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Know details about Dabigatran etexilate drug ?

 Dabigatran Etexilate 

Brand name:- Pradaxa 

Dabigatran etexilate is an anticoagulant used for the prevention of venous thromboembolic events or stroke in patients with recent elective hip or knee replacement surgery and atrial fibrillation.Dabigatran Etexilate is a novel oral anticoagulant (NOAC). It works by preventing the formation of blood clots in the body.

Pharmacodynamic:-

Dabigatran etexilate is a double prodrug that is hydrolyzed to the active dabigatran by intestinal and hepatic carboxylesterases.Dabigatran is a reversible competitive thrombin inhibitor that directly inhibits the conversion by thrombin of fibrinogen to fibrin, impairing the clotting process and acting as an anticoagulant. Dabigatran use prolongs coagulation markers such as the activated partial thromboplastin time (aPTT), ecarin clotting time (ECT), thrombin time (TT), and dilute thrombin time (dTT), but not the international normalized ratio (INR), which cannot be used in this context as it can in warfarin monitoring.

As with all anticoagulant therapies, dabigatran carries a risk of bleeding, which may increase with concomitant use of antiplatelet agents, fibrinolytic therapy, heparins, or chronic NSAID use, and should be monitored for. Premature discontinuation of dabigatran, in the absence of an alternative anticoagulant, also carries an increased risk of thromboembolic events. Due to the risk of an epidural or spinal hematoma, dabigatran should generally not be used in the context of neuraxial anesthesia or spinal puncture; if such use is unavoidable, careful monitoring should be employed. Dabigatran should not be used in patients with prosthetic heart valves due to an increased occurrence of major bleeding and thromboembolic events. Dabigatran is a substrate of the P-gp transporter and should generally not be administered together with P-gp inhibitors or inducers, especially in patients with impaired renal function. Lastly, dabigatran or any other direct-acting oral anticoagulant should not be administered in patients with triple-positive antiphospholipid syndrome (APS) due to an increased risk of recurrent thrombotic events. In case of the need for emergency reversal, idarucizumab is available for use in adult patients; the safety and efficacy of idarucizumab has not been established in pediatric patients yet, for whom reversal may be achieved through hemodialysis, prothrombin complex concentrates, or recombinant FVIIa. However, none of these have been sufficiently evaluated in clinical trials..

 Pharmacokinetics:- 

Dabigatran has a half-life of approximately 12–14 h and exerts a maximum anticoagulation effect within 2–3 hours after ingestion.[citation needed] Fatty foods delay the intestinal absorption of dabigatran, although the bioavailability of the drug is unaffected. One study showed that absorption may be moderately decreased if taken with a proton pump inhibitor. Dabigatran excretion through P-glycoprotein pumps is slowed in patients taking strong p-glycoprotein pump inhibitors such as quinidine, verapamil, and amiodarone, thus raising plasma levels of dabigatran.

Dabigatran is available as dabigatran etexilate mesilate, formulated as the prodrug dabigatran etexilate.

Mechanism of action:- 

Dabigatran reversibly binds to the active site on the thrombin molecule, preventing thrombin-mediated activation of coagulation factors. Furthermore, dabigatran can inactivate thrombin even when thrombin is fibrin-bound; it reduces thrombin-mediated inhibition of fibrinolysis and, therefore, may enhance fibrinolysis.

Used:- 

Used to prevent stroke and harmful blood clots (such as in your legs or lungs) if you have a certain type of irregular heartbeat (atrial fibrillation). Dabigatran is also used to treat blood clots in the veins of your legs (deep vein thrombosis) or lungs (pulmonary embolism) and to reduce the risk of them occurring again. This medication may also be used to prevent these blood clots from forming after hip replacement surgery. Dabigatran is an anticoagulant that works by blocking a certain substance (a clotting protein called thrombin) in your blood. This helps to keep blood flowing smoothly in your body.Dabigatran should not be used to prevent blood clots from forming after artificial heart valve replacement.

Side effects:- 

Common side effects of Dabigatran Etexilate:- 


Nausea, Anemia (low number of red blood cells), Gastrointestinal bleeding, Dyspepsia, Diarrhea, Abdominal pain, Nosebleeds, Skin bleeding,
Easy bruising, minor bleeding (such as nosebleed, bleeding from cuts), upset stomach, or heartburn may occur.

Dose:- AS DIRECTED BY YOUR DOCTOR.


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