Antiplatelet agents play an essential role in the treatment of acute coronary syndrome (ACS). Aspirin and thienopyridines comprise the major classes of antiplatelet therapies demonstrated to be of benefit in the treatment of ACS. Thienopyridines are a class of drugs that function via inhibition of the adenosine diphosphate (ADP) P2Y12 platelet receptors. While clopidogrel remains in extensive use in clinical practice, it cannot meet the needs in many clinical conditions because of its pharmacological limitations. In recent years, newly developed P2Y12 antagonists, such as prasugrel and ticagrelor, have proven to be of higher efficacy and less resistance. As a third generation thienopyridine, prasugrel exerts a much more rapid and consistent inhibitory effect on platelet aggregation than clopidogrel. Treatment with ticagrelor, nonthienopyridine oral antiplatelet drug, significantly reduced the rate of death from vascular causes, myocardial infarction, or stroke without an increase in the rate of overall major bleeding as compared with clopidogrel. The present review aims to discuss the current knowledge on the safety and efficacy of new oral antiplatelet agents including prasugrel and ticagrelor.
Acute Coronary Syndrome ; Adenosine ; Adenosine Diphosphate ; Aspirin ; Blood Platelets ; Hemorrhage ; Myocardial Infarction ; Piperazines ; Platelet Aggregation ; Platelet Aggregation Inhibitors ; Pyridines ; Stroke ; Thienopyridines ; Thiophenes ; Ticlopidine ; Prasugrel Hydrochloride

Thienopyridines are antiplatelet agents used in post-percutaneous coronary angioplasty patients and patients with acute coronary syndrome, stroke, and peripheral arterial disease. Ticlopidine has been shown to reduce the incidence of stent thrombosis, but it may also cause serious hematological side effects. Among the thienopyridines, clopidogrel is considered to be a safe alternative to ticlopidine because of its decreased incidence of hematological adverse effects. However, some hematological side effects can occur and may be fatal. In this case, a 47-year-old man complained of dyspnea and generalized edema. He had been taking clopidogrel after coronary angioplasty. His laboratory findings showed acute renal failure, microangiopathic hemolytic anemia, and thrombocytopenia, which were consistent with hemolytic uremic syndrome (HUS). After discontinuing clopidogrel and undergoing plasma exchange, he recovered fully. To our knowledge, this is the first reported case of clopidogrel-induced HUS in Korea.
Acute Coronary Syndrome ; Acute Kidney Injury ; Anemia, Hemolytic ; Angioplasty ; Dyspnea ; Edema ; Hemolytic-Uremic Syndrome ; Humans ; Incidence ; Korea ; Middle Aged ; Peripheral Arterial Disease ; Plasma Exchange ; Platelet Aggregation Inhibitors ; Stents ; Stroke ; Thienopyridines ; Thrombocytopenia ; Thrombosis ; Ticlopidine

The role of platelets in atherogenesis, acute coronary syndrome and the development of complications from percutaneous coronary intervention is relatively well known. Until recently, aspirin was the only antiplatelet agent available for the primary and secondary prevention of coronary heart disease. Recently, there has been a substantial expansion in the antiplatelet armamentarium as well as in the understanding of the clinical importance of antiplatelet therapy in patients with coronary heart disease. The benefits and limitations of the currently available antiplatelet agents including aspirin, thienopyridines (ticlopidine and clopidogrel), and the platelet glycoprotein IIb/IIIa inhibitors in the primary and secondary prevention of coronary heart disease and special clinical situations, such as unstable angina, acute myocardial infarction and percutaneous coronary intervention are discussed.
Acute Coronary Syndrome ; Angina, Unstable ; Aspirin ; Atherosclerosis ; Blood Platelets ; Coronary Disease ; Glycoproteins ; Humans ; Myocardial Infarction ; Percutaneous Coronary Intervention ; Platelet Aggregation Inhibitors ; Secondary Prevention ; Thienopyridines

Oral platelet aggregation inhibitors are widely used for the treatment and prevention of cardiovascular diseases, including coronary stent thrombosis. Premature discontinuation following percutaneous coronary intervention would pose a grave risk of in-stent thrombosis, acute myocardial infarction and eventual death. Although they share the same mechanism of adenosine diphosphate P2Y12 platelet receptor inhibition, they belong to either the chemical class of thienopyridines (clopidogrel, prasugrel, and ticlopidine) or cyclopentyl-triazolo-pyrimidines (ticagrelor and cangrelor). This case describes the first documented cross-reactive hypersensitivity of clopidogrel towards both its fellow thienopyridine, prasugrel, as well as the structurally dissimilar ticagrelor, and its subsequent successful desensitisation.
Adenosine Diphosphate ; Blood Platelets ; Cardiovascular Diseases ; Cross Reactions ; Desensitization, Immunologic ; Hypersensitivity ; Myocardial Infarction ; Percutaneous Coronary Intervention ; Platelet Aggregation Inhibitors ; Prasugrel Hydrochloride ; Stents ; Thienopyridines ; Thrombosis

The role of platelets is well known in the atherogenesis, acute coronary syndrome and development of complications of percutaneous coronary intervention. Until recently, aspirin was the only antiplatelet agent available for the primary and secondary prevention of coronary heart disease. Over the past several years, there has been a substantial expansion in our antiplatelet armamentarium, as well as in our understanding of the clinical importance of antiplatelet therapy in patients with coronary artery disease. The benefits and limitations of the currently available antiplatelet agents, including aspirin, thienopyridines (ticlopidine and clopidogrel) and the platelet glycoprotein IIb/IIIa blockers, in the secondary prevention of coronary heart disease, and high-risk clinical situations, such as unstable angina, acute myocardial infarction and percutaneous coronary intervention, have been reported. Antiplatelet agents should be used, in proper combination, in all relevant cases, as they have been shown to improve the prognosis of various forms of high-risk patients with coronary artery disease.
Acute Coronary Syndrome ; Angina, Unstable ; Angioplasty, Balloon, Coronary ; Aspirin ; Atherosclerosis ; Blood Platelets ; Coronary Artery Disease* ; Coronary Disease ; Coronary Vessels* ; Glycoproteins ; Humans ; Myocardial Infarction ; Percutaneous Coronary Intervention ; Platelet Aggregation Inhibitors* ; Prognosis ; Secondary Prevention ; Thienopyridines

To explore novel ADP receptor inhibitors with anti-thrombotic activity, eighteen compounds were synthesized and their structures were confirmed by 1H NMR and MS. The results showed that the activity of compound C1 was superior to ticlopidine in platelet aggregation inhibition tests in vivo and worthy for further investigation. Compounds A4, B2, C4 and C7 possessed moderate platelet aggregation inhibitory activities.
Animals ; Male ; Molecular Structure ; Platelet Aggregation ; drug effects ; Platelet Aggregation Inhibitors ; chemical synthesis ; chemistry ; pharmacology ; Purinergic P2Y Receptor Antagonists ; chemical synthesis ; chemistry ; pharmacology ; Random Allocation ; Rats ; Rats, Wistar ; Thienopyridines ; chemical synthesis ; chemistry ; pharmacology

No abstract available.
Hemorrhage ; Ticlopidine

No abstract available.
Diabetes Mellitus ; Stents ; Ticlopidine

No abstract available.
Jaundice, Obstructive* ; Pancytopenia* ; Ticlopidine*

No abstract available.
Bupropion ; Sexual Behavior ; Ticlopidine