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Block 6 > Intro to CNS Pharm > Flashcards

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
Q

Act involved in

A

cognitive function
memory
movement control

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26
Q

Ach receptors

A

metabotropic- M1, M3 excitatory, M2, M4 inhibitory

ionotropic- nicotinic, excitatory

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27
Q

catecholamine synthesis

A

tyramine –> dopa –> dopamine –> NE –> E

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28
Q

catecholamine activity termination

A

COMT
reuptake
MAO

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29
Q

COMT breaks down

A

DA, NE, E, levodopa

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30
Q

COMT located in

A

postsynaptic neurons and glia- synaptic

liver- circulating

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31
Q

MAO breaks down

A

amines

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32
Q

MAO located in

A

GI, liver- circulating, food

nerve terminals, post- released

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33
Q

forms of MAO, locations, and substrates

A

MAO-A- liver + brain, catecholamines, 5HT, tyramine

MAO-B- brain, platelets, DA, tyramine

34
Q

too much tyramine

A

hypertensive crisis

35
Q

dopamine pathway

A

nigrostriatal
tuberoinfundibulnar
mesolimbic

36
Q

nigrostriatal pathway

A

dopamine

substantia nigra to neostratum

37
Q

function of nigrostriatal pathway

A

postural control
voluntary movement
lost in parkinson’s

38
Q

function of tuberoinfundibulnar pathway

A

inhibits prolactin secretion

39
Q

function of mesolimbic pathway

A

affect
emotion
cognition

40
Q

mesolimbic pathway

A

dopamine

ventral tegmental area to limbic regions

41
Q

excess mesolimbic

A

schizophrenia

42
Q

stimulation of mesolimbic

A

reward

addiction

43
Q

deficiency of mesolimbic

A

ADHD

depression

44
Q

dopamine receptors

A

D1- stimulates adenylyl cyclase on post synaptic

D2- inhibits adenylyl cyclase and dopamine release/synthesis; on post, cell bodies, axon terminals

45
Q

D1 function and location

A

stimulates adenylyl cyclase

post

46
Q

D2 function and location

A

inhibits adenylyl cyclase and dopamine release/synthesis

post, cell bodies, axon terminals

47
Q

NE pathway

A

locus ceruleus to cerebral cortex, thalamus, hypothalamus, cerebellum, spinal cord

48
Q

NE released in response to

A 
external stimuli
arousal/stimulation
learning
memory
mood
49
Q

NE dysfunction

A

ADHD
depression disorders
anxiety disorders

50
Q

NE receptors

A

alpha1- excitatory post
alpha2- presynaptic- decrease Ca influx; post- inhibitory
beta- excitatory post

51
Q

alpha1 NE receptor

A

excitatory post

52
Q

alpha2 NE receptor

A

presynaptic- decrease Ca influx

post- inhibitory

53
Q

beta NE receptor

A

excitatory post

54
Q

serotonin pathways

A

dorsal raphe nucleus to amygdala, hippocampus, cerebral cortex and spinal cord

55
Q

serotonin function

A

mood, fear/anxiety, emotional memory
inhibition of physiological sexual response (spinal cord)
vomit stimulation (spinal cord)

56
Q

5HT1a receptor

A

cell body- decreases firing

postsynpatic- inhibitory

57
Q

5HT1d receptor

A

axon terminal- decrease release and firing

58
Q

5HT2a receptor

A

post excitatory

59
Q

5HT3 receptor

A

post excitatory

CTZ- nausea/vomiting

60
Q

serotonin dysfunction

A

schizophrenia
depression
anxiety

61
Q

histamine pathway

A

hypothalamus to many areas

62
Q

histamine function

A

arousal
body temp
vascular dynamics

63
Q

histamine receptors

A

excitatory

neurons, vessels, glia

64
Q

GABA

A

major inhibitory NT of CNS

brain and brainstem

65
Q

GABA receptors

A

Cl channels
hyper polarize
5 subunits
deficient in anxiety

66
Q

glycine

A

inhibitory used in interneurons of spinal cord and brainstem

pain transmission, respiration, motor coordination

67
Q

strychnine

A

glycine antagonist

68
Q

glutamate

A

main excitatory NT

69
Q

glutamate receptors

A

metabotropic- modulate NMDA activity

ionotropic- NMDA/AMPA increase Ca conductance

70
Q

opioids are

A

inhibitory

71
Q

endogenous opioids

A

enkephalins
beta-endorphin
dynorphin
endomorphin

72
Q

opioid receptors

A

mu, kappa- drug targets

delta, epislon- not

73
Q

mu receptor effects

A

sedation
euphoria
significant respiratory depression

74
Q

kappa receptor effects

A

hypnosis
dysphoria
less respiratory depression

75
Q

effects of opioids

A 
mitosis
N/V
cough suppression
histamine release- facial flushing
facial itching
dependence
withdrawal effects
76
Q

triad of opioid overdose

A

unconscious
respiratory depression
miosis

77
Q

withdrawal effects

A 
cramps, N/V
muscle aches/spasms
goosebumps
increased secretions
increased pain sensitivity
craving
78
Q

endogenous endocannabinoid

A

anadamide

79
Q

function of endocannabinoids

A 
mood
appetite
pain sensation
smooth muscle tone
immune function
80
Q

endocannabinoid receptor

A

CB1- metabotropic, inhibitory

Block 6 (24 decks)

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