SEMESTER (KINCHEN) COMPLETE SOUTHEASTERN LOUISIANA
UNIVERSITY
What is pharmacodynamics? -
Answer-The relationship between drug concentration and the biological effect: decides appropriate drug
dosing.
Are all drugs induced by the interaction of ligand to receptors? -
Answer-No, some drugs are non- receptor mediated and are caused by the physical or chemical
properties of the drug.
For example, osmotic laxatives do not require receptor interaction to render effect.
Ex: detran, ammonium chloride
How are receptors characterized? -
Answer-As protein structures, single or complex multiprotein subunits.
What is affinity? -
Answer-Describes how well a particular ligand/compound is drawn and held at a receptor binding site.
What is the relationship between affinity and (Kd) equilibrium dissociation constant? -
Answer-The smaller the equilibrium dissociation constant, the higher affinity.
Kd = Koff/Kon, ligand has more tendency to be bound than unbound!
Increase in ligand/compound concentration yields? -
Answer-Increased likelihood that Brownian motion of the particular molecule will bring it to a receptor
to interact.
The greater the concentration of drug, the more likely it is that a drug molecule will be occupying a
receptor site at any given time.
, A ligand's shape and chemical makeup affects? -
Answer-The length of interactions and strength of binding forces.
What is intrinsic activity? -
Answer-the magnitude of response elicited that a ligand has at a receptor site.
What do low doses on the dose-response curve demonstrate? -
Answer-A certain number of receptors need to be occupied before any response is observed.
What does a Rmax (maximal response) represent on the log-dose response curve? -
Answer-A maximum response has been achieved an further activation of receptors will not yield increase
in magnitude of response: the tissue is unable to produce a greater response.
What effects dose the microenviroment have on receptors? -
Answer-Changes in pH can change the conformation or charges on amino acids/protein receptors in
various places on the receptor complex thereby altering the function of the protein complex.
What is an agonist? -
Answer-An exogenous substance that mimics and endogenous compounds as well as blocking them from
interacting at a receptor site.
What is a partial agonist? -
Answer-A compound with good receptor affinity but weaker intrinsic activity that a normal endogenous
agonist.
Example: buprenorphine at the mu-opioid receptor
What is a super agonist? -
Answer-A compound that elicit greater affects at a receptor that the endogenous agonist.