Vorapaxar

What is Vorapaxar?

• Vorapaxar (Zontivity) is a protease-activated receptor-1 (PAR-1) antagonist used for the reduction of thrombotic cardiovascular events in patients with a history of myocardial infarction (MI) or with peripheral arterial disease (PAD).

What are the uses of this medicine?

Zontivity is a prescription medicine used to treat people who have

• had a heart attack or
• reduced blood flow in their legs (peripheral arterial disease).
• Zontivity is used with aspirin and/or clopidogrel to lower your chance of having another serious problem with your heart or blood vessels, such as heart attack, stroke, or death.

How does this medicine work?

• Vorapaxar (vor" a pax' ar) is an inhibitor of the protease-activated receptor 1 (PAR-1) that is found on platelets and is activated by thrombin resulting in platelet aggregation and formation of a vascular clot.
• The aggregation of platelets also plays an important role in the growth of atheromatous plaques, which can lead to coronary, cerebral and peripheral arterial occlusions.
• In large clinical trials, vorapaxar therapy has been shown to decrease the frequency of recurrence of myocardial infarction and cardiovascular events in patients at high risk of complications of atherosclerosis.

Who Should Not Use this medicine ?

This medicine cannot be used in patients with:

• have had a stroke or "mini stroke" (also known as transient ischemic attack or TIA)
• have had bleeding in your brain
• currently have unusual bleeding, such as bleeding in your head, stomach or intestines (an ulcer).

If you have a stroke, TIA, or bleeding in your brain while taking Zontivity your doctor should stop your treatment with Zontivity. Follow your doctor's instructions about stopping Zontivity.

What drug interactions can this medicine cause?

• Avoid concomitant use of Zontivity with strong inhibitors of CYP3A (e.g., ketoconazole, itraconazole, posaconazole, clarithromycin, nefazodone, ritonavir, saquinavir, nelfinavir, indinavir, boceprevir, telaprevir, telithromycin and conivaptan).
• Avoid concomitant use of Zontivity with strong inducers of CYP3A (e.g., rifampin, carbamazepine, St. John's Wort and phenytoin).

Is this medicine FDA approved?

• This medicine is approved in the year 2014.

How should this medicine be used?

Recommended Dosage:

• Take one tablet of Zontivity 2.08 mg orally once daily, with or without food.

Administration

• Take Zontivity exactly as prescribed by your doctor.
• Take Zontivity 1 time each day.
• Take Zontivity with or without food.
• Take Zontivity with aspirin and/or clopidogrel as prescribed by your doctor.
• Do not stop taking Zontivity without first talking to the doctor who prescribed it for you.
• If you take too much Zontivity, call your doctor, or go to the nearest emergency room right away.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Tablets: 2.08 mg vorapaxar.

This medicine is available in fallowing brand namesː

• Zontivity '

What side effects can this medication cause?

The most common side effects of this medicine include:

• Bleeding including life-threatening and fatal bleeding, is the most commonly reported adverse reaction.
• Anemia (low level of red blood cells)
• Depression
• Rash

What special precautions should I follow?

• Like other antiplatelet agents, Zontivity increases the risk of bleeding. Avoid concomitant use of warfarin or other anticoagulants.
• Avoid concomitant use of Zontivity with strong CYP3A inhibitors or inducers.

What to do in case of emergency/overdose?

Management of overdosage:

• There is no known treatment to reverse the antiplatelet effect of Zontivity, and neither dialysis nor platelet transfusion can be expected to be beneficial if bleeding occurs after overdose.
• Inhibition of platelet aggregation can be expected for weeks after discontinuation of normal dosing .
• There is no standard test available to assess the risk of bleeding in an overdose situation.

Can this medicine be used in pregnancy?

• Available data from postmarketing experience with Zontivity use in pregnant women are insufficient to evaluate for a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes.

Can this medicine be used in children?

• The safety and effectiveness of Zontivity in pediatric patients have not been established.

What are the active and inactive ingredients in this medicine?

• Active ingredient: vorapaxar sulfate

• Inactive ingredients:
• Tablet: lactose monohydrate, microcrystalline cellulose, croscarmellose sodium, povidone, and magnesium stearate
• Film coating: lactose monohydrate, hypromellose, titanium dioxide, triacetin (glycerol triacetate), and iron oxide yellow

Who manufactures and distributes this medicine?

• Manufactured for:

Aralez Pharmaceuticals US Inc. 300 Interpace Parkway Morris Corporate Center 1, Building C3 Parsippany NJ 07054 United States

What should I know about storage and disposal of this medication?

• Store Zontivity at room temperature between 68°F to 77°F (20°C to 25°C).
• Keep Zontivity in the bottle it comes in.
• Keep the bottle tightly closed.
• The Zontivity bottle contains a desiccant packet to help keep your medicine dry (protect it from moisture). Keep the desiccant packet in the bottle. Do not throw away the desiccant packet.
• Store blister packs of Zontivity in the original package it comes in.

• Dailymed label info on Vorapaxar
• FDA Vorapaxar