Rivaroxaban

pharmacological · immune-hematologic · cardiovascular · Oral

Rivaroxaban. Selective, reversible direct FXa inhibitor. First DOAC approved. Once-daily dosing in AF reflects the receptor binding profile… Oral half-life 6.2 h.

Selective, reversible direct FXa inhibitor. First DOAC approved. Once-daily dosing in AF reflects the receptor binding profile rather than plasma t½ (t½ ~7–11 h would otherwise suggest BID). Andexanet alfa specific reversal available.

PK: Xu 2012 (PMID:22242932), oral ONE-COMPARTMENT population fit in 2290 acute-coronary-syndrome patients — the same structure the solver uses — verbatim "The estimated absorption rate, apparent clearance and volume of distribution were 1.24 h(-1) ..., 6.48 l h(-1) ... and 57.9 l". The half-life is that fit's own ln2 x V/CL = 6.19 h rather than a second paper's number, and it sits inside the independently measured "5.7-9.2 h at steady state" (PMID:16328318). F is pinned to 1 BECAUSE 57.9 L is apparent (V/F). The measured bioavailability is a conditional floor, not a constant: "high oral bioavailability (>= 80%)" holds up to 10 mg fasted or fed, but at 15-20 mg only WITH food, and fasted exposure at those doses is "less than dose proportional" (PMID:23458226). Values stored until 2026-09-06 were unsourced, and the 10.7 h half-life was the midpoint of "mean 10.6 vs 10.8 h", the two arms of PMID:32959922. CAVEAT: clearance falls with age, AUC "41% higher in elderly" (PMID:23381840), with terminal half-life 11-13 h in the elderly against 5-9 h in young adults. The warfarin review PMID:15911722 was removed from this record; it never mentions rivaroxaban.

Pharmacokinetics

Related compounds

Sources: PMID:23999929, PMID:15748242, PMID:22242932, PMID:16328318, PMID:23458226, PMID:23381840