Lecture set 1 Flashcards
Pharmacology
interactions of drug with the receptor
Drug receptor interactions and their mechanisms
Pharmacodynamics
The physiological effects of a drug and the mechanism of their actions
Pharmacokinetics
Absorption, distribution, transformation, and xenobiotics (foreign drugs to the body)
Describe the characteristics of drugs
Drugs are defined by their actions (agonist vs antagonist)
Drugs can be solid liquid or gas
they can have covalent, electrostatic, and hydrophobic interactions with the receptors
The size, shape, and charge are very important when determining selectivity
Identify the site of drug action
A receptor is needed to have a chemical response to a drug
agonist
antagonist
orthosteric
inverse agonist
particle agonist
PAM and NAM
relate affinity to the law of mass action and receptor occupancy
a smaller KD value means that the drug has a high affinity to the receptor and binds more tightly to the receptor
- Drugs Kon and Koff
If the drug has a very fast Kon and a very slow Koff the affinity will be higher and the value of KD will be lower
if a drug have a very slow Kon and a very fast Koff the affinity is low and the KD value is higher
outline components in a receptor binding assay
We take a radio/labeled drug and put it in a solution with receptors and filter it out to get the total amount of binding as well as the nonspecific binding and by subtracting those we can get the specific binding and by looking at the specific binding on the graph we can then get the IC50 value of the drug. With that we can apply the Cheng-prusoff equation to compare it to other drugs
Use the principles of receptor binding to measure affinity
Total – Nonspecific = Specific
Bmax and Kd is calculated upon the specific curve
apply receptor affinity to receptor selectivity
the affinity/selectivity of a drug depends on how it reacts to the other receptors that it is binding to
describe the relevance of Bmax to drug action
Bmax is the number of receptors on a given cell or tissue
It allows drug to look at full occupancy of receptors without fully saturating them
Cheng-Prusoff equation
IC50/[1+ L/KD]= Ki
What does Cheng-Prusoff equestion tell us about a drug
By using this equation we can test every drug in the world against a receptor to compare the affinity of the said drug against a variety of receptors
Laboratory can test data from other researchers, it helps to “normalize the research”
