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MSS - CV Exam 2 > Intro to ANS Pharmacology > Flashcards

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
Q

types of mAChR?

A

M1-5

M2 - heart, nerve, smooth muscle
M3 -glands, smooth muscle, endothelium

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26
Q

M2

A

inhibits cAMP production

slows heart rate

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27
Q

M3

A

activates IP3 and DAG production

constricts smooth muscle

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28
Q

adrenergic neurotransmission?

A

catecholamines

no enzyme breakdown

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29
Q

synthesis of dopamine

A

tyrosine enters cell

-tyrosine hydroxylase turns tyrosine to dopamine

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30
Q

catecholamines

A

dopamine, NE, E

primary precursor - tyrosine

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31
Q

synthesis of NE and E

A

dopamine enters vesicle and is converted to NE or E

NE > E in adrenal medulla

32
Q

norepinephrine receptors?

A

alpha, beta - end organ

alpha-2, beta-2 - presynaptic membrane

33
Q

NE recycling?

A

shuttled back into cell

-broken down or recycled

34
Q

cocaine

A

blocks NE membrane transporter

35
Q

catecholamine synthesis?

A

tyrosine > dopa > dopa > NE > E

**don’t worry about enzymes

36
Q

what occurs in nerve cytoplasm?

A

tyrosine to dopamine

37
Q

what happens vesicle?

A

dopamine to NE

38
Q

what occurs in adrenal medulla?

A

NE to E (chromafin cells)

39
Q

Na+ dependent tyrosine transporter

A

transporter tyrosine into nerve terminal

40
Q

vesicular monoamine transporter

A

aka VMAT-2

transports NE, Epi, DA, and serotonin into vesicles

release upon action potential and Ca2+ influx

41
Q

NE transporter

A

aka NET

imports NE into nerve terminal

DAT

42
Q

reserpine

A

only drug you need to know

used to be used for BP

inhibits transporter VMAT-2
-less NE release

43
Q

major mechanisms that terminates catecholamine action?

A

reuptake

NET and DAT

after reuptake, catecholamines stored in vesicles by VMAT-2

44
Q

metabolism of catecholamines?

A

MAO

COMT

45
Q

two subsets of adrenergic receptors?

A

alpha and beta

46
Q

DA receptors

A

GPCR

47
Q

alpha receptor

A

GPCR

48
Q

beta receptor

A

GPCR

49
Q

alpha 1

A

E > NE

50
Q

beta 3

A

adipose

NE < E

51
Q

alpha 2

A

E > NE

52
Q

beta 1

A

E = NE

53
Q

beta 2

A

E > NE

54
Q

autonomic ?

A

usually alpha 1

alpha 2 found pre-junctionally

55
Q

beta 2

A

smooth muscle in sympathetics

56
Q

beta 1

A

cardiac muscle

  • sympathetic
  • increase force and rate of contraction
57
Q

alpha 1 receptors

A

contraction of smooth muscle***
-regardless of location

  • vascular smooth muscle - vasoconstriction
  • glandular smooth muscle
58
Q

beta 2 receptors

A

relax smooth muscle***
-vasodilation

beta 2 agonists used for asthma

epi-pen target

59
Q

muscarinic receptors

A

contract smooth muscle

-different intracellular signaling than alpha-1, but still results in contraction

60
Q

beta-1

A

increases heart rate

61
Q

end organs

A

dual innervation of S and PS

62
Q

smooth muscle in vascular?

A

no parasympathetic innervation

Discrepancy:
ACh and muscarinic agonists give IV results in vasodilation b/c of NO release

63
Q

NO?

A

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
Q

nitroglycerine

A

can result in vasodilation

-GTP > cGMP - vasodilation

65
Q

the big tables?

A

understand the general trends of receptors and S and PS effects

66
Q

adrenal medulla

A

ACh binds to Nn AChR and results in localized depolarization at chromaffin cells

release of 80% Epi and 20% NE

67
Q

cholinomimetic

A

mimic ACh
-acetylcholinesterase inhibitors
AChR agonists

68
Q

cholinoceprot-blocking drugs

A

AChR antagonists

69
Q

sympathomimetic agents

A

mimic or enhance alpha and beta receptors

  • enhance catecholamine synthesis
  • block reuptake
70
Q

adrenoceptor-blocking drugs?

A

alpha and beta receptor antagonists

71
Q

cocaine

A

inhibits neutrotransmitter uptake adrenergic receptors

72
Q

inhibition of NT release?

A

botulinum - cholinergic

bretylium - adrenergic

73
Q

M2

A

cardiac muscle

74
Q

M3

A

smooth muscle

75
Q

cotransmitters in vesicles?

A

NPY, ATP, NE

76
Q

beta3

A

increased lipolysis

77
Q

alpha2

A

vascular smooth m. contraction
decreased insulin secretion
decreased NE release

MSS - CV Exam 2 (7 decks)

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