PHARMACOLOGY Flashcards
What term is used to describe the ability of a drug to ACTIVATE receptor once it is bound?
EFFICACY
Agonist interaction with a receptor is ___:
Dynamic–> will jump on and off repeatedly
What are important features of a concentration response curve (CR)? (4)
- THRESHOLD
- MAX RESPONSE
- SHAPE (Linear from 20-80%)
- [AGONIST] Producing 50% max (EC50) (**IMPORTANT)
What features of CR graph might change between agonists?
- SHAPE of curve
- MAX response
What is potency?
- How much of a drug is needed to produce an effect
The further to the left of a graph the curve is the MORE or LESS potent it is ?
- MORE POTENT
Which feature of CR graphs is used to measure potency?
- EC50
What can you use AGONIST POTENCY to identify?
- Receptor Subtypes
What is the order of preference for alpha adrenoceptors in terms of whether they bind to Iso, NA, or A
NA->A>Iso
What is the order of preference for beta adrenoceptors in terms of whether they bind to Iso, NA, or A
Iso>A->NA
If we make [] high enough will drug start to lose selectivity?
- YES!
What is used for confirmation of potency once it has been ranked via agonists?
- Antagonists
What is Propanolol?
- Antagonist competes with NA
- Can’t activate receptor BUT stops NA from getting to receptor
Agonists have ___ but no ____:
Affinity but no efficacy
What is the orthosteric sire?
- Same active site that the agonist binds to
