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Drug Extraction Ratio

The document discusses drug extraction ratios and hepatic drug clearance. It defines extraction ratio as the fraction of a drug removed from perfusing blood during its passage through an organ like the liver. Drugs with high extraction ratios have a large first-pass effect and low oral bioavailability. Hepatic clearance is determined by liver blood flow, the fraction of free drug, and intrinsic liver clearance. The ratio of hepatic clearance to liver blood flow is the extraction ratio, which can be high, intermediate, or low. Rowland's equation relates hepatic clearance to these factors. Drugs are classified as having high, low, or intermediate extraction ratios depending on their dependence on liver blood flow or metabolic capacity.

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Heru Fajar Syaputra
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485 views8 pages

Drug Extraction Ratio

The document discusses drug extraction ratios and hepatic drug clearance. It defines extraction ratio as the fraction of a drug removed from perfusing blood during its passage through an organ like the liver. Drugs with high extraction ratios have a large first-pass effect and low oral bioavailability. Hepatic clearance is determined by liver blood flow, the fraction of free drug, and intrinsic liver clearance. The ratio of hepatic clearance to liver blood flow is the extraction ratio, which can be high, intermediate, or low. Rowland's equation relates hepatic clearance to these factors. Drugs are classified as having high, low, or intermediate extraction ratios depending on their dependence on liver blood flow or metabolic capacity.

Uploaded by

Heru Fajar Syaputra
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© © All Rights Reserved
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DRUG EXTRACTION

RATIO
R1
EXTRACTION

• Removal of a drug by an organ can be specified as the extraction ratio, that is, the fraction or
percentage of the drug removed from the perfusing blood during its passage through the organ
• Drugs that have a high hepatic extraction ratio have a large first-pass effect and the bioavailability
of these drugs after oral administration is low.
HEPATIC DRUG CLEARANCE

• Liver metabolism is the major route for elimination for a wide variety of drugs & it can be affected by a variety of
parameters.

• Hepatic drug clearance can be defined as the volume of blood perfusing the liver that is cleared of the drug per unit
of time. There are three major parameters that determine drug elimination by the liver:

• blood flow through the liver (Q), which reflects drug delivery to the liver
• the fraction of drug in the blood that is free or not bound to plasma proteins and capable of interacting with hepatic enzymes (f)
• the intrinsic ability of hepatic enzymes to metabolize the drug, which is commonly refered to as “intrinsic clearance” (Clint).
Intrinsic clearance is the ability of the liver to remove drug in the absence of flow limitations and binding to cells or proteins in
the blood.

• The ratio of the hepatic clearance of a drug to the hepatic blood flow is called the extraction ratio of the drug. Extraction
ratio can be generally classified as high (>0.7), intermediate (0.3-0.7) or low (<0.3) according to the fraction of drug
removed during one pass through the liver.

https://tmedweb.tulane.edu/pharmwiki/doku.php/hepatic_drug_clearance
ROWLAND'S EQUATION

• Hepatic Clearance: Cl(h) = Q [(f x Clint)/(Q+ f x Clint)]

• Q = hepatic blood flow


• f = fraction of free drug (not bound)

• Clint = intrinsic capacity of the hepatocytes to metabolize a drug

https://tmedweb.tulane.edu/pharmwiki/doku.php/hepatic_drug_clearance
DRUG CATEGORIES:

• High extraction ratio. These drugs are rapidly and extensively cleared from the blood by the liver
(e.g. in a single pass). Their clearance depends primarily on hepatic blood flow, and binding to
blood components is not an obstacle for extraction; the extraction is said to be non-restrictive or
blood flow dependent.

• Low extraction ratio. These drugs are not efficiently cleared by the liver and are extracted less
avidly and incompletely from hepatic blood. Their clearance is relatively independent of hepatic
blood flow, and is primarily determined by the intrinsic metabolizing capacity of the liver and by
the free drug fraction.

• Intermediate extraction ratio. Hepatic clearance of these drugs is dependent on both hepatic
blood flow, intrinsic metabolising capacity of the liver and the free drug fraction.

https://tmedweb.tulane.edu/pharmwiki/doku.php/hepatic_drug_clearance
Drugs with "Flow Dependent" hepatic clearance (high hepatic extraction ratio)
• morphine
• lidocaine
• verapamil
• propranolol
• nitroglycerin

Drugs with "Capacity-Limited" hepatic clearance (low hepatic extraction ratio)


• warfarin
• phenytoin

Drugs with intermediate hepatic extraction


• aspirin
• quinidine
• codeine
• nortriptyline
TERIMAKASIH

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