Antiplatelet
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Antiplatelet
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 due ...
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Anticoagulants
Anticoagulants, commonly known as blood thinners, are chemical substances that prevent or reduce coagulation of blood, prolonging the clotting time. Some of them occur naturally in blood-eating animals such as leeches and mosquitoes, where they help keep the bite area unclotted long enough for the animal to obtain some blood. As a class of medications, anticoagulants are used in therapy for thrombotic disorders. Oral anticoagulants (OACs) are taken by many people in pill or tablet form, and various intravenous anticoagulant dosage forms are used in hospitals. Some anticoagulants are used in medical equipment, such as sample tubes, blood transfusion bags, heart–lung machines, and dialysis equipment. One of the first anticoagulants, warfarin, was initially approved as a rodenticide. Anticoagulants are closely related to antiplatelet drugs and thrombolytic drugs by manipulating the various pathways of blood coagulation. Specifically, antiplatelet drugs inhibit platelet aggre ...
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Aspirin
Aspirin, also known as acetylsalicylic acid (ASA), is a nonsteroidal anti-inflammatory drug (NSAID) used to reduce pain, fever, and/or inflammation, and as an antithrombotic. Specific inflammatory conditions which aspirin is used to treat include Kawasaki disease, pericarditis, and rheumatic fever. Aspirin is also used long-term to help prevent further heart attacks, ischaemic strokes, and blood clots in people at high risk. For pain or fever, effects typically begin within 30 minutes. Aspirin works similarly to other NSAIDs but also suppresses the normal functioning of platelets. One common adverse effect is an upset stomach. More significant side effects include stomach ulcers, stomach bleeding, and worsening asthma. Bleeding risk is greater among those who are older, drink alcohol, take other NSAIDs, or are on other blood thinners. Aspirin is not recommended in the last part of pregnancy. It is not generally recommended in children with infections because of the risk of ...
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Adenosine Diphosphate (ADP) Receptor Inhibitor
Adenosine diphosphate ( ADP) receptor inhibitors are a drug class of antiplatelet agents, used in the treatment of acute coronary syndrome (ACS) or in preventive treatment for patients who are in risk of thromboembolism, myocardial infarction or a stroke. These drugs antagonize the P2Y12 platelet receptors and therefore prevent the binding of ADP to the P2Y12 receptor. This leads to a decrease in aggregation of platelets, prohibiting thrombus formation. The P2Y12 receptor is a surface bound protein found on blood platelets. They belong to G protein-coupled purinergic receptors (GPCR) and are chemoreceptors for ADP. The first drug introduced in this class was ticlopidine but due to adverse effects it is not much used today. Ticlopidine, clopidogrel and prasugrel (Efient) are all thienopyridines that cause irreversible inhibition of P2Y12 receptor. They are all prodrugs which need to be converted to an active metabolite in-vivo to inhibit the P2Y12 receptor. On the other hand, nov ...
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Clopidogrel
Clopidogrel — sold under the brand name Plavix, among others — is an antiplatelet medication used to reduce the risk of heart disease and stroke in those at high risk. It is also used together with aspirin in heart attacks and following the placement of a coronary artery stent (dual antiplatelet therapy). It is taken by mouth. Its effect starts about two hours after intake and lasts for five days. Common side effects include headache, nausea, easy bruising, itching, and heartburn. More severe side effects include bleeding and thrombotic thrombocytopenic purpura. While there is no evidence of harm from use during pregnancy, such use has not been well studied. Clopidogrel is in the thienopyridine-class of antiplatelets. It works by irreversibly inhibiting a receptor called P2Y12 on platelets. Clopidogrel was patented in 1982, and approved for medical use in 1997. It is on the World Health Organization's List of Essential Medicines. In 2020, it was the 29th most commonly ...
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Clopidogrel
Clopidogrel — sold under the brand name Plavix, among others — is an antiplatelet medication used to reduce the risk of heart disease and stroke in those at high risk. It is also used together with aspirin in heart attacks and following the placement of a coronary artery stent (dual antiplatelet therapy). It is taken by mouth. Its effect starts about two hours after intake and lasts for five days. Common side effects include headache, nausea, easy bruising, itching, and heartburn. More severe side effects include bleeding and thrombotic thrombocytopenic purpura. While there is no evidence of harm from use during pregnancy, such use has not been well studied. Clopidogrel is in the thienopyridine-class of antiplatelets. It works by irreversibly inhibiting a receptor called P2Y12 on platelets. Clopidogrel was patented in 1982, and approved for medical use in 1997. It is on the World Health Organization's List of Essential Medicines. In 2020, it was the 29th most commonly ...
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Ticagrelor
Ticagrelor, sold under the brand name Brilinta among others, is a medication used for the prevention of stroke, heart attack and other events in people with acute coronary syndrome, meaning problems with blood supply in the coronary arteries. It acts as a platelet aggregation inhibitor by antagonising the P2Y12 receptor. The drug is produced by AstraZeneca. The most common side effects include dyspnea (difficulty breathing), bleeding and raised uric acid level in the blood. It was approved for medical use in the European Union in December 2010, and in the United States in July 2011. In 2020, it was the 247th most commonly prescribed medication in the United States, with more than 1million prescriptions. Medical uses In the US, ticagrelor is indicated to reduce the risk of stroke in people with acute ischemic stroke or high-risk transient ischemic attack. In the EU, ticagrelor, co-administered with acetylsalicylic acid (aspirin), is indicated for the prevention of atherothrom ...
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Ticagrelor
Ticagrelor, sold under the brand name Brilinta among others, is a medication used for the prevention of stroke, heart attack and other events in people with acute coronary syndrome, meaning problems with blood supply in the coronary arteries. It acts as a platelet aggregation inhibitor by antagonising the P2Y12 receptor. The drug is produced by AstraZeneca. The most common side effects include dyspnea (difficulty breathing), bleeding and raised uric acid level in the blood. It was approved for medical use in the European Union in December 2010, and in the United States in July 2011. In 2020, it was the 247th most commonly prescribed medication in the United States, with more than 1million prescriptions. Medical uses In the US, ticagrelor is indicated to reduce the risk of stroke in people with acute ischemic stroke or high-risk transient ischemic attack. In the EU, ticagrelor, co-administered with acetylsalicylic acid (aspirin), is indicated for the prevention of atherothrom ...
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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 ...
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P2Y Receptor
P2Y receptors are a family of purinergic G protein-coupled receptors, stimulated by nucleotides such as adenosine triphosphate, adenosine diphosphate, uridine triphosphate, uridine diphosphate and UDP-glucose.To date, 8 P2Y receptors have been cloned in humans: P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, P2Y12, P2Y13 and P2Y14. P2Y receptors are present in almost all human tissues where they exert various biological functions based on their G-protein coupling. P2Y receptors mediate responses including vasodilation, blood clotting, and immune response. Due to their ubiquity and variety in function, they are a common biological target in pharmacological development. Structure P2Y receptors are membrane proteins belonging to the class A family of G protein-coupled receptors (GPCRs). P2Y receptor proteins display large-scale structural domains typical of GPCRs, consisting of seven hydrophobic transmembrane helices connected by three short extracellular loops and three variably siz ...
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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 ...
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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 ...
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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 ...
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