Danaparoid
Brand name:- Orgaran.
Danaparoid is a preparation containing mainly heparan sulfate which is a heparin - like substance found in many tissues, having less potent anticoagulant action than heparin. Danaparoid is obtained from pig gut mucosa , and is used in cases with heparin induced thrombocytopenia.
Pharmacodynamic:-
Danaparoid contains a mixture of heparan sulfate, dermatan sulfate and chondroitin sulfate in amounts of approximately 84%, 12% and 4%, respectively . Danaparoid is as an antithrombotic agent that prevents the formation of fibrin in the coagulation pathway. It has a high antifactor Xa to antifactor IIa (thrombin) activity that primarily works via antithrombin III-mediated inhibition of factor Xa . The ratio of antifactor Xa to antifactor II activity is ≥ 20:1 . Danaparoid has a minor effect on platelet function and aggregation Label. In a worldwide compassionate-use programme involving a total of 667 patients with heparin-induced thrombocytopenia (HIT), treatment with danaparoid resulted in 93% of successful outcomes in resolving HIT .
In healthy volunteers, danaparoid caused significantly less prolongation o f the activated partial thromboplastin time (APTT) and was associated with a significantly lower thrombin time than unfractionated heparin (UFH) and low molecular weight heparins (LMWHs) . Danaparoid displays lower lipolytic activity than UFH in vitro and in healthy individuals, leading to lower plasma levels of free fatty acids . Danaparoid has been associated with the cross-reactivity with pathogenic heparin-induced platelet-factor (PF4) antibodies, which occurs in about 10 % or more by in vitro testing .The clinical relevance of this effect is not fully understood .
Mechanism of action:-
In the coagulation cascade leading to clot formation, factor X and factor II requires activation to promote subsequent conversion of fibrinogen to fibrin. The mechanism of action of danaparoid resulting in anticoagulant and antithrombic effects involves a complex interaction between 2 components, factor IIa and in particular, factor Xa . Via binding to antithrombin and inducing a conformational change 4, danaparoid enhances and catalyzes the the binding of factor Xa to antithrombin, which induces antithrombin-mediated inactivation of factor Xa. This leads to inhibition of thrombin generation and subsequently, thrombus formation . Danaparoid also weakly enhances antithrombin III and heparin cofactor II inactivation of factor IIa . There is evidence that danaparoid also suppresses the activation of factor IX which, in conjunction with simultaneous inhibition of factor X, may lead to antithrombic effects .
Used:-
Danaparoid is used to prevent deep venous thrombosis, a condition in which harmful blood clots form in the blood vessels of the legs. These blood clots can travel to the lungs and can become lodged in the blood vessels of the lungs, causing a condition called pulmonary embolism. Danaparoid is used for several days after hip replacement surgery, while you are unable to walk. It is during this time that blood clots are most likely to form.
Side effects:-
Bleeding, low platelet & Possibly Asthma exacerbations, due to allergies to sulfites contained within the medicine (no case has been reported to date).
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