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Direct thrombin inhibitors (DTIs) are a class of medication that act as anticoagulants (delaying blood clotting) by directly inhibiting the enzyme thrombin. 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. Oral medication A medication is a licenced drug taken to cure or reduce symptoms of an illness or medical condition. ...
An anticoagulant is a substance that prevents coagulation; that is, it stops blood from clotting. ...
The coagulation of blood is a complex process during which blood forms solid clots. ...
Ribbon diagram of the enzyme TIM. TIM is catalytically perfect, meaning its conversion rate is limited, or nearly limited, to its substrate diffusion rate. ...
Thrombin (activated Factor II) is a coagulation protein that has many effects in the coagulation cascade. ...
Heparin is a highly sulfated glycosaminoglycan widely used as an injectable anticoagulant. ...
Warfarin (also known under the brand names of Coumadin®, Jantoven®, Marevan®, and Waran®) is an anticoagulant medication that is administered orally or, very rarely, by injection. ...
Types
There are two 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.[1] Hirudin is a naturally ocurring peptide in the salivary glands of medicinal leeches (Hirudo medicinalis) that has a blood anticoagulant property. ...
Bivalent Hirudin and derivatives were originally discovered in Hirudo medicinalis: Hirudin is a naturally ocurring peptide in the salivary glands of medicinal leeches (Hirudo medicinalis) that has a blood anticoagulant property. ...
Basic Chemical and Pharmacological Properties Bivalirudin is an anticoagulant and acts as direct thrombin antagonist. ...
Lepirudin is an anticoagulant which functions as a direct thrombin inhibitor. ...
Univalent Univalent DTIs include: Argatroban is a small molecule direct thrombin inhibitor. ...
Ximelagatran (Exanta®, H 376/95) is an anticoagulant that has been investigated extensively but is awaiting approval by the Food and Drug Administration (FDA). ...
Dabigatran is an anticoagulant from the class of the direct thrombin inhibitors. ...
Uses Bivalent DTIs enjoy limited use in circumstances where heparin would be indicated but cannot be used, such as the acute coronary syndrome ("unstable angina"). As they are administered by injection (intravenous, intramuscular or subcutaneous), they are less suitable for long-term treatment.[1] Heparin is a highly sulfated glycosaminoglycan widely used as an injectable anticoagulant. ...
There are different forms of heart disease: Coronary heart disease Ischaemic heart disease Cardiovascular disease The study of heart disease is Cardiology This is a disambiguation page — a navigational aid which lists pages that might otherwise share the same title. ...
An intravenous drip in a hospital Intravenous therapy or IV therapy is the administration of liquid substances directly into a vein. ...
Intramuscular injection is an injection of a substance directly into a muscle. ...
The subcutis is the layer of tissue directly underlying the cutis. ...
Argatroban (as well as the hirudins) are used for heparin-induced thrombocytopenia, a rare but serious complication of heparin treatment that requires anticoagulation (as it increases both arterial and venous thrombosis risk) but not with the putative agent, heparin.[1] Heparin-induced thrombocytopenia (HIT) with or without thrombosis (HITT) is thrombocytopenia (low platelet counts) due to the administration of heparin. ...
Thrombosis is the formation of a clot or thrombus inside a blood vessel, obstructing the flow of blood through the circulatory system. ...
Ximelagatran showed good efficacy compared with warfarin in several trials in prevention and treatment of deep vein thrombosis and as thromboprophylaxis in atrial fibrillation.[1] Development was stopped by manufacturer AstraZeneca, however, because of reports of liver enzyme derangements and liver failure.[2] Dabigatran is under development for similar indications. Ximelagatran (Exanta®, H 376/95) is an anticoagulant that has been investigated extensively but is awaiting approval by the Food and Drug Administration (FDA). ...
This article is about Deep-vein thrombosis. ...
Atrial fibrillation (AF or afib) is an abnormal heart rhythm (cardiac arrhythmia) which involves the two small, upper heart chambers (the atria). ...
AstraZeneca PLC (LSE: AZN, NYSE: AZN), is a large Anglo-Swedish pharmaceutical company formed on 6 April 1999 by the merger of Swedish Astra AB and British Zeneca Group. ...
Liver function tests (LFTs or LFs), are groups of clinical biochemistry laboratory blood assays designed to give a doctor or other health professional information about the state of a patients liver. ...
Liver failure is the final stage of liver disease. ...
Monitoring There is no therapeutic drug monitoring widely available for DTIs, in contrast with warfarin (INR) and heparin (APTT). The ecarin clotting time, although not in general clinical use, would be the most appropriate monitoring test.[1] Therapeutic drug monitoring is a branch of clinical chemistry that specialises in the measurement of medication levels in blood. ...
Reference - ^ a b c d e Di Nisio M, Middeldorp S, Büller H (2005). "Direct thrombin inhibitors.". N Engl J Med 353 (10): 1028-40. PMID 16148288.
- ^ AstraZeneca (February 14, 2006). AstraZeneca Decides to Withdraw Exanta. Press release. Retrieved on 2006-05-08.
A news release, press release or press statement is a written or recorded communication directed at members of the news media for the purpose of announcing something claimed as having news value. ...
2006 (MMVI) is a common year starting on Sunday of the Gregorian calendar. ...
May 8 is the 128th day of the year in the Gregorian Calendar (129th in leap years). ...
| Antithrombotics (thrombolytics, anticoagulants, and antiplatelet drugs) (B01) edit | | Vitamin K antagonists: | Acenocoumarol, Clorindione, Dicumarol (Dicoumarol}, Diphenadione, Ethyl biscoumacetate, Phenprocoumon, Phenindione, Tioclomarol, Warfarin Thrombolytic drugs are used in medicine to dissolve blood clots in a procedure termed thrombolysis. ...
An anticoagulant is a substance that prevents coagulation; that is, it stops blood from clotting. ...
An antiplatelet drug is a member of a class of pharmaceuticals that decreases platelet aggregation and inhibits thrombus formation. ...
A section of the Anatomical Therapeutic Chemical Classification System. ...
Acenocoumarol is a anticoagulant that functions as a vitamin K antagonist (like warfarin). ...
Dicumarol (or Dicoumarol) is a anticoagulant that functions by as a Vitamin K antagonist (similar to warfarin). ...
Phenprocoumon is a anticoagulant, functioning as a Vitamin K antagonist. ...
Phenindione is an anticoagulant which functions as a Vitamin K antagonist. ...
Warfarin (also known under the brand names of Coumadin®, Jantoven®, Marevan®, and Waran®) is an anticoagulant medication that is administered orally or, very rarely, by injection. ...
| Heparin group (Platelet
aggregation inhibitors): | Antithrombin III, Bemiparin, Dalteparin, Danaparoid, Enoxaparin, Heparin, Nadroparin, Parnaparin, Reviparin, Sulodexide, Tinzaparin Antithrombin is a small molecule that inactivates several enzymes of the coagulation system. ...
Dalteparin is a low molecular weight heparin. ...
Danaparoid sodium (Orgaran®) is an anticoagulant that works by inhibiting thrombin. ...
Enoxaparin is a low molecular weight heparin manufactured by Sanofi-Aventis. ...
Heparin is a highly sulfated glycosaminoglycan widely used as an injectable anticoagulant. ...
In medicine, low molecular weight heparin (LMWH) is a class of medication used as an anticoagulant in diseases that feature thrombosis, as well as for prophylaxis in situations that lead to a high risk of thrombosis. ...
| Other Platelet
aggregation inhibitors: | Abciximab, Acetylsalicylic acid (Aspirin), Aloxiprin, Beraprost, Ditazole, Carbasalate calcium, Cloricromen, Clopidogrel, Dipyridamole, Epoprostenol, Eptifibatide, Indobufen, Iloprost, Picotamide, Prasugrel, Ticlopidine, Tirofiban, Treprostinil, Triflusal Abciximab (previously known as c7E3 Fab), 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. ...
A very old bottle of Aspirin Aspirin or acetylsalicylic acid is a drug in the family of salicylates, often used as an analgesic (against minor pains and aches), antipyretic (against fever), and anti-inflammatory. ...
Clopidogrel (IPA: ) is a potent oral antiplatelet agent often used in the treatment of coronary artery disease, peripheral vascular disease, and cerebrovascular disease. ...
Dipyridamole is a drug that inhibits platelet aggregation and causes vasodilation. ...
Prostacyclin is a member of the family of lipid molecules known as eicosanoids. ...
Eptifibatide (Integrilin®, Millennium Pharmaceuticals) is a anti-coagulant that selectively blocks the platelet glycoprotein IIb/IIIa receptor. ...
iloprost, an inhalation solution, is sold under the name Ventavis® and is used to treat pulmonary arterial hypertension (PAH). ...
Prasugrel is a novel platelet inhibitor developed by Sankyo and produced by Ube and currently under clinical development in cooperation with Eli Lilly for acute coronary syndromes planned for PCI. Categories: Biochemistry stubs | Pharmacology stubs ...
Ticlopidine is a drug used for its antiplatelet action. ...
// Basic Chemical and Pharmacological Information Tirofiban is a synthetic, nonpeptide inhibitor acting at glycoprotein-(GP)-receptors, type IIb/IIIa, in human thrombocytes. ...
Trepostinil is a synthetic analogue of prostacyclin, used to treat pulmonary hypertension. ...
| | Enzymes: | Alteplase, Ancrod, Anistreplase, Brinase, Drotrecogin alfa, Fibrinolysin, Protein C, Reteplase, Saruplase, Streptokinase, Tenecteplase, Urokinase In blood coagulation, tissue plasminogen activator (tPA) is an enzyme (EC 3. ...
// Basic Chemical, Pharmacological, and Marketing Information Ancrod (also known under its former brand name Arwin® and recently Viprinex®) is an anticoagulant with a triple mode of action. ...
Anistreplase is a thrombolytic drug. ...
// Basic Chemical, Pharmacological and Marketing Data Drotrecogin alpha (activated) is a recombinant form of human activated protein C that has antithrombotic, antiinflammatory, and profibrinolytic properties. ...
// Basic Information Fibrinolysin is an enzyme derived from plasma of bovine origin or extracted from cultures of certain bacteria. ...
Protein C is a major physiological anticoagulant. ...
Reteplase (Retavase®) is a thrombolytic drug, used to treat heart attacks by breaking up the clots that cause them. ...
Streptokinase is an extracellular metallo-enzyme produced by beta-haemolytic streptococcus and is used as an effective and cheap clot-dissolving medication in some cases of myocardial infarction (heart attack) and pulmonary embolism. ...
Tenecteplase is an enzyme used as a thrombolytic drug. ...
Urokinase, also called urokinase-type Plasminogen Activator (uPA) is an enzyme (EC 3. ...
| | Direct thrombin inhibitors: | Argatroban, Bivalirudin, Dabigatran, Desirudin, Hirudin, Lepirudin, Melagatran, Ximelagatran Argatroban is a small molecule direct thrombin inhibitor. ...
Basic Chemical and Pharmacological Properties Bivalirudin is an anticoagulant and acts as direct thrombin antagonist. ...
Dabigatran is an anticoagulant from the class of the direct thrombin inhibitors. ...
Hirudin is a naturally ocurring peptide in the salivary glands of medicinal leeches (Hirudo medicinalis) that has a blood anticoagulant property. ...
Lepirudin is an anticoagulant which functions as a direct thrombin inhibitor. ...
Ximelagatran (Exanta®, H 376/95) is an anticoagulant that has been investigated extensively but is awaiting approval by the Food and Drug Administration (FDA). ...
Ximelagatran (Exanta®, H 376/95) is an anticoagulant that has been investigated extensively but is awaiting approval by the Food and Drug Administration (FDA). ...
| | Other antithrombotics: | Dabigatran, Defibrotide, Dermatan sulfate, Fondaparinux, Rivaroxaban Dabigatran is an anticoagulant from the class of the direct thrombin inhibitors. ...
// Basic Data Defibrotide is a deoxyribonucleic acid derivative (single stranded) derived from cow lung or porcine mucosa. ...
Dermatan sulfate is a glycosaminoglycan, formerly called a mucopolysaccharide, found mostly in skin, but also in blood vessels, heart valves, tendons, and lungs. ...
Fondaparinux (Arixtra) is a medication that is an anticoagulant. ...
Rivaroxaban (also known as BAY 59-7939) is an oral anticoagulant under development by Bayer. ...
| | Non-medicinal: | Citrate, EDTA, Oxalate An anticoagulant is a substance that prevents coagulation; that is, it stops blood from clotting. ...
Chemical strucutre of citric acid. ...
EDTA is the chemical compound ethylenediaminetetraacetic acid. ...
An oxalate (called also: ethanedioate) is a salt or ester of oxalic acid. ...
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