Intro to CNS Pharm Flashcards

1
Q

drugs enter the CNS

A

transcellularly

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2
Q

factors affecting CNS drug movment

A

lipophilicity

size

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3
Q

sites of CNS drug action (7)

A
post synaptic receptors
axon terminal receptors
synthesis/release/transport
release
breakdown
reuptake pump
membrane and ion channels
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4
Q

mechanisms of increasing neuronal activity

A
excitatory agonism
inhibitory antagonism
increase release
prolong presence of excitatory
increase excitability
prolong recovery
*can also increase inhibitory action
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5
Q

mechanisms of decreasing neuronal activity

A

inhibitory agonism
excitatory antagonism
decrease excitability
decrease excitatory release

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6
Q

physiological antagoinsm

A

2 things have different mechanisms

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7
Q

pharmacological antagonism

A

2 things have the same mechanism- competing for the same receptor

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8
Q

description of how voltage gated Na channel works

A

closed at rest
opens with certain depolarization
inactivation gate shuts at certain depolarization

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9
Q

voltage gated Na channel is a drug target for

A

epilepsy

anesthesia

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10
Q

ion used in GABAa receptor

A

Cl

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11
Q

structure of GABAa receptor

A

5 summits with various binding sites for several moleucles

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12
Q

GABAa receptor inhibitory or excitatory

A

inhibitory- lets Cl in which hyperpolrizes

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13
Q

transient receptor potential channels

A

nonselective cation channels

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14
Q

TRP channels involved in

A

pain sensation, sensory signaling, CNS

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15
Q

TRP channels activated by

A

cannabinoids

capsaicin

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16
Q

metabotropic receptors

A

G protein coupled
slow
modulate

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17
Q

inotropic receptors

A

fast

information transmission

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18
Q

Na, K, Ca

A

stimulatory cations in inotropic receptors

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19
Q

Cl

A

inhibitory anion in inotropic receptors

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20
Q

Gq Gs

A

stimulatory for metabotropic receptors

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21
Q

Gi

A

inhibitory for metabotropic receptors

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22
Q

phasic release

A

transient release by bursts of APs

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23
Q

tonic relesae

A

constant low level release from basal neuronal activity

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24
Q

acetylcholine brain structures

A

ventral forebrain to cortex and hippocampus

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25
Act involved in
cognitive function memory movement control
26
Ach receptors
metabotropic- M1, M3 excitatory, M2, M4 inhibitory | ionotropic- nicotinic, excitatory
27
catecholamine synthesis
tyramine --> dopa --> dopamine --> NE --> E
28
catecholamine activity termination
COMT reuptake MAO
29
COMT breaks down
DA, NE, E, levodopa
30
COMT located in
postsynaptic neurons and glia- synaptic | liver- circulating
31
MAO breaks down
amines
32
MAO located in
GI, liver- circulating, food | nerve terminals, post- released
33
forms of MAO, locations, and substrates
MAO-A- liver + brain, catecholamines, 5HT, tyramine | MAO-B- brain, platelets, DA, tyramine
34
too much tyramine
hypertensive crisis
35
dopamine pathway
nigrostriatal tuberoinfundibulnar mesolimbic
36
nigrostriatal pathway
dopamine | substantia nigra to neostratum
37
function of nigrostriatal pathway
postural control voluntary movement lost in parkinson's
38
function of tuberoinfundibulnar pathway
inhibits prolactin secretion
39
function of mesolimbic pathway
affect emotion cognition
40
mesolimbic pathway
dopamine | ventral tegmental area to limbic regions
41
excess mesolimbic
schizophrenia
42
stimulation of mesolimbic
reward | addiction
43
deficiency of mesolimbic
ADHD | depression
44
dopamine receptors
D1- stimulates adenylyl cyclase on post synaptic | D2- inhibits adenylyl cyclase and dopamine release/synthesis; on post, cell bodies, axon terminals
45
D1 function and location
stimulates adenylyl cyclase | post
46
D2 function and location
inhibits adenylyl cyclase and dopamine release/synthesis | post, cell bodies, axon terminals
47
NE pathway
locus ceruleus to cerebral cortex, thalamus, hypothalamus, cerebellum, spinal cord
48
NE released in response to
``` external stimuli arousal/stimulation learning memory mood ```
49
NE dysfunction
ADHD depression disorders anxiety disorders
50
NE receptors
alpha1- excitatory post alpha2- presynaptic- decrease Ca influx; post- inhibitory beta- excitatory post
51
alpha1 NE receptor
excitatory post
52
alpha2 NE receptor
presynaptic- decrease Ca influx | post- inhibitory
53
beta NE receptor
excitatory post
54
serotonin pathways
dorsal raphe nucleus to amygdala, hippocampus, cerebral cortex and spinal cord
55
serotonin function
mood, fear/anxiety, emotional memory inhibition of physiological sexual response (spinal cord) vomit stimulation (spinal cord)
56
5HT1a receptor
cell body- decreases firing | postsynpatic- inhibitory
57
5HT1d receptor
axon terminal- decrease release and firing
58
5HT2a receptor
post excitatory
59
5HT3 receptor
post excitatory | CTZ- nausea/vomiting
60
serotonin dysfunction
schizophrenia depression anxiety
61
histamine pathway
hypothalamus to many areas
62
histamine function
arousal body temp vascular dynamics
63
histamine receptors
excitatory | neurons, vessels, glia
64
GABA
major inhibitory NT of CNS | brain and brainstem
65
GABA receptors
Cl channels hyper polarize 5 subunits deficient in anxiety
66
glycine
inhibitory used in interneurons of spinal cord and brainstem | pain transmission, respiration, motor coordination
67
strychnine
glycine antagonist
68
glutamate
main excitatory NT
69
glutamate receptors
metabotropic- modulate NMDA activity | ionotropic- NMDA/AMPA increase Ca conductance
70
opioids are
inhibitory
71
endogenous opioids
enkephalins beta-endorphin dynorphin endomorphin
72
opioid receptors
mu, kappa- drug targets | delta, epislon- not
73
mu receptor effects
sedation euphoria significant respiratory depression
74
kappa receptor effects
hypnosis dysphoria less respiratory depression
75
effects of opioids
``` mitosis N/V cough suppression histamine release- facial flushing facial itching dependence withdrawal effects ```
76
triad of opioid overdose
unconscious respiratory depression miosis
77
withdrawal effects
``` cramps, N/V muscle aches/spasms goosebumps increased secretions increased pain sensitivity craving ```
78
endogenous endocannabinoid
anadamide
79
function of endocannabinoids
``` mood appetite pain sensation smooth muscle tone immune function ```
80
endocannabinoid receptor
CB1- metabotropic, inhibitory