Pharmacology Test #4 Dr. Flekenstein 11/28/16 Flashcards
Define Pharmacology
Branch of medicine concerned with the uses, effects, and modes of action of drugs (Focus on therapeutic effects of drugs)
Define Toxicology
“The dose makes the poison”
What is pharmacokinetics?
-The action of the body on drugs
What is pharmacodynamics?
-The action of drugs on the body
Dose, Drug concentration, and Drug metabolism are examples of what?
-Pharmacokinetics
What does ADME stand for?
- Absorption
- Distribution
- Metabolism
- Elimination
What is an agonist?
-A drug or natural ligand
What do agonists do?
-Activate receptors (Rc)
If you have a log does on the x-axis what is typically the shape of the curve?
-Sigmoidal
What do antagonists do?
-Bind to receptors (Rc) but do not activate it
T/F
Antagonists interfere with agonists
True
What direction does the dose response curve shift if there are antagonists?
To the right
Where do allosteric activators bind?
-Somewhere away/different from the agonist site
What type of effect do you get from allosteric activators?
-Potentiates effects
Where does the allosteric inhibitor bind?
-Binds a receptor site separate from agonist site
Are allosteric inhibitors and activators competitive or competitive?
-Non-competitive
Is the active or inactive receptors usually favored?
-Inactive
T/F
There is always some active and inactive receptors at any given time
True
What do full agonists have a higher affinity for?
-Active receptor
What do partial agonists have an affinity for?
-Intermediate affintiy for Both Inactive and active receptors
What do inverse agonists have a higher affinity for?
-Inactive receptor
What does a conventional antagonists have an affinity for?
-Equal affinity for Ra and Ri
Drug concentration where effect or receptor occupancy are half maximal is the _____ and ____ respectively.
- EC50
- Kd
What is Kd?
-Where 1/2 of receptors are bound
What is EC 50?
-Concentration where you get 50% of drug effect
What is Emax?
-Where you get your maximal effect
What is IC50?
-The concentration of drug where you have 50% of effect blocked
When you have an agonists with a competitive antagonist what happens to the EC50?
-Shifts to the right
When you have an agonist with a noncompetitive antagonist what happens to the EC50?
-Doesn’t shift at all
What is the plateau dose?
-Maximum effect
What is the threshold dose?
-The smallest dose that causes a measurable effect
If you can exert a maximum effect without all receptors being bound what does that mean?
-You have spare receptors
If you put a partial agonist in with a full agonist what can occur?
-The partial agonist can inhibit some of the effect of the full agonist by occupying some of the receptors that the full agonist use leading to an intermediate effect
T/F
With enough partial agonist you can have the same max effect as a full agonist
False
You can not get the same max effect as a full agonist
What are the three types of drug-receptor interactions?
- Additive
- Synergistic
- Antagonistic
What is an additive drug-receptor interactions?
-Drug effect equals sum of individual effects. 1+1=2 Example: acetometaphine relieves 50% and Ibuprofen relieves 50% and together they relieves 100 %
What is synergistic drug-receptor interactions?
-Effect is greater than sum (1+1=5)
What is antagonistic drug-receptor interactions?
-Drug blocking ability (1+1=1/2)
T/F
Chemical antagonists involve receptors
False
-They do not involve receptor
T/F
Physiological antagonists involve endogenous regulatory pathways mediated by different receptors
True
What refers to the number of receptors that must be activated to yield a maximum response?
-Efficacy
What is efficacy?
-Maximum effect of drug
If you have a drug with high efficacy what percentage of receptors do you need to stimulate?
-Small percentages
If you have the relative concentrations of two or more drugs that produced the same drug effect what do you have?
-Potency
Therapeutic index is calculated how?
-Toxic over Therapeutic (TD50/ED50)
Do you want a higher or lower therapeutic index when making a drug?
-Higher (example 100 or 2)
What does the therapeutic range fall between?
-Toxic dose and therapeutic dose
T/F
You use your blood concentration to measure if you are in the therapeutic range
True
What does a wide margin of safety mean?
-Large difference between toxic and therapeutic dose
The amount of drug that gets to target are inversely proportional to what two things?
- Distance from site
- Amount of tissue that it must pass through
What is parenteral administration of a drug?
-Not by way of intestine or GI tract
What is/are an/some example of a parenteral administration?
- Intravenous (IV)
- Intramuscular
- Subcutaneous
What is the fastest ways for drugs to be administered to the system?
- IV
- Inhalation
What is an advantage of intramuscular drug administrations?
-You can give large volumes
What is enteral drug administration?
-By way of the intestine or GI tract
What are examples of enteral drug aministrations?
- Buccal or sublingual
- Oral
- Rectal
What are three features of oral administration?
- Most unpredictable
- Absorption via duodenum
- First pass metabolism
What is first pass metabolism?
-The liver degrades drugs
