vorapaxar

Therapeutic Classification: antiplatelet agents

Pharmacologic Classification: protease-activated receptor-1 (PAR-1) antagonists

Indications ⬆ ⬇

REMS

To reduce thrombotic cardiovascular events in patients who have a history of MI or peripheral arterial disease (can be used with aspirin and/or clopidogrel).

Action ⬆ ⬇

Acts as an antagonist of the protease-activated receptor-1 on platelet surfaces. Inhibits platelet aggregation.

Therapeutic effects:

Decreased cardiovascular events.

Pharmacokinetics ⬆ ⬇

Absorption: Completely absorbed (100%) following oral administration.

Distribution: Unknown.

Protein Binding: >99%.

Metabolism/Excretion: Extensively metabolized by the liver via the CYP3A4 and CYP2J2 isoenzymes; one metabolite (M20) has antiplatelet activity (20% of parent compound). Excreted mostly in feces (58%) and some in urine (25%) as metabolites.

Half-Life: Effective half-life: 3–4 days, terminal elimination half-life: 8 days (range 5–13 days, similar for M20).

Time/Action Profile ⬆ ⬇

(antiplatelet effect)

ROUTE	ONSET	PEAK	DURATION
PO	within 1 wk	unknown	4 wk

Contraind./Precautions ⬆ ⬇

Contraindicated in:

History of stroke, transient ischemic attack, or intracranial hemorrhage;
Active pathologic bleeding;
Concurrent use of anticoagulants, including warfarin;
Severe hepatic impairment (↑ risk of bleeding);
OB: Pregnancy (may risk of maternal bleeding/hemorrhage);
Lactation: Lactation.

Use Cautiously in:

Existing risk factors for bleeding, including ↑ age, ↓ body weight, ↓ renal/hepatic function, concurrent chronic NSAIDs, other antiplatelet agents, or history of bleeding disorders;
Pedi: Safety and effectiveness not established in children;
Geri: Older adults may be at risk of bleeding.

Adv. Reactions/Side Effects ⬆ ⬇

Interactions ⬆ ⬇

Drug-drug:

Strong CYP3A inhibitors, including clarithromycin, conivaptan, itraconazole, ketoconazole, nefazodone, nelfinavir, posaconazole, or ritonavir, may ↑ levels and risk of bleeding; avoid concurrent use.
Strong CYP3A inducers, including carbamazepine, phenytoin, and rifampin, may ↓ levels and effectiveness; avoid concurrent use.
↑risk of bleeding with anticoagulants, other antiplatelet agents, fibrinolytics, chronic NSAID use, SSRIs, or SNRIs; avoid concurrent use of warfarin or other anticoagulants.

Drug-Natural Products:

St. John's wort may ↓ levels and effectiveness; avoid concurrent use.

Route/Dosage ⬆ ⬇

PO (Adults ): 2.08 mg once daily.

Availability ⬆ ⬇

Tablets: 2.08 mg

Assessment ⬆ ⬇

Assess for signs and symptoms of bleeding periodically during therapy.

Implementation ⬆ ⬇

PO: Administer once daily without regard to food.
- Administer with aspirin or clopidogrel according to directions.

Patient/Family Teaching ⬆ ⬇

Instruct patient to take vorapaxar as directed. Do not stop therapy without consulting health care professional. Advise patient to read Medication Guide before starting therapy and with each Rx refill in case of changes.
Caution patient to notify health care professional immediately if signs and symptoms of bleeding (bleeding that is severe or cannot be controlled; pink, red, or brown urine; vomiting blood or coffee ground–like vomit; red or black tar-like stools; coughing up blood or blood clots) occur.
Advise patient to notify health care professional of medication regimen before treatment or surgery.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected and to avoid breastfeeding during therapy. Use during pregnancy increases risk of maternal bleeding and hemorrhage. If pregnancy is detected, discontinue vorapaxar as soon as possible.

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Pronunciation ⬇

Classifications ⬆ ⬇