Abstract

REVIEW ON CHEMISTRY AND PHARMACOLOGY OF DABIGATRAN A POTENT ANTICOAGULANT

Jyoti Thakur, Amit Chaudhary, Diksha Choudhary, Bhupendra Tomar, M. P. Tanwar, G. C. Verma.

ABSTRACT

Direct Coagulase Inhibitors category of medication that acts as anticoagulants (delaying blood clotting) by directly inhibiting the accelerator coagulase (factor II a). Thrombin is a serine protease that plays a key role in blood clotting, which makes it a promising target for the treatment of thrombotic diseases. Anticoagulant a drug called as blood diluter prevents, treats, and reduces the risk of blood clots. They work by preventing blood coagulation to form a clot in the vital organs such as the heart, lungs, and brain. It is a direct thrombin inhibitor, and functions by directly inhibiting both free and fibrin- bound thrombin. There is one specific antidote, idarucizumab, which reverses the effect of dabigatran. It is a competitive, synthetic, and reversible direct thrombin inhibitor. By inhibiting thrombin it disrupts the coagulation cascade and inhibits the formation of clots. It is used to prevent stroke and systemic embolism in patients with atrial fibrillation, in whom anticoagulation therapy is indicated. It also decreases the risk of venous thromboembolic events in patients that have undergone total hip or knee replacement surgery. We designed and synthesized dabigatran etexilate acid salt. The biological evaluations reveal that the compounds possess moderate activity of antiplatelet aggregation induced by thrombin in vitro.

Keywords: Dabigatran Etexilate; Thrombin inhibitor; Anti coagulant; Atrial fibrillation.