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Pharmacodynamics Flashcards

1
Q

pharmacodynamics

A

what the drug does to the body

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2
Q

mechanism of action

A

how drug achieves its effect at the site of action

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3
Q

mechanism of action (5)

A
  1. provides new drug therapy treatment
  2. optimize drug dosage
  3. reduce drug resistance
  4. discover new indications for existing drug
  5. safer drug therapies
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4
Q

factors that affect degree of drug binding and response

A
  1. recognition of drug at receptor
  2. concentration of drug at site of the receptor
  3. amount of drug needed to produce effect
  4. density of receptors on cell surface
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5
Q

fundamentals of drug action

A

D + R ↔ DR Complex → Effect

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6
Q

threshold

A

minimum number of drug receptor complexes required for a response to occur

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7
Q

Saturation

A

point when all receptors are bound/occupied by drug

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8
Q

most receptors are proteins

A

true

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9
Q

drug receptors are commonly named for the substance it interacts best with and stimulates/activates (ie insulin)

A

true

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10
Q

drug-receptor actions

A

determine quantitative relationship between dose & effects,, receptor binding affinity determines drug concentration

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11
Q

factors affecting drug-receptor responses

A
  1. affinity
  2. selectivity
  3. drug efficacy
  4. potency
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12
Q

affinity

A

strength of binding between a drug and its receptor

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13
Q

drug affinity is dictated by:

A
  1. size
  2. shape
  3. bonding (IMF)
  4. stereochemistry
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14
Q

K1 < K2

A

dissosiate

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15
Q

K1 > K2

A

form

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16
Q

K3

A

events that occur following receptor binding

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17
Q

affinity drug size

A

< 1000 MW units allows movement
> 1000 MW units unable to diffuse between body compartments

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18
Q

affinity drug shape

A

chirality, enantiomers (mirrored image)

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19
Q

enantiomers

A

diffuse in their ability to bind to and alter the function of receptors

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20
Q

racemic mixture vs S isomers

A

racemic mixture (S/R isomers)
S isomers increase absorption and longer half life

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21
Q

affinity drug receptor binding

A

depends on type of chemical bonds that can be established between drug and receptor (covalent vs non-covalent)

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22
Q

Seletivity

A

preference for acting at certain binding sites or receptors. may equate to less side effects

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23
Q

receptor distribution

A

nonselective antagonists are not used, preferred method is using selective drugs that target specific area.

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24
Q

amount of drug bound is affected by

A

quantity of receptor binding sites, receptor and tissue type, amount of drug available

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25
drug efficacy
ability of drug to initiate biological effect or stimulate receptor in a way that produces a pharmacological response
26
drugs can have affinity but lack efficacy
true
27
drug efficacy is dependent on
drug receptor complexes and intrinsic activity of drug
28
Emax
maximal efficacy of drug (assuming all receptors are occupied by drug and no increase in response observed with higher concentrations of drug)
29
intrinsic activity
ability of the receptor bound drug to activate the receptor and initiate downstream events
30
drugs are categorized based on intrinsic activity at a given receptor
agonist and antagonist
31
receptor agonist
drugs that interacts with and activates receptors (can resemble naturally occurring hormone)
32
types of agonist
full, partial, inverse
33
full agonist
maximal efficacy
34
partial agonist
less than maximal
35
inverse agonist
produce < 0 response
36
receptor antagonist
intrinsic activity of 0, no effect, block action of endogenous agonists (possess affinity, lack efficacy)
37
types of antagonists
competitive, noncompetitive, functional
38
competitive antagonist
reversible, competes with an agonist, decreases potency same efficacy
39
noncompetitive antagonist
irreversible, decreases maximum efficacy
40
allosteric antagonist
binds to another site and prevents activation by agonist
41
functional/physiologic antagonist
2 drugs causing opposing effects
42
potency
amount of drug needed to produce an effect
43
dose response curve
effect of dose on magnitude of pharmacologic response
44
EC50
concentration of drug producing 50% of max response
45
measure of drug potency
↓ EC50, ↑ potency
46
Arithmetic scale dose response curve
rate of change rapid at first, becomes progressively smaller as dose increase, difficult to analyze
47
logarithmic scale dose response curve
proportionate doses occur at equal intervals, able to plot drugs with different dose ranges on same scale
48
logarithmic scale used to
compare drug potencies
49
drug dosage goal
maximize efficacy limit toxicity
50
subtherapeutic
too low of dose = ineffective
51
supretherapeutic
too high of a dose = adverse side effects
52
therapeutic index
measure of drug safety
53
LD50 vs TD50
lethal dose vs toxic dose
54
LD50
dose that kills 50% subjects
55
TD50
dose that poisons 50%
56
ED50
dose that produces a therapeutic effect in 50%
57
large therapeutic index
increased margin of safety, wide therapeutic window (nicotine)
58
small therapeutic index
narrow therapeutic window, small difference in concentration between desired therapeutic effect and unwanted side effects (warfarin)
59
certain safety factor
accounts for different line slopes LD1/ED99
60
you want a certain safety factor
greater than 1 to indicate safety
61
Enzymes
control a number of metabolic processes, requires selective toxicity
62
enzyme inhibition
competitive, non-competitve, irreversible blockage at substrate or cofactor binding site
63
reverse transcriptase
turns viral RNA into DNA
64
integrase
integration into host DNA
65
protease
final cutes and packaging new HIV
66
transport systems
transmembrane proteins involved in movement of ions/molecules
67
targets of drug actions
enzymes, transport systems, receptors
68
transport systems
facilitated diffusions / active transport
69
ligand gated ion channel
increase/decrease opening of an ion channel to let ions pass in/out of cell
70
transporters
molecules that are too large or not lipid soluble require transport into cells
71
receptors
most drugs act on receptors/transduction (receptor coupling)
72
drug receptor interactions
type of receptor a drug interacts with depends on chemical nature
73
hydrophilic drug
interacts with receptors on cell surface
74
lipophilic drug
enters cells through cell membrane, interacts with receptors
75
G protein coupled receptors
7 transmembrane domans, largest and most diverse group. external to cell, drug binding occurs on extracellular side
76
activation of G protein coupled receptor
GTP binds to Beta-gamma subunit, BY migrates and interacts with other molecules & G protein is hydrolyzed and converted to GDP
77
second messagers
small, non-protein water soluble molecules or ions (cAMP, Ca2+)
78
albuterol (therapeutic GPCR)
activates b-adrenergic GPCRs
79
Antipsychotic agents
block GPCR that normally bind to dopamine or serotonin
80
enzyme linked receptors
drug binds to extracellular domain of a receptor, activates multiple signaling pathways (insulin receptor)
81
intracellular receptor
not located on plasma membrane, able to pass through (lipid soluble ligand) --> steroids/hormones
82
targets of intraceullar ligands
proteins, enzymes, RNA, ribosomes
83
signal transduction
1. signal amplification 2. Protect cell from excessive stimulation
84
signal amplifcation
G protein linked receptor, enzyme linked receptor GOAL is to multiple original signal
85
desensitization / downregulation
repeated or continuous administration of an agonist
86
tachyphyllaxis
receptor is desensitized after repeated stimulation
87
the time it takes to recover
refractory period
88

Pharmacology (13 decks)

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