Drug Guide
Vorapaxar Sulfate
Classification
Therapeutic: Antiplatelet agent
Pharmacological: Protease-activated receptor-1 antagonist
FDA Approved Indications
- Secondary prevention of thrombotic cardiovascular events in patients with a history of myocardial infarction or peripheral arterial disease
Mechanism of Action
Vorapaxar is a selective antagonist of protease-activated receptor-1 (PAR-1), blocking thrombin-induced and collagen-induced platelet aggregation, thus reducing clot formation.
Dosage and Administration
Adult: Hemorrhage risk dictates initial dose of 2.08 mg (stronger loading dose), followed by a maintenance dose of 2.08 mg once daily. Importantly, it should be used in conjunction with aspirin or other antiplatelet therapy.
Pediatric: Not approved for pediatric use.
Geriatric: Use with caution; no specific dose adjustment, but increased bleeding risk requires careful assessment.
Renal Impairment: No specific dose adjustment indicated, but caution is advised.
Hepatic Impairment: No specific dose adjustment; use with caution.
Pharmacokinetics
Absorption: Rapidly absorbed after oral administration.
Distribution: Widely distributed; volume of distribution approximately 130 liters.
Metabolism: Metabolized primarily via CYP3A4/5 enzymes.
Excretion: Primarily excreted in feces, with minimal urinary excretion.
Half Life: Approximately 20 hours.
Contraindications
- Active pathological bleeding
- History of hemorrhagic stroke
Precautions
- Use with caution in patients with increased risk of bleeding, recent surgery, or trauma; monitor for signs of bleeding.
Adverse Reactions - Common
- Bleeding (e.g., hematoma, hemorrhage) (Common)
Adverse Reactions - Serious
- Major bleeding, including intracranial hemorrhage (Less common but serious)
Drug-Drug Interactions
- Other anticoagulants or antiplatelet agents (e.g., aspirin, clopidogrel) may increase bleeding risk.
Drug-Food Interactions
- No significant interactions identified.
Drug-Herb Interactions
- Limited data; avoid complementary herbs with bleeding risk (e.g., ginkgo, ginseng).
Nursing Implications
Assessment: Monitor for signs of bleeding, perform platelet counts, and assess bleeding risk before and throughout therapy.
Diagnoses:
- Risk for bleeding
- Impaired tissue perfusion
Implementation: Administer as prescribed, monitor bleeding, educate patient on signs of bleeding.
Evaluation: Effectiveness in preventing thrombotic events; absence of bleeding episodes.
Patient/Family Teaching
- Report any unusual bleeding, bruising, or signs of hemorrhage.
- Avoid activities that may cause injury or bleeding.
- Inform healthcare providers of all medications and supplements.
Special Considerations
Black Box Warnings:
- Bleeding risk is increased; contraindicated in certain bleeding disorders.
- Caution in use in patients with a history of stroke or intracranial hemorrhage.
Genetic Factors: Genetic variations affecting CYP3A4 may influence metabolism.
Lab Test Interference: May affect coagulation tests; interpret with caution.
Overdose Management
Signs/Symptoms: Excessive bleeding, hematoma, petechiae.
Treatment: Discontinue drug immediately; provide supportive care; consider blood products or agents to reverse bleeding if necessary.
Storage and Handling
Storage: Store at room temperature, 20°C to 25°C (68°F to 77°F).
Stability: Stable under recommended storage conditions, consult package insert for expiration date.