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Q3 Pharm Cholinergics > Adrenergic Stimulants > Flashcards

Adrenergic Stimulants Flashcards

(109 cards)

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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
Affinity of EpiNE, NE, and Isoproterenol on β Receptors?
Iso ++ for all Epi = NE for β1 Epi ++, NE - - for β2 NE >> Epi for β3
26
Route of Action for β Receptors?
activate adenylyl cyclase -> ↑ cAMP
27
β1 Receptor agonist? Causes?
Dobutamine ↑ rate/force on heart contraction ↑ AV conduction velocity/automaticity ↑ renin secretion by kidney
28
β2 Receptor agonist? Causes?
Albuterol ``` weaker cardiac effects Relax resp, uterine, GI smooth mm Relax BV to skeletal mm Promote K+ uptake by skeletal mm ↑ glycogenolysis/glucogenesis ```
29
β3 Receptor agonist? Causes?
none lipolysis in fat cells
30
NE doesn't effect lungs, why?
mostly β2 receptors, has no affinity for them
31
Isoproterenol doesn't effect most BV why?
mostly α receptors, no affinity
32
Dopamine (DA) Receptors important to? (3)
brain | renal and splanchinic vasculature
33
D1 receptors route of action? Causes?
stim adenylyl cyclase dilate renal BV
34
D2 receptors route of action? Causes?
inhibit adenylyl cyclase -> open K+ channels -> ↓ Ca2+ infulx inhibits release of transmitters from terminal
35
Sympathomimetic drugs do? Effect depends on? (3)
mimic effects of neurotransmitters proportion of α β activity drug possesses, distribution of α β receptors in tissue, reflex responses
36
Atherosclerosis affects α receptors and baroreceptors how?
↑ effects of α receptors ↓ effects of baro
37
NE (Levophed) affects what receptors?
⍺ and β1 minor β2 (⍺ = β1 >> β2)
38
Levophed administered? Duration?
IV very short (rapid metabolism)
39
Levophed primary effect?
⍺ -> vasoconstriction -> ↑ both S and D blood pressure β1 -> ↑ HR but baroreceptors will override
40
Levophed effects on blood flow? CO?
↓ flow to kidney, spleen, liver no Δ
41
Levophed side effect?
vasoconstrict injection site -> necrosis
42
Levophed primarily used to?
reverse hypotension
43
Administration of Atropine before Levophed results in?
block vagal reflex of baroreceptors | = HR ↑
44
EpiNE (Adrenaline) effects what receptors?
⍺, β1, β2
45
Adrenaline administered? Duration?
injection short
46
Adrenaline effect depends on?
dose
47
Adrenaline effects on ⍺?
vasoconstriction -> SBP (initially both BP, then DBP drops due to β2) ↓ insulin secretion
48
Adrenaline effects on β1?
↑ HR and contraction force (inotropic and chronotropic) ↑ renin secretion
49
Adrenaline effects on β2?
dilate BV to skeletal mm -> ↓ DBP (*overrides ⍺ ) ↑ glycogenolysis (↑ blood glucose) bronchodilation
50
Inotrpoic means?
affects contractility
51
Chronotropic means?
affects rate/timing
52
Adrenaline effects on β3?
↑ lipolysis in fat cells = ↑ free fatty acid
53
Overall result of Adrenaline?
↑ systolic pressure, ↑ HR little Δ in mean pressure ↑ blood glucose bromchodilation
54
Adrenaline low/slow dose results in?
mainly β2 stim (vasodilation): ↑ HR, contractility, coronary blood flow = ↑ CO and O2 consumption constricted BF to skin, musoca, kidney = ↑ SBP/DBP
55
Adrenaline high/rapid dose results in?
mainly ⍺ stim (vasoconstriction): | ↑↑ SBP/DBP
56
Primary use of Adrenaline (EpiNE)? (5)
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
Adrenaline side-effects? (6)
``` tremor throbbing HA ↑↑ BP/hypertension (if β-block) tachycardia angina cerebral hemorrhage ```
58
Ephedrine (Ephedra) administered? Duration?
oral long
59
Ephedra acts on what receptors?
⍺ and β (similar to Adrenaline)
60
Main effects of Ephedra?
bronchodilation CNS stim high BP and stroke
61
Overall effects of ⍺ Agonists?
vasoconstriction -> ↑ peripheral vasc resistance ↑ BP -> ↓ HR (reflex)
62
Phenylephrine affects what receptors? | Neofrin, Neo-Synephrine
⍺1
63
Neofrin/Syn effects on ⍺1 receptors?
typical ⍺ Agonist + | vasoconstriction of nasal and up resp bv
64
Neofrin/Syn used to tx? (3)
1) decongestant 2) pupil dilation for eye exam 3) hypotensive emergency
65
Neofrin/Syn side-effects?
rebound congestion | caution for HTN pts (↑ HTN)
66
Methoxamine (Vasoxyl) similar to?
Phenylephrine | use IV for hypotension
67
Pseudophedrine (Sudafed) affects what receptors?
⍺
68
Pseudophedrine effects on ⍺ receptors? Side-effects?
similar to Phenylephrine, more effective orally than Pheny caution for HTN
69
Xylometazoline/Oxymetazoline affect what receptors? | Otrivin/Afrin
direct ⍺ agonists
70
Xylometazoline/Oxymetazoline administered? Side-effects?
topically rebound congestion from receptor down-regulation
71
Tetrahydrozoline/Naphazoline affect what receptors? (Visine) How?
⍺ vasoconstriction
72
Tetrahydrozoline/Naphazoline contraindicated for?
narrow-angle glaucoma, | HTN
73
Clonadine (Catapres) affects what receptors?
⍺2
74
Clonadine effects on ⍺2?
stim ⍺2 in CNS presyn terminal -> ↓ NE release (↓ SNS) -> ↓ BP
75
Clonadine used to tx?
HTN, hot flashes, withdrawal/cravings, pre-anesthesia (↓ amount needed)
76
Clonadine administered?
oral | transdermal patch
77
Clonadine side-effects?
dry mouth, sedation, erect dysfxn severe HTN if abruptly stopped
78
Methyldopa (Aldomet) affects what receptors? Effects?
⍺2 similar to Clonadine
79
Apraclonidine (Iopidine) affects what receptors? Effects?
⍺2 ↓ aqueous humor -> ↓ IO pressure
80
Isoproterenol (Isuprel) affects what receptors?
β >> ⍺
81
Isoproterenol effects on β receptors?
vasodilation of skeletal mm and renal/mesenteric vascular beds ↓ BP -> reflex ↑ HR
82
Isoproterenol used to tx?
emergency cardiac arrest/complete heart block
83
Isoproterenol side-effects?
tachycardia, palp, arrhyth
84
Dobutamine (Dobuterex) affects what receptors?
β1
85
Dobutamine effects on β1?
inotropic (↑ CO/contractility)
86
Dobutamine used for? (3)
stress tests cardiac shock CHF
87
Dobutamine side-effects?
HTN pt: ↑ HR and BP
88
Albuterol (Ventolin) affects what receptors?
β2
89
Albuterol used to tx?
asthma
90
Albuterol side-effects?
tachycardia mm tremors HA
91
Dopamine (Intropin) affects what receptors?
D1 in renal vascular beds
92
Dopamine effects on D1? Used to tx?
vasodilation -> ↑ renal BF -> ↑ filtration/Na+ excretion cardiac shock
93
High [Dopamine] affects what other receptors?
β1, ⍺1 and adrenergic NE release
94
Dopamine side-effects? (6)
``` N/V tachycardia angina arrhyth HA peripheral vasoconstriction ```
95
Fenoldopam (Corlopam) affects what receptors?
D1
96
Fenoldopam effects on D1? Used to tx?
dilation of vascular beds -> ↓ BP severe HTN
97
Amphetamine affects what receptors?
INDIRECT action on adrenergic and DA, esp in brain (CNS)
98
Amphetamine effects on adrenergic/DA receptors? CNS? Peripheral?
release NE/DA CNS: ↑ euphoria, alertness, motor activity ↓ appetite, need for sleep Peripheral: tachycardia, HTN, psychosis, contracts urinary sphincter
99
Amphetamine overdose effects?
cerebral hemorr, convulsions, coma
100
Amphetamine use to tx? (2)
enuresis (bladder control) | ADHD (methyphenidate/Ritalin)
101
Cocaine affects what receptors?
INDIRECT action on NE/DA terminals | inhibits reuptake
102
Cocaine effects on NE/DA receptors?
similar to amphetamines more intense/shorter acting powerful vasoconstrictor
103
Cocaine side-effects?
MI, HTN, stroke | psychosis
104
Cocaine used for?
nasopharyngeal surgery (vasoconst, local anesthesia)
105
Tyramine affects what receptors?
INDIRECT action on adrenergic terminals
106
Tyramine effects on NE terminals?
releases NE, | displaces NE in vesicle -> becomes false transmitter (octopamine)
107
Tyramine found in? (2)
food | tyrosine by-product
108
Tyramine results in?
tachyphylaxis (↓ response from prolonged exposure)
109
Tyramine contraindication?
MAO inhibitors stop MAO from metabolizing tyramine = massive NE release = severe HTN

Q3 Pharm Cholinergics (7 decks)

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