How Do Protease Activated Receptor-1 (PAR-1) Inhibitors Work?

Reviewed on 6/14/2021

WHAT ARE PROTEASE-ACTIVATED RECEPTOR-1 (PAR-1) INHIBITORS AND HOW DO THEY WORK?

Protease-activated receptor-1 (PAR-1) inhibitors are a new class of antiplatelet agents used to reduce the risk of a heart attack in people with coronary artery disease who are at an increased risk for atherosclerotic occlusive thrombotic events. PAR-1 inhibitors work by inhibiting thrombin-related platelet aggregation.

A tear in the lining of the coronary artery with a disease exposes inactive platelets to collagen and other factors present in the plasma. These factors activate the platelets to become sticky and aggregate at the site of the tear. These activated platelets release molecules that trigger a cascade of coagulation factors and increase thrombin. Thrombin is responsible for the formation of a fibrin net that traps platelets and red blood cells and forms a blood clot to seal the injured area.

Thrombin is also responsible for activating circulating platelets by binding with PAR-1 receptors present on the surface of the platelets. One molecule of thrombin can activate multiple PAR-1 receptors. Thrombin also amplifies the coagulation factors, increasing thrombin, fibrin, and activated platelets, and thus, the size of the clot increases in such a way that the artery is occluded, resulting in myocardial infarction (heart attack).

PAR-1 inhibitors bind to PAR-1 receptors and prevent the activation of the receptor, and thus, platelet aggregation and

HOW ARE PROTEASE-ACTIVATED RECEPTOR-1 (PAR-1) INHIBITORS USED?

  • PAR-1 inhibitors are taken orally and used together with other medications, such as aspirin and clopidogrel to help prevent heart attacks and strokes in people who have had a heart attack or have poor blood flow (peripheral arterial disease).

WHAT ARE SIDE EFFECTS OF PROTEASE-ACTIVATED RECEPTOR-1 (PAR-1) INHIBITORS?

Common side effects of PAR-1 inhibitors include:

The information contained herein is not intended to cover all possible side effects, precautions, warnings, drug interactions, allergic reactions, or adverse effects. Check with your doctor or pharmacist to make sure these drugs do not cause any harm when you take them along with other medicines. Never stop taking your medication and never change your dose or frequency without consulting your doctor.

SLIDESHOW

Heart Disease: Symptoms, Signs, and Causes See Slideshow

WHAT ARE DRUG NAMES OF PROTEASE-ACTIVATED RECEPTOR-1 (PAR-1) INHIBITORS?

Drug name includes:

References
https://reference.medscape.com/drugs/protease-activated-receptor-1-par-1-inhibitors

https://pubmed.ncbi.nlm.nih.gov/26398717/

Health Solutions From Our Sponsors