Description
Dabigatran etexilate mesylate is a clinical direct thrombin inhibitor and a new type of oral anticoagulant. It can inhibit the formation of thrombus by reversibly and potently competing with the fibrin-specific binding site of thrombin to block fibrin generation.
Chemical Properties
Off-White to Pale Yellow Solid
Uses
Nonpeptide, direct thrombin inhibitor. Antithrombotic.
Clinical Use
Dabigatran Etexilate Mesylate is a direct thrombin inhibitor indicated to reduce the risk of stroke and systemic embolism in patients with nonvalvular atrial fibrillation.
Definition
ChEBI: A methanesulfonate salt obtained by reaction of dabigatran etexilate with one equivalent of dabigatran etexilate. A prodrug for dabigatran, a thrombin inhibitor and anticoagulant which is used for the prevention of stroke and systemic embolism.
Biological Activity
Dabigatran etexilate mesylate (BIBR 1048MS) is an orally active prodrug of Dabigatran. Dabigatran etexilate mesylate has anticoagulant properties and can prevent venous thromboembolism and stroke due to atrial fibrillation.
Mechanism of action
Dabigatran etexilate mesylate is a prodrug of dabigatran that is metabolized in the body and converted to the active dabigatran. Compared with warfarin, dabigatran etexilate mesylate does not require frequent monitoring of coagulation function and dose adjustment during treatment, and there are fewer interactions between drugs and is not affected by eating, thus improving patients' medication compliance.
Side effects
The most common adverse reactions to Dabigatran Etexilate Mesylate (150 mg) were bleeding and gastrointestinal events (i.e. dyspepsia, nausea, epigastric pain, gastrointestinal bleeding, and diarrhoea). Very few patients experienced drug hypersensitivity (including urticaria, rash and pruritus), anaphylactic oedema, anaphylactic reactions and anaphylaxis.
in vivo
Dabigatran etexilate mesylate (BIBR 1048MS; oral; 10, 20 and 50 mg/kg for rats and 1, 2.5 and 5 mg/kg for monkeys) has dose- and time-dependent anticoagulant effects and has maximum effects between 30 and 120 min after administration, respectively.Dabigatran etexilate mesylate maximally and significantly prolongs partial thromboplastin time (aPTT) to 25.2, 38.4 and 78.3 s in 30 min after 10, 20 and 50 mg/kg oral doses, respectively.Dabigatran etexilate mesylate maximally prolongs the aPTT to 34.3 s, 44.0 s, and 63.0 s, respectively, 2h after 1, 2.5 or 5 mg/kg doses in the monkey.
