Intro to CNS Pharm Flashcards Preview

Block 6 > Intro to CNS Pharm > Flashcards

Flashcards in Intro to CNS Pharm Deck (80):
1

drugs enter the CNS

transcellularly

2

factors affecting CNS drug movment

lipophilicity
size

3

sites of CNS drug action (7)

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

4

mechanisms of increasing neuronal activity

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

5

mechanisms of decreasing neuronal activity

inhibitory agonism
excitatory antagonism
decrease excitability
decrease excitatory release

6

physiological antagoinsm

2 things have different mechanisms

7

pharmacological antagonism

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

8

description of how voltage gated Na channel works

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

9

voltage gated Na channel is a drug target for

epilepsy
anesthesia

10

ion used in GABAa receptor

Cl

11

structure of GABAa receptor

5 summits with various binding sites for several moleucles

12

GABAa receptor inhibitory or excitatory

inhibitory- lets Cl in which hyperpolrizes

13

transient receptor potential channels

nonselective cation channels

14

TRP channels involved in

pain sensation, sensory signaling, CNS

15

TRP channels activated by

cannabinoids
capsaicin

16

metabotropic receptors

G protein coupled
slow
modulate

17

inotropic receptors

fast
information transmission

18

Na, K, Ca

stimulatory cations in inotropic receptors

19

Cl

inhibitory anion in inotropic receptors

20

Gq Gs

stimulatory for metabotropic receptors

21

Gi

inhibitory for metabotropic receptors

22

phasic release

transient release by bursts of APs

23

tonic relesae

constant low level release from basal neuronal activity

24

acetylcholine brain structures

ventral forebrain to cortex and hippocampus

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