Pharmacodynamics Flashcards
What is the definition of Pharmacodynamics?
The effect the drug has on the body; Drug to Body
What is the process called when a drug–receptor complex initiates alterations in biochemical and/or molecular activity of a cell?
signal transduction
What is a naturally occurring small molecule or a drug that binds to a site on a receptor protein and activates it?
agonist
What happens to the receptor state’s equilibrium with the binding of agonists?
the equilibrium shifts from R (inactive receptor) to R*(active receptor) to produce a biologic effect.
What occupies the receptor but does not increase the fraction of R* and may stabilize the receptor in the inactive state?
antagonist
True or False: The magnitude of biological effect is directly related to the fraction of R*.
True
What are the richest sources of receptors?
proteins that transduce extracellular signals into intracellular responses.
What are the 4 families of receptors?
1) ligand-gated ion channels
2) G protein– coupled receptors
3) enzyme-linked receptors
4) intracellular receptors
What is a measure of the amount of drug necessary to produce an effect of a given magnitude?
Potency
What is the magnitude of response a drug causes when it interacts with a receptor?
Efficacy
What kind of agonist has intrinsic activities greater than zero but less than one, cannot produce the same Emax as a full agonist, and may even be an antagonist to the full agonist?
Partial agonists
What is the agonists that stabilizes the inactive R form and cause R* to convert to R, has an intrinsic activity less than zero, reverse the activity of receptors, and exert the opposite pharmacological effect of agonists?
Inverse agonist
What binds to a receptor with high affinity but possesses zero intrinsic activity and decreases the effect of an agonist when present?
antagonist
What is it called when both the antagonist and the agonist bind to the same site on the receptor in a reversible manner and prevents an agonist from binding to its receptor and maintains the receptor in its inactive state. ?
competitive antagonist
What is it called when antagonists bind covalently to the active site of the receptor, thereby reducing the number of receptors available to the agonist?
Irreversible antagonist