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Psychopharmacology > Exam 1: Dynamics > Flashcards

Exam 1: Dynamics Flashcards

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1
Q

Pharmacodynamics

A

study of physiological and biochemical interaction of drug molecules with target tissue that is responsible for ultimate effects of drug

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2
Q

Large protein molecules located on cell surface/within cells that are initial sites of action of biological active agents

A

receptor

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3
Q

Two types of receptors

A

cell surface-extracellular

Intracellular: cytoplasm/nucleus

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4
Q

Most hormones that acat on brain to influence neural events use ___ receptor

A

intracellular

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5
Q

high affinity

A

attach most readily

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6
Q

low effiacy

A

can attach, but doesn’t do anything

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7
Q

antagonist

A

block effect

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8
Q

agonist

A

act as NT

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9
Q

Partial agonists

A

efficacy less than full agonists, but more than antagonist

-effect, but not as much

Technically some intrinsic activity

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10
Q

Inverse agonists

A

initiate biological action, but action is opposite to agonist

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11
Q

Receptor number modification

A

long term regulation:

up-regulation: increase receptors

down regulation: decrease receptors

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12
Q

Receptors modified in sensitivity

A

more rapid regulation via 2nd messengers

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13
Q

The idea that receptor proteins have different characteristics in different target tissue

A

receptor subtypes

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14
Q

Does response curve

A

describes the extent of biological/behavioral effect (mean response in population) produced by given [drug]

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15
Q

ED50

A

dose that produces 1/2 maximal effect

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16
Q

ED100

A

maximum response occurs at does which we assume receptors fully occupied

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17
Q

Potency

A

absolute amount of drug necessary to produce a specific effect

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18
Q

maximum on y-axis

A

efficacy

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19
Q

TD50

A

does at which 50% of the population experiences a particular toxic effect

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20
Q

Therapeutic index

A

TI= TD50 / ED50

LD50 / ED 50

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21
Q

Factor index

A

dose of drug that is lethal to 1% of the population compared with the dose that is therapeutically effective in 99% of the population (LD1 / ED99)

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22
Q

Competitive Antagonists

A

can be displaced from sites by excess of agonist because increase [drug] competes more effectively for fixed receptors

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23
Q

Noncompetitive antagonists

A

drugs that reduce effects of agonists in ways other than competing for the receptor.

e.i. binding to portion of receptor other than agonist binding site

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24
Q

Physiological antagonism

A

two drugs that act in 2 distinct ways but interact in such a way that they reduce each other’s effectiveness in the body

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25
Potentiation
situation in which combo of 2 drugs produces effects that are greater than the sum of their individual effects.
26
Radioligand binding
used to study number of receptors in given region
27
Radioligand: to measure amount of ligand that binds to sites we are concerned with, add
very high [nonradioactive competing ligand] to some tubes to show most radioactive binding displaced.
28
radioligand: ___ binding subtracted when data for specific binding calculated
nonspecific
29
Saturability
finite # receptors in tissue.
30
Point at which binding curve plateus
Bmax
31
If you compare rate of dissociation with rate of binding, you get ___
Kd
32
Kd
dissociation constant, measure of drug affinity for specific receptor
33
Autoradiogarphy
use radio ligand on slides instead of ground up tissue shows radio bound ligand and its location, good fro studying effects of brain lesions.
34
In vivo receptor binding
shows researcher where particular drug/NT binds in intact animal
35
Dose response curves only show
POTENCY
36
Increase potency
decrease ED50 (EC50?)
37
Increase potency
lower x-axis value
38
Increase efficacy
increase Bmax
39
Factors determining drug potency
1) Accessibility (kinetics) 2) affinity (dynamics) 3) intrinsic activity (dynamics)
40
affinity
drug binds to receptors quantitative measure of attraction between drug molecules and receptors
41
intrinsic activity
cellular response
42
k1
D + R --> DR Rate at which drug ASSOCIATES with receptor
43
k2
DR --> D + R Rate at which drug DISSOCIATES from receptor
44
how do you measure drug affinity?
3H radio ligand label Substitute 3H (tritium) in for hydrogen Tritium= PNN
45
QNB
binds to acetylcholine mucurinic receptors
46
Beta particle emission: radio isotope
Tritium PNN unstable, so decays to helium-3 PPN
47
Radioligand receptor binding is...
transient, reversible, selective saturable, displacement
48
increase affinity: k1 ___ k2 ___
k1 fast | k2 slow
49
kd =
k2/k1
50
kd (dissociation), how do we determine?
saturation experiment [radioligand] that labeled 50% receptor in sample
51
Ki (inhibition constant), how do we determine?
Competition experiment, [drug] that displaces 50% of radio ligand bound in sample
52
Affinity of drug for receptor
Kd
53
total number of receptors
Bmax
54
Saturation experiment
3H ligand tissue prep incubation for 1 hour total binding = Specific binding (SB) +NSB (bound to membrane) ``` T= total binding SB = T - NSB ``` Y-axis: SRB x-axis: [radioligand]
55
Increase affinity means ____ Kd
lower Kd
56
Competition experiment: radioactive form of drug not available
allows direct comparison of affinities of several different drugs Same as saturation, but now varied amounts of competitor ligand too y-axis: % SB of RL x-axis: log [competitor] M
57
increasing affinity
decrease KI
58
Intrinsic Activity:
activation of cellular activity by drug
59
Agonist
increase affinity, mimic NT (similar cell response) | fully/partially stimulate receptors (intrinsic activity)
60
Antagonist
Increase affinity, block receptors (no NT response) no intrinsic activity, don't stimulate receptors NO INTRINSIC ACTIVITY
61
Affinity
molecular attraction between drug and receptor
62
Intrinsic Activity
Activation of Cellular activity by drug
63
Partial + Full agonist
weaker than if just full
64
Primary site of drug action
synapse
65
3 Ways to remove a transmitter
1) Enzymes 2) Reuptake 3) Glial Reuptake
66
Ionotropic Receptors
Fast synaptic transmission (ms) Subunits around central ion ions go through
67
Ionotropic examples
acetylcholine GABA-A 5-HT3
68
Metabotropic
cell surface receptors regulate activity Slower (s) peptides alpha/beta subunits activate effectors Agonist receptor bind > Gprotein dissociation PHOSPHORYLATION
69
G sub salpha
increase phosphorylation
70
G sub i
decrease phosphorylation
71
Metabotropic receptor examples
Acetylcholine [M], monoamines, peptides
72
M2/M4
Increase K+ influx | Decrease adenylyl cyclase
73
M1/M3/M5
increase phosphoinositide
74
What can phosphorylation do?
``` receptor up down regulation ion channel open/close Enzyme activation/deactivation Neurotransmitter release dendritic growth cell metabolism ```
75
Amino acid NT
Glutamate GABA Glycine
76
Monoamines
Dopamine, Norepinephrine, Epinephrine, and Serotonin
77
Peptides
Opioids, Orexin, CRF, BDNF
78
Novel/Gases
NO, CO, H2S
79
Purines
ATP, Adenosine
80
Catecholamines
D, N, E
81
Indoleamine
Serotonin

Psychopharmacology (16 decks)

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