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However, significant hepatic extraction still occurs because of second pass metabolism, whereby a fraction of venous blood travels through the hepatic portal vein and hepatocytes. The four primary systems that affect the first pass effect of a drug are the enzymes of the gastrointestinal lumen , gut wall enzymes, bacterial enzymes, and hepatic ...
The free fraction is a parameter in pharmacokinetics and receptor-ligand kinetics. One speaks of two different free fractions: Plasma free fraction, previously referred to as ƒ 1, [1] is now referred to as ƒ P according to consensus nomenclature. [2] Tissue free fraction (ƒ ND), previously referred to as ƒ 2 [1]
The fourth edition reviewer noted that “all other related books seem to pale by comparison”. [6] The 6th edition published in 1980 was praised for the extensive bibliography, but also noted that, although “this book is recommended to all those who prescribe drugs”, it had become “too large to be used by medical students as a routine ...
The fraction of bound receptors is known as occupancy. The relationship between occupancy and pharmacological response is usually non-linear. This explains the so-called receptor reserve phenomenon i.e. the concentration producing 50% occupancy is typically higher than the concentration producing 50% of maximum response.
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In pharmacology, the area under the plot of plasma concentration of a drug versus time after dosage (called “area under the curve” or AUC) gives insight into the extent of exposure to a drug and its clearance rate from the body. [2]