30:718:409 Lecture 30: Antithrombotics_Lecture-3_ClassNotes

• School: Rutgers University
• Department: Pharmacology and Toxicology
• Course: 30:718:409
• Professor: Dr. Lavoie and Dr. Chakalamanil

Document Summary

Elevated camp levels decrease platelet aggregation through decreased mobilization of calcium. increases nitric oxide synthesis in neutrophils. Triflusal is rapidly absorbed and metabolized to an active metabolite. In a clinical trial in stroke patients it showed comparable efficacy to aspirin: possible advantage: may have less bleeding side effects, currently available in several foreign countries, there are three purinergic nucleotide receptors, p2x1. A ligand-gated ion channel activated by atp. Activation leads to platelet shape change and transient aggregation: p2y12. At low conc, p2y1 is activated (ec50 of 0. 3um)-> leads to platelet shape change. At higher conc, p2y12 is activated (ec50 of 2 um)-> leads to aggregation. Atp activates p2x1, a ligand-gated ion channel, triggering rapid influx of ca+2, leading to platelet shape change and aggregation. P2y1 and p2y12 are gpcrs: p2y12 antagonists can be divided into. Inactivates p2y12 by disulfide covalent formation between the drug and the receptor: ticlopidine, clopidogrel, prasugrel, cangrelor, ticagrelor.