocardial infarction, and urgent target vessel revascularization in these high-risk patients. Its use is often considered when other antiplatelet therapies are insufficient or when a rapid and potent antiplatelet effect is needed.
Dosage
Adult Dosage:
* Acute Coronary Syndrome (ACS) and PCI: Typically administered intravenously as a bolus of 180 mcg/kg, followed immediately by a continuous infusion of 2 mcg/kg/min. A second bolus of 180 mcg/kg is administered 10 minutes after the first bolus. The infusion is usually continued for 18-24 hours following PCI or until hospital discharge, up to a maximum of 72 hours.
Route of Administration: Intravenous (IV)
Pediatric Dosage: The safety and efficacy of Eptifibatide in pediatric patients have not been established. Therefore, it is generally not recommended for use in children.
Indications
* Acute Coronary Syndrome (ACS) – Unstable Angina
* Acute Coronary Syndrome (ACS) – Non-ST-Segment Elevation Myocardial Infarction (NSTEMI)
* Percutaneous Coronary Intervention (PCI), including angioplasty and stenting
Contraindications
* Active major bleeding
* History of bleeding diathesis
* Severe uncontrolled hypertension
* Recent major surgery or trauma (within the past 6 weeks)
* History of stroke within the past 30 days or any history of hemorrhagic stroke
* Intracranial neoplasm, arteriovenous malformation, or aneurysm
* Thrombocytopenia (platelet count < 100,000/mm³)
* Severe renal impairment (creatinine clearance < 30 mL/min) or dialysis dependence
* Hypersensitivity to Eptifibatide or any of its components
* Concurrent or planned administration of another GP IIb/IIIa inhibitor
FAQ
Q: What is Eptifibatide used for?
A: Eptifibatide is used to prevent blood clots in patients with acute coronary syndromes (like unstable angina and NSTEMI) and during percutaneous coronary intervention (PCI).
Q: How is Eptifibatide administered?
A: It is administered intravenously, usually as a bolus followed by a continuous infusion.
Q: What are the common side effects of Eptifibatide?
A: The most common side effect is bleeding. Other potential side effects include thrombocytopenia (low platelet count) and hypersensitivity reactions.
Q: How long does Eptifibatide stay in your system?
A: Eptifibatide has a short half-life, and its effects on platelet function usually resolve within a few hours after stopping the infusion.
Q: Can Eptifibatide be used in patients with kidney problems?
A: It should be used with caution in patients with moderate renal impairment, and it is contraindicated in patients with severe renal impairment. Dosage adjustments may be necessary.
Q: What other medications should be avoided while taking Eptifibatide?
A: Other medications that increase the risk of bleeding, such as NSAIDs, warfarin, and other antiplatelet agents, should be used with caution. Concomitant use of another GP IIb/IIIa inhibitor is contraindicated.
Q: What should I do if I experience bleeding while taking Eptifibatide?
A: Report any signs of bleeding to your healthcare provider immediately.
Q: Is Eptifibatide safe for pregnant or breastfeeding women?
A: Eptifibatide should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Caution should be exercised when administering Eptifibatide to a nursing woman.
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