How does dabigatran etexilate work?

How does dabigatran etexilate work?

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.

What is the pharmacological action of dabigatran?

Dabigatran is a potent, synthetic, reversible, non-peptide thrombin inhibitor. The inhibition of thrombin results in decreased formation of fibrin and reduces thrombin-stimulated platelet aggregation and thus prevents the formation of thrombi.

Is dabigatran a direct thrombin inhibitor?

Dabigatran etexilate: an oral direct thrombin inhibitor for prophylaxis and treatment of thromboembolic diseases. Pharmacotherapy.

What is the half life of dabigatran?

Table 2.

Property Warfarin Dabigatran
Onset of action 36–72 h 0.5–2 h
Elimination half-life 20–60 h 12–14 h
Duration of action 48–96 h 24 h
Stable, predictable pharmacokinetics No Yes

Can I take vitamin D with dabigatran?

No interactions were found between Pradaxa and Vitamin D3. This does not necessarily mean no interactions exist. Always consult your healthcare provider.

What is the most common side effect of Pradaxa?

The most frequent adverse reactions leading to discontinuation of PRADAXA were bleeding and gastrointestinal events (i.e., dyspepsia, nausea, upper abdominal pain, gastrointestinal hemorrhage, and diarrhea).

How is dabigatran activated?

Understanding the role of thrombin in coagulation is central to a discussion of the mechanism of action of dabigatran and other anticoagulants. Endothelial injury results in the exposure of tissue factor which interacts with activated factor VII to initiate the coagulation cascade.

What are the side effects of dabigatran?

The most common side effect of dabigatran is bleeding more easily than normal, such as having nosebleeds, bleeding gums and bruising. It tends to happen in the first few weeks of treatment or if you’re unwell. Always carry your anticoagulant alert card with you.

Is bivalirudin reversible?

The binding of bivalirudin to thrombin is reversible as thrombin slowly cleaves the bivalirudin-Arg3-Pro4 bond, resulting in recovery of thrombin active site functions.

Which are direct thrombin inhibitors?

Currently, four parenteral direct inhibitors of thrombin activity are FDA-approved in North America: lepirudin, desirudin, bivalirudin and argatroban. Of the new oral DTIs, dabigatran etexilate is the most studied and promising of these agents.

What is the antidote for dabigatran?

Idarucizumab (Praxbind) is the first drug specifically designed to be an antidote for or a prophylaxis against major bleeding in patients taking the anticoagulant dabigatran (Pradaxa).

Can dabigatran be stopped?

Do not stop taking dabigatran without talking to your doctor first. If you stop taking dabigatran, the rate at which your blood clots will return to what it was before you started taking it, usually within a day or two of stopping.

Which is the active metabolite of O dabigatran etexilate?

o Dabigatran etexilate is cleaved by esterase-catalyzed hydrolysis to the active metabolite dabigatran following oral administration. Dabigatran undergoes hepatic glucuronidation to active acyl glucuronide isomers with similar activity as the parent compound, but these isomers account for less than 10% of total dabigatran in the plasma.

Are there any drug interactions with dabigatran etexilate?

Drug Interactions. Cobicistat: May increase serum concentrations of the active metabolite(s) of Dabigatran Etexilate. Monitor therapy Collagenase (Systemic): Anticoagulants may enhance the adverse/toxic effect of Collagenase (Systemic). Specifically, the risk of injection site bruising and/or bleeding may be increased.

How long does it take for dabigatran to reach steady state?

Dabigatran plasma concentrations and anticoagulant effects are dose dependent and predictable, and peak within 0.5 to 2 hours (average, 1.5 hours) of oral administration. Steady-state dabigatran concentrations are achieved ≈3 days after multiple-dose administration in healthy volunteers.

How is dabigatran a reversible direct thrombin inhibitor?

Prodrug lacking anticoagulant activity that is converted in vivo to the active dabigatran, a specific, reversible, direct thrombin inhibitor that inhibits both free and fibrin-bound thrombin.

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