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01 Drug Absorption (Notes) Atf
01 Drug Absorption (Notes) Atf
com
Last edited: 7/26/2022
OUTLINE
I) ROUTE OF ADMINISTRATION III) FACTORS AFFECTING IV) BIOAVAILABILITY (F) VI) REVIEW QUESTIONS
II) MECHANISM OF ABSORPTION ABSORPTION V) FACTORS AFFECTING VII) REFERENCES
(A) TRANSPORT MECHANISMS (A) PH BIOAVAILABILITY
(B) ABSORPTION IN OTHER ROUTES (B) BLOOD FLOW (A) SOLUBILITY OF THE DRUG
(C) TOTAL SURFACE AREA + (B) INSTABILITY OF THE
CONTACT TIME ENVIRONMENT
(D) P-GLYCOPROTEIN (C) FIRST-PASS EFFECT
I) ROUTE OF ADMINISTRATION
Absorption is the administration of a drug and the process of getting it into the circulation, therefore, understanding different
routes of administration is important.
TRANSPORT MECHANISMS
The transport mechanisms by which different drugs pass through the cell membrane depend on the characteristics of the drug,
such as size, solubility, and charge.
(1) Simple (Passive) Diffusion (3) Active Transport
Drug characteristics: Small or Hydrophobic (lipophilic) Drug characteristics: Large or Hydrophilic
Mechanism: Passive movement of molecules from areas Mechanism: Movement of molecules from areas of lower
of high concentration to areas of lower concentration concentration to areas of higher concentration (against its
concentration gradient), and this requires energy (ATP).
Figure 7: Endocytosis
Rectal route: the drug has to move across the gastrointestinal tract layers in there
Intradermal, Subcutaneous, Intramuscular: the drug has to pass through different layers of the skin and tissues before it gets to
the nearby capillaries
Intravenous: the drug moves directly into the bloodstream (without having to pass through a membrane)
●On the other hand, if the patient has slow transit time, as
in the case of constipation, there is so much time for the
drug to be absorbed (↑ contact time with the cells of the
GIT)
o Therefore there is ↑ absorption.
(D) P-GLYCOPROTEIN
REMEMBER:
Mechanisms of drug transportation:
• Passive Diffusion
• Active Diffusion
• Facilitated Diffusion
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• Endocytosis
Factors Affecting
↓ Absorption ↑ Absorption
Absorption
Contact Time ↓ contact time (e.g., diarrhea) ↑ contact time (e.g., constipation)
(i) Definition:
●This is the fraction of the drug that enters the systemic circulation.
(2) Bioavailability with IV vs Oral Administration
●When a drug is administered via the IV route, it does not pass through any membrane.
o The amount of drug that is administered and that gets absorbed in the bloodstream is 100%, therefore bioavailability of IV
drugs is 100%.
●However, if a drug is administered orally or through other routes that require passing through membranes, absorption is
affected by various factors such as pH, blood flow patterns, surface area, contact time, solubility of the drug, size of the drug,
etc.
o All the blood that is administered will not enter the blood stream so bioavailability will not be 100%.
(i) Calculating Bioavailability (F): (ii) Bioavailability is determined via this formula:
●If the drug is given IV, it will reach 100% and with time it
will decrease until it is completely eliminated as it will be
metabolized and excreted.
o The area under the curve (AUC) will determine that.
●If the drug is given orally, the concentration will rise but it
would not reach 100%. With time the concentration will fall
as it becomes metabolized and excreted.
Figure 16: Bioavailability with IV vs Oral Administration, orally
administered drugs have lower bioavailability than IV
administered drugs.
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