Usage
- Abciximab is prescribed as an adjunct to percutaneous coronary intervention (PCI) for the prevention of cardiac ischemic complications in patients undergoing PCI. It is also used for unstable angina not responding to conventional medical therapy when PCI is planned within 24 hours.
- Pharmacological Classification: Glycoprotein IIb/IIIa receptor inhibitor, Antiplatelet agent.
- Mechanism of Action: Abciximab binds to the glycoprotein (GP) IIb/IIIa receptor on the surface of platelets, preventing the binding of fibrinogen, von Willebrand factor, and other adhesive molecules. This inhibition of the GP IIb/IIIa receptor blocks the final common pathway of platelet aggregation, thereby reducing the risk of thrombus formation.
Alternate Names
- International Nonproprietary Name (INN): Abciximab
- Brand Name: ReoPro
How It Works
- Pharmacodynamics: Abciximab produces dose-dependent inhibition of platelet function. A single intravenous bolus dose of 0.25-0.30 mg/kg results in approximately 80% blockade of platelet GP IIb/IIIa receptors and nearly complete inhibition of platelet aggregation within two hours. Platelet function generally recovers within 48 hours, although abciximab can remain in circulation bound to platelets for up to 15 days.
- Pharmacokinetics: Administered intravenously. After a 0.25 mg/kg bolus and a continuous infusion of 10 µg/min, relatively constant free plasma concentrations are achieved. Free plasma abciximab concentrations fall rapidly for approximately six hours after the infusion is stopped and then decline more slowly.
- Mode of Action: Abciximab is a glycoprotein IIb/IIIa receptor antagonist. It binds to the receptor on activated platelets, preventing fibrinogen and von Willebrand factor from binding, thus inhibiting platelet aggregation. It also binds to the vitronectin receptor and the Mac-1 receptor.
- Receptor Binding: Glycoprotein IIb/IIIa receptor, vitronectin (αvβ3) receptor, Mac-1 receptor.
- Elimination Pathways: Primarily renal excretion.
Dosage
Standard Dosage
Adults:
- PCI: 0.25 mg/kg intravenous bolus 10-60 minutes before PCI, followed by a continuous intravenous infusion of 0.125 µg/kg/min (maximum 10 µg/min) for 12 hours.
- Unstable Angina (with planned PCI within 24 hours): 0.25 mg/kg IV bolus followed by a continuous infusion of 10 µg/min for 18-24 hours, concluding one hour after PCI.
Children:
- Use and dose must be determined by a doctor. Safety and efficacy have not been established in pediatric patients.
Special Cases:
- Elderly Patients: No specific dose adjustments are typically required, but careful monitoring for bleeding is essential.
- Patients with Renal Impairment: Severe renal impairment requiring hemodialysis is a contraindication. Dose adjustments may be needed in other cases of renal impairment, though specific recommendations are not consistently provided.
- Patients with Hepatic Dysfunction: Severe hepatic impairment is a contraindication. Dose adjustments may be needed in other cases of hepatic dysfunction, though specific recommendations are not consistently provided.
- Patients with Comorbid Conditions: Close monitoring for bleeding is particularly important in patients with comorbidities that increase bleeding risk.
Clinical Use Cases
- Abciximab’s clinical use is primarily focused on PCI and unstable angina when PCI is imminent. It is not indicated for routine use in intubation, surgical procedures, mechanical ventilation, general ICU use, or specific emergency situations like cardiac arrest.
Dosage Adjustments
- Dose adjustments may be necessary in patients with renal or hepatic impairment, though specific recommendations are not consistently provided. Close monitoring of these patients is essential.
Side Effects
Common Side Effects
- Bleeding (including at the injection site)
- Nausea
- Vomiting
- Back pain
- Headache
- Dizziness
- Hypotension
Rare but Serious Side Effects
- Severe or uncontrolled bleeding
- Thrombocytopenia
- Allergic reactions (including anaphylaxis)
Long-Term Effects
Limited data are available on long-term effects, but potential complications could include chronic anemia related to bleeding.
Adverse Drug Reactions (ADR)
- Major bleeding
- Severe thrombocytopenia
- Anaphylaxis
Contraindications
- Active internal bleeding
- Recent (within six weeks) significant gastrointestinal or genitourinary bleeding
- History of stroke within two years or stroke with significant residual neurological deficit
- Bleeding diathesis
- Recent (within six weeks) major surgery or trauma
- Thrombocytopenia (platelet count < 100,000 cells/µL)
- Intracranial neoplasm, arteriovenous malformation, or aneurysm
- Severe uncontrolled hypertension
- History of vasculitis
- Hypersensitivity to abciximab or murine proteins
Drug Interactions
- Other anticoagulants (e.g., heparin, warfarin, oral anticoagulants)
- Antiplatelet agents (e.g., aspirin, clopidogrel, ticlopidine)
- Thrombolytics
- NSAIDs
- Some herbal supplements (e.g., devil’s claw, ginger, ginkgo biloba)
Pregnancy and Breastfeeding
- Pregnancy Safety Category: C
- Fetal risks are unknown. Abciximab should be used during pregnancy only if clearly needed.
- It is unknown whether abciximab is excreted in breast milk. Use with caution during breastfeeding, especially with newborns or preterm infants.
Drug Profile Summary
- Mechanism of Action: Glycoprotein IIb/IIIa receptor inhibitor, prevents platelet aggregation.
- Side Effects: Bleeding, nausea, vomiting, back pain, headache. Rarely, severe bleeding, thrombocytopenia, allergic reactions.
- Contraindications: Active bleeding, recent stroke, thrombocytopenia, recent major surgery or trauma, intracranial abnormalities, severe hypertension.
- Drug Interactions: Anticoagulants, antiplatelet agents, thrombolytics.
- Pregnancy & Breastfeeding: Use with caution.
- Dosage: 0.25 mg/kg bolus followed by a 0.125 µg/kg/min infusion (max 10 µg/min).
- Monitoring Parameters: Platelet count, bleeding time, hemoglobin, signs of bleeding.
Popular Combinations
- Aspirin and heparin are commonly used in conjunction with abciximab during PCI.
Precautions
- Closely monitor for bleeding.
- Caution in patients with renal or hepatic impairment.
- Monitor platelet count.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Abciximab?
A: For PCI: 0.25 mg/kg IV bolus followed by a 0.125 µg/kg/min infusion (max 10 µg/min) for 12 hours. For unstable angina: 0.25 mg/kg IV bolus followed by 10 µg/min infusion for 18-24 hrs, concluding one hour post-PCI.
Q2: What is the mechanism of action of Abciximab?
A: Abciximab is a glycoprotein IIb/IIIa receptor antagonist. It blocks platelet aggregation by preventing the binding of fibrinogen and von Willebrand factor to activated platelets.
Q3: What are the major side effects of Abciximab?
A: Bleeding is the most common and significant side effect.
Q4: When is Abciximab contraindicated?
A: Abciximab is contraindicated in patients with active bleeding, recent stroke, thrombocytopenia, or recent major surgery/trauma.
Q5: What are the key drug interactions with Abciximab?
A: Abciximab interacts with other anticoagulants and antiplatelet agents, increasing the risk of bleeding.
Q6: Can Abciximab be used during pregnancy?
A: It should be used during pregnancy only if clearly needed. The safety profile in pregnancy is not well established.
Q7: What monitoring is necessary during Abciximab therapy?
A: Close monitoring of platelet count, signs of bleeding, hemoglobin levels, and other coagulation parameters is essential.
Q8: How is Abciximab administered?
A: Abciximab is administered intravenously as an initial bolus followed by a continuous infusion.
Q9: How long does the effect of Abciximab last?
A: Platelet function generally recovers within 48 hours, though abciximab can remain in circulation longer.
Q10: What is the role of Abciximab in PCI?
A: It reduces the risk of ischemic complications, such as acute myocardial infarction and the need for repeat revascularization procedures, during and after PCI.
