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Drug Bioavailability and Elimination Explained

The document discusses drug bioavailability, which is the percentage of a drug dose that reaches the bloodstream, and factors affecting distribution, including blood flow, lipid solubility, molecular size, and ionization. It also outlines the elimination process, which consists of excretion and biotransformation, primarily occurring in the kidneys and liver. Understanding these concepts is essential for determining how effectively a drug acts in the body.

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7 views16 pages

Drug Bioavailability and Elimination Explained

The document discusses drug bioavailability, which is the percentage of a drug dose that reaches the bloodstream, and factors affecting distribution, including blood flow, lipid solubility, molecular size, and ionization. It also outlines the elimination process, which consists of excretion and biotransformation, primarily occurring in the kidneys and liver. Understanding these concepts is essential for determining how effectively a drug acts in the body.

Uploaded by

shadiaa365
Copyright
© All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
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Download as PDF, TXT or read online on Scribd

Drug bioavaibiltiy distribution and

elimination
 The relationship between the drug dose and
the amount ultimately delivered to the blood-
stream is defined as bioavailability and is
generally expressed as a percentage.
 If a 1 gram dose of a drug is administered by
mouth, and half of that reaches the systemic
circulation, the drug is 50% bioavailable
 Bioavailability Rate at which a drug is
absorbed and be-comes available to the tar-get
tissue.
 Once a drug is absorbed into the bloodstream it can be
carried throughout the body. This process is called
distribution, and is a reversible process; while some
molecules may be in-teracting.
 The delivery of a drug from the bloodstream to the site of
drug action primarily depends on blood flow, capillary
permeability, the degree of binding (at-tachment) of the
drug to blood and tissue proteins, and the relative lipid-
solubility of the drug molecule.
 The process by which a drug reversibly leaves the blood
stream and enters the interstitium (extracellular fluid)
and/or the cells or tissues.”
 Blood flow to different organs of the body is not
equal:
 The most vitally important or-gans of the body
receive the greatest supply of blood. These
organs include the brain, liver, and kidneys.
 Skeletal muscle and bone receive less blood, and
adiposetissue (fat) receivesthe least
1. Lipid Solubility
Greater the lipid solubility, more is the distribution and vice versa
2. Molecular size
Larger the size, less is the distribution. Smaller sized drugs are more extensively distributed.
3. Degree of Ionization
Drugs exist as weak acids or weak bases when being distributed. Drugs are trapped when present in
the ionized form, depending upon the pH of the medium. This fact can be used to make the drug
concentrated in specific compartments
Tissue binding:
 Different drugs have different affinity for different cells. All cells do not bind the same drugs
 refers to the irreversible removal of drug from
the body by all routes of elimination.
Elimination may be divided into two major
components:
 Excretion
 Biotransformation
 is the removal of the intact drug. Most drugs
are excreted by the kidney into the urine. Other
pathways include the excretion of drug into
bile, sweat, saliva, or milk.
 Biotransformation (drug metabolism) converts
the drug in the body to a metabolite that is
excreted more readily.
 Enzymes involved in biotransformation are
located mainly in the liver. Other tissues such
as the kidney, lung, small intestine, and skin
contain biotransformation enzymes.

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