Zontivity: Uses, Side Effects and Dosage

What is ZONTIVITY^™ used for?

ZONTIVITY™ is used in combination with aspirin to reduce blood clots in blood vessels in patients who have had a heart attack. ZONTIVITY™ can be used with or without clopidogrel.

ZONTIVITY™ is not recommended for children and adolescents under 18 years of age.

How does ZONTIVITY^™ work?

• ZONTIVITY™ is type of medicine called a protease-activated receptor-1 (PAR-1) antagonist.
• ZONTIVITY™ helps prevent platelets (blood cells) from sticking together and forming a clot that can block an artery.

What are the ingredients in ZONTIVITY^™?

Medicinal ingredient: vorapaxar sulfate

Non-medicinal ingredients: croscarmellose sodium, lactose monohydrate, magnesium stearate, microcrystalline cellulose, and povidone.

In addition, the film coating contains the following inactive ingredients: hypromellose, iron oxide yellow, lactose monohydrate, titanium dioxide and triacetin (glycerol triacetate).

ZONTIVITY^™ comes in the following dosage form:

Film-coated tablet 2.5 mg.

Do not use ZONTIVITY^™ if you:

• have ever had a stroke or "mini stroke" (also known as transient ischemic attack or TIA) or if you have a stroke while taking ZONTIVITY^™.

• have had bleeding in the brain or if you have bleeding in the brain while taking

  ZONTIVITY^™.

• currently have unusual bleeding, such as bleeding in your head, stomach or intestines (ulcers).
• are allergic to vorapaxar or any of the ingredients in ZONTIVITY™.

To help avoid side effects and ensure proper use, talk to your healthcare professional before you take ZONTIVITY^™. Talk about any health conditions or problems you may have or have had, and about any allergies including if you:

• have had bleeding problems in the past.
• have a history of stroke or "mini-stroke" (also known as transient ischemic attack or TIA).
• have had a serious injury or surgery within the past 2 weeks.
• plan to have surgery or a dental procedure.
• have low blood pressure and have recently had a medical procedure.

• have a history of stomach ulcers (open sores that develop in the stomach) or colon polyps

  (fleshy growths in the intestine).

• have liver or kidney problems.

• are pregnant or plan to become pregnant. It is not known if ZONTIVITY™ will harm your unborn baby. You and your doctor should decide if you will take ZONTIVITY™.

• are breast-feeding. It is not known if ZONTIVITY™ passes into your breast milk. You and your doctor should decide if you will take ZONTIVITY™ or breastfeed. You should not take ZONTIVITY™ and breastfeed at the same time.

• have a rare hereditary condition that means you should not eat lactose. ZONTIVITY™ contains lactose. The conditions include:

  • galactose intolerance
  • Lapp lactase deficiency
  • glucose-galactose malabsorption.

Tell all of your doctors and dentists that you are taking ZONTIVITY™. They should talk to the doctor who prescribed ZONTIVITY™ for you before you have any surgery or invasive procedure.

Other warnings you should know about:

• Increased risk of bleeding when taking ZONTIVITY™:

  • ZONTIVITY™ and other similar drugs can increase the risk of bleeding, including bleeding in the brain. This bleeding has sometimes led to death.
  • The risk of bleeding is higher when taking ZONTIVITY™ than when just receiving standard care of aspirin and clopidogrel.
  • ZONTIVITY™ increases the risk of bleeding in patients who are already at risk for bleeding. You may be more at risk if you are elderly, have a low body weight, have kidney or liver problems. Your doctor will determine if ZONTIVITY™ is the right treatment for you.

  • You may have more bleeding while taking ZONTIVITY™ if you have a history of bleeding disorders and you take certain medicines. The medicines are:

    • Blood thinners such as, warfarin, heparin, rivaroxaban, apixaban, dabigatran
    • Fibrinolytic drugs that help prevent blood clots from forming such as, alteplase, reteplase and tenecteplase
    • Nonsteroidal anti-inflammatory drugs such as, ibuprofen, naproxen, aspirin, diclofenac, celecoxib
    • Antidepressants from the classes called selective serotonin reuptake inhibitors and serotonin norepinephrine reuptake inhibitors, such as citalopram, escitalopram, fluoxetine, paroxetine, sertraline, duloxetine, venlafaxine
• If you have a stroke, mini-stroke, or bleeding in the brain while taking ZONTIVITY™, your doctor should stop your ZONTIVITY™. Follow your doctor's instructions about stopping ZONTIVITY™.
• Do not stop taking ZONTIVITY™ without talking to the doctor who prescribes it for you. If you stop taking ZONTIVITY™ because of bleeding, or for other reasons, your risk of heart attack or stroke may increase.

Tell your healthcare professional about all the medicines you take, including any prescription and non-prescription drugs, vitamins, minerals, dietary and natural and herbal supplements, or alternative medicines.

ZONTIVITY™ may affect the way other medicines work, and other medicines may affect how ZONTIVITY™ works.

The following may interact with ZONTIVITY™ such as:

• prasugrel, ticagrelor (antiplatelet medicines that help prevent blood clots)
• indinavir, nelfinavir, ritonavir or saquinavir (HIV protease inhibitors)
• boceprevir or telaprevir (hepatitis C medicines)
• itraconazole, ketoconazole, posaconazole or voriconazole (anti-fungal medicines)
• clarithromycin (antibiotic)
• rifampin (a medicine for tuberculosis and other bacterial infections)
• carbamazepine or phenytoin (anti-seizure medicines)
• warfarin, heparin, rivaroxaban, apixaban or dabigatran (blood thinner medicines)
• grapefruit juice
• St. John’s wort (Hypericum perforatum) (herbal medicine)

Know the medicines you take. Keep a list of them to show your doctor and pharmacist when you get a new medicine. When you are unsure, ask your doctor or pharmacist if your medicine interacts with ZONTIVITY™.

How to take ZONTIVITY™:

• Take ZONTIVITY™ exactly as prescribed by your doctor.
• Do not stop taking ZONTIVITY™ without first talking to the doctor who prescribed it for you.

Usual dose:

• Take one ZONTIVITY™ tablet each day. You can take ZONTIVITY™ with or without food.

Overdose:

If you think you have taken too much ZONTIVITY™, contact your healthcare professional, hospital emergency department or regional Poison Control Centre immediately, even if there are no symptoms.

Missed Dose:

• If you forget a dose, take it as soon as you remember.
• If it is nearly time for the next dose, skip the missed dose.
• Do not take two doses at the same time.

What are possible side effects from using ZONTIVITY™?

These are not all the possible side effects you may feel when taking ZONTIVITY™. If you experience any side effects not listed here, contact your healthcare professional.

ZONTIVITY™ (and similar drugs) can cause bleeding that can be serious and sometimes lead to death.

Possible side effects with ZONTIVITY™ include:

• double vision
• anemia (low number of red blood cells in blood)
• bruising and bleeding more easily
• more likely to have nose bleeds or bleeding of your gums

Serious side effects and what to do about them

If you have a troublesome symptom or side effect that is not listed here or becomes bad enough to interfere with your daily activities, talk to your healthcare professional.

Reporting Side Effects

You can help improve the safe use of health products for Canadians by reporting serious and unexpected side effects to Health Canada. Your report may help to identify new side effects and change the product safety information.

3 ways to report:

• Online at MedEffect (http://hc-sc.gc.ca/dhp-mps/medeff/index-eng.php)
• By calling 1-866-234-2345 (toll-free);

• By completing a Consumer Side Effect Reporting Form and sending it by:

  • Fax to 1-866-678-6789 (toll-free), or

  • Mail to: Canada Vigilance Program

    Health Canada, Postal Locator 0701E Ottawa, ON

    K1A 0K9

    Postage paid labels and the Consumer Side Effect Reporting Form are available at MedEffect (http://hc-sc.gc.ca/dhp-mps/medeff/index-eng.php).

NOTE: Contact your health professional if you need information about how to manage your side effects. The Canada Vigilance Program does not provide medical advice.

Storage:

Store ZONTIVITY™ at room temperature (15°C - 30°C) in the original package until use.

Keep out of reach and sight of children.

If you want more information about ZONTIVITY™:

• Talk to your healthcare professional
• Find the full product monograph that is prepared for healthcare professionals and includes this Patient Medication Information by visiting the Health Canada website (http://www.hc-sc.gc.ca/index-eng.php); the manufacturer’s website www.xspirerx.com, or by calling (601) 605-0664.

Last revised: OCT 27, 2022

^™ Trademark of Merck Sharp & Dohme Corp. Used under license.

* All other trademarks are the property of their respective owners.