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Psychopharmacology > Lecture 6: Pharmacodynamics > Flashcards

Lecture 6: Pharmacodynamics Flashcards

1
Q

pharmacodynamics

A

the study of what drugs do to the body

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2
Q

dissociation constant

A

Kd; equilibrium constant that measures propensity of larger object to separate (dissociate) reversibly into smaller components. the drug concentration (in moles) at which half of the receptors are bound to the drug

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3
Q

dissociation constants for drug-receptor or transmitter-receptor interactions can be in ___

A

nM to muM range

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4
Q

definition of receptor

A

large molecule; site where naturally-ocurring signaling molecules produce biological effect

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5
Q

agonistic action

A

binding to the site of the normal endogenous neurotransmitter which initiates a similar cellular response

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6
Q

allosteric action

A

binding to nearby site can facilitate transmitter binding

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7
Q

antagonistic action

A

binding to receptor site can block access of transmitter to normal binding site

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8
Q

4 types of receptor structure

A
  1. ionotropic
  2. metabotropic
  3. carrier proteins (transporters)
  4. degradative enzymes
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9
Q

3 steps of ionotropic receptor binding

A
  1. NT molecules bind to protein sites in receptor channel
  2. binding causes channel to open immediately
  3. when channel opens, ions are able to move into or out of the neuron
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10
Q

what does GABA stand for?

A

gamma aminobutyric acid

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11
Q

two broad classes of GABA receptors and types

A

GABAa (ionotropic)

GABAb (metabotropic)

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12
Q

how many protein subunits does the GABAa receptor have?

A

5

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13
Q

names of GABAa receptor subunits

A

gamma2
beta2 (2)
alpha1 (2)

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14
Q

how many membrane spanning domains does a subunit have?

A

4 - helices

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15
Q

polypeptides

A

amino acids linked by peptide bonds

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16
Q

4 important parts of GABAa receptor

A
  1. chloride channel
  2. GABA site
  3. barbiturate site
  4. benzodiazepine site
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17
Q

metabotropic receptors

A

G protein-coupled receptors (GPCRs)

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18
Q

metabotropic receptors induce the release of ___ which can trigger ___

A

intracellular protein

second messengers

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19
Q

what are 3 of the 5 examples of processes metabotropic receptors control?

A
  1. ion channel function
  2. energy metabolism
  3. cell division/differentiation
  4. neuron excitability
  5. gene expression
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20
Q

when G proteins bind ___ they are on, and when they bind ___ they are off

A 
guanosine triphosphate (GTP)
guanosine diphosphate (GDP)
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21
Q

4 steps in G protein activation of an ion channel

A
  1. NT molecule binds to GPCR
  2. transmitter binding activates GPCR
  3. activated subunit of GPCR moves to nearby ion channel
  4. when G protein subunit attaches to ion channel, it opens, allowing ion flow
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22
Q

two major processes/enzymes triggered by G protein activation

A
  1. phospholipid hydrolysis

2. adenylyl cyclase

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23
Q

phospholipid hydrolysis second messengers

A
  1. DG

2. IP3

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24
Q

major adenylyl cyclase 2nd messenger

A

cAMP (cyclic adenosine monophosphate)

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25
consequence of presynaptic change in channel activity
change in amt of NT released
26
consequence of postsynaptic change in channel activity
change in firing pattern of neuron or cell
27
drugs can be ___ specific than endogenous ligands
more
28
carrier proteins
transporters; bind to NTs to transport them back to presynaptic neurons
29
2 drugs that block carrier proteins
SSRIs (block 5HT) | cocaine (blocks DA and NE)
30
net effect of transporter blockage
increase amount of NT available in synaptic cleft
31
two gradients affecting ion flow
1. voltage gradient | 2. concentration gradient
32
degradative enzymes
function to break down NTs
33
___ are used as pesticides and nerve gases
irreversible acetylcholine esterase inhibitors
34
___ are used as cognitive enhancers in alzheimer's disease and to increase muscle contractions in myasthenia gravis
reversible AChE inhibitors
35
monoamine oxidase inhibitors inhibit ___ breakdown of ___ and ___
presynaptic | NE & DA
36
optical isomers
molecular optical images, like left and right hand
37
+ or D isomer rotates ___, and - or L isomer rotates ___
clockwise | counterclockwise
38
50/50 combination of D and L is called a ___
racemic mixture
39
___ can occur if ligand activation is chronically blocked. example of drug type that causes this?
1. up regulation/supersensitivity | 2. antipsychotics that block DA receptors
40
dose response curves (37); what are the two x axes used?
1. percentage of subjects responding | 2. intensity of response
41
4 variables DRCs give info about
1. potency 2. slope 3. efficacy 4. variability
42
potency
concentration at which drug produces desired effect; usually attach more tightly than less potent drugs. high affinity does not equal high potency
43
what is the difference between potency and affinity?
potency is a function of both efficacy and affinity; for a drug to be potent, it must both bind strongly and initiate a strong response. an antagonist can have high affinity but no potency
44
slope
linear central part of curve which indicates how sharply effect changes with each change in dose
45
if a small change in dose produces a large change in effective, slope is ___
steep
46
if a large change in dose produces small changes in effect, the slope is ___
shallow
47
efficacy
the maximum effect obtainable with higher doses producing no additional effect
48
what is the difference between potency and efficacy?
some drugs may be potent, but might never be able to produce a peak response no matter how much is given
49
a drug that is more efficacious produces a ___ peak than a less efficacious drug
higher/greater maximum
50
spare receptors
maximum effect obtainable with a drug can occur when not all of the receptors have been bound by ligand
51
variability
individ difference in drug response can include potency, max effect, or slope
52
4 types of DRCs
1. full agonistic 2. partial agonistic 3. antagonistic 4. inverse agonistic
53
a partial agonist has a similar action to a full agonist, but is less ___
efficacious
54
antagonist
blocks or limits action of ligand, but has no effect of its own (no potency)
55
inverse agonist
binding to receptor site produces effect opposite to that of the endogenous ligand
56
allosteric modulators
affect receptor response by binding to site that is diff from site to which endogenous ligand binds
57
positive allosteric modulators ___ response to endogenous ligand
increase
58
negative allosteric modulators ___ effect of endogenous ligand
diminish
59
ED50
drug dose that produces desired effect in 50% of subjects
60
LD50
lethal dose for 50% of test subjects
61
TI
therapeutic index; ratio of LD50 to ED50
62
TR
therapeutic ratio; dose that causes adverse fx in 50% of pop to dose that causes therapeutic effect in 50%
63
the greater the TI, the ____ the drug
safer
64
TI =
LD50/ED50
65
The lower the ED50, the ___ the potency. the lower the TI, the ____ the safety
potency | safety
66
double-blind tests with placebo run-in period
every patient given a placebo for a week; those who respond positively removed
67
nocebo effect
negative expectation of phenom causes it to have more negative effect
68
polypharmacy
combining meds to improve outcome
69
pharmacodynamic redundancy
two drugs have same or overlapping mechanisms of action
70
pharmacodynamic interaction
two drugs may oppose each other. e.g. antipsychotic blocks DA type 2 receptors, while ADHD stimulant increases DA levels
71
pharmacokinetic interactions
one drug may affect another drug's ADME
72
axes of a graph of PK axes of a graph of PD combination graph?
1. concentration vs. time 2. effect vs. conc(log) 3. PK/PD - effect vs. time

Psychopharmacology (22 decks)

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