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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 ...
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 ...
Rivaroxaban (Xarelto) was the first approved FXa inhibitor to become commercially available in Europe and Canada in 2008. [1] The second one was apixaban (Eliquis), approved in Europe in 2011 [2] and in the United States in 2012. [3] The third one edoxaban (Lixiana, Savaysa) was approved in Japan in 2011 and in Europe and the US in 2015. [4]
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.
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]
[14] [15] Renal clearance and degradation account for the most part for the systemic clearance of desulfatohirudins and there is accumulation of the drug in patients with chronic kidney disease. These drugs should not be used in patients with impaired renal function, since there is no specific antidote available to reverse the effects. [14]
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}}}}