ANS part 2: adrenergic Flashcards

1
Q

alpha 1 agonists

A
  1. methoxamine
  2. phenylephrine
  3. pseudoephedrine
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2
Q

alpha 2 agonists

A
  1. clonidine
  2. alpha-methyldopa
  3. Methylnorepinephrine
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3
Q

beta 1 agonists

A

dobutamine

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4
Q

beta 2 agonist

A

salbutamol

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5
Q

beta 3 agonist

A
  • brl37344

- mirabegron

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6
Q

the sympathetic NS can have different types of receptors. what are they and what do they innervate?

A
  • adrenergic (for adrenal medulla)
  • noradrenergic (smooth m, heart, glands)
  • dopamine d1 (renal b.v)
  • acetalcholine muscarinic (sweat glands, b.v., skeletal muscles)
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7
Q

adrenergic receptors are what type of receptor

A

GPCR

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8
Q

alpha 1 agonist binds to what g protein/activation?

A

Gq (excitation)

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9
Q

beta 1 and beta 2 agonist binds to what g protein/activation?

A

Gs (excitation)

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10
Q

alpha 2 binds to what g protein/activation?

A

Gi (inhibition)

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11
Q

alpha receptors have a high affinity for

A

E > NE&raquo_space; isoproterenol

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12
Q

Non-specific antagonist for alpha receptors

A

phentolamine

Phenoxybenzamine

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13
Q

alpha 1 and 2 receptors are found

A

on blood vessels

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14
Q

binding to alpha 1 causes

A

vasoconstriction (and BP increases)

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15
Q

binding to alpha 2 causes

A

vasodilation

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16
Q

binding to alpha 1 causes excitation or inhibition of Gq?

A

excitation

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17
Q

alpha 1 receptors are found pre or post synaptic?

A

POST

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18
Q

Ag of alpha 1

A

methoxamine
phenylephrine
Pseudoephidrine

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19
Q

Antag of alpha 1 and action

A

prazosin, vasodilation

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20
Q

binding to alpha 2 causes excitation or inhibition?

A

inhibition of Gi

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21
Q

where is alpha 2 receptor found (pre or post synaptic)

A

PRE AND POST

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22
Q

Ag alpha 2 receptor and action

A

clonidine

Alpha methyldopa methylnorpinephrine, vasodilation

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23
Q

Antag of alpha 2 receptor and action

A

yohimbine, vasocontriction

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24
Q

affinity of beta receptors to agonists

A

isoproterenol&raquo_space; E > NE

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25
Q

antagonist of beta receptors

A

propranolol

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26
Q

location of beta 1

A

heart

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27
Q

location of beta 2

A

respiratory system

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28
Q

location of beta 3

A

adipose tissue

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29
Q

antag beta 1

A

atenolol

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30
Q

effect of dobutamine

A
  • increase HR

- increase chronotropy

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31
Q

effect of salbutamol

A

-bronchoDILATION

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32
Q

what is salbutamol used to treat

A
  • asthma

- COPD

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33
Q

what does brl3744 do

A
  • increase body temp

- decrease fat

34
Q

what does atenolol do

A
  • decrease HR

- decrease BP

35
Q

what 2 agonists bind to both alpha and beta

A

-NE and E

36
Q

NE has an affinity for which beta receptor

A

beta 1 (heart)

37
Q

E has an affinity for which beta receptor

A

beta 1 and 2 (heart and resp. - use to treat asthma attack)

38
Q

dopamine has a high affinity for which receptor

A

D1 and D2 (dopamine receptors)

39
Q

isoproterenol has a high affinity for which receptor

A

beta 1 and 2

40
Q

fenoldopam has a high affinity for which receptor

A

D1

41
Q

what are the 5 endogenous adrenergic agonists

A

catecholamines:

  1. dopamine
  2. NE/E
  3. NA/A
42
Q

agonist for beta 2

A
  • albuterol
  • terbutaline
  • metaproternol
  • ritodrine
43
Q

all CA’s are synthesized from

A

tyrosine

44
Q

order of CA molecules that are synthesized

A

tyrosine -> dopa -> dopamine -> norepi -> epi

45
Q

dopamine is metabolised by what enzyme to form what

A

dopamine -> DOPAC (via MAO: monoamine oxidase)

46
Q

DOPAC is metabolized by what enzyme to form what

A

COMT to form HVA

47
Q

where is MAO found

A

mitochondrial surface

48
Q

where is COMT found

A

cytoplasm

49
Q

NA and A are metabolised by COMT and MAO to form what

A

VMA

50
Q

Epi binding to alpha1 causes

A

vasoconstriction, increase BP, and reflex bradycardia

51
Q

Epi binding to beta 1 causes

A

increase BP, inotropic and chronotropic

52
Q

Epi binding to beta 2 causes

A
  • bronchodilation

- coronary vasodilation (more blood to heart to help with increased BP)

53
Q

what are the systemic therapeutic indications for Epi

A
  1. cardiac arrest
  2. hypotension/shock
  3. bronchospasm
  4. hypersensitivity reactions/anaphylactic shock
54
Q

what are the topical therapeutic indications for Epi

A
  1. prolongued action of local anesthetics

2. topical hemostatic

55
Q

is NE a potent agonist for alpha and beta?

A

only alpha and beta 1

*weak beta 2 agonist

56
Q

effect of NE

A
  • B1: increase BP
  • inotropic and chronotropic
  • A1: vasoconstriction
  • mydriasis
57
Q

what is NE used to treat

A

shock (with severe hypotension)

58
Q

low doses of dopamine will cause

A

renal and splanchnic vasodilation

59
Q

high doses of dopamine will cause

A
  • vasodilation

- increased renal blood flow, diuresis, and natriuresis

60
Q

why does dopamine have limited CNS access

A
  • high polarity

- peripheral metabolism

61
Q

what is dopamine used to treat

A
  • severe hypertension

- shock (cardiogenic, renal failure)

62
Q

methoxamine administered intravenously has ___(faster/slower) effects and activity compared to intramuscularly

A

faster and higher

63
Q

what is methoxamine used to treat

A
  • hypotensive states
  • maintain BP during surgery
  • paroxysmal atrial tachycardia
64
Q

what effect does phenylephrine have

A
  • lower HR

- increase stroke output

65
Q

what is phenylephrine used to treat

A

-hypotensive state

66
Q

what is pseudoephedrine used to treat

A

nasal decongestion

67
Q

what is clonidine used to treat

A

hypertension

68
Q

what are 3 adverse effects of clonidine

A
  1. dry mouth
  2. sedation
  3. bradycardia
69
Q

what is alpha-methyldopa used to treat

A

hypertension

70
Q

how does alpha-methyldopa work

A

inhibits DOPA decarboxylase, so prevents the formation of CA’s

71
Q

what is dobutamine used to treat

A

congestive heart failure

72
Q

what is salbutamol used to treat

A
  • asthma
  • chronic bronchitis
  • pulmonary emphysema
73
Q

what is mirabegron used to treat

A

overactive bladder

74
Q

mechanism of action for amphetamine

A
  • increase release of NE/DA
  • inhibit MAO
  • alpha agonist
75
Q

CNS stimulation effects of amphetamine (D-amph)

A
  • sleep and fatigue reversal
  • stim medullary respiratory center
  • suppress appetite
  • psychosis
  • potential for abuse and addiction
76
Q

PNS stimulation effects of amphetamine (L-amph)

A
  • increase cardiovascular

- GI (dry mouth, metallic taste, nausea, vomiting, diarrhea)

77
Q

name 4 indirect adrenergic agonists

A
  1. amphetamine
  2. methylphenidate
  3. moclobemide
  4. phenelzine
78
Q

methylphenidate is a mild CNS stimulator. what is it used to treat

A
  • ADHD

- narcolepsy

79
Q

MAO inhibitors work by

A

inhibiting MAO, so increase monoamines in CNS

80
Q

what are MAO inhibitors used to treat

A

depression

81
Q

name 2 indirect acting adrenergic antagonists and what they do

A
  1. alpha-methyldopa (inhibits DOPA-decarboxylase)

2. reserpine (inhibit vesicular transport)

82
Q

give 2 examples of MAO inhibitors

A
  • moclobemid (reversible)

- phenelzine (irreversible)