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The primary administration data for the 3 newly approved NOACs are shown in the Figure. All 3 have similar biologic half-lives (T½), but the dosing is twice daily (bid) for dabigatran and apixaban, or once daily (qd) for rivaroxaban based on the results of ROCKET AF. Renal excretion is highest for dabigatran, significant for rivaroxaban, and smaller for apixaban. This characteristic becomes important in patients with declining creatine clearance (CrCl), when impact of dose and clearance becomes important. All 3 of these NOACs have interactions with the P-glycoprotein (Pgp) system, and the Factor Xa inhibitors have interactions with the cytochrome P450 3A4 (CYP3A4) system. Gastroesophageal reflux disease (GERD) is of concern with dabigatran but not with the factor Xa inhibitors. Superiority to warfarin has been demonstrated with dabigatran and apixaban, versus noninferiority with rivaroxaban (discussed in the following Figures). Finally, for many physicians the important question with these NOACs will be reversal of the anticoagulation. [101][102]
Reiffel JA. Am J Med 2013; 126: 00-00.
[101] Prothrombin complex concentrates to reverse warfarin-related bleeding. Med Lett Drugs Ther. 2011;53:78-79.
[102] Eerenberg ES, Kamphuisen PW, Sijpkens MK, Meijers JC, Buller HR, Levi M. Reversal of rivaroxaban and dabigatran by prothrombin complex concentrate: a randomized, placebo-controlled, crossover study in healthy subjects. Circulation. 2011;124:1573-1579.