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Unit 1- Pharmacodynamics Flashcards

1
Q

Pharmacodynamics

A

Relationship between drug concentration and intensity of action at the receptor level

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2
Q

Types of Drug Targets

A

Enzyme, carrier, ion channel, receptor

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3
Q

Receptor Usage

A

When the interaction triggers a cascade of events for signal transmission

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4
Q

Binding Site

A

Drug molecule must bind with target and result in a response

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5
Q

Drug

A

Molecule that interacts with molecular components of an organism to produce biochemical and physiological changes, exogenous ligands

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6
Q

Enzymes

A

Enzymes as targets are inhibited

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7
Q

Cyclooxygenase Enzymes

A

Targeted by NSAIDs to suppress proinflammatory prostaglandins

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8
Q

Acetylcholinesterase Enzyme

A

Cholinesterase inhibitors prevent metabolism of acetylcholine

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9
Q

Antibiotics

A

May inhibit enzymes in cell wall biosynthesis, nucleic acid metabolism and repair, or protein synthesis

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10
Q

Carriers

A

Membrane transport proteins targeted by drugs

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11
Q

Na+/K+/2Cl- Carrier

A

Targeted by diuretics in the nephron

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12
Q

Sodium Pump Carriers

A

Targeted by digitalis

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13
Q

K+/H+ Carrier

A

Targeted by proton pump inhibitors in the gastric parietal cells

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14
Q

Ion Channels

A

Voltage gated calcium channels targeted by calcium channel blockers

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15
Q

Receptors

A

Regulatory proteins that play a roll in cell communication

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16
Q

GPCRs

A

Largest family of receptors involved in almost all physiological processes, most drugs act on GPCRs

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17
Q

Beta 2 Adrenergic Receptor

A

Albuterol binding activates adenylate cyclase forming cAMP and causing smooth muscle cell relaxation in the airways

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18
Q

Ligands

A

The exogenous compounds that bind receptors

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19
Q

Endogenous Ligands

A

Endogenous transmitters

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20
Q

Occupancy Theory

A

Drug response is a linear function of drug occupancy at the receptor level, drug has to occupy all receptors to achieve a maximal effect

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21
Q

Unliganded Receptor in Occupancy Theory

A

Is silent with no basal activity

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22
Q

Concept of Efficacy

A

The more receptors occupied by a drug the greater the response

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23
Q

Antagonist in Occupancy Theory

A

A drug with null efficacy but that blocks access of the receptor to other ligands

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24
Q

Two-State Model

A

Receptor exists in active and inactive form in dynamic equilibrium, ligand binding can shift equilibrium

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25
Agonist in Two-State Model
A drug with a higher affinity for the active state will drive equilibrium to active and activate the receptor
26
Full Agonist in Two-State Model
A drug that highly favors the active state and drives the receptor all the way to active to get a maximal response
27
Partial Agonist in Two-State Model
A drug only has moderately higher affinity for the active state and has lower effect than a full agonist
28
Inverse Agonist in Two-State Model
A drug has higher affinity for the inactive state and drives equilibrium to inactive
29
Neutral Agonist in Two-State Model
Antagonist, binds the active and inactive states in equal affinity and will not alter equilibrium, but acts as a competitive antagonist
30
Antagonist vs Neutral Agonist
Antagonist has no intrinsic activity, a neutral agonist binds equally to both states of receptors
31
Primary Agonist
Binds to the same site as endogenous ligands
32
Allosteric Agonist
Drug that binds to a different region of the receptor than endogenous ligands
33
Receptor Antagonists
Prevent the action of natural agonists
34
Drug Affinity
The ability of a drug to bind to a receptor
35
Constant of Affinity
Numerical representation of drug affinity
36
Drug Receptor Complexes
Binding of drugs to receptors that is responsible for drug action
37
Drug Efficacy
Drug ability to initiate changes that lead to the production of responses
38
Level of Maximal Response
Highest response an agonist can achieve, characterized by efficacy
39
Drug Potency
Concentration of a drug required to achieve a given effect, expressed by EC50
40
EC50
Concentration of agonist that produces 50% of its maximal response
41
Potency and EC50
Potency varies inversely with EC50, higher potency requires lower EC50
42
Requiring Potent Drugs
Spot on treatments, eyedrops, and intra-articular administration
43
Potency of Antagonist
Effect of inhibition, determined by IC50
44
IC50
Concentration of antagonist that reduces agonist response by 50%
45
Competitive Antagonism
Antagonists act on the same receptor as the agonist
46
Reversible Competitive Antagonism
Antagonism can be reversed when agonist concentration is increased
47
Irreversible Competitive Antagonism
Displacement of antagonist from its binding site cannot be achieved by increasing agonist concentration
48
How to investigate receptor function?
Use irreversible competitive antagonists as experimental probes
49
Dose Response Curve and Competitive Antagonism
Agonist curve is shifted to the right: potency decreases because it depends on dosage but efficacy remains the same
50
Noncompetitive Antagonism
The drug blocks the agonist response at a downstream point in the cascade of events
51
Dose Response Curve and Noncompetitive Antagonism
Maximal efficacy of the agonist is reduced
52
Drug Specificity
Most drugs can be agonist or antagonist and do not have specificity to one type of receptor
53
Submaximal Drug Response
Increase dose of the drug to increase therapeutic effect
54
Clinical Efficacy
Therapeutic effectiveness of a drug in patients
55
Intrinsic Efficacy
Capacity of agonists to activate a receptor
56
Antagonist Efficacy
No intrinsic efficacy (no receptor activation) but clinical efficacy (therapeutic effect)
57
Quantal Dose Response Relationships
Relationship between dose of a drug and proportion of a population of patients that respond to it, used to determine the dose at which most of the population responds
58
ED50
Median effective dose, dose at which 50% of subjects exhibit a therapeutic response to a drug
59
TD50
Median toxic dose, dose at which 50% of subjects experience a toxic effect
60
LD50
Median lethal dose, dose at which 50% of subjects die
61
Therapeutic Index
Ratio of TD50 to ED50, used as a measure of drug safety
62
Certain Safety Factor
CSF should be >1, a dose effective in 99% of the population is less than what would be lethal in 1% of the population
63
Therapeutic Window
Range of drug doses that provides therapeutic efficacy with minimal toxicity, range between ED50 and the start of the toxicity curve

Pharmacology (32 decks)

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