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ATC code B01 Antithrombotic agents is a therapeutic subgroup of the Anatomical Therapeutic Chemical Classification System, a system of alphanumeric codes developed by the World Health Organization (WHO) for the classification of drugs and other medical products.
The most commonly used anticoagulants in clinical practice, warfarin and the heparin series of anticoagulants and fondaparinux, act to inhibit the action of Factor Xa in various degrees. Traditional models of coagulation developed in the 1960s envisaged two separate cascades, the extrinsic (tissue factor (TF)) pathway and the intrinsic pathway.
Heparin, also known as unfractionated heparin (UFH), is a medication and naturally occurring glycosaminoglycan. [3] [4] Heparin is a blood anticoagulant that increases the activity of antithrombin. [5] It is used in the treatment of heart attacks and unstable angina. [3] It can be given intravenously or by injection under the skin. [3]
Antistasin, the first discovered naturally occurring direct Xa inhibitor Rivaroxaban, the first synthetic direct Xa inhibitor marketed as a drug Prior to the introduction of direct factor Xa inhibitors, vitamin K antagonists such as warfarin were the only oral anticoagulants for over 60 years, and together with heparin have been the main blood ...
Apart from using unfractionated heparin instead, it may be possible to reduce the dose and/or monitor the anti-Xa activity to guide treatment. [ 3 ] The most common side effects include bleeding, which could be severe or even fatal, allergic reactions, injection site reactions, and increases in liver enzyme tests, usually without symptoms. [ 13 ]
Factor Xa can help to prevent the inactivation of factor Va by protecting factor Va from activated protein C. [21] It is likely that factor Xa and activated protein C compete for similar sites on factor Va. [9] Factor Xa is inhibited by the antithrombin III/heparin system, which also acts to inhibit thrombin. [9]
Factor Xa was identified as a promising target for the development of new anticoagulants in the early 1980s. In 1987 the first factor Xa inhibitor, the naturally occurring compound antistasin, was isolated from the salivary glands of the Mexican leech Haementeria officinalis. Antistasin is a polypeptide and a potent Xa inhibitor.
Heparin increases the affinity of antithrombin to thrombin (as well as factor Xa). The direct thrombin inhibitors, a newer class of medication, directly inhibit thrombin by binding to its active site. Recombinant thrombin is available as a powder for reconstitution into aqueous solution.