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Q3 Pharm Cholinergics > Adrenergic Stimulants > Flashcards

Adrenergic Stimulants Flashcards

1
Q

NE released from?

Stimulates?

A

nerves

α and β1 receptors

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2
Q

Epinephrine released from?

Stimulates?

A

adrenal medulla (into circulation)

α and β receptors

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3
Q

NE made how?

A

Tyrosine into terminal ->
+ tyrosine hydroxylase = L-DOPA ->
Dopamine -> NE

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4
Q

EpiNE made how?

A

from NE in adrenal medulla

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5
Q

What releases NE from terminal?

A

amphetamine

tyramine

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6
Q

What inhibits NE from reuptake?

A

cocaine

antidepressants

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7
Q

NE metabolized by what on reuptake?

A

MOA (Monoamine oxidase),

COMT

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8
Q

Adrenergic Stim constricts bv to?

What receptors?

A

skin, kidney, mucous membranes

α1

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9
Q

Adrenergic Stim relaxes bv to?

What receptors?

A

skeletal mm

β2

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10
Q

Adrenergic Stim of M receptors does what?

A

↑ saliva and sweat glands

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11
Q

Adrenergic Stim of β2 receptors does what?

A

relax gut wall and bronchiloes

relax bv to skeletal mm

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12
Q

Adrenergic Stim of β receptors does what?

A

excite cardiac
glycogenolysis, lipolysis
modulate insuin and renin

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13
Q

Adrenergic Stim of CNS does what?

A

respiratory stim
wakefulness
↓ appetite

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14
Q

Adrenergic Stim of α2 receptors does what?

A

inhibit transmitter release

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15
Q

Action of Direct-acting drugs on noradrenergic (NE) terminals?

A

directly stim α and β receptors

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16
Q

Actions of Indirect-acting drugs on noradrenergic terminals? (3)

A 
↑ release of NE (tyramine)
inhibit reuptake (cocaine)
inhibit catabolism (MAO inhibitor)
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17
Q

Denervation (depletion of NE) in Noradrenergic terminal has what effect on indirect-acting drugs?

What drug denerves NE terminals?

A

stops effect

Resperine

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18
Q

Denervation (depletion of NE) in Noradrenergic terminal has what effect on direct-acting drugs?

A

none or enhance effect

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19
Q

α Receptors respond to what neurotrans?

A

Epi and NE

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20
Q

α1 Receptors are excitatory or inhibitory?

Route of action?

A

excitatory

IP3 -> ↑ Ca2+ -> DAG -> activates PKC

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21
Q

α1 Receptors agonist?

Causes?

A

Phenylephrine

Vasoconstriction, ↑ vascular resistance
Vasoconstriction nasal mucosa (↓ congestion)
Dilate pupils
Contract genitourinary (continence)
Stim Pilomotor (hair erection)
Glycogenolysis/Glucogenesis
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22
Q

α2 Receptors are excitatory or inhibitory?

Route of action?

A

inhibitory: (U) presynap where ↓ neurotrans release

↓ adenylyl cyclase -> ↓ cAMP

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23
Q

α2 Receptors agonist?

Causes?

A

Clonidine

inhibit NE release -> ↓ BP

inhibit ACh release ->:
↓ intestinal tone/secretions,
Platelet aggregation,
Vasoconstrict coronary, renal, mucosal, skin,
↓ insulin secretion
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24
Q

Affinity of EpiNE, NE, and Isoproterenol on α Receptors?

A

EpiNE = NE&raquo_space; Iso

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25
Q

Affinity of EpiNE, NE, and Isoproterenol on β Receptors?

A

Iso ++ for all
Epi = NE for β1
Epi ++, NE - - for β2
NE&raquo_space; Epi for β3

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26
Q

Route of Action for β Receptors?

A

activate adenylyl cyclase -> ↑ cAMP

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27
Q

β1 Receptor agonist?

Causes?

A

Dobutamine

↑ rate/force on heart contraction
↑ AV conduction velocity/automaticity
↑ renin secretion by kidney

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28
Q

β2 Receptor agonist?

Causes?

A

Albuterol

weaker cardiac effects
Relax resp, uterine, GI smooth mm
Relax BV to skeletal mm
Promote K+ uptake by skeletal mm
↑ glycogenolysis/glucogenesis
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29
Q

β3 Receptor agonist?

Causes?

A

none

lipolysis in fat cells

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30
Q

NE doesn’t effect lungs, why?

A

mostly β2 receptors, has no affinity for them

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31
Q

Isoproterenol doesn’t effect most BV why?

A

mostly α receptors, no affinity

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32
Q

Dopamine (DA) Receptors important to? (3)

A

brain

renal and splanchinic vasculature

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33
Q

D1 receptors route of action?

Causes?

A

stim adenylyl cyclase

dilate renal BV

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34
Q

D2 receptors route of action?

Causes?

A

inhibit adenylyl cyclase ->
open K+ channels ->
↓ Ca2+ infulx

inhibits release of transmitters from terminal

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35
Q

Sympathomimetic drugs do?

Effect depends on? (3)

A

mimic effects of neurotransmitters

proportion of α β activity drug possesses,
distribution of α β receptors in tissue,
reflex responses

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36
Q

Atherosclerosis affects α receptors and baroreceptors how?

A

↑ effects of α receptors

↓ effects of baro

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37
Q

NE (Levophed) affects what receptors?

A

⍺ and β1
minor β2

(⍺ = β1&raquo_space; β2)

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38
Q

Levophed administered?

Duration?

A

IV

very short (rapid metabolism)

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39
Q

Levophed primary effect?

A

⍺ -> vasoconstriction ->
↑ both S and D blood pressure

β1 -> ↑ HR but baroreceptors will override

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40
Q

Levophed effects on blood flow?

CO?

A

↓ flow to kidney, spleen, liver

no Δ

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41
Q

Levophed side effect?

A

vasoconstrict injection site -> necrosis

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42
Q

Levophed primarily used to?

A

reverse hypotension

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43
Q

Administration of Atropine before Levophed results in?

A

block vagal reflex of baroreceptors

= HR ↑

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44
Q

EpiNE (Adrenaline) effects what receptors?

A

⍺, β1, β2

45
Q

Adrenaline administered?

Duration?

A

injection

short

46
Q

Adrenaline effect depends on?

A

dose

47
Q

Adrenaline effects on ⍺?

A

vasoconstriction -> SBP
(initially both BP, then DBP drops due to β2)

↓ insulin secretion

48
Q

Adrenaline effects on β1?

A

↑ HR and contraction force
(inotropic and chronotropic)

↑ renin secretion

49
Q

Adrenaline effects on β2?

A

dilate BV to skeletal mm ->
↓ DBP (*overrides ⍺ )

↑ glycogenolysis (↑ blood glucose)

bronchodilation

50
Q

Inotrpoic means?

A

affects contractility

51
Q

Chronotropic means?

A

affects rate/timing

52
Q

Adrenaline effects on β3?

A

↑ lipolysis in fat cells = ↑ free fatty acid

53
Q

Overall result of Adrenaline?

A

↑ systolic pressure, ↑ HR
little Δ in mean pressure

↑ blood glucose

bromchodilation

54
Q

Adrenaline low/slow dose results in?

A

mainly β2 stim (vasodilation):
↑ HR, contractility, coronary blood flow = ↑ CO and O2 consumption

constricted BF to skin, musoca, kidney = ↑ SBP/DBP

55
Q

Adrenaline high/rapid dose results in?

A

mainly ⍺ stim (vasoconstriction):

↑↑ SBP/DBP

56
Q

Primary use of Adrenaline (EpiNE)? (5)

A

1) anaphylactic shock
2) cardiac arrest/complete heart block
3) ↓ diffusion of local anesthesia (vasoconstr)
4) glaucoma (↑ removal, ↓ production aqueous humor)
5) severe asthma (bronchodil)

57
Q

Adrenaline side-effects? (6)

A 
tremor
throbbing HA
↑↑ BP/hypertension (if β-block)
tachycardia
angina
cerebral hemorrhage
58
Q

Ephedrine (Ephedra) administered?

Duration?

A

oral

long

59
Q

Ephedra acts on what receptors?

A

⍺ and β (similar to Adrenaline)

60
Q

Main effects of Ephedra?

A

bronchodilation
CNS stim
high BP and stroke

61
Q

Overall effects of ⍺ Agonists?

A

vasoconstriction -> ↑ peripheral vasc resistance

↑ BP -> ↓ HR (reflex)

62
Q

Phenylephrine affects what receptors?

Neofrin, Neo-Synephrine

A

⍺1

63
Q

Neofrin/Syn effects on ⍺1 receptors?

A

typical ⍺ Agonist +

vasoconstriction of nasal and up resp bv

64
Q

Neofrin/Syn used to tx? (3)

A

1) decongestant
2) pupil dilation for eye exam
3) hypotensive emergency

65
Q

Neofrin/Syn side-effects?

A

rebound congestion

caution for HTN pts (↑ HTN)

66
Q

Methoxamine (Vasoxyl) similar to?

A

Phenylephrine

use IV for hypotension

67
Q

Pseudophedrine (Sudafed) affects what receptors?

A

⍺

68
Q

Pseudophedrine effects on ⍺ receptors?

Side-effects?

A

similar to Phenylephrine,
more effective orally than Pheny

caution for HTN

69
Q

Xylometazoline/Oxymetazoline affect what receptors?

Otrivin/Afrin

A

direct ⍺ agonists

70
Q

Xylometazoline/Oxymetazoline administered?

Side-effects?

A

topically

rebound congestion from receptor down-regulation

71
Q

Tetrahydrozoline/Naphazoline affect what receptors?
(Visine)

How?

A

⍺

vasoconstriction

72
Q

Tetrahydrozoline/Naphazoline contraindicated for?

A

narrow-angle glaucoma,

HTN

73
Q

Clonadine (Catapres) affects what receptors?

A

⍺2

74
Q

Clonadine effects on ⍺2?

A

stim ⍺2 in CNS presyn terminal ->
↓ NE release (↓ SNS) ->
↓ BP

75
Q

Clonadine used to tx?

A

HTN,
hot flashes,
withdrawal/cravings,
pre-anesthesia (↓ amount needed)

76
Q

Clonadine administered?

A

oral

transdermal patch

77
Q

Clonadine side-effects?

A

dry mouth, sedation, erect dysfxn

severe HTN if abruptly stopped

78
Q

Methyldopa (Aldomet) affects what receptors?

Effects?

A

⍺2

similar to Clonadine

79
Q

Apraclonidine (Iopidine) affects what receptors?

Effects?

A

⍺2

↓ aqueous humor -> ↓ IO pressure

80
Q

Isoproterenol (Isuprel) affects what receptors?

A

β&raquo_space; ⍺

81
Q

Isoproterenol effects on β receptors?

A

vasodilation of skeletal mm and renal/mesenteric vascular beds

↓ BP -> reflex ↑ HR

82
Q

Isoproterenol used to tx?

A

emergency cardiac arrest/complete heart block

83
Q

Isoproterenol side-effects?

A

tachycardia, palp, arrhyth

84
Q

Dobutamine (Dobuterex) affects what receptors?

A

β1

85
Q

Dobutamine effects on β1?

A

inotropic (↑ CO/contractility)

86
Q

Dobutamine used for? (3)

A

stress tests
cardiac shock
CHF

87
Q

Dobutamine side-effects?

A

HTN pt: ↑ HR and BP

88
Q

Albuterol (Ventolin) affects what receptors?

A

β2

89
Q

Albuterol used to tx?

A

asthma

90
Q

Albuterol side-effects?

A

tachycardia
mm tremors
HA

91
Q

Dopamine (Intropin) affects what receptors?

A

D1 in renal vascular beds

92
Q

Dopamine effects on D1?

Used to tx?

A

vasodilation -> ↑ renal BF -> ↑ filtration/Na+ excretion

cardiac shock

93
Q

High [Dopamine] affects what other receptors?

A

β1, ⍺1 and adrenergic NE release

94
Q

Dopamine side-effects? (6)

A 
N/V
tachycardia
angina
arrhyth
HA
peripheral vasoconstriction
95
Q

Fenoldopam (Corlopam) affects what receptors?

A

D1

96
Q

Fenoldopam effects on D1?

Used to tx?

A

dilation of vascular beds ->
↓ BP

severe HTN

97
Q

Amphetamine affects what receptors?

A

INDIRECT action on adrenergic and DA, esp in brain (CNS)

98
Q

Amphetamine effects on adrenergic/DA receptors?

CNS?

Peripheral?

A

release NE/DA

CNS:
↑ euphoria, alertness, motor activity
↓ appetite, need for sleep

Peripheral:
tachycardia, HTN, psychosis,
contracts urinary sphincter

99
Q

Amphetamine overdose effects?

A

cerebral hemorr, convulsions, coma

100
Q

Amphetamine use to tx? (2)

A

enuresis (bladder control)

ADHD (methyphenidate/Ritalin)

101
Q

Cocaine affects what receptors?

A

INDIRECT action on NE/DA terminals

inhibits reuptake

102
Q

Cocaine effects on NE/DA receptors?

A

similar to amphetamines
more intense/shorter acting

powerful vasoconstrictor

103
Q

Cocaine side-effects?

A

MI, HTN, stroke

psychosis

104
Q

Cocaine used for?

A

nasopharyngeal surgery (vasoconst, local anesthesia)

105
Q

Tyramine affects what receptors?

A

INDIRECT action on adrenergic terminals

106
Q

Tyramine effects on NE terminals?

A

releases NE,

displaces NE in vesicle -> becomes false transmitter (octopamine)

107
Q

Tyramine found in? (2)

A

food

tyrosine by-product

108
Q

Tyramine results in?

A

tachyphylaxis (↓ response from prolonged exposure)

109
Q

Tyramine contraindication?

A

MAO inhibitors

stop MAO from metabolizing tyramine =
massive NE release =
severe HTN

Q3 Pharm Cholinergics (7 decks)

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