Module 8 Drug Receptor Interactions Flashcards
1
Q
Simple Occupancy Theory
A
- Intensity of drug response proportional to quantity of receptors
- Maximal response occurs when all receptors occupied
2
Q
Modified Occupancy Theory
A
- Response intensity proportional to occupied receptors
- 2 drugs on same receptor can have different binding strengths
- 2 drugs on same receptor can have different activation abilities
3
Q
Affinity
A
- Attraction of drug to receptor
- Primary determinant of drug potency
4
Q
Intrinsic Activity
A
- Ability of drug to activate receptor
- Reflected in efficacy
5
Q
Interaction Classifications
A
- Agonist
- Antagonists
- Partial agonist
6
Q
Agonist Definition
A
- Molecule binds to receptor causing activation
- Mimic action of endogenous ligands
7
Q
Antagonist Definition
A
- Molecules bind to receptor causing no activation
8
Q
Partial Agonist Definition
A
- Molecules bind to receptor, minimal activation ability
9
Q
Agonist Characteristics
A
- Includes hormones & neurotransmitters (endogenous)
- Affinity
- Intrinsic activity
- Increase/decrease physiological response
10
Q
Partial Agonist Characteristics
A
- Minimal/moderate intrinsic activity
- Act as antagonists, block full agonist binding
11
Q
Antagonist Characteristics
A
- Affinity
- Prevent endogenous binding
- Require presence of agonist
- Treat drug overdose
12
Q
Antagonist Examples
A
- Beta blockers
- Antihistamines
- Gastric acid reducers
- Opioid receptor blockers
13
Q
Antagonist Types
A
- Competitive
- Irreversible
- Allosteric
14
Q
Competitive Antagonists
A
- Binding at same site as agonist
- Reversible
- Equal affinity of antagonist & agonist, higher conc wins binding site
- Effects overpowered by increasing agonist conc
15
Q
Irreversible Antagonists
A
- Binding at same site as agonist
- Irreversible
- Response intensity dependant on agonist bound to receptor
- Effects last until receptor replaced
