Module 7 Dose Response Relationships Flashcards
1
Q
Pharmacodynamics
A
- Study of what drug does to body
- Biological & chemical effects
- Mechanisms to produce effects
2
Q
Dose Response Curves
A
- Increasing dose increases response
- Monotonic
- Semi-logarithmic, not linear
3
Q
Dose Response Curve Phases
A
- 1, dose too low to cause response
- 2, graded response & nearly linear
- 3, larger dose, toxicity risk
4
Q
Efficacy
A
- Measure of effectiveness of drug at certain dose
5
Q
Maximal Efficacy
A
- Maximum effect drug can achieve
- Maximum height of dose curve
6
Q
Potency
A
- Amount of drug to elicit response
- Compare drugs of same effect
7
Q
Higher Potency
A
- Smaller dose to achieve effect
8
Q
Determining Potency
A
- Compare dose required to produce half max response
- ED50
- Lower ED50 = high potency
9
Q
Drug Receptors
A
- Cellular macromolecules
- Binding of molecule to target
- Complex produce biological effect
10
Q
Antacid Actions
A
- Neutralize stomach acid
- Provide relief of GI disorders
- No target cell for binding
11
Q
Receptor Types
A
- Ligand gated ion channels
- G-protein coupled receptors
- Enzyme linked receptors
- Intracellular receptors
12
Q
Gated Ion Channels
A
- Ion movement causes instantaneous changes in function
- Ions require special channels
13
Q
Ligands
A
- Drug/endogenous molecules
- Control open/close of channels
14
Q
GABA Receptor
A
- Type of ligand gated channel
- Neurotransmitter
- Opens channel
- Allows chloride into cell
15
Q
Benzodiazepine Drug Class
A
- Bind to GABA receptor
- Allow chloride into cell
16
Q
GABA Activation
A
- Sedation
- Muscle relaxation
- Increase intracellular chloride
17
Q
G-Protein Coupled Receptors (GPCRs)
A
- Seven transmembrane spanning protein receptor
- G-protein with 3 subunits
- Effector molecule (enzyme)
18
Q
GPCR Actions
A
- Binding of ligand to GPCR activates G-protein
- G-protein dissociates from receptor
- Effector is activated
- Short time response
19
Q
GPCR Neurotransmitters
A
- Norepinephrine
- Serotonin
- Histamine
20
Q
Enzyme Linked Receptors
A
- Span cell membrane
- Ligand binding outside membrane
- Enzyme catalytic site inside membrane
21
Q
Enzyme Linked Receptor Response
A
- Binding to ligand outside activates enzyme inside
- Very rapid
22
Q
Insulin Receptors
A
- Enzyme linked receptor
- Causes phosphorylation & effector activation
- Increases translocation of glucose transporters too membrane
- Increased glucose uptake & utilization
23
Q
Intracellular Receptors
A
- Inside cell
- Transcription factors
- Highly lipid soluble
24
Q
Access to Intracellular Receptors
A
- Ligands must cross membrane
- Diffusion/drug transport protein
25
Q
Intracellular Receptor Binding
A
- Binding of ligand causes translocation of complex to nucleus
- Binding to DNA
- Stimulates messenger RNA
26
Q
Intracellular Receptor Response
A
- Delayed protein synthesis
27
Q
Intracellular Receptor Ligand Examples
A
- Steroid hormones
- Testosterone
- Estrogen
28
Q
Receptor Selectivity
A
- Bind to one receptor
- Less likely to produce side effects
- Side effects may occur if multiple receptors
