Intro to ANS Pharmacology Flashcards

1
Q

drug receptor

A

aka drug target

cellular macromolecule with which the drug interacts to elicit a cellular response

proteins or DNA

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2
Q

agonist

A

activates a receptor to signal as direct result of binding

some activate all signaling cascades, while others only choose 1 or 2 signaling cascades
-full vs selective

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3
Q

antagonist

A

bind to receptors but do not activate generation of signal

interefere with ability of agonist to activeate the receptor

some suppress basal signaling of receptors of receptors constitutively active

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4
Q

somatic

A

consciously controlled

-movement, respiration, posture

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5
Q

ANS

A

unconscious action

-CO, blood flow, digestion

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6
Q

sympathetic

A

thoracolumbar

fight or flight

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7
Q

parasympathetic

A

craniosacral

rest and digest

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8
Q

S and PS

A

typically oppose each other

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9
Q

parasympathetic neurotransmitter?

A

ACh

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10
Q

parasympathetic receptors?

A

nAChR

mAChR

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11
Q

sympathetic neurotransmitter?

A

NE > Epi (DA); AcH

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12
Q

sympathetic receptor?

A

a, B, D, nAChR, mAChR

**alpha and beta adrenergic

-postganglionic

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13
Q

somatic neurotransmitter

A

ACh

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14
Q

preganglionic neurotransmitters?

A

always ACh on nACHr

-both S and PS

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15
Q

two exceptions?

A

sweat glands

  • sympathetic
  • only occurs in response to muscarinic ACh

adrenal medulla
-releases epinephrine (fight/flight)
-to do this:
nAChR activated by ACh

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16
Q

4 steps of junctional transmission?

A

synthesis of ACh
storage
release
destruction

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17
Q

cholinergic neurotransmission

A

junctional transmission
ACh signaling
end-organ effects

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18
Q

ACh synthesis?

A

Acetyl CoA and choline

by ChAT

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19
Q

breakdown of ACh?

A

choline and acetate

by acetylcholinesterase

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20
Q

nAChR

A

ionotropic (ligand gated ion channels)

  • brain, autonomic ganglia, adrenal medulla
  • excitatory

agonists:acetylcholine/nicotine

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21
Q

mAChR

A

metabotropic (G protein coupled receptor)

  • CNS, autonomic ganglia, effector organs
  • excitatory and inhibitory
  • sweat secretion

agonists: ACh, muscarine

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22
Q

adrenal medulla

A

sympathetic nAChR

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23
Q

Nm receptors?

A

skeletal muscles

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24
Q

Nn receptors?

A

postganglionic cell body

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25
types of mAChR?
M1-5 M2 - heart, nerve, smooth muscle M3 -glands, smooth muscle, endothelium
26
M2
inhibits cAMP production | slows heart rate
27
M3
activates IP3 and DAG production | constricts smooth muscle
28
adrenergic neurotransmission?
catecholamines no enzyme breakdown
29
synthesis of dopamine
tyrosine enters cell | -tyrosine hydroxylase turns tyrosine to dopamine
30
catecholamines
dopamine, NE, E primary precursor - tyrosine
31
synthesis of NE and E
dopamine enters vesicle and is converted to NE or E NE > E in adrenal medulla
32
norepinephrine receptors?
alpha, beta - end organ | alpha-2, beta-2 - presynaptic membrane
33
NE recycling?
shuttled back into cell | -broken down or recycled
34
cocaine
blocks NE membrane transporter
35
catecholamine synthesis?
tyrosine > dopa > dopa > NE > E **don't worry about enzymes
36
what occurs in nerve cytoplasm?
tyrosine to dopamine
37
what happens vesicle?
dopamine to NE
38
what occurs in adrenal medulla?
NE to E (chromafin cells)
39
Na+ dependent tyrosine transporter
transporter tyrosine into nerve terminal
40
vesicular monoamine transporter
aka VMAT-2 transports NE, Epi, DA, and serotonin into vesicles release upon action potential and Ca2+ influx
41
NE transporter
aka NET imports NE into nerve terminal DAT
42
reserpine
only drug you need to know used to be used for BP inhibits transporter VMAT-2 -less NE release
43
major mechanisms that terminates catecholamine action?
reuptake NET and DAT after reuptake, catecholamines stored in vesicles by VMAT-2
44
metabolism of catecholamines?
MAO | COMT
45
two subsets of adrenergic receptors?
alpha and beta
46
DA receptors
GPCR
47
alpha receptor
GPCR
48
beta receptor
GPCR
49
alpha 1
E > NE
50
beta 3
adipose NE < E
51
alpha 2
E > NE
52
beta 1
E = NE
53
beta 2
E > NE
54
autonomic ?
usually alpha 1 alpha 2 found pre-junctionally
55
beta 2
smooth muscle in sympathetics
56
beta 1
cardiac muscle - sympathetic - increase force and rate of contraction
57
alpha 1 receptors
contraction of smooth muscle*** -regardless of location - vascular smooth muscle - vasoconstriction - glandular smooth muscle
58
beta 2 receptors
relax smooth muscle*** -vasodilation beta 2 agonists used for asthma epi-pen target
59
muscarinic receptors
contract smooth muscle | -different intracellular signaling than alpha-1, but still results in contraction
60
beta-1
increases heart rate
61
end organs
dual innervation of S and PS
62
smooth muscle in vascular?
no parasympathetic innervation Discrepancy: ACh and muscarinic agonists give IV results in vasodilation b/c of NO release
63
NO?
ACh muscarinic activation on endothelial cells - results in NO sythesis - NO goes to smooth muscle to result in vasodilation conversion of GTP to cyclic GMP results in VASODILATION EDRF - endothelium derived relaxing factor (NO)
64
nitroglycerine
can result in vasodilation | -GTP > cGMP - vasodilation
65
the big tables?
understand the general trends of receptors and S and PS effects
66
adrenal medulla
ACh binds to Nn AChR and results in localized depolarization at chromaffin cells release of 80% Epi and 20% NE
67
cholinomimetic
mimic ACh -acetylcholinesterase inhibitors AChR agonists
68
cholinoceprot-blocking drugs
AChR antagonists
69
sympathomimetic agents
mimic or enhance alpha and beta receptors - enhance catecholamine synthesis - block reuptake
70
adrenoceptor-blocking drugs?
alpha and beta receptor antagonists
71
cocaine
inhibits neutrotransmitter uptake adrenergic receptors
72
inhibition of NT release?
botulinum - cholinergic | bretylium - adrenergic
73
M2
cardiac muscle
74
M3
smooth muscle
75
cotransmitters in vesicles?
NPY, ATP, NE
76
beta3
increased lipolysis
77
alpha2
vascular smooth m. contraction decreased insulin secretion decreased NE release