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Apixaban is a highly selective, orally bioavailable, and reversible direct inhibitor of free and clot-bound factor Xa. Factor Xa catalyzes the conversion of prothrombin to thrombin, the final enzyme in the coagulation cascade that is responsible for fibrin clot formation. [ 25 ]
The renal clearance ratio or fractional excretion is a relative measure of the speed at which a constituent of urine passes through the kidneys. [ 1 ] [ 2 ] It is defined by following equation: c l e a r a n c e r a t i o o f X = C x C i n {\displaystyle clearance\ ratio\ of\ X={\frac {C_{x}}{C_{in}}}}
Direct factor Xa inhibitors include rivaroxaban, apixaban and edoxaban, and are types of direct oral anticoagulant (DOAC), which are blood thinning drugs, one of the classes of antithrombotic drugs.
In these cases, clearance is almost synonymous with renal clearance or renal plasma clearance. Each substance has a specific clearance that depends on how the substance is handled by the nephron. Clearance is a function of 1) glomerular filtration , 2) secretion from the peritubular capillaries to the nephron , and 3) reabsorption from the ...
Substance Approximate molecular mass (g/mol) [1] Effective molecular radius [1] conc. in ultrafiltrate / conc. in blood plasma [1]; sodium: 23: 0.1: 1.0 potassium: 39: 0.14: 1.0 chloride: 35.5
Creatinine clearance exceeds GFR due to creatinine secretion, [4] which can be blocked by cimetidine. Both GFR and C Cr may be accurately calculated by comparative measurements of substances in the blood and urine, or estimated by formulas using just a blood test result ( eGFR and eC Cr ) The results of these tests are used to assess the ...
Fractional excretion of other substances can be measured to determine kidney clearance including urea, uric acid, and lithium. These can be used in patients undergoing diuretic therapy, since diuretics induce a natriuresis. Thus, the urinary sodium concentration and FE Na may be higher in patients receiving diuretics in spite of prerenal ...
The p-methoxy group of apixaban connects to S1 pocket of FXa but does not appear to have any interaction with any residues in this region of FXa. The pyrazole N-2 nitrogen atom of apixaban interacts with Gln-192 and the carbonyl oxygen interacts with Gly-216. The phenyl lactam group of apixaban is positioned between Tyr-99 and Phe-174 and due ...