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Antiplatelet Agent
An antiplatelet drug (antiaggregant), also known as a platelet agglutination inhibitor or platelet aggregation inhibitor, is a member of a class of pharmaceuticals that decrease platelet aggregation and inhibit thrombus formation. They are effective in the arterial circulation where anticoagulants have little effect. They are widely used in primary and secondary prevention of thrombotic cerebrovascular or cardiovascular disease. Antiplatelet therapy with one or more of these drugs decreases the ability of blood clots to form by interfering with the platelet activation process in primary hemostasis. Antiplatelet drugs can reversibly or irreversibly inhibit the process involved in platelet activation resulting in decreased tendency of platelets to adhere to one another and to damaged blood vessels' endothelium. Choice A 2006 review states: "...low-dose aspirin increases the risk of major bleeding 2-fold compared with placebo. However, the annual incidence of major bleeding du ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pharmacology
Pharmacology is a branch of medicine, biology and pharmaceutical sciences concerned with drug or medication action, where a drug may be defined as any artificial, natural, or endogenous (from within the body) molecule which exerts a biochemical or physiological effect on the cell, tissue, organ, or organism (sometimes the word ''pharmacon'' is used as a term to encompass these endogenous and exogenous bioactive species). More specifically, it is the study of the interactions that occur between a living organism and chemicals that affect normal or abnormal biochemical function. If substances have medicinal properties, they are considered pharmaceuticals. The field encompasses drug composition and properties,functions,sources,synthesis and drug design, molecular and cellular mechanisms, organ/systems mechanisms, signal transduction/cellular communication, molecular diagnostics, interactions, chemical biology, therapy, and medical applications and antipathogenic capabilities. ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Prasugrel
Prasugrel, sold under the brand name Effient in the US, Australia and India, and Efient in the EU) is a medication used to prevent formation of blood clots. It is a platelet inhibitor and an irreversible antagonist of P2Y12 ADP receptors and is of the thienopyridine drug class. It was developed by Daiichi Sankyo Co. and produced by Ube and marketed in the United States in cooperation with Eli Lilly and Company. Prasugrel was approved for use in the European Union in February 2009, and in the US in July 2009, for the reduction of thrombotic cardiovascular events (including stent thrombosis) in people with acute coronary syndrome (ACS) who are to be managed with percutaneous coronary intervention (PCI). Medical uses Prasugrel is used in combination with low dose aspirin to prevent thrombosis in patients with acute coronary syndrome, including unstable angina pectoris, non-ST elevation myocardial infarction (NSTEMI), and ST elevation myocardial infarction (STEMI), who are plann ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Thromboxane Synthase Inhibitors
Thromboxane A synthase 1 (, platelet, cytochrome P450, family 5, subfamily A), also known as TBXAS1, is a cytochrome P450 enzyme that, in humans, is encoded by the ''TBXAS1'' gene. Function This gene encodes a member of the cytochrome P450 superfamily of enzymes. The cytochrome P450 proteins are monooxygenases that catalyze many reactions involved in drug metabolism and synthesis of cholesterol, steroids, and other lipids. However, this protein is considered a member of the cytochrome P450 superfamily on the basis of sequence similarity rather than functional similarity. This endoplasmic reticulum membrane protein catalyzes the conversion of prostaglandin H2 to thromboxane A2, a potent vasoconstrictor and inducer of platelet aggregation, and also to 12-Hydroxyheptadecatrienoic acid (i.e. 12-(''S'')-hydroxy-5''Z'',8''E'',10''E''-heptadecatrienoic acid or 12-HHT) an agonist of Leukotriene B4 receptors (i.e. BLT2 receptors) and mediator of certain BLT2 receptor actions. The enz ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Thromboxane Inhibitor
Thromboxane is a member of the family of lipids known as eicosanoids. The two major thromboxanes are thromboxane A2 and thromboxane B2. The distinguishing feature of thromboxanes is a 6-membered ether-containing ring. Thromboxane is named for its role in blood clot formation (thrombosis). Production Thromboxane-A synthase, an enzyme found in platelets, converts the arachidonic acid derivative prostaglandin H2 to thromboxane. Mechanism Thromboxane acts by binding to any of the thromboxane receptors, G-protein-coupled receptors coupled to the G protein Gq. Functions Thromboxane is a vasoconstrictor and a potent hypertensive agent, and it facilitates platelet aggregation. It is in homeostatic balance in the circulatory system with prostacyclin, a related compound. The mechanism of secretion of thromboxanes from platelets is still unclear. They act in the formation of blood clots and reduce blood flow to the site of a clot. If the cap of a vulnerable plaque erodes or ruptures ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dipyridamole
Dipyridamole (trademarked as Persantine and others) is a nucleoside transport inhibitor and a PDE3 inhibitor medication that inhibits blood clot formation when given chronically and causes blood vessel dilation when given at high doses over a short time. Medical uses * Dipyridamole is used to dilate blood vessels in people with peripheral arterial disease and coronary artery disease * Dipyridamole has been shown to lower pulmonary hypertension without significant drop of systemic blood pressure * It inhibits formation of pro-inflammatory cytokines (MCP-1, MMP-9) in vitro and results in reduction of hsCRP in patients. * It inhibits proliferation of smooth muscle cells in vivo and modestly increases unassisted patency of synthetic arteriovenous hemodialysis grafts. * It increases the release of tissue plasminogen activator from brain microvascular endothelial cells. * It results in an increase of 13-hydroxyoctadecadienoic acid and decrease of 12-hydroxyeicosatetraenoic acid in ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Adenosine Reuptake Inhibitor
An adenosine reuptake inhibitor (AdoRI) is a type of drug which acts as a reuptake inhibitor for the purine nucleoside and neurotransmitter adenosine by blocking the action of one or more of the equilibrative nucleoside transporters (ENTs). This in turn leads to increased extracellular concentrations of adenosine and therefore an increase in adenosinergic neurotransmission. List of AdoRIs * Acadesine * Acetate * Barbiturates * Benzodiazepines * Calcium channel blockers * Carbamazepine * Carisoprodol * Cilostazol * Cyclobenzaprine * Dilazep * Dipyridamole * Estradiol * Ethanol * Flumazenil * Hexobendine * Hydroxyzine * Indomethacin * Inosine * KF24345 * Meprobamate * Nitrobenzylthioguanosine * Nitrobenzylthioinosine * Papaverine * Pentoxifylline * Phenothiazines * Phenytoin * Progesterone * Propentofylline * Propofol * Puromycin * R75231 * RE 102 BS * Soluflazine * Toyocamycin * Tracazolate * Tricyclic antidepressants See also * Adenosinergic * Reuptake inhibit ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tirofiban
Tirofiban, sold under the brand name Aggrastat, is an antiplatelet medication. It belongs to a class of antiplatelets named glycoprotein IIb/IIIa inhibitors. Tirofiban is a small molecule inhibitor of the protein-protein interaction between fibrinogen and the platelet integrin receptor GP IIb/IIIa and is the first drug candidate whose origins can be traced to a pharmacophore-based virtual screening lead. Tirofiban has been available as a generic medication in the United States since April 2021. Medical uses Tirofiban is indicated to reduce the rate of thrombotic cardiovascular events (combined endpoint of death, myocardial infarction, or refractory ischemia/repeat cardiac procedure) in people with non-ST elevation acute coronary syndrome. Contraindications and precautions Tirofiban is contraindicated in patients with: * Known hypersensitivity to any component of tirofiban. * History of thrombocytopenia with prior exposure to tirofiban. * Active internal bleeding, or histor ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Eptifibatide
Eptifibatide (Integrilin, Millennium Pharmaceuticals, also co-promoted by Schering-Plough/Essex), is an antiplatelet drug of the glycoprotein IIb/IIIa inhibitor class. Eptifibatide is a cyclic heptapeptide derived from a disintegrin protein () found in the venom of the southeastern pygmy rattlesnake ('' Sistrurus miliarius barbouri''). It belongs to the class of the arginin-glycin-aspartat-mimetics and reversibly binds to platelets. Eptifibatide has a short half-life. The drug is the third inhibitor of GPIIb/IIIa that has found broad acceptance after the specific antibody abciximab and the non-peptide tirofiban entered the global market. Indications Eptifibatide is used to reduce the risk of acute cardiac ischemic events (death and/or myocardial infarction) in patients with unstable angina or non-ST-segment-elevation (e.g., non-Q-wave) myocardial infarction (i.e., non-ST-segment elevation acute coronary syndromes) both in patients who are to receive non surgery (conservative) ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Abciximab
Abciximab, a glycoprotein IIb/IIIa receptor antagonist manufactured by Janssen Biologics BV and distributed by Eli Lilly under the trade name ReoPro, is a platelet aggregation inhibitor mainly used during and after coronary artery procedures like angioplasty to prevent platelets from sticking together and causing thrombus (blood clot) formation within the coronary artery. It is a glycoprotein IIb/IIIa inhibitor. While abciximab has a short plasma half-life, due to its strong affinity for its receptor on the platelets, it may occupy some receptors for weeks. In practice, platelet aggregation gradually returns to normal about 96 to 120 hours after discontinuation of the drug. Abciximab is made from the Fab fragments of an immunoglobulin that targets the glycoprotein IIb/IIIa receptor on the platelet membrane. Indications for use Abciximab is indicated for use in individuals undergoing percutaneous coronary intervention (angioplasty with or without stent placement). The use of abc ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Glycoprotein IIB/IIIA Inhibitor
In medicine, glycoprotein IIb/IIIa inhibitors, also GpIIb/IIIa inhibitors, is a class of antiplatelet agents. Several GpIIb/IIIa inhibitors exist: * abciximab (abcixifiban) (ReoPro) * eptifibatide (Integrilin) * tirofiban (Aggrastat) * roxifiban * orbofiban Use Glycoprotein IIb/IIIa inhibitors are frequently used during percutaneous coronary intervention (angioplasty with or without intracoronary stent placement). They work by preventing platelet aggregation and thrombus formation. They do so by inhibition of the GpIIb/IIIa receptor on the surface of the platelets. They may also be used to treat acute coronary syndromes, without percutaneous coronary intervention, depending on TIMI risk. They should be given intravenously. The oral form is associated with increased mortality and hence should not be given. In integrin nomenclature glycoprotein IIb/IIIa is called αIIbβ3. History Their development arose from the understanding of Glanzmann's thrombasthenia Glanzmann's thr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Vorapaxar
Vorapaxar (brand name Zontivity, formerly known as SCH 530348) is a thrombin receptor (protease-activated receptor, PAR-1) antagonist based on the natural product himbacine, discovered by Schering-Plough and developed by Merck & Co. Medical uses Vorapaxar is used for persons with a history of myocardial infarction (heart attack) or persons with peripheral arterial disease Peripheral artery disease (PAD) is an abnormal narrowing of arteries other than those that supply the heart or brain. When narrowing occurs in the heart, it is called coronary artery disease, and in the brain, it is called cerebrovascular diseas .... Studies have shown that this medication can reduce the rate of combined endpoint cardiovascular death, MI, stroke, and urgent coronary revascularization. Contraindications Vorapaxar is contraindicated for people with a history of stroke, transient ischemic attack, or intracerebral hemorrhage. In studies of vorapaxar on persons with prior ischemic stroke, there ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cilostazol
Cilostazol, sold under the brand name Pletal among others, is a medication used to help the symptoms of intermittent claudication in peripheral vascular disease. If no improvement is seen after 3 months, stopping the medication is reasonable. It may also be used to prevent stroke. It is taken by mouth. Common side effects include headache, diarrhea, dizziness, and cough. Serious side effects may include decreased survival in those with heart failure, low platelets, and low white blood cells. Cilostazol is a phosphodiesterase 3 inhibitor which works by inhibiting platelet aggregation and dilating arteries. Cilostazol was approved for medical use in the United States in 1999. It is available as a generic medication. In 2019, it was the 347th most commonly prescribed medication in the United States, with more than 800thousand prescriptions. Medical uses Cilostazol is approved for the treatment of intermittent claudication in the United States and United Kingdom. Cilostazol is a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
