Atrial fibrillation, which affects more than 2 million Americans, involves very fast and uncoordinated contractions of the heart’s two upper heart chambers (atria) and is one of the most common types of abnormal heart rhythm.
Mechanism of action:
Dabigatran and its acyl glucuronides are competitive, direct thrombin inhibitors. Because thrombin (serine protease) enables the conversion of fibrinogen into fibrin during the coagulation cascade, its inhibition prevents the development of a thrombus. Both free and clot-bound thrombin, and thrombin-induced platelet aggregation are inhibited by the active moieties.
The safety and efficacy of Pradaxa were studied in a clinical trial comparing Pradaxa with the anticoagulant warfarin. In the trial, patients taking Pradaxa had fewer strokes than those who took warfarin.
At recommended therapeutic doses, dabigatran etexilate prolongs the aPTT, ECT, and TT. With an oral dose of 150 mg twice daily the median peak aPTT is approximately 2x control. Twelve hours after the last dose the median aPTT is 1.5x control, with less than 10% of patients exceeding 2x control.
As with other approved anti-clotting drugs, bleeding, including life-threatening and fatal bleeding, was among the most common adverse reactions reported by patients treated with Pradaxa. Gastrointestinal symptoms, including an uncomfortable feeling in the stomach (dyspepsia), stomach pain, nausea, heartburn, and bloating also were reported.
Pradaxa was approved with a Medication Guide that informs patients of the risk of serious bleeding. The guide will be distributed each time a patient fills a prescription for the medication.
Pradaxa, manufactured by Boehringer Ingelheim Pharmaceuticals Inc. of Ridgefield, Conn., will be available in 75 milligram and 150 milligram capsules.
http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm230241.htm
http://www.pradaxa.com/pdf/PI_PRADAXA.pdf
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