The extraction ratio of an organ of elimination (e.g. the liver or the kidneys) can be viewed as the measure of the organ’s relative efficiency in eliminating the drug from the systemic circulation over a single pass through the organ. The extraction ratio may range from 0 to 1. An extraction ration close to 0 … See more When a drug is mainly eliminated by the liver or by the kidney, it is essential to know the extraction ratio of the drug through this organ to be able to evaluate which conditions … See more Intrinsic clearance (CLint): theoretical unrestricted maximum clearance of unbound drug by an eliminating organ, in absence of blood … See more The extraction ratio can be assessed by using the following formula which relates the rate of elimination of the drug to its rate of presentation to the organ of elimination. This … See more Webextraction. Hepatic extraction ratio (ER) is the fraction of drug entering the liver that is extracted. Morphine has a high intrinsic hepatic clearance and about 60% of morphine …
Effect of Liver Disease on Pharmacokinetics - ScienceDirect
WebNov 21, 2024 · The hepatic extraction ratio is determined largely by the free (unbound) fraction of the drug and by the intrinsic clearance rate; Intrinsic clearance is the … WebUnder first-order conditions the activity of the hepatic drug-metabolizing enzymes may be closely approximated by the ratio of the in vitro kinetic constants Vmax and Km, which in turn is equivalent to the intrinsic clearance of the drug. In theory, after appropriate consideration for liver weight, blood flow and rug binding in the blood, the intrinsic … rogue the x-men
Use of intrinsic clearance for prediction of human hepatic
WebThe sensitivity of organ clearance of a drug to changes in binding within blood depends on its unbound clearance. If unbound clearance is low, relative to organ blood flow, the extraction ratio (and clearance) will always be low and dependent on plasma binding. If the extraction ratio is high, elimination becomes perfusion rate-limited and ... WebJul 30, 2024 · E = extraction ratio, F = bioavailability in the gut wall (gut, G) and the liver (hepatic, H). CL int is the whole-organ intrinsic clearance in the gut wall and liver, Ka indicates the absorption rate constant and the fraction unbound in blood and gut wall are described with f u,B and f u,G respectively. WebApr 11, 2024 · Candidate drugs may exhibit higher unbound intrinsic clearances (CLint,u) in human liver microsomes (HLM) relative to human hepatocytes (HH), posing a challenge as to which value is more predictive of in vivo clearance (CL). This work was aimed at better understanding the mechanism(s) underlying this 'HLM:HH disconnect' via examination of … rogue throw deadly throw macro