Bivalirudin
   HOME
*





Bivalirudin
Bivalirudin (Bivalitroban), sold under the brand names Angiomax and Angiox and manufactured by The Medicines Company, is a direct thrombin inhibitor (DTI). Chemically, it is a synthetic congener of the naturally occurring drug hirudin, found in the saliva of the medicinal leech ''Hirudo medicinalis''. Bivalirudin lacks many of the limitations seen with indirect thrombin inhibitors, such as heparin. A short, synthetic peptide, it is a potent and highly specific inhibitor of thrombin that inhibits both circulating and clot-bound thrombin, while also inhibiting thrombin-mediated platelet activation and aggregation. Bivalirudin has a quick onset of action and a short half-life. It does not bind to plasma proteins (other than thrombin) or to red blood cells. Therefore, it has a predictable antithrombotic response. There is no risk for heparin-induced thrombocytopenia or heparin-induced thrombosis-thrombocytopenia syndrome. It does not require a binding cofactor such as antithrombin ...
[...More Info...]      
[...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]  


picture info

Percutaneous Coronary Intervention
Percutaneous coronary intervention (PCI) is a non-surgical procedure used to treat narrowing of the coronary arteries of the heart found in coronary artery disease. The process involves combining coronary angioplasty with stenting, which is the insertion of a permanent wire-meshed tube that is either drug eluting (DES) or composed of bare metal (BMS). The stent delivery balloon from the angioplasty catheter is inflated with media to force contact between the struts of the stent and the vessel wall (stent apposition), thus widening the blood vessel diameter. After accessing the blood stream through the femoral or radial artery, the procedure uses coronary catheterization to visualise the blood vessels on X-ray imaging. After this, an interventional cardiologist can perform a coronary angioplasty, using a balloon catheter in which a deflated balloon is advanced into the obstructed artery and inflated to relieve the narrowing; certain devices such as stents can be deployed to keep ...
[...More Info...]      
[...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]  


Direct Thrombin Inhibitor
Direct thrombin inhibitors (DTIs) are a class of medication that act as anticoagulants (delaying blood clotting) by directly inhibiting the enzyme thrombin (factor IIa). Some are in clinical use, while others are undergoing clinical development. Several members of the class are expected to replace heparin (and derivatives) and warfarin in various clinical scenarios. Types There are three types of DTIs, dependent on their interaction with the thrombin molecule. ''Bivalent'' DTIs (hirudin and analogs) bind both to the active site and exosite 1, while univalent DTIs bind only to the active site. The third class of inhibitors, which are gaining importance recently, is the allosteric inhibitors. Bivalent Hirudin and derivatives were originally discovered in ''Hirudo medicinalis'': * Hirudin * Bivalirudin (transient inhibition - is cleaved by thrombin) * Lepirudin * Desirudin Univalent Univalent DTIs include: * Argatroban * Inogatran * Melagatran (and its prodrug ximelagatran) * Dabiga ...
[...More Info...]      
[...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]  


Direct Thrombin Inhibitors
Direct thrombin inhibitors (DTIs) are a class of medication that act as anticoagulants (delaying blood clotting) by directly inhibiting the enzyme thrombin (factor IIa). Some are in clinical use, while others are undergoing clinical development. Several members of the class are expected to replace heparin (and derivatives) and warfarin in various clinical scenarios. Types There are three types of DTIs, dependent on their interaction with the thrombin molecule. ''Bivalent'' DTIs (hirudin and analogs) bind both to the active site and exosite 1, while univalent DTIs bind only to the active site. The third class of inhibitors, which are gaining importance recently, is the allosteric inhibitors. Bivalent Hirudin and derivatives were originally discovered in ''Hirudo medicinalis'': * Hirudin * Bivalirudin (transient inhibition - is cleaved by thrombin) * Lepirudin * Desirudin Univalent Univalent DTIs include: * Argatroban * Inogatran * Melagatran (and its prodrug ximelagatran) * Dabiga ...
[...More Info...]      
[...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]  


picture info

Intravenous Therapy
Intravenous therapy (abbreviated as IV therapy) is a medical technique that administers fluids, medications and nutrients directly into a person's vein. The intravenous route of administration is commonly used for rehydration or to provide nutrients for those who cannot, or will not—due to reduced mental states or otherwise—consume food or water by mouth. It may also be used to administer medications or other medical therapy such as blood products or electrolytes to correct electrolyte imbalances. Attempts at providing intravenous therapy have been recorded as early as the 1400s, but the practice did not become widespread until the 1900s after the development of techniques for safe, effective use. The intravenous route is the fastest way to deliver medications and fluid replacement throughout the body as they are introduced directly into the circulatory system and thus quickly distributed. For this reason, the intravenous route of administration is also used for the consump ...
[...More Info...]      
[...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]  


picture info

Congener (chemistry)
In chemistry, congeners are chemical substances "related to each other by origin, structure, or function". Common origin and structure Any significant quantity of a polyhalogenated compound is by default a blend of multiple molecule types because each molecule forms independently, and chlorine and bromine do not strongly select which site(s) they bond to. *Polychlorinated biphenyls (PCBs) are a family of 209 congeners. * Polybrominated biphenyls and polychlorinated diphenyl ethers are also families of 209 congeners. Similarly polychlorinated dibenzodioxins, polychlorinated dibenzofurans, polychlorinated terphenyls, polychlorinated naphthalene, polychloro phenoxy phenol, and polybrominated diphenyl ethers (PBDEs) ( pentabromodiphenyl ether, octabromodiphenyl ether, decabromodiphenyl ether), etc. are also groups of congeners. Common origin *Congener (alcohol), substances other than alcohol (desirable or undesirable) also produced during fermentation. *Congeners of oleic acids ca ...
[...More Info...]      
[...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]  


Hirudin
Hirudin is a naturally occurring peptide in the salivary glands of blood-sucking leeches (such as ''Hirudo medicinalis'') that has a blood anticoagulant property. This is fundamental for the leeches’ habit of feeding on blood, since it keeps a host's blood flowing after the worm's initial puncture of the skin. Hirudin (MEROPS I14.001) belongs to a superfamily (MEROPS IM) of protease inhibitors that also includes haemadin (MEROPS I14.002) and antistasin (MEROPS I15). Structure During his years in Birmingham and Edinburgh, John Berry Haycraft had been actively engaged in research and published papers on the coagulation of blood, and in 1884, he discovered that the leech secreted a powerful anticoagulant, which he named hirudin, although it was not isolated until the 1950s, nor its structure fully determined until 1976. Full length hirudin is made up of 65 amino acids. These amino acids are organized into a compact N-terminal domain containing three disulfide bonds and a C-termi ...
[...More Info...]      
[...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]  


picture info

Hirudo Medicinalis
''Hirudo medicinalis'', the European medicinal leech, is one of several species of leeches used as "medicinal leeches". Other species of ''Hirudo'' sometimes also used as medicinal leeches include '' H. orientalis'', ''H. troctina'', and '' H. verbana''. The Asian medicinal leech includes '' Hirudinaria manillensis'', and the North American medicinal leech is '' Macrobdella decora''. Morphology The general morphology of medicinal leeches follows that of most other leeches. Fully mature adults can be up to 20 cm in length, and are green, brown, or greenish-brown with a darker tone on the dorsal side and a lighter ventral side. The dorsal side also has a thin red stripe. These organisms have two suckers, one at each end, called the anterior and posterior suckers. The posterior is used mainly for leverage, whereas the anterior sucker, consisting of the jaw and teeth, is where the feeding takes place. Medicinal leeches have three jaws (tripartite) that resemble saws, on which ...
[...More Info...]      
[...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]  


picture info

Heparin
Heparin, also known as unfractionated heparin (UFH), is a medication and naturally occurring glycosaminoglycan. Since heparins depend on the activity of antithrombin, they are considered anticoagulants. Specifically it is also used in the treatment of heart attacks and unstable angina. It is given intravenously or by injection under the skin. Other uses for its anticoagulant properties include inside blood specimen test tubes and kidney dialysis machines. Common side effects include bleeding, pain at the injection site, and low blood platelets. Serious side effects include heparin-induced thrombocytopenia. Greater care is needed in those with poor kidney function. Heparin is contraindicated for suspected cases of vaccine-induced pro-thrombotic immune thrombocytopenia (VIPIT) secondary to SARS-CoV-2 vaccination, as heparin may further increase the risk of bleeding in an anti-PF4/heparin complex autoimmune manner, in favor of alternative anticoagulant medications (such as arg ...
[...More Info...]      
[...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]  


picture info

Thrombin
Thrombin (, ''fibrinogenase'', ''thrombase'', ''thrombofort'', ''topical'', ''thrombin-C'', ''tropostasin'', ''activated blood-coagulation factor II'', ''blood-coagulation factor IIa'', ''factor IIa'', ''E thrombin'', ''beta-thrombin'', ''gamma-thrombin'') is a serine protease, an enzyme that, in humans, is encoded by the ''F2'' gene. Prothrombin (coagulation factor II) is proteolytically cleaved to form thrombin in the clotting process. Thrombin in turn acts as a serine protease that converts soluble fibrinogen into insoluble strands of fibrin, as well as catalyzing many other coagulation-related reactions. History After the description of fibrinogen and fibrin, Alexander Schmidt hypothesised the existence of an enzyme that converts fibrinogen into fibrin in 1872. Prothrombin was discovered by Pekelharing in 1894. Physiology Synthesis Thrombin is produced by the enzymatic cleavage of two sites on prothrombin by activated Factor X (Xa). The activity of factor Xa is greatly ...
[...More Info...]      
[...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]  




Heparin-induced Thrombocytopenia
Heparin-induced thrombocytopenia (HIT) is the development of thrombocytopenia (a low platelet count), due to the administration of various forms of heparin, an anticoagulant. HIT predisposes to thrombosis (the abnormal formation of blood clots inside a blood vessel) because platelets release microparticles that activate thrombin, thereby leading to thrombosis. When thrombosis is identified the condition is called heparin-induced thrombocytopenia and thrombosis (HITT). HIT is caused by the formation of abnormal antibodies that activate platelets. If someone receiving heparin develops new or worsening thrombosis, or if the platelet count falls, HIT can be confirmed with specific blood tests. The treatment of HIT requires stopping heparin treatment, and both protection from thrombosis and choice of an agent that will not reduce the platelet count any further. Several alternatives are available for this purpose; mainly used are danaparoid, fondaparinux, argatroban, and bivalirudin. W ...
[...More Info...]      
[...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]  


picture info

Angina
Angina, also known as angina pectoris, is chest pain or pressure, usually caused by ischemia, insufficient blood flow to the Cardiac muscle, heart muscle (myocardium). It is most commonly a symptom of coronary artery disease. Angina is typically the result of vascular occlusion, obstruction or vasospasm, spasm of the coronary arteries, arteries that supply blood to the heart muscle. The main mechanism of coronary artery obstruction is atherosclerosis as part of coronary artery disease. Other causes of angina include cardiac arrhythmia, abnormal heart rhythms, heart failure and, less commonly, anemia. The term derives from the Latin ''angere'' ("to strangle") and ''pectus'' ("chest"), and can therefore be translated as "a strangling feeling in the chest". There is a weak relationship between severity of angina and degree of oxygen deprivation in the heart muscle, however, the severity of angina does not always match the degree of oxygen deprivation to the heart or the risk of a ...
[...More Info...]      
[...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]  


picture info

NSTEMI
A myocardial infarction (MI), commonly known as a heart attack, occurs when blood flow decreases or stops to the coronary artery of the heart, causing damage to the heart muscle. The most common symptom is chest pain or discomfort which may travel into the shoulder, arm, back, neck or jaw. Often it occurs in the center or left side of the chest and lasts for more than a few minutes. The discomfort may occasionally feel like heartburn. Other symptoms may include shortness of breath, nausea, feeling faint, a cold sweat or feeling tired. About 30% of people have atypical symptoms. Women more often present without chest pain and instead have neck pain, arm pain or feel tired. Among those over 75 years old, about 5% have had an MI with little or no history of symptoms. An MI may cause heart failure, an irregular heartbeat, cardiogenic shock or cardiac arrest. Most MIs occur due to coronary artery disease. Risk factors include high blood pressure, smoking, diabetes, lack of exercis ...
[...More Info...]      
[...Related Items...]     OR:     [Wikipedia]   [Google]   [Baidu]