Cholinergics Flashcards
1
Q
Carbachol description
A
non selective muscarinic and nicotoinic receptor agonist
2
Q
Carbachol actions
A
used as ocular agent because it causes miosis and increases aqueous humor outflow
3
Q
Carbachol Indications
A
open angle glaucoma
4
Q
Carbachol Toxicity
A
DUMBBEELSS, but topical so not liekly
5
Q
Carbachol
-What is the duration of activity and why?
A
long because it’s not efficiently broken down by AChE
6
Q
Bethanechol Description
A
non selective muscarinic receptor agonist
7
Q
Bethanechol Actions
A
used to increase detrusor muscle tone and GI motility post op
8
Q
Bethanechol Indications (3)
A
urinary retention,
neurogenic bladder
GERD
9
Q
bethanechol Toxicity (3)
A
reflex tachy from vasodilation
bronchoconstriction
increased secretory activity (sweat, GI, respiratory secretions)
10
Q
Bethanechol Route
A
Oral
11
Q
Pilocarpine brand name
A
Salagen
12
Q
Pilocarpine descrption
A
non selective muscarinic receptor agonist
13
Q
Pilocarpine actions
A
muscarinic receptor activations
14
Q
Pilocarpine Indications (4)
A
glaucoma–acute angle and open
dry mouth/xerostomia
sjogren syndrome
head and neck cancer associated radiation
15
Q
Pilocarpine Toxicity
A
reflex tachy from vasodilation
bronchoconstriction
increased secretory activity (sweat, GI, respiratory secretions)
16
Q
Pilocarpine Route (2)
A
eye drops
oral
17
Q
Methacholine Description
A
non selective muscarinic agonist
18
Q
Methacholine Action
A
used to diagnose bronchial hyperactivity ie methacholine challenge
19
Q
Methacholine Indications
A
only used for asthma diagnosis
20
Q
Methacholine Route
A
inhaled only
21
Q
Varenicline brand name
A
Chantix
22
Q
Varenicline description
A
Nicotinic receptor partial agonist
23
Q
Varenicline Actions
A
as a partial agonist it reduces cravings for and decreases the pleasurable effects of cigarettes by inhibiting the ability of nicotine to stimulate the mesolimbic dopamine system
24
Q
Varenicline Indications
A
smoking cessation
nicotine withdrawal
25
Varenicline Toxicity
bronchospasm
| nicotine dependence transference
26
Varenicline route
oral
27
Nicotine route (3)
gum, patch nasal
28
metoclopramide description
indirect acting presynaptic cholinomimetic
29
metoclopramide action
acts by stimulating presynaptic receptors to trigger ACh release
30
Edrophonium Description
short acting reversible AChE inhibitor/ indirect agonist
31
Edrophonium action
blocks AChE
32
Edrophonium Indications
used to diagnose myasthenia gravis
33
Edrophonium Toxicity
DUMBBEELSS
34
Edrophonium brand name
tensilon
35
Edrophonium Half life
10-30 minutes
36
Edrophonium route
IV
37
Does Edrophonium cross BBB
highly charged does not cross BBB
38
Neostigmine description
intermediate length reversible cholinesterase inhibitor
39
Neostigmine Action
increases acetylcholine availability
40
Neostigmine indications (3)
Myasthenia Gravis
nondepolarizing neuromuscular blockade reversal
urinary retention
41
Neostigmine Toxicity
DUMBBEELSS
42
Neostigmine routes
| 3
IV
IM
SC
43
Does neostigmine enter CNS?
no
44
Pyridostigmine descrption
intermediate length reversible cholinesterase inhibitor
45
pyridostigmine action
stimulates nicotinic and muscarinic ACh receptors
46
pyridostigmine indications
myasthenia gravis treatment
47
pyridostigmine toxicity
DUMBBEELSS
48
pyridostigmine oral bioavailability (qualitiative)
low
49
Does pyridostigmine cross the BBB?
no
50
Physostigmine description
intermediate length reversible cholinesterase inhibitor
51
physostigmine actions
stimulates nicotinic and muscarinic receptors
52
physostigmine indications (5)
glaucoma
alzheimers
delayed gastric emptying
undo anticholinergic toxicity/overdose in CNS
non depolarizing neuromuscular blockade reversal
53
physostigmine toxicity
DUMBBEELSS
54
physostigmine route 2
IV
| IM
55
does physostigmine cross BBB
yes, so not used for MG treatment
56
Donepezil brand name
Aricept
57
other dugs in Donepezil class
Rivastigmine
| Galatamine
58
Donepezil description
intermediate length reversible cholinesterase inhibitor
59
Donepezil actions
indirectly stimulates nicotinic and muscarinic recpetors
60
Donepezil Indications
Alzheimer's associated dementia
61
Donepezil Toxicity
GI upset
62
does donepezil cross BBB?
yes
63
Donepezil bioavailability
100%
64
Rivastigmine
- description
- indications
- route
intermediate length reversible AChE inhibitor (same class as Donepezil)
-GI UPset
_patch
65
Galantamine description
AChE inhibitor (same class as Donepezil) and Nn agonist)
66
Echothiphate description
long acting irreversible cholinesterase inhibitor
67
Echothiophate action
binds irreversibly to AChE
68
Echothiophate indications
glaucoma
| topical
69
Echothiophate toxicity (2)
lacrimation
| stinging
70
Echothiphate indications
glaucoma
71
echothiophate route
topical b/c very long half-life
72
Atropine drugs in same class (2)
homatropine
| tropicamide
73
Atropine description
direct muscarinic antagonist
74
Atropine Action
prevents ACh binding
| so lowers activity of muscles and glands regulated by PNS
75
Atropine Indications (4)
organophosphate poisoning (given w/ pralidoxime)
pupil dilation
bradycardia
reduce secretions
76
Atropine Toxicity (9)
```
mad as a hatter
blind as a bat
dry as a bone
red as a beet
hot as a hare
urinary retention
bronchodilation
constipation
tachy
```
77
Atropine Route (3)
SC
IM
IV
78
Pralidoxime aka
2-PAM
79
Pralidoxime Description
reactivates cholinesterase
80
Pralidoxime Actions
Binds to organophosphate and accelerates AChE reactivation
81
Pralidoxime/ 2-PAM toxicity
anticholinergic effects
82
pralidoxime/ 2 pam route (2)
IV
| IM
83
which drug does military have stockpile of self-injectors
pralidoxime
84
Benztropine brand name
cogentin
85
benztropine description
muscarinic (some m1 specificity)
| histamine receptor blockade
86
Benztropine actions
centrally acting anticholinergic/antihistamine agent
87
Benztropine indications
parkinsonism
dystonia
extrapyramidal symptoms
88
Benztropine toxicity
anticholinergic
89
Benztropine route (2)
IM
| IV
90
Scopolamine description
muscarinic blocker
91
scopolamine actions
blocks muscarinic receptors, some M1 specificity
| anti-emetic
92
Scopolamine Indications (2)
motion sickness
| dilate eyes
93
Scopolamine Toxicity
anticholinergic
94
Scopolamine Route (2)
transdermal
95
can Scopolamine cross BBB
yes
96
Ipratropium brand name
Atrovent HFA
97
Ipratropium ---similar drug in same class
Tiotropium
98
Ipratropium Description
muscarinic blocker
99
Ipratropium action
inhaled bronchodilator (M3)
100
Ipratropium indications (2)
asthma
| COPD
101
Ipratropium toxicity
rare and only through overdosing
dry mouth and sedation
other anticholinergic effects
102
Ipratropium route
inhaled
103
is ipratropium faster or slower than Beta 2 agonists?
slower
104
ipratropium duration
6-8 hrs
105
tiotropium brand name
Spiriva
106
Dicyclomine brand name
Bentyl
107
Dicyclomine Description`
non-selective muscarinic receptor blocker
108
dicyclomine actions
relaxes smooth muscle
| inhibits bradykinin and histamine induced bowel spasms
109
dicyclomine indications
IBS
110
dicyclomine toxicity
anticholinergic
111
dicyclomine route
oral
112
Glycopyrrolate description
muscarinic blocker
113
oxybutinin description
muscarinic blocker
114
Succinylcholine Description
Depolarizing nicotinic NMJ blocker and ACh receptor agonist
115
Succinylcholine Actions
complete muscle relaxation'
| flaccid paralysis
116
Succinylcholine indicaitons
short term muscle relaxation in anesthesia, ICU, intubation
117
Succinylcholine Toxicity (3)
rhabdomyolysis w/ hyperkalemia w/ ventricular dysrhythmias
cardiac arrest
death if given to peeps with undiagnosed myopathy
118
Succinylcholine route
IV
119
succinylcholine contraindication
patient lacking AChE
120
succinylcholine caveat
can't be reversed
121
Tubocurarine description
Benzylisoquinoline Non depolarizing Nm NMJ blocker --reversible
122
Tubocurarine actions
blocks Nm receptor and leads to flaccid skeletal paralysis
123
Tubocurarine indications
muscle relaxation for surgery
124
Tubocurarine roxicity
| 6
```
respiratory failure
paralysis in fully conscious
tachy
hypertension
histmaine release
ganglionic and muscarinic side effects
```
125
Tubocurarine duration
30-60 minutes
126
What drug is primarily used to reverse nondepolarizing nicotinic NMJ receptor blockers
neostigmine
127
Pancuronium description
aminosteroid nondepolarizing nicotinic NMJ receptor blocker
128
Vercuronium Description
aminosteroid nicotnic NMJ blocker, reversible
129
Vercuronium actions
flaccid paralysis
130
Vercuronium indication (2)
muscle relaxer for surgery
| used for executions
131
Vercuronium toxicity (6)
```
special training required for admin
respiratory failure
paralysis in awake individual
tachycardia
HTN
histamine release
ganglionic and muscarinic side effects
```
132
Vercuronium duration
30-60 minutes
133
Vercuronium caveat
caution with hepatic impairment
134
aminosteroids are what class of cholinergic
non depolarizing nicotinic NMJ blocker
135
Benzylisoquinolines are what class of cholinergic?
non depolarizing nicotinic NMJ blocker
136
Cisatracurium brand name
nimbex
137
Cisatracurium descrption
Benzylisoquinoline Nm NMJ blocker--reversible
138
Cisatracurium actions
blocks receptors and leads to flaccid skeletal muscle paralysis
139
Cisatracuriumindications
muscle relaxation for surgery
140
Cisatracurium toxicity
```
respiratory failure
paralysis in fully conscious patients
tachycardia
HTN
histamine release
ganglion and muscarinic effects
```
141
Cisatracurium duration
30-60 minutes
142
Rocuronium description
aminosteroid nondepolarizing nicotinic NMJ receptor blocker
143
Trimethaphan description
Nn ganglionic blocker --reversible
144
Trimethaphan brand name
arfonad
145
Tubocurarine brand name
curare
146
Trimethaphan indications
rarely used in hyertensive crisis or dissecting aortic aneurysm
147
Botox descrption
inhibitor of ACh release
148
Botox Actions
interferes w/ vesicle docking proteins on interior of nerve membrane , so ACh can't be released
149
Botox indications
```
wrinkles
muscle weakness
diplopia
blurred vision
ptosis
dysphagia
dysphonia
dysarthria
urinary incontinence
breathing difficulties
```
150
M1 receptors
- located where
- mechanism
- 2nd messenger
- Action
nerve endings
Gq
increased IP3 and DAG cascade
activate myenteric plexus
151
M2 receptors
- located where
- mechanism
- 2nd messenger
- Action
heart
Gi
decreased CAMP, activate K channels
slows SA Node/ HR
152
M3 receptors
- located where
- mechanism
- 2nd messenger
- Action
smooth muscles, glands, endothelium
Gq
increased IP3, DAG
contract detrusor muscle, increase secretions
153
Nn
- located where
- mechanism
- 2nd messenger
- Action
ANS ganglia
N-K ion channel
Na
depolarizes postganglionic fiber and evokes AP
154
Nm
- located where
- mechanism
- 2nd messenger
- Action
NMJ
Na-K ion channel
Na
depolarizes muscle cell--leads to contraction
155
DUMBBEELSS for acetylcholine overdose stands for
```
diarrhea
urination
miosis
bronchorrhea
bradycardia
excitation of skeletal muscles
emesis
salivation
sweating
```
156
What are signs of anticholinergic overdose?
```
mad as a hatter- delirium
Blind as a bat: mydriasis--dilation and lack of accomodation
Dry as a Bone: reduces secrtions
Hot as hare: elevated body temp
Red as a beet: skin flushing
urinary retention:
bronchodilation
constipation
tachycardia
HTN
```
