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14-September-2008 18:02:39 - Anticoagulant An anticoagulant is a substance that prevents coagulation; that is, it stops blood from clotting. A group of pharmaceuticals called anticoagulants can be used in vivo as a medication for thrombotic disorders. Some chemical compounds are used in medical equipment, such as test tubes, blood transfusion bags, and renal dialysis equipment. Contents 1 As medications 1.1 Vitamin K antagonists 1.1.1 Adverse effects 1.1.2 Available agents 1.2 Heparin and derivative substances 1.2.1 Low molecular weight heparin 1.2.2 Synthetic pentasaccharide inhibitors of factor Xa 1.2.3 Major pharmaceutical Heparin recall due to contamination 1.3 Direct thrombin inhibitors 2 Anticoagulants outside the body 3 See also 4 References As medications Anticoagulants are given to people to stop thrombosis blood clotting inappropriately in the blood vessels. This is useful in primary and secondary prevention of deep vein thrombosis, pulmonary embolism, myocardial infarctions and strokes in those who are predisposed. Vitamin K antagonists The oral anticoagulants are a class of pharmaceuticals that act by antagonizing the effects of vitamin K. Examples include warfarin. It is important to note that they take at least 48 to 72 hours for the anticoagulant effect to develop fully. In cases when any immediate effect is required, heparin must be given concomitantly. Generally, these anticoagulants are used to treat patients with deep-vein thrombosis DVT, pulmonary embolism PE, atrial fibrillation AF, and mechanical prosthetic heart valves. Adverse effects Patients aged 80 years or more may be especially susceptible to bleeding complications with a rate of 13 bleeds per 100 person-years.1 These oral anticoagulants are used widely as poisons for mammalian pests, especially rodents. For details, see rodenticide and warfarin. Available agents Warfarin Coumadin This is the main agent used in the U.S. and UK2 Acenocoumarol and phenprocoumon This is used more commonly outside the U.S. and the UK Brodifacoum Rat poison, not used medically Phenindione Heparin and derivative substances Heparin is a biological substance, usually made from pig intestines. It works by activating antithrombin III, which blocks thrombin from clotting blood. Heparin can be used in vivo by injection, and also in vitro to prevent blood or plasma clotting in or on medical devices. Vacutainer brand test tubes containing heparin are usually colored green. Low molecular weight heparin Low molecular weight heparin is a more highly processed product that is useful as it does not require monitoring of the APTT coagulation parameter it has more predictable plasma levels and has fewer side effects. Synthetic pentasaccharide inhibitors of factor Xa Fondaparinux is a synthetic sugar composed of the five sugars pentasaccharide in heparin that bind to antithrombin. It is a smaller molecule than low molecular weight heparin. Idraparinux Major pharmaceutical Heparin recall due to contamination In March 2008 major recalls of Heparin were announced by pharmaceuticals due to a suspected and unknown contamination of the raw Heparin stock imported from China 3 4. The U.S. Food and Drug Administration was quoted as stating that at least 19 deaths were believed linked to a raw Heparin ingredient imported from the People's Republic of China, and that they had also received 785 reports of serious injuries associated with the drug's use. According to the New York Times: 'Problems with heparin reported to the agency include difficulty breathing, nausea, vomiting, excessive sweating and rapidly falling blood pressure that in some cases led to life-threatening shock'. Direct thrombin inhibitors Main article: direct thrombin inhibitor Another type of anticoagulant is the direct thrombin inhibitor.5 Current members of this class include argatroban, lepirudin, bivalirudin, and dabigatran. An oral direct thrombin inhibitor, ximelagatran Exanta was denied approval by the Food and Drug Administration FDA in September 2004 1 and was pulled from the market entirely in February 2006 after reports of severe liver damage and heart attacks. 2 Anticoagulants outside the body Laboratory instruments, test tubes, blood transfusion bags, and medical and surgical equipment will get clogged up and become nonoperational if blood is allowed to clot. Chemicals can be added to stop blood clotting. Apart from heparin, most of these chemicals work by binding calcium ions, preventing the coagulation proteins from using them. EDTA is denoted by mauve or purple caps on Vacutainer brand test tubes. This chemical strongly and irreversibly binds calcium. It is in a powdered form. Citrate is usually in blue Vacutainer tube. It is in liquid form in the tube and is used for coagulation tests, as well as in blood transfusion bags. It gets rid of the calcium, but not as strongly as EDTA. Correct proportion of this anticoagulant to blood is crucial because of the dilution. It can be in the form of sodium citrate or ACD. Oxalate has a mechanism similar to that of citrate. It is the anticoagulant used in fluoride grey top tubes. For the meaning of more colors, see Vacutainer#including coagulants. See also Anticoagulation in pregnancy References ^ Hylek EM, Evans-Molina C, Shea C, Henault LE, Regan S 2007. Major hemorrhage and tolerability of warfarin in the first year of therapy among elderly patients with atrial fibrillation. Circulation 115 21: 2689-96. doi:10.1161/CIRCULATIONAHA.106.653048. PMID 17515465. ^ Ron Winslow; Avery Johnson 2007-12-10. Race Is on for the Next Blood Thinner, Wall Street Journal, p. A12. Retrieved on 2008-01-06. ...in a market now dominated by one of the oldest mainstay pills in medicine: the blood thinner warfarin. At least five next-generation blood thinners are in advanced testing to treat or prevent potentially debilitating or life-threatening blood clots in surgery and heart patients. First candidates could reach the market in 2009. ^ New York Times, March 6, 2008, Drug Tied to China Had Contaminant, F.D.A. Says, retrieved 2008-03-07 ^ New York Times, March 7, 2008, German Authorities Report Problems With Blood Thinner, retrieved 2008-03-07 ^ Di Nisio M, Middeldorp S, Büller HR 2005. Direct thrombin inhibitors. N. Engl. J. Med. 353 10: 1028-40. doi:10.1056/NEJMra044440. PMID 16148288. v d e Antithrombotics thrombolytics, anticoagulants and antiplatelet drugs B01 Antiplatelet drugs Glycoprotein IIb/IIIa inhibitors Abciximab Eptifibatide Tirofiban ADP receptor/P2Y12 inhibitors Clopidogrel Ticlopidine Prasugrel Prostaglandin analogue PGI2 Beraprost Prostacyclin Iloprost Treprostinil COX inhibitors Acetylsalicylic acid/Aspirin Aloxiprin Carbasalate calcium Other Ditazole Cloricromen Dipyridamole Indobufen Picotamide Triflusal Anticoagulants Vitamin K antagonists inhibit II, VII, IX, X Acenocoumarol Clorindione Coumatetralyl Dicoumarol Dicumarol Diphenadione Ethyl biscoumacetate Phenprocoumon Phenindione Tioclomarol Warfarin Heparin group/ glycosaminoglycans low molecular weight heparin Bemiparin, Certoparin, Dalteparin, Enoxaparin, Nadroparin, Parnaparin, Reviparin, Tinzaparin heparinoid Danaparoid, Sulodexide, Dermatan sulfate Direct thrombin II inhibitors Argatroban Bivalirudin Dabigatran Desirudin Hirudin Lepirudin Melagatran Ximelagatran Factor Xa inhibitors Apixaban Otamixaban Rivaroxaban oligosaccharides Fondaparinux, Idraparinux Other Defibrotide Ramatroban Antithrombin III Protein C Drotrecogin alfa Thrombolytic drugs/ fibrinolytics plasminogen activators: TPA Alteplase, Reteplase, Tenecteplase UPA Urokinase, Saruplase Streptokinase Anistreplase Monteplase other serine endopeptidases: Ancrod Fibrinolysin Brinase Non-medicinal Citrate EDTA Oxalate v d e Major drug groups Gastrointestinal tract/metabolism A stomach acid Antacids, H2 antagonists, Proton pump inhibitors Antiemetics Laxatives Antidiarrhoeals/Antipropulsives Anti-obesity drugs Anti-diabetics Vitamins Dietary minerals Blood and blood forming organs B Antithrombotics Anticoagulants, Antiplatelets, Thrombolytics Antihemorrhagics Cardiovascular system C cardiac therapy/antianginals Cardiac glycosides, Antiarrhythmics, Cardiac stimulant Antihypertensives Diuretics Vasodilators Beta blockers renin-angiotensin system ACE inhibitors, Angiotensin II receptor antagonists, Renin inhibitors Antihyperlipidemics Skin D Emollients Cicatrizant Antipruritics Reproductive system G Hormonal contraception Fertility agents SERMs Sex hormones Endocrine system H Corticosteroids Sex hormones Thyroid hormones Antithyroid agent Infections and infestations J, P Antibiotics Antivirals Vaccines Antifungals Antiparasitic Antiprotozoals, Anthelmintics Malignant and immune disease L Anticancer agents Immunostimulators Immunosuppressants Muscles, bones, and joints M Anabolic steroids Anti-inflammatories NSAID Antirheumatics Corticosteroids Muscle relaxants Brain and nervous system N Anesthetics General, Local Analgesics Anticonvulsants Mood stabilizers Psycholeptic Anxiolytics, Antipsychotics, Hypnotics/Sedatives Psychoanaleptic Antidepressants, Stimulants/Psychostimulants Respiratory system R Bronchodilators Decongestants H1 antagonists Other ATC V Antidotes Contrast media Radiopharmaceuticals Dressing Retrieved from http://en..org/wiki/Anticoagulant Categories: Anticoagulants Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page Languages Türkçe العربية Català Česky Deutsch Español Euskara Français Italiano Nederlands 日本語 ‪Norsk nynorsk‬ Polski Português РуÑ?Ñ?кий СрпÑ?ки / Srpski Suomi Svenska Türkçe УкраїнÑ?ька This page was last modified on 5 September 2008, at 13:00
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