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pharm1 S.Horvath > ANS reversal agents > Flashcards

ANS reversal agents Flashcards

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1
Q

what converts dopamine to NE

A

dopamine beta hyroxylase

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2
Q

how is norepinephrine metabolized

A

reuptake (70%), the rest metabolized by monamine oxidase (MAO) and catecholomethyltranserase (COMT)

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3
Q

the alpha 1 receptor is ____synaptic

A

post

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4
Q

alpha 1 works in the

A

periphery

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5
Q

alpha 2 receptor is ___synaptic

A

pre

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6
Q

beta 1 receptor is in the

A

heart

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7
Q

beta 2 is in the

A

other smooth muscle

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8
Q

activation of alpha 1 increases

A

intracellular calcium

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9
Q

alpha 1 causes smooth muscle ___ and peripheral vaso___

A

contraction, vasoconstriction

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10
Q

which anticholinergics are tertiary amines

A

atropine and scopolamne

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11
Q

which anticholinergics are quaternary ammonium

A

glycopyrrolate

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12
Q

electrostatic attachment occurs with

A

edrophonium (competitive)

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13
Q

formation of caramyl esters occurs with

A

neo, phyido, physo (competitive)

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14
Q

phosphorylation occurs with

A

organophosphates and echothiophate (non-competitive inhibition)

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15
Q

how do AchE inhibitors work

A

they reversibly inhibit AchE, which indirectly increases the concentration of Ach at the neuromuscular junction. since more ach is present, it is better able to compete for the alpha binding sites on the nicotinic receptor and antagonize the block

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16
Q

neostigmine is ___ potent than pyridostigmine

A

more

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17
Q

50% of ___ is metabolized by the liver

A

neostigmine

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18
Q

which drugs are quaternary amines

A

endro, neo, phyrido

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19
Q

quaternary pass thru BBB?

A

no

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20
Q

tertiary amine pass thru BBB?

A

yes!

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21
Q

which is tertiary amine

A

physostigmine

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22
Q

AchE inhibitors cause ____ side effects

A

parasympathetic

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23
Q

why do AchE inhibitors cause cholinergic side effects

A

because there is more ach at the muscarinic receptor.

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24
Q

cholinergic side effects are

A

diarrhea , urination, miosis, bradycardia, bronchoconstriction, emesis, lacrimation, laxation, salivation

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25
whats the only AchE inhibitor that diffuses across BBB
physostigmine
26
whats the best AchE inhibitor to antagonize a block with 90% twitch suppression
neo
27
which drugs produce reversible inhibition of AcheE by forming a caramel ester complex at the esteratic site... block the enzymes ability to hydrolyze Ache
neo and pyrido and pyrido
28
which enzyme forms a reversible electrostatic attachment
edro
29
neo edro pyrido. which is most potent
neo
30
neo edro pyrido. which is least potent
edro
31
which drugs prolong the duration of succs
neo and pyrido
32
pyrido edro neo . which has fastest onset
endro
33
pyrido edro neo which has slowest onset
pyrido
34
atropine can be mixed with
edro
35
glyco can be mixed with
neostigmine
36
glyco and edro in the same syringe will cause profound
bradycardia (same with administering atropine after edro)
37
Atropine and scopolamine structure
tertiary amines, liophillic
38
glyco structure
quaternary ammonium, does not pass thru lipophilic membranes
39
sugammadex affinity for amino steroids > > >
rec>vec>panc
40
which drug competitive inhibition, electrostatic attachment
edro
41
metabolism of edro and pyrido
75% renal, 25% hepatic
42
metabolism of neo
50% renal, 50% hepatic
43
neostigmine is ___ in infants and children
faster
44
which antimuscarinics pass thru BBB
atropine and scop
45
roc metabolism
primary biliary
46
sugmmadex metabolism
excreted unchanged by kidneys
47
SNS stim effect on bronchial smooth muscle
relaxation
48
PNS stim effect on bronchial smooth muscle
contraction
49
PNS stim effect on gallbladder
contraction
50
PNS stim effect on urinary
smooth muscle contraction, sphincter relaxation
51
PNS stim on GI tract
inc motility, secretion, sphincter relaxation
52
SNS stim on liver
glycogenolysis
53
PSN stim on liver
glycogen synthesis
54
SNS stim on eye
mydriasis
55
pNS stim on eye
miosis
56
SNS stim on pancreas
dec beta cell secretion
57
down regulation
extended exposure to agonists reduces the number, but not their response. results in tachyphylaxis
58
up regulation
chronic depletion of catecholamines or use of antagonists increases the number of receptors but not their sensitivity. may account for withdrawal syndrome with BB
59
receptor uncoupling occurs ___, while sequestration occurs ___
rapidly, slowly
60
pheochromocytoma
renal tumor. uncontrolled release of catecholamines due to an adrenal gland tumor. constant SNS stimulation. pump out epi and norepinephrine constantly.
61
sympathomimetics
compounds that resemble catecholamines except that hydroxyl groups are not present in both the 3 and 4 positions of the benzene ring
62
where is epi released from
adrenal medulla , triggered by calcium ion influx
63
presynaptic effect we would see with AchE inhibitor?
fasciculation at high doses
64
direct effect of anti cholinesterase ?
super high dose causes NMB blockade
65
what is the most important determinant of relative potency ?
affinity
66
influence of age with neo
infants
67
edrophonium and age
no change
68
nicotinic effects occur at
NM junction and autonomic ganglia
69
muscarinic effects include
bradycardia, salivation, bronchoconstriction, miosis, hyperperistalsis, and increased risk of PONV
70
eye effects from anti cholinesterase
miosis, inability to focus on near vision, dec IOP
71
pulm effects from anti cholinesterase
bronchoconstriction, increased airway resistance
72
how are anti cholinesterase used to tx myasthenia graves?
increase ACh at the nmj
73
potency of anti cholinesterase is determined by
NMB being antagonized, speed of spontaneous recovery, and depth of NMB when reversal is initiated
74
whats the purpose of an anticholinergic drug
blocks the side effects of the muscarinic receptors
75
administer reversal only after twitch height has recovered to
>10%
76
what can prevent you from properly reversing someone?
abx, hypothermia, resp acidosis, hypoK, metabolic acidosis
77
physostigmine CNS effects
antagonizes adverse CNS effects of certain drugs
78
which drug decreases post-op somnolence after volatile anesthetic and reverses CNS effects of ketamine
physo
79
which drug is used for post op analgesia and post op shivering
physo
80
which drug is used for diagnosis and management of cv arrhythmias
physo
81
most two significant OD muscarinic effects
bronchoconstriction and bradycardia
82
OD nicotinic effects
skeletal muscle weakness to paralysis and apnea
83
organophsphate anticholinesterases
insecticides and nerve agents - rapidly absorbed - highly lipid soluble - irreversible binding
84
what do you give for OD
atropine (for antimuscarinic effects) and pralidoxime (acetylcholinesterase reactivator)
85
anticholinergics antagonize the effects of Ach at ____ receptors
muscarinic
86
muscarinic receptors are located
heart, salivary glands, smooth muscle GI and Gu tracts
87
anticholinergics MOA
competitive antagonists. compete with Ach at the cholinergic/muscarinic receptors
88
m1
CNS and stomach
89
m2
lungs and heart
90
m3
CNS , airway, smooth muscle, glandular tissue
91
m4 and m5
CNS
92
m3 causes
bronchodilation
93
which drug causes mydriasis and cycloplegia
glyco
94
which anticholinergic drug causes most sedation
scop
95
which anticholinergic has an increased incidence of memory deficits
atropine
96
delated arousal in first 30 min after cessation of anestheisa in patients reversed with
atropine/neostigmine
97
which anticholinergics cross the placenta
atropine and scop
98
which is the best antisialogogue
scop > glco > atropine
99
which has a longer DOA - scop or glyco
glyco
100
how does atropine treat intra op bradycardia
blocks the effects of ACh on the SA node
101
overdose symptoms of anticholinergics
anti-rest and digest. dry mouth, increased temp, dry and flushed skin skeletal weakness, orthostatic hypotension, fatal events
102
treatment for OD of anti-cholinergic
physo - may need to repeat dose since it Is metabolized rapidly
103
sugar has a ___ center and ____ exterior
hydrophobic, hydrophilic
104
sugga is not recommended for use in
severe renal impairment
105
use secondary contraception for ___ post suggamedex
one week

pharm1 S.Horvath (18 decks)

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