Chapter 3 (E1) Flashcards
Administering drugs, absorption, and distribution in the body
The study of how drugs move through the body and are metabolized.
What is pharmacokinetics?
What does ADME stand for?
Absorption, Distribution, Metabolism, Elimination
List the 6 main elements present in the body.
H, O, N, C, P, Ca
Water makes up 60% of the body’s content. What percentages do lipids, proteins, and bones (+ electrolytes, trace metals, etc.) make up?
Lipids - 15%
Proteins - 15%
Bones and other - 10%
Rank the body’s level of organization from low to high, starting with cells and ending with organ systems.
1) Cells
2) Tissues
3) Organs
4) Organ systems
Basic unit of a biological system.
What is a cell?
Similar cells that act together to perform function.
What is a tissue?
What are the 4 types of tissues and their functions?
1) Connective - join tissues
2) Epithelial - protective layer
3) Muscle - motion
4) Nervous - communication
Multiple tissue types that work together.
What is an organ?
List the 5 vital organs.
Heart
Brain
Lungs
Liver
Kidneys
Cooperation of functionally related organs.
What is an organ system?
Drugs find targets at the cellular level. Why is this so important?
Changes at the cellular level impact many tissues and even organs
What is the goal of absorption?
Getting the drug into the bloodstream
The fraction of the drug that enters the bloodstream via a specific route.
What is bioavailability (F)?
This route of delivery involves the GI tract.
What is enteral?
This route of delivery involves absorption via non-digestive routes, such as IV, IM, or SubQ.
What is parenteral?
This route of delivery involves direct application on site of action (e.g., auricular, conjunctival, or cutaneous).
What is topical?
Drug concentration in the plasma of the blood. This is a density unit.
What is C(p)?
Area of C(p) of drug between minimum and maximum concentration to be effective.
What is the therapeutic window?
In oral administration, each sequential dose adds to the last but stays within the therapeutic window.
What is accumulation?
What are 3 benefits of oral drugs?
Easy (to take), cheap, designed for extended release
What are 3 problems with taking oral drugs?
1st pass metabolism
Enzymatic degradation
Longer absorption process
When are drugs typically used by injection?
Life-threatening situations
What does “bolus” refer to?
A single dose given all at once
What does “infusion” refer to?
The drip
What is the difference between IV bolus and IM bolus?
IV - dose goes to heart
IM - dose settles in depot
What does SC or SubQ refer to?
Under skin
{ }% of blood is plasma while { }% is cells.
54%
46%
What is the difference between plasma and serum?
Serum is merely plasma minus the clotting factor
Drugs tests look for affinity for…
Binding
This blood protein binds acidic drugs.
What is albumin?
This blood protein binds basic drugs.
What is glycoprotein?
Is cis or trans-conformation preferred by the body?
Cis
What charge must a drug hold to cross the cell membrane?
None, it must be neutral
How do drugs handle proton transfers when they’re in the interstitial fluid or bilayer?
Drugs are designed with weakly acidic and basic sites
List Lipinsky’s Rule of 5 (NOTE: there are actually 4; 5 just refers to the multiples of 5).
MW </= 500 g/mol
log P </= 5
HBD </= 5
HBA </= 10
What type of drug transport does Lipinsky’s Rules apply to? Passive diffusion or carrier proteins?
Passive diffusion
What is the purpose of carrier proteins?
To act as catalysts to help drugs too polar to cross membrane
What are the 2 types of carrier proteins and their characteristics?
1) Equilibrative - passive (no energy); relies on [ ] or charge gradient
2) Concentrative - active; relies on energy from ATP
Why is carrier protein transport utilized to some degree despite being used less than passive diffusion?
Some drugs mimic molecules in the body (e.g., amino acids, nucleosides, and small polypeptides)
The special protective measure of capillaries in the brain, which protects against bacterial infections and excludes over 99% of large molecules and 98% of small molecules.
What is the blood-brain barrier?
How do Lipinsky’s Rules change with the BBB?
MW </= 400 g/mol
Log P unchanged
HBD </= 3
HBA </= 7
What do the number of HBAs and HBDs make up in Lipinsky’s Rules?
Polar surface area
What are metabolism and elimination, and what organs are associated with them?
Metabolism - chemical mods of drugs; liver
Elimination - removal of drugs from body; kidneys+
