Is dabigatran a direct thrombin inhibitor?
Dabigatran etexilate: an oral direct thrombin inhibitor for the management of thromboembolic disorders.
How does dabigatran bind to thrombin?
Dabigatran is a small (472 Da) peptidomimetic that directly inhibits thrombin by binding to its active site via ionic interactions.
What clotting factors does dabigatran inhibit?
Conclusion: Dabigatran affects the activities of many coagulation factors, including factors II, V, VIII, and IX, as well as the antifactor VIII inhibitor.
How is dabigatran metabolized?
Dabigatran is metabolized via conjugation into four acyl glucuronides, each of which is a direct thrombin inhibitor with less than 10% of the activity of the parent compound [23]. Dabigatran neither is metabolized by nor induces any cytochrome P450 subtype [22].
How is dabigatran distributed?
Distribution volume of dabigatran is 60-70 l, its half-life is 12-24 h and its oral biodisposability is 7% [1,3]. Dabigatran is eliminated in urine and stools. It is mainly excreted in a non-metabolized form by urine by 80%, and conjugated with glucoronic acid and eliminated in stools by 20%.
How do I monitor my dabigatran?
The time between last intake of dabigatran and blood collection must be determined as this influences dabigatran levels and thus the results of the coagulation assay. A dilute thrombin clotting time assay such as the Hemoclot® Thrombin Inhibitor (HTI) assay is the recommended assay to determine dabigatran drug levels.
Is dabigatran a factor 2 inhibitor?
Mechanism of action. Dabigatran is a selective direct competitive thrombin inhibitor that binds to and inhibits both circulating and thrombus-bound thrombin (factor IIa). It produces a rapid onset of predictable anticoagulation.
Does dabigatran affect PT INR?
International normalized ratio (INR) Regardless of the reagent used, dabigatran has little effect on the PT and INR at clinically relevant plasma concentrations [15].
What is a high level of dabigatran in thrombin?
Note that dabigatran levels greater than 40 ng/mL result in thrombin times greater than 200 seconds. Plasma-diluted thrombin time assay sensitivity to dabigatran.
How are dabigatran levels measured?
Other methods proposed to measure dabigatran levels are the thrombin time (TT), ecarin clotting time, and TT by Hemoclot thrombin inhibitor assay (Aniara). 4 These assays have linearity coefficients that range from 0.8568 to 0.9164 in multiple dose trials.
What is the plasma-diluted thrombin time used for?
Hello, Deanna, and thank you for your question. We use the plasma-diluted thrombin time to measure the direct thrombin inhibitors [DTIs] dabigatran, argatroban, or bivalirudin.
What is the normal thrombin time for DTI?
A normal thrombin time in many laboratories is less than 21 seconds. When measuring DTIs, the test plasma is first diluted 1:10 with imidazole buffer, then one part of the dilution is added to two parts pooled normal plasma.