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The monitoring of warfarin and keeping the international normalized ratio (INR) between 2.0 and 3.0, along with avoiding over and under treatment, has driven a search for an alternative. [3] [14] A naturally occurring inhibitor of factor Xa was reported in 1971 by Spellman et al. from the dog hookworm. [15]
Enoxaparin sodium, sold under the brand name Lovenox among others, is an anticoagulant medication (blood thinner). [11] It is used to treat and prevent deep vein thrombosis (DVT) and pulmonary embolism (PE) including during pregnancy and following certain types of surgery. [ 11 ]
Like semuloparin, bemiparin is classified as an ultra-LMWH because of its low molecular mass of 3600 g/mol on average. [3] ( Enoxaparin has 4500 g/mol.) These heparins have lower anti-thrombin activity than classical LMWHs and act mainly on factor Xa, reducing the risk of bleeding.
Thrombin demonstrates a high level of allosteric regulation. [2] Allosterism in thrombin is regulated by the exosites 1 and 2 and the sodium binding site. A recent patent review has shown that the general consensus among researchers is that allosteric inhibitors may provide a more regulatable anticoagulant. [3]
Given the fact that HIT predisposes strongly to new episodes of thrombosis, simply discontinuing the heparin administration is insufficient. Generally, an alternative anticoagulant is needed to suppress the thrombotic tendency while the generation of antibodies stops and the platelet count recovers.
The low molecular weight of both sulodexide fractions allows for extensive oral absorption compared to unfractionated heparin.The pharmacological effects of sulodexide differ substantially from other glycosaminoglycans and are mainly characterized by a prolonged half-life and reduced effect on global coagulation and bleeding parameters. [1]
Edoxaban, sold under the brand name Lixiana among others, is an anticoagulant medication and a direct factor Xa inhibitor. [3] It is taken by mouth. [3]Compared with warfarin it has fewer drug interactions.
Danaparoid sodium (Orgaran) is an anticoagulant [1] with an antithrombotic action due to inhibition of thrombin generation (TGI) by two mechanisms: indirect inactivation of Factor Xa via AT and direct inhibition of thrombin activation of Factor IX (an important feedback loop for thrombin generation).