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Fundamentals of Drug Action Pt.2
Pharm. Chapter 3 Pt. 2
106
Pharmacology
12th Grade
01/28/2013

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Term
What effects drug absorption and distribution?
Definition
the route of administration, blood flow at site of absorption, chemical properties of the drug
Term
What is enteral route of administration?
Definition
through digestive tract, orally or retically
Term
What is the parenteral route of administration?
Definition
bypasses the digestive tract(injections, inhalers, pumps, etc)
Term
What are two things that determine the chemical properties of the drug?
Definition
lipophilic or hydrophilic
Term
How does blood flow at the site of absorption affect absorption?
Definition
higher the blood flow, the higher the distribution
Term
What is a natural ligand?
Definition
normal molecule that binds to a receptor and activates it
Term
What is an artifical ligand?
Definition
drug molecule that binds to a receptor
Term
What is an agoinist?
Definition
activates receptor at same level as natural ligand
Term
Where is the first place that all oral medications go after absorption?
Definition
the liver
Term
How does absorption of liquid formations occur?
Definition
immediately bioavaliable, some absorbed into the oral mucosa, no digestion required prior to absorption
Term
What must happen to solid formations?
Definition
they must be broken down, go through mechanical digestion in the stomach, then be absorbed into the small intestines
Term
All oral forms are distributed to the BLANK before entering BLANK
Definition
liver, general distribution
Term
What is first pass metabolism?
Definition
some of the drug is metabolized before it gets into general circulation
Term
What is the pH of the stomach? Small intestines?
Definition
stomach- ~2
intestines 7-8
Term
What does metabolism do?
Definition
inactivates drugs for excretion, but some drugs are activated by this!
Term
Where does enterohepatic circulation take plce?
Definition
between the small intestine and liver, affects amount absorbed into systemic circulation
Term
Are drugs that aren't metabolized always excreted?
Definition
no, they can recirculate through the system
Term
What does an antagonist do?
Definition
binds to a receptor and turns off all activity
Term
Injected formulations are immediately BLANK.
Definition
bioavaliable
Term
When is the blood flow rate like when distribution is rapid? Slower?
Definition
-distributed rapidly when blood flow rate is high
-slower distribution when blood flow rate is low
Term
What does it mean if a drug has slower release?
Definition
has extended duration of action, given in place where blood flow is low so it slowly releases into the blood stream
Term
If a drug is highly lipophilic what does that mean?
Definition
a greater percent of bound drug at given time(less active)
Term
Are ions hydrophilic or lipophilic?
Definition
hydrophilic
Term
What type of administration is used for hydrophilic drugs?
Definition
parenteral because these can't cross a membrane,
Term
What does it mean if something is hydrophilic?
Definition
it is water soluble and can be dissolved in plasma
Term
What are ions?
Definition
elements or molecules that gain or loose and electron
Term
What type of drugs ionize in solution?
Definition
weak acids or bases will ionize in solution
Term
Does ionization do the same thing for every molecule?
Definition
no, it creates different properties for individual molecules
Term
What type of charge do ions have?
Definition
Positive(cation) or negatine(anion)
Term
what is pKa?
Definition
the pH at which 50% of the drug is ionized
Term
Can ionized drugs cross the plasma membrane?
Definition
no because they form hydrogen bonds, they easily dissolve in plasma but cannot cross membrane
Term
What happens to nonionized drugs?
Definition
they are easily absorbed, don't dissolve in plasma, don't have the ability to form hydrogen bonds
Term
What are weak acids like at a lower pH?
Definition
nonionized, that means they are more lipophilic and can cross membranes (oral formations absorbed in he stomach because the pH is 2)
Term
What are weak bases like at a higher pH?
Definition
more nonionized(oral formulations absorbed in the small intestine pH of 7-8)
Term
**See notes for m ore information on weak acids and bases**
Definition
Term
Why are there a lot of side effects with medications dealing with the brain?
Definition
because it has to be a high enough dose to where some will get through the blood brain barrier
Term
What does a drug have to be to be able to pass the placenta?
Definition
lipophilic
Term
What do lipophilic drugs bind to?
Definition
plasma proteins, bound drug is not bioavaliable, only free drug is therapeutic
Term
Where are plasma proteins made?
Definition
in the liver
Term
What is the distribution of drugs affected by? (5)
Definition
1.size and blood flow to the organ
2.drug solubility
3.plasma protein binding
4.barriers
5.Etc.
Term
What does anthopathic mean?
Definition
drug has hyprophobic and hydrophilic properties
Term
Distribution of lipophilic drugs can cause what?
Definition
drug interactions because of a limited amount of plasma proteins in the blood
Term
What happens when two lipophilic drugs compete for plasma proteins?
Definition
they will compete and the more lipophilic one will win, drug that looses will not be bound at normal %, this drug is more free
Term
What is another word for drug metabolism?
Definition
biotransformation
Term
What is drug metabolism?
Definition
chemical changes in the drug in order to make excretion more likely, mediated by emzymes
Term
What does metabolism do to the drug?
Definition
polarizes the drug so metabolite will be water soluble
-decreases lopophilicity
-decreases binding to plamsa proteins
-decreases retention in the body
Term
What are the three mechanisms of biotransformation?
Definition
-active drug to inactive metabolite
-inactive prodrug(not active until metabolized) to active metabolite
-active drug to active metabolite
Term
What does a drug+metabolic enzyme produce?
Definition
metabolite(product)
Term
what does an effective drug level mean?
Definition
that the same amount of drug is going into the body as coming out.
Term
when there is a effective drug level what is decreased?
Definition
side effects
Term
This is maintaining at least the therapeutic level of the drug in the blood?
Definition
A steady-state drug level
Term
in order to keep a steady state of drug level the dose can fluctuate ______ but will not ____ _______ the therapeutic level.?
Definition
Above, Drop Below
Term
The amount of time necessary for the concentration of the drug to decrease by 50% is called the?
Definition
Half life
Term
how many half lives are necessary to remove nearly all the drug or to build it to a steady state level?
Definition
5-6 half lives
Term
what is Zero- order Kinetics?
Definition
is when the drug is eliminated at a constant rate in spite of the amount of drug present (ex. Alcohol, Aspirin)
Term
Why does the body eliminate the drug at a constant rate despite the amount in zero- order kinetic reaction?
Definition
because some drugs use metabolic enzymes that get saturated and the amount doesn't matter they cannot increase the reaction.
Term
what BAD thing can happen with zero order kinetic reactions?
Definition
can build up to toxic levels quickly
Term
How many phases of metabolize are there?
Definition
2
Term
Where does phase 1 of metabolism happen in the body?
Definition
Liver
Term
what kind of drugs go through phase 1 metabolism?
Definition
lipophilic drugs because they need extra metabolism for easy excretion
Term
are Lipophilic drugs easily retained in the body?
Definition
yes
Term
where are the metabolic enzymes located?
Definition
in the liver
Term
is phase 1 metabolism effected by age?
Definition
yes
Term
besides age what else affects phase 1 metabolism?
Definition
drug interactions
Term
what are 3 types of reactions that a drug can under go in phase 1 metabolism?
Definition
1. oxidation
2. Hydrolysis
3. Reduction
Term
what is metabolism based on?
Definition
enzymes
Term
what does aging cause to happen to enzyme production?
Definition
decreases, therefor decreasing metabolism
Term
because there is a litmited supply of available enzymes for a drug what will the drug do?
Definition
end up competing for the enzyme for metabolism
Term
how will Drugs with increased affinity for enzymes bind and metabolize?
Definition
Normally
Term
How will drugs with a lower affinity bind and metabolize?
Definition
lower than normal binding and lower than normal metabolism
Term
in metabolism, an increase in enzymes =?
Definition
an increase in metabolism
Term
in metabolism, a decrease in enzymes =?
Definition
a decrease in metabolism
Term
If a drug has a low affinity will it have more or less side effects?
Definition
More
Term
During metabolism in the liver in phase 1, a lipophilic drug will cause 2 types of enzymes, what are they?
Definition
Induction and inhibition
Term
what is induction?
Definition
certain drugs cause an increased production of enzymes, this will lead to faster metabolism
Term
what is inhibition?
Definition
production of enzyme decrease, and metabolism rate decrease.
Term
All drugs go through phase ____ but not all go through phase ___?
Definition
2, 1
Term
Lipophilic drugs go through phase_____?
Definition
one and two
Term
phase 2 metabolism takes place in the?
Definition
Blood
Term
what enzymes facilitate the process of phase 2?
Definition
Transferase enzyme.
Term
What takes place in Phase 2 metabolism?
Definition
the lipophilic drugs are bound to water soluble compounds such as acids, by doing this they are more easily excreted.
Term
in phase 2 are the same types of enzymes that are in the liver metabolizing the drugs?
Definition
No, transferase enzymes are in phase 2
Term
Does age, other drugs or metabolism get affected in phase 2?
Definition
NOpe
Term
what are the 3 types of renal (urine) routes of excretion?
Definition
1. Glomerular filtration
2. Active tubular secretion
3. Passive tubular diffusion
Term
what is Glomerular filtration?
Definition
metabolite enters filtrate directly from glomerulus into Bowman's capsule
Term
what is active tubular secretion?
Definition
Pumps that transport metabolites directly into filtrate ager Bowman's capsule
Term
This type of excretion requires Energy?
Definition
Active tubular secretion
Term
what is Passive tubular diffusion?
Definition
Through channels into filtrate after Bowman's capsule.
Term
What excretion route does NOT require energy?
Definition
Passive tubular diffusion
Term
what is another type of excretion besides Renal?
Definition
Extrarenal
Term
where does extrarenal take place?
Definition
Happens outside of Kidneys
Term
what are the different types of extrarenal excretions?
Definition
pulmonary
Biliary
Salivary
Gingival crevicular fluid
sweat or milk
Term
what is the modt common route of excretion?
Definition
via Kidneys
Term
what is pulmonary excretion?
Definition
we breath it out
Term
what is biliary excretion?
Definition
excretion through feces
Term
what is skin and milk secretion?
Definition
through the skin as sweat and mammary glands as milk
Term
what types of renal excretion can happen after the glomerulus?
Definition
Active tubular secretion and Passive tubular diffusion
Term
How does Compliance play a role as a factor affecting frug action within the body?
Definition
the patient has to take the drug and take it when they are supposed to
Term
How does Psychologic factors play a role as a factor affecting frug action within the body?
Definition
if a patient believes that the drug will help them and they will get better, they will (the Placebo effect)
Term
How does tolerance of the body play a role as a factor affecting frug action within the body?
Definition
the body adjust to the the drug, if a tolerance is built up it may take more of the drug to get the same effect as a lower dose did previously.
Term
How does pathologic state play a role as a factor affecting frug action within the body?
Definition
Depends on how sick the patient is for how quick the drug will work, (state of the body and organs)
Term
How does time play a role as a factor affecting frug action within the body?
Definition
night = drug lasts longer due to slower metabolism
Term
How does sex play a role as a factor affecting frug action within the body?
Definition
male vs. female may metabolize the drug faster or slower.
Term
How does genetics play a role as a factor affecting frug action within the body?
Definition
some people produce more enzymes and metabolize drugs more quickly and vise versa.
Term
How does age/weight play a role as a factor affecting frug action within the body?
Definition
weight plays a role because heavier people with more fat = the lipophilic drugs wanting to stay with the fat longer and not go to the blood stream= slower reactions.
Age- may metabolize faster when young and slower as person ages
Term
How does environment play a role as a factor affecting frug action within the body?
Definition
altitude, chemicals and other factor in the surroundings can affect the way the drugs react in the body
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