Vorapaxar

Vorapaxar is used to reduce thrombotic cardiovascular events in patients with a history of heart attack (myocardial infarction or MI), or with peripheral arterial disease.

Vorapaxar is available under the following different brand names: Zontivity.

Dosages of Vorapaxar:

Dosage Forms and Strengths

Tablet

• 2.08mg

Dosage Considerations – Should be Given as Follows:

Thromboembolism

• Indicated to reduce thrombotic cardiovascular events in patients with a history of MI or with peripheral arterial disease
• 2.08 mg orally once daily in combination with either aspirin and/or clopidogrel (according to their indications or standard of care); there is limited clinical experience with other antiplatelet drugs and none with vorapaxar as the only antiplatelet agent

Dosage Modifications

• Renal impairment: No dose adjustment is required
• Mild-to-moderate hepatic impairment: No dose adjustment required
• Severe hepatic impairment: Not recommended; based on the increased inherent risk of bleeding in patients with severe hepatic impairment

• Results from clinical trials have shown vorapaxar reduces the rate of a combined endpoint of cardiovascular death, heart attack (myocardial infarction/MI), stroke, and urgent coronary
• Safety and efficacy not established in pediatric patients

Administration

• May take with or without food

Common side effects of Vorapaxar include:

• Bleeding
• Anemia
• Depression
• Rashes, skin eruptions
• Double vision

This document does not contain all possible side effects and others may occur. Check with your physician for additional information about side effects.

• Severe interactions of vorapaxar include:
  • apixaban
  • defibrotide
  • rivaroxaban
• Vorapaxar has serious interactions with at least 46 different drugs.
• Vorapaxar has moderate interactions with at least 73 different drugs.
• Vorapaxar has no listed mild interactions with other drugs.

Warnings

• This medication contains vorapaxar. Do not take Zontivity if you are allergic to vorapaxar or any ingredients contained in this drug.

Black Box Warnings

• Do not use in patients with a history of stroke, transient ischemic attack (TIA), or intracranial hemorrhage (ICH)
• Increases risk of bleeding, including ICH and fatal bleeding

Contraindications

• History of stroke, TIA, or ICH because of an increased risk of ICH in this population
• Active pathologic bleeding

Effects of Drug Abuse

• No information is available.

Short-Term Effects

• See "What Are Side Effects Associated with Using Vorapaxar?"

Long-Term Effects

• See "What Are Side Effects Associated with Using Vorapaxar?"

Cautions

• Discontinue in patients who experience a stroke, TIA, or ICH
• Antiplatelet agents, including vorapaxar, increase the risk of bleeding, including ICH and fatal bleeding (see Black Box Warnings)
• Strong CYP3A inhibitors increase and inducers decrease vorapaxar exposure; avoid coadministration

Pregnancy and Lactation

• Based on the potential for serious adverse reactions (such as maternal bleeding/hemorrhage) and long half-life which makes it effectively irreversible, discontinue vorapaxar therapy when pregnancy is detected and initiate alternative therapy with a shorter duration of action. Available data from postmarketing experience with use in pregnant women are insufficient to evaluate for a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes.
• There are no data on the presence of vorapaxar or metabolites in human milk, its effects on the breastfed infant, or milk production. When vorapaxar was administered to lactating rats, the drug was actively secreted in the milk of rats. When a drug is present in animal milk, it is likely the drug will be present in human milk. Because of the potential for serious adverse reactions in breastfed infants, such as bleeding, breastfeeding is not recommended during treatment with vorapaxar.