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P1 Spring - Pharm Sci > adrenergic quiz > Flashcards

adrenergic quiz Flashcards

1
Q

2 main adrenergic neurotransmitters

A

epi and NE

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2
Q

Epi is syn and stored in the

A

adrenal medulla (making it a neurohormone)

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3
Q

Epi has a different response at different levels meaning it is

A

concentration dependent

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4
Q

Epi at low concentrations

A

has predominant beta effects more than alpha

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5
Q

Epi at high concentrations

A

engages beta and alpha receptors at the same degree

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6
Q

in the heart, Epi

A

increases HR, FOC, SV, CO, BP

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7
Q

in the lungs, Epi

A

bronchodilation occurs

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8
Q

in the vasculature, Epi

A

low concentrations = beta = vasodilation (decrease TPR)

high concentrations = alpha engaged = constriction (increase TPR)

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9
Q

is epi appropriate for asthma attack

A

yes B2 engaged = bronchodilation

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10
Q

epi with an anesthetic

A

vasoconstriction; anesthetic is kept localized; good for prolonged procedures

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11
Q

NE is synthesized and stored

A

sympathetic post ganglionic neuron

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12
Q

NE targets which receptors

A

beta1, alpha1, alpha2

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13
Q

NE at the heart

A

increases HR, FOC, CO

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14
Q

NE at the lungs

A

no clinical observation is observed

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15
Q

NE in the vasculature

A

vasoconstriction (alpha1)

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16
Q

Dopamine is syn and stored in the terminal of the

A

sympathetic postganglionic neuron

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17
Q

DA targets which receptors at different concentrations meaning it is

A

D1, beta1, alpha1; concentration dependent

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18
Q

at low concentrations DA

A

has the highest affinity (lowest kd); leads to vasodilation of gut and renal by lowering TPR; good for maintaining good kidney function

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19
Q

at mild concentrations DA

A

engages B1 receptors as well as D1; leads to vasodilation, increasing HR and CO

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20
Q

at high concentrations DA

A

engages alpha1 (B1 and D1 also); it causes vasoconstriction, increasing TPR, CO; it can be effected by vagal response

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21
Q

at the kidney DA

A

increases RBF and increases GFR (only at low doses due to D1)

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22
Q

at the heart DA

A

increases HR, FOC, (through B1 engagement at mid to high conc)

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23
Q

at the vasculature

A

decreases TPR (some due to D1) increases TPR (alpha1 engagement)

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24
Q

therapeutic uses for dopamine

A

shock, hypotension, poor tissue perfusion, low CO

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25
sympathomimetics
synthetic receptor agonists mimic the actions of catecholamines
26
alpha 1 receptor agonists
phenylephrine naphazoline oxymetazoline tetrahydrozoline topical, decongestants, vasoconstrictors in cornea
27
alpha 2 receptor agonists
clonidine guanfacine methyldopa activate alpha 2 and therefore decrease SNS outflow decrease HR, TPR, BP upregulation of peripheral B1 and alpha1
28
beta 1 agonists
dobutamine IV only; preserves CO; increases HR and FOC; decompensated heart failure; low CO = risk to vital organs; can only use for 3 days due to downregulation
29
Beta 2 agonists
albuterol (SABA) terbutaline salmeterol (LABA) good for bronchodilation; good for patients with asthma
30
isoproterenol
non selective B1 and B2 agonist
31
beta blockers are used to treat
hypertension, chronic angina, heart failure
32
in treating hypertension and chronic angina, beta blockers work to
decrease CO, FOC, HR; block the effects of NE on the heart; improve blood flow and decrease oxygen
33
beta 1 antagonists also effect the RAA system
block the beta 1 receptors on the JG cells of the kidney which are responsible for the activation of the RAA pathway
34
cardioselective beta blockers are more selective for
B1 than B2
35
why would these agents be favored over non selective
they specifically block B1 more than B2 good for patients that have COPD or asthma or diabetes diabetes blocking B2 would lead to decreased insulin secretion and decreases tissue sensitivity to insulin
36
nonselective B blockers increase the change of developing
type 2 diabetes
37
ISA
intrinsic sympathomimetic activity; partial agonist
38
agents with ISA include
pindolol, acebutolol, labetalol bind to the receptor and have the same ability to turn it on but not to the same ability; could be used to reduce the degree of bradycardia or limit the effect on lipid profile
39
Labetalol has ISA at beta 2 receptors
will cause B2 stimulation and vasodialate reducing TPR and reducing BP; nonselective; don't want to mess with B2 still full agonist to open airways is always better
40
carvedilol
blocks alpha 1, blocks L type CC, anti-oxidant vasodilation, decreased HR, limited oxidative damaged seen in heart failure
41
nebivolol
increased NO production in vasculature causes vasodilation; maybe B3
42
labetalol
B1 antagonist; B2 ISA; alpha1 blocked affects glucuronidation pathway; gives vasodilation, happens on JG cells good at lowering BP
43
nearly all B blockers are eliminated by
the liver 2D6
44
which B blockers are eliminated by the kidney
nadolol and atenolol and 50% of bisopropol
45
esmolol
has a half life of 10 minutes; metabolized by gut (plasma) esterases; shorter half life = quicker response; given IV
46
nadolol has a half life of ___
24 hours; making it the longest for a B blocker
47
most hepatically cleared have a half life of
4-6 hours
48
atenolol has a half life of
12 hours
49
4 diff types of adverse effects associated with B blockers
lipids CNS sexual dysfunction, hypoglycemia
50
lipid adverse effect
increased LDL, increased VLDL; decreased HDL wouldn't use this medication on statin therapy
51
glaucoma
role of beta receptors on aqueous humor production
52
thyrotoxicosis
thyroid hormone increases the expression of beta receptors | increase production of thyroid hormone by way of B1
53
tremor
activation of B2 receptors can cause tremors; trigger for excess symp activity
54
migraine
beta blockers; mechanism is unknown; effective in preventing migraines
55
alpha blockers are primarily used in the treatment of
BPH and hypertension (not as good as others)
56
the least selective of alpha antagonists
``` phent, PB2 outside vasculature decreases blood to tissues necrosis occurs give an IV of alpha blocker around site where it occurs ```
57
the first alpha 1 selective antagonists ___ led to the development of ___ and ___
prazonsin; terozosin and doxazosin
58
alpha 1 antagonist use in treating BPH
decrease growth and contraction of prostatic tissues
59
the different types of alpha 1 receptor subtypes include
A, B, D
60
the most predominant subtype in the prostate is the
alpha 1 a
61
the most predominant alpha 1 receptor subtype in the vasculature is
B and D
62
what counseling would you give to someone on an alpha 1 antagonist
get up slowly; take a bedtime; due to orthostatic hypotension (dilates arterioles and effects venous tone)
63
what is an ADR associated with tamsulosin
floppy iris syndrome | alpha 1 A receptors are located on the dilator muscles of the iris and it can lead to atrophy of the muscle
64
which neurons use ACh
parasymp, nicotinic, muscarinic, neuromuscular
65
cholinergic
any system affected by or involving ACh
66
M3
"secretory" (SLUD) any muscle contraction including smooth muscle circulatory muscles in the eye constrict
67
M2
"cardiac" decrease HR slows SA node slows down AV node
68
M1
cholinergic pathways Alzheimer's; circuits involved in memory and cognition neural receptor
69
muscarinic agonist would lead to what
increased SLUD and decreased HR
70
muscarinic agonists would treat
tachycardia, dry mouth, constipation, glaucoma
71
muscarinic antagonists would lead to
decreased SLUD and increased HR
72
muscarinic antagonists would treat
urinary urgency eye surgery IBS (type D)
73
nicotinic receptors
ligand gated Na+ ion channels
74
nicotinic receptors are found in (2)
autonomic ganglia | neuromuscular junction
75
autonomic ganglia
Ng | parasymp or symp
76
neuromuscular junction
some selective nicotinic Nm could paralyze someone with a nicotinic blocker
77
AChE
where ACh is released, this enzyme is present, highest turnover rate of all enzymes
78
lack of AChE
lack of breakdown of ACh increase SLUD decrease HR in brain = increase cholinergic activity (treatment of Alz)
79
ACh antagonist could treat
COPD/asthma
80
quaternary ammonium compound is (in ACh and choline)
unable to get into the CNS | unable to cross BBB
81
rotamers
rotational conformers of norepinephrine play a role in which receptors are activated beta 1, alpha 1, and alpha 2 can twist to activate all three receptors despite it being 1 molecule
82
Receptors use __ to define a ligand binding site
side chains of AA
83
interactions of drugs with ligand binding site (3)
1. H bonds - one of the polar groups needs an H to donate to form the H bond 2. ionic bond - very strong (not as covalent) can help hold drugs in receptor active site 3. van der waals - hydrophobic interactions; lipid or nonpolar areas of a molecule interacting with non polar
84
affinity (B2 adrenergic agonists)
want a highly potent agent / low dose
85
activation (B2 adrenergic agonists)
full or partial agonist
86
lipophilicity (B2 adrenergic agonists)
does play a role in B2 receptor selectivity and for some of the long acting beta 2 agonists (LABA)

P1 Spring - Pharm Sci (9 decks)

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