- Side Effects
- Drug Interactions
- Pregnancy & Breastfeeding
- What Else to Know
Generic Name: vorapaxar
Brand Name: Zontivity
Drug Class: Antiplatelet Agents, Cardiovascular; Thrombin Inhibitors; Protease Activated Receptor-1 (PAR-1) Inhibitors
What is vorapaxar, and what is it used for?
Vorapaxar is a medication used to reduce the risk of blood clot formation and consequent blood vessel blocks in adult patients with a history of heart attack (myocardial infarction) or peripheral artery disease (PAD). Vorapaxar reduces the rate of a combined endpoint of cardiovascular death, myocardial infarction (MI), stroke, and need for emergency coronary artery bypass grafting (CABG) surgery (urgent coronary revascularization [UCR]). Vorapaxar is usually administered with other anticoagulants such as acetylsalicylic acid and/or clopidogrel.
When a blood vessel is injured, the first activity in blood clotting (coagulation) process is the aggregation of platelets which form a plug to arrest bleeding (hemostasis). Other specialized insoluble proteins known as coagulation factors in the blood continue the process. Coagulation is an important process for achieving hemostasis, however, people with a history of MI or PAD have a high risk of developing clots that can block blood vessels. Vorapaxar hinders clot formation by inhibiting the aggregation of platelets.
Vorapaxar belongs to a class of drugs known as protease activated receptor-1 (PAR-1) inhibitors. Vorapaxar binds to PAR-1, a protein molecule expressed on platelets, and inhibits platelet aggregation induced by thrombin and thrombin receptor agonist peptide (TRAP). Thrombin is a unique molecule that plays an important role in both coagulation and anticoagulation processes. PAR-1 is found in many types of cells, including smooth muscle, nerve and endothelial cells, but vorapaxar’s effect on these cells has not been assessed.
- Do not use vorapaxar in patients with a history of stroke, transient ischemic attack (TIA) or intracranial hemorrhage (ICH), vorapaxar increases the risk for ICH and fatal bleeding in these patients. Discontinue vorapaxar if a patient develops stroke, TIA or ICH.
- Do not use vorapaxar in patients with pathological bleeding such as ICH or peptic ulcers.
- Antiplatelet agents, including vorapaxar increase the risk for bleeding, including ICH and fatal bleeding.
- Consider the patient's underlying risks for bleeding before prescribing vorapaxar. General risk factors for bleeding include:
- Advanced age
- Low body weight
- History of bleeding disorders
- Impaired liver or kidney function
- Concurrent use of certain medications such as anticoagulants, fibrinolytic therapy, chronic nonsteroidal anti-inflammatory drugs [NSAIDS], selective serotonin reuptake inhibitors, serotonin norepinephrine reuptake inhibitors
- Avoid concomitant use of other anticoagulants such as warfarin
- Evaluate for bleeding in any patient who has low blood pressure and has recently undergone coronary angiography, percutaneous coronary intervention, coronary artery bypass graft surgery, or other surgical procedures.
- Withholding vorapaxar for a short period to manage an acute bleeding episode is not useful, because significant antiplatelet effects last for 4 weeks after discontinuation of the drug.
- Consider the patient's underlying risks for bleeding before prescribing vorapaxar. General risk factors for bleeding include:
- Vorapaxar is metabolized by the liver enzyme CYP3A. Avoid concomitant use with other drugs that are strong inducers or inhibitors of CYP3A. Strong CYP3A inhibitors increase and inducers decrease vorapaxar exposure.
IMAGESBrowse through our medical image collection to see illustrations of human anatomy and physiology See Images
What are the side effects of vorapaxar?
Common side effects of vorapaxar include:
- Bleeding events, including:
- Clinically significant bleeding
- Any organ bleeding
- Gastrointestinal bleeding
- Moderate or severe bleeding
- Severe bleeding
- Intracranial hemorrhage
- Fatal bleeding
- Low red blood cell count (anemia)
- Skin reactions including:
- Wide-spread rashes (exanthemas)
- Double vision (diplopia)
Call your doctor immediately if you experience any of the following symptoms or serious side effects while using this drug:
- Serious heart symptoms include fast or pounding heartbeats, fluttering in your chest, shortness of breath, and sudden dizziness;
- Severe headache, confusion, slurred speech, severe weakness, vomiting, loss of coordination, feeling unsteady;
- Severe nervous system reaction with very stiff muscles, high fever, sweating, confusion, fast or uneven heartbeats, tremors, and feeling like you might pass out; or
- Serious eye symptoms include blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights.
This is not a complete list of all side effects or adverse reactions that may occur from the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may also report side effects or health problems to the FDA at 1-800-FDA-1088.
What are the dosages of vorapaxar?
- 2.08 mg
- Indicated to reduce thrombotic cardiovascular events in patients with a history of myocardial infarction (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
- Renal impairment: No dose adjustment 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, MI, stroke, and urgent coronary revascularization (UCR)
- May take with or without food
- Safety and accuracy not established
Vorapaxar prevents platelet aggregation and overdose can further increase the risk of bleeding. The antiplatelet effects can last for weeks after discontinuation of vorapaxar. There is no known treatment to reverse the effect of vorapaxar. Neither dialysis nor platelet transfusion is expected to be beneficial if bleeding occurs after overdose.
What drugs interact with vorapaxar?
Inform your doctor of all medications you are currently taking, who can advise you on any possible drug interactions. Never begin taking, suddenly discontinue, or change the dosage of any medication without your doctor’s recommendation.
- Severe interactions of vorapaxar include:
- Vorapaxar has serious interactions with at least 57 different drugs.
- Vorapaxar has moderate interactions with at least 74 different drugs.
- Mild interactions of vorapaxar include:
The drug interactions listed above are not all of the possible interactions or adverse effects. For more information on drug interactions, visit the RxList Drug Interaction Checker.
It is important to always tell your doctor, pharmacist, or health care provider of all prescription and over-the-counter medications you use, as well as the dosage for each, and keep a list of the information. Check with your doctor or health care provider if you have any questions about the medication.
Pregnancy and breastfeeding
- Animal reproductive studies did not show fetal harm, and available data on the use of vorapaxar in pregnant women are insufficient to determine a drug-associated risk for major birth defects or adverse maternal or fetal outcomes.
- If a patient becomes pregnant, discontinue vorapaxar because of its long half-life and potential for serious hemorrhage in the mother, and initiate alternate treatment with a drug that has a shorter duration of action.
- There are no data on the presence of vorapaxar or its metabolites in breastmilk. The drug is excreted in rat’s milk, and likely will be present in human milk as well. Nursing mothers should avoid breastfeeding while on treatment with vorapaxar, because of the potential for serious bleeding in the breastfed infant.
What else should I know about vorapaxar?
- Take vorapaxar exactly as prescribed. Do not discontinue on your own without checking with your prescribing physician.
- You may bleed and bruise easily. Exercise care to avoid injury. Report to your physician if you experience any unexpected, prolonged or excessive bleeding, or find blood in your stool or urine.
- Inform other physicians and dentists that you are taking vorapaxar, if you require any surgical or dental procedure and ask them to consult with your prescribing physician before stopping vorapaxar.
- Store vorapaxar safely out of reach of children.
- In case of overdose, seek medical help or contact Poison Control.
Vorapaxar is a medication used to reduce the risk of blood clot formation and consequent blood vessel blocks in adult patients with a history of heart attack (myocardial infarction) or peripheral artery disease (PAD). Common side effects of vorapaxar include bleeding events, low red blood cell count (anemia), depression, skin reactions, and double vision (diplopia).
Multimedia: Slideshows, Images & Quizzes
Heart Disease: Causes of a Heart Attack
Heart disease prevention includes controlling risk factors like diet, exercise, and stress. Heart disease symptoms in women may...
Am I Having a Heart Attack? Symptoms of Heart Disease
Heart attacks symptoms vary greatly for men and women, from anxiety and fatigue to nausea and sweating. Learn the warning signs...
Blood Clots: 4 Signs You Could Have One
Blood clots can be deadly medical emergencies that can form in different parts of your body. Learn the warning signs that you...
Picture of Blood Clot
Blood that has been converted from a liquid to a solid state. See a picture of Blood Clot and learn more about the health topic.
DVT: Dos and Don’ts After a Blood Clot
If you’ve had a blood clot, like a deep vein thrombosis (DVT) or pulmonary embolism (PE), you might need to make a few changes...
Related Disease Conditions
Blood Clots (in the Leg)
Blood clots can form in the heart, legs, arteries, veins, bladder, urinary tract, and uterus. Risk factors include high blood pressure and cholesterol, diabetes, smoking, and family history. Symptoms and treatment depend on the location of the clot.
Heart Attack (Myocardial Infarction): Early Warning Signs, Symptoms, Causes, and Treatment
A heart attack occurs when a blood clot completely obstructs a coronary artery supplying blood to the heart muscle. Learn about warning signs, causes, complications, risk factors, and treatment.
How Serious Is a Blood Clot in the Lungs?
A blood clot is a solid or semisolid clump of blood. When the tissues of our body are injured, excessive blood loss is prevented by the clotting of blood. When a blood clot occurs inside the blood vessels it may lead to serious medical conditions. When a blood clot occurs inside the arteries to the lungs, the condition is called pulmonary embolism (PE).
Heart Attack vs. Stroke
Heart attack usually is caused by a clot that stops blood flow supplying oxygen to an area of heart muscle, which results in heart muscle death. Stroke or "brain attack" is caused by a loss of blood supply to the brain (usually a blood clot) or by hemorrhagic stroke (bleeding within the brain), which results in brain tissue death. Both heart attack and stroke usually come on suddenly, produce similar symptoms, can be disabling, and can be fatal. The classic symptoms and warning signs of heart attack are different. Classic heart attack warning signs are chest pain or discomfort, shortness of breath, pain that radiates to the shoulders, back, arms, belly, jaw, or teeth, sweating, fainting, and nausea and vomiting. Moreover, woman having a heart attack may have additional symptoms like abdominal pain or discomfort, dizziness, clammy skin, and moderate to severe fatigue. The classic symptoms and warning signs that a person is having a stroke are confusion or loss of consciousness, sudden severe headache, speech problems, problems seeing out of one or both eyes, and numbness or weakness of only one side of the body. Moreover, a woman having a stroke may have additional warning symptom and signs like shortness of breath, disorientation, agitation, behavioral changes, weakness, nausea, vomiting, seizures, and hiccups. Recognition of stroke symptoms is vital for emergency treatment. The acronym "FAST" stands for recognition of Facial drooping, Arm weakness, Speech difficulty, and a Time for action. If you experience the symptoms heart attack or stroke (FAST) or see them develop in another person, then contact 911 immediately.
How Do You Know If You Have a Blood Clot in Your Leg?
Blood clots are clumps of blood formed when the blood changes from a fluid to a semisolid form. When a blood clot is formed in one of the large veins in the legs or arms, the condition is called deep vein thrombosis (DVT). A blot clot in your leg can hamper the flow of oxygen and nutrients to the affected area. An untreated DVT may cause the clot to grow bigger and break in small pieces that can travel to other organs, such as the heart and lungs, causing serious consequences.
What Is the Difference Between a Thrombus and a Blood Clot?
What makes a thrombus different from a blood clot? Learn about the differences between a thrombus and a blood clot, and how these conditions are treated.
Heart Attack vs. Heartburn
Heartburn is a symptom of another disease or medical problem and can be described as a feeling of burning in the chest accompanied by symptoms of nausea, vomiting, or a sour taste or food stuck in the back of the throat. Heart attack occurs when an artery in the heart is completely blocked by a blood clot, which causes that portion of heart muscle to die. Heart attack also has symptoms of chest pain, nausea, and vomiting, however, other warning signs and symptoms of a heart attack are unusual weakness or fatigue, and persistent and/or increased severity of symptoms over a few minutes. Heart attack is a life threatening emergency. If you think you or someone you are with is having a heart attack, call 911 immediately for urgent medical treatment. It may save your life.
What Does a Blood Clot Feel Like?
Blood clots are semi-solid masses of blood that may be immobile (thrombosis) and impede blood flow or dislodge to other parts of the body (embolism). Deep vein clots, if dislodged, can travel through veins through the lungs to the arteries in the lungs. This is referred to as a pulmonary embolism and can be deadly. Blood clots can also lead to a heart attack or stroke.
Heart Attack Prevention Overview
Heart attacks are the major causes of unexpected, sudden death among men and women. A heart attack also is a significant cause of heart failure. The process of developing atherosclerosis (hardening of the arteries) begins early in life. Heart attack prevention should begin in childhood because the atherosclerosis process can not be reversed. The risk of having a heart attack increases if you have diseases or conditions such as high blood pressure, diabetes, and other heart conditions.
Vitamins & Exercise: Heart Attack Prevention Series
Vitamins and exercise can lower your risk for heart attack and heart disease. Folic acid, vitamins, and homocysteine levels are interconnected and affect your risk for heart disease or heart attack. For better heart health, avoid the following fried foods, hard margarine, commercial baked goods, most packaged and processed snack foods, high fat dairy, and processed meats such as bacon, sausage, and deli meats.
Can You Have Sex Right After a Heart Attack?
It is important not to put any pressure on yourself or your heart after heart attack. Initially, you might feel less interested in sex. That is perfectly normal, and the feeling goes away quickly.
Treatment & Diagnosis
- Heart Attack: A Tale of Two Heart Attacks
- FLAP Doubles Risk of Heart Attack
- The Cox-2 Inhibitors Controversy: Q&A with Dr. Shiel
- Heart Attack Prevention From a Doctor's Perspective
- Heart Attack Risk and Medicated Stents
- How Pie Prevents Blood Clots
- Heart Attack - New Blood Test For Earlier Accurate Diagnosis
- Pulmonary Embolism -Lung Blood Clot Risk Factors In Women
- Cancer,Stroke & Heart Attack Risks- ReducedThrough Walking
- Heart Health- Little Aspirin A Day Stops Big Heart Attack!
- Higher Chance of Blood Clots Forming?
- Heartburn or Heart Attack? Emergency In Flight
- Proven measures to prevent heart attacks and strokes?
- Any promising measures that may prevent heart attacks?
- Mr. Cheney's Chest Pain - And Heart Attack
- What Should Cholesterol Levels Be After Heart Attack?
- Can Gallbladder Problems Cause Blood Clots?
- Do Women Have Different Heart Attack Symptoms?
- Will My Diet Slip Increase the Risk of Heart Attack?
- Can Asthma Cause a Heart Attack?
Medications & Supplements
Healthy Heart Resources
Health Solutions From Our Sponsors
Report Problems to the Food and Drug Administration
You are encouraged to report negative side effects of prescription drugs to the FDA. Visit the FDA MedWatch website or call 1-800-FDA-1088.