Zontivity
Zontivity Uses, Dosage, Side Effects, Food Interaction and all others data.
Zontivity is a tricyclic himbacine-derived selective inhibitor of protease activated receptor (PAR-1) indicated for reducing the incidence of thrombotic cardiovascular events in patients with a history of myocardial infarction (MI) or with peripheral arterial disease (PAD). By inhibiting PAR-1, a thrombin receptor expressed on platelets, vorapaxar prevents thrombin-related platelet aggregation.
Trade Name | Zontivity |
Availability | Prescription only |
Generic | Vorapaxar |
Vorapaxar Other Names | Vorapaxar |
Related Drugs | Xarelto, clopidogrel, Plavix, Brilinta, rivaroxaban, ticagrelor, Zontivity |
Weight | 2.08mg, |
Type | Oral tablet |
Formula | C29H33FN2O4 |
Weight | Average: 492.5817 Monoisotopic: 492.242435759 |
Protein binding | Vorapaxar is extensively bound (>99%) to human plasma proteins, such as human serum albumin. |
Groups | Approved |
Therapeutic Class | |
Manufacturer | |
Available Country | United States, |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Zontivity is a platelet aggregation inhibitor used to reduce thrombotic cardiovascular events in patients with a history of myocardial infarction (MI) or peripheral arterial disease (PAD).
Zontivity is indicated for the reduction of thrombotic cardiovascular events in patients with a history of myocardial infarction (MI) or peripheral arterial disease (PAD). It is usually co-administered with acetylsalicylic acid (ASA) and/or clopidogrel, and should therefore be administered as an addition to these medications as it has not been studied alone.
Zontivity is also used to associated treatment for these conditions: Cardiovascular Events
How Zontivity works
Zontivity inhibits platelet aggregation through the reversible antagonism of protease-activated receptor 1 (PAR-1), also known as thrombin receptor. PARs are a family of G-protein coupled receptors highly expressed on platelets and activated by serine protease activity of thrombin to mediate thrombotic response. By blocking PAR-1 activating, vorapaxar inhibits thrombin-induced platelet aggregation and thrombin receptor agonist peptide (TRAP)-induced platelet aggregation. Zontivity does not inhibit platelet aggregation induced by other agonists such as adenosine diphosphate (ADP), collagen or a thromboxane mimetic.
Toxicity
There is an increased risk of bleeding and intracranial hemorrhage (ICH), which is why the use of vorapaxar is contraindicated in patients with a history of stroke, trans-ischemic attack (TIA), ICH, or active pathological bleeding such as peptic ulcer. Animal studies have suggested that there is a low probability of embryo/fetal toxicities, however there are no adequate and well-controlled studies describing use in pregnant women. Zontivity should also be avoided during breastfeeding as it is unknown whether vorapaxar or its metabolites are excreted in human milk, however it has been shown to be actively secreted in the milk of rats.
Food Interaction
- Avoid herbs and supplements with anticoagulant/antiplatelet activity. Additive antiplatelet activity may increase the risk of bleeding. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.
- Avoid St. John's Wort. This herb induces the CYP3A metabolism of vorapaxar and may reduce its serum concentration.
- Exercise caution with grapefruit products. Coadministration of vorapaxar with moderate CYP3A4 inhibitors does not require intervention, but coadministration with strong inhibitors should be avoided.
- Take with or without food.
Zontivity Drug Interaction
Major: bivalirudin, warfarin, ibuprofenUnknown: pseudoephedrine / triprolidine, fluticasone / salmeterol, calcium carbonate, multivitamin with minerals, docusate, misoprostol, metformin, chondroitin / glucosamine / methylsulfonylmethane, terazosin, sitagliptin, atorvastatin, metoprolol, nitroglycerin, amlodipine, acetaminophen, finasteride, pantoprazole
Zontivity Disease Interaction
Volume of Distribution
424 L
Elimination Route
After oral administration, vorapaxar is rapidly absorbed and peak concentrations occur at a median tmax of 1 hour under faster conditions. Zontivity may be taken with or without food as ingestion with a high-fat meal did not result in meaningful changes in AUC. The mean absolute bioavailability is 100%.
Half Life
Zontivity has an effective half life of 3-4 days and an apparent terminal half life of 8 days.
Elimination Route
Zontivity is primarily eliminated as its metabolite M19 through the feces (91.5%), and partially eliminated in the urine (8.5%).
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