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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 ]
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 ...
Side effects may include bleeding, most commonly from the nose, gastrointestinal tract (GI) or genitourinary system. [2] Compared to the risk of bleeding with warfarin use, direct factor Xa inhibitors have a higher risk of GI bleeding, but lower risk of bleeding in the brain. [2]
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 ...
The primary sign of augmented renal clearance is an increase in the creatinine clearance well above that which would be considered normal. Commonly, ARC is defined as a creatinine clearance of greater than 130 mL/min, but the effects of increased clearance on therapy are not directly correlated to a specific number.
Therefore, their use in patients with creatinine clearance rate <30 mL/min may need to be avoided. [12] Apart from using unfractionated heparin instead, it may be possible to reduce the dose and/or monitor the anti-Xa activity to guide treatment. [3]
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}}}}
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