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Pharmacology > Cholinergics > Flashcards

Cholinergics Flashcards

1
Q

Carbachol description

A

non selective muscarinic and nicotoinic receptor agonist

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2
Q

Carbachol actions

A

used as ocular agent because it causes miosis and increases aqueous humor outflow

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3
Q

Carbachol Indications

A

open angle glaucoma

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4
Q

Carbachol Toxicity

A

DUMBBEELSS, but topical so not liekly

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5
Q

Carbachol

-What is the duration of activity and why?

A

long because it’s not efficiently broken down by AChE

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6
Q

Bethanechol Description

A

non selective muscarinic receptor agonist

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7
Q

Bethanechol Actions

A

used to increase detrusor muscle tone and GI motility post op

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8
Q

Bethanechol Indications (3)

A

urinary retention,
neurogenic bladder
GERD

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9
Q

bethanechol Toxicity (3)

A

reflex tachy from vasodilation
bronchoconstriction
increased secretory activity (sweat, GI, respiratory secretions)

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10
Q

Bethanechol Route

A

Oral

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11
Q

Pilocarpine brand name

A

Salagen

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12
Q

Pilocarpine descrption

A

non selective muscarinic receptor agonist

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13
Q

Pilocarpine actions

A

muscarinic receptor activations

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14
Q

Pilocarpine Indications (4)

A

glaucoma–acute angle and open
dry mouth/xerostomia
sjogren syndrome
head and neck cancer associated radiation

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15
Q

Pilocarpine Toxicity

A

reflex tachy from vasodilation
bronchoconstriction
increased secretory activity (sweat, GI, respiratory secretions)

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16
Q

Pilocarpine Route (2)

A

eye drops

oral

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17
Q

Methacholine Description

A

non selective muscarinic agonist

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18
Q

Methacholine Action

A

used to diagnose bronchial hyperactivity ie methacholine challenge

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19
Q

Methacholine Indications

A

only used for asthma diagnosis

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20
Q

Methacholine Route

A

inhaled only

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21
Q

Varenicline brand name

A

Chantix

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22
Q

Varenicline description

A

Nicotinic receptor partial agonist

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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

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24
Q

Varenicline Indications

A

smoking cessation

nicotine withdrawal

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25
Q

Varenicline Toxicity

A

bronchospasm

nicotine dependence transference

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26
Q

Varenicline route

A

oral

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27
Q

Nicotine route (3)

A

gum, patch nasal

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28
Q

metoclopramide description

A

indirect acting presynaptic cholinomimetic

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29
Q

metoclopramide action

A

acts by stimulating presynaptic receptors to trigger ACh release

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30
Q

Edrophonium Description

A

short acting reversible AChE inhibitor/ indirect agonist

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31
Q

Edrophonium action

A

blocks AChE

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32
Q

Edrophonium Indications

A

used to diagnose myasthenia gravis

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33
Q

Edrophonium Toxicity

A

DUMBBEELSS

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34
Q

Edrophonium brand name

A

tensilon

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35
Q

Edrophonium Half life

A

10-30 minutes

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36
Q

Edrophonium route

A

IV

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37
Q

Does Edrophonium cross BBB

A

highly charged does not cross BBB

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38
Q

Neostigmine description

A

intermediate length reversible cholinesterase inhibitor

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39
Q

Neostigmine Action

A

increases acetylcholine availability

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40
Q

Neostigmine indications (3)

A

Myasthenia Gravis
nondepolarizing neuromuscular blockade reversal
urinary retention

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41
Q

Neostigmine Toxicity

A

DUMBBEELSS

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42
Q

Neostigmine routes

3

A

IV
IM
SC

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43
Q

Does neostigmine enter CNS?

A

no

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44
Q

Pyridostigmine descrption

A

intermediate length reversible cholinesterase inhibitor

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45
Q

pyridostigmine action

A

stimulates nicotinic and muscarinic ACh receptors

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46
Q

pyridostigmine indications

A

myasthenia gravis treatment

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47
Q

pyridostigmine toxicity

A

DUMBBEELSS

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48
Q

pyridostigmine oral bioavailability (qualitiative)

A

low

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49
Q

Does pyridostigmine cross the BBB?

A

no

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50
Q

Physostigmine description

A

intermediate length reversible cholinesterase inhibitor

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51
Q

physostigmine actions

A

stimulates nicotinic and muscarinic receptors

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52
Q

physostigmine indications (5)

A

glaucoma
alzheimers
delayed gastric emptying
undo anticholinergic toxicity/overdose in CNS
non depolarizing neuromuscular blockade reversal

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53
Q

physostigmine toxicity

A

DUMBBEELSS

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54
Q

physostigmine route 2

A

IV

IM

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55
Q

does physostigmine cross BBB

A

yes, so not used for MG treatment

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56
Q

Donepezil brand name

A

Aricept

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57
Q

other dugs in Donepezil class

A

Rivastigmine

Galatamine

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58
Q

Donepezil description

A

intermediate length reversible cholinesterase inhibitor

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59
Q

Donepezil actions

A

indirectly stimulates nicotinic and muscarinic recpetors

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60
Q

Donepezil Indications

A

Alzheimer’s associated dementia

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61
Q

Donepezil Toxicity

A

GI upset

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62
Q

does donepezil cross BBB?

A

yes

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63
Q

Donepezil bioavailability

A

100%

64
Q

Rivastigmine

  • description
  • indications
  • route
A

intermediate length reversible AChE inhibitor (same class as Donepezil)
-GI UPset
_patch

65
Q

Galantamine description

A

AChE inhibitor (same class as Donepezil) and Nn agonist)

66
Q

Echothiphate description

A

long acting irreversible cholinesterase inhibitor

67
Q

Echothiophate action

A

binds irreversibly to AChE

68
Q

Echothiophate indications

A

glaucoma

topical

69
Q

Echothiophate toxicity (2)

A

lacrimation

stinging

70
Q

Echothiphate indications

A

glaucoma

71
Q

echothiophate route

A

topical b/c very long half-life

72
Q

Atropine drugs in same class (2)

A

homatropine

tropicamide

73
Q

Atropine description

A

direct muscarinic antagonist

74
Q

Atropine Action

A

prevents ACh binding

so lowers activity of muscles and glands regulated by PNS

75
Q

Atropine Indications (4)

A

organophosphate poisoning (given w/ pralidoxime)
pupil dilation
bradycardia
reduce secretions

76
Q

Atropine Toxicity (9)

A 
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
Q

Atropine Route (3)

A

SC
IM
IV

78
Q

Pralidoxime aka

A

2-PAM

79
Q

Pralidoxime Description

A

reactivates cholinesterase

80
Q

Pralidoxime Actions

A

Binds to organophosphate and accelerates AChE reactivation

81
Q

Pralidoxime/ 2-PAM toxicity

A

anticholinergic effects

82
Q

pralidoxime/ 2 pam route (2)

A

IV

IM

83
Q

which drug does military have stockpile of self-injectors

A

pralidoxime

84
Q

Benztropine brand name

A

cogentin

85
Q

benztropine description

A

muscarinic (some m1 specificity)

histamine receptor blockade

86
Q

Benztropine actions

A

centrally acting anticholinergic/antihistamine agent

87
Q

Benztropine indications

A

parkinsonism
dystonia
extrapyramidal symptoms

88
Q

Benztropine toxicity

A

anticholinergic

89
Q

Benztropine route (2)

A

IM

IV

90
Q

Scopolamine description

A

muscarinic blocker

91
Q

scopolamine actions

A

blocks muscarinic receptors, some M1 specificity

anti-emetic

92
Q

Scopolamine Indications (2)

A

motion sickness

dilate eyes

93
Q

Scopolamine Toxicity

A

anticholinergic

94
Q

Scopolamine Route (2)

A

transdermal

95
Q

can Scopolamine cross BBB

A

yes

96
Q

Ipratropium brand name

A

Atrovent HFA

97
Q

Ipratropium —similar drug in same class

A

Tiotropium

98
Q

Ipratropium Description

A

muscarinic blocker

99
Q

Ipratropium action

A

inhaled bronchodilator (M3)

100
Q

Ipratropium indications (2)

A

asthma

COPD

101
Q

Ipratropium toxicity

A

rare and only through overdosing
dry mouth and sedation
other anticholinergic effects

102
Q

Ipratropium route

A

inhaled

103
Q

is ipratropium faster or slower than Beta 2 agonists?

A

slower

104
Q

ipratropium duration

A

6-8 hrs

105
Q

tiotropium brand name

A

Spiriva

106
Q

Dicyclomine brand name

A

Bentyl

107
Q

Dicyclomine Description`

A

non-selective muscarinic receptor blocker

108
Q

dicyclomine actions

A

relaxes smooth muscle

inhibits bradykinin and histamine induced bowel spasms

109
Q

dicyclomine indications

A

IBS

110
Q

dicyclomine toxicity

A

anticholinergic

111
Q

dicyclomine route

A

oral

112
Q

Glycopyrrolate description

A

muscarinic blocker

113
Q

oxybutinin description

A

muscarinic blocker

114
Q

Succinylcholine Description

A

Depolarizing nicotinic NMJ blocker and ACh receptor agonist

115
Q

Succinylcholine Actions

A

complete muscle relaxation’

flaccid paralysis

116
Q

Succinylcholine indicaitons

A

short term muscle relaxation in anesthesia, ICU, intubation

117
Q

Succinylcholine Toxicity (3)

A

rhabdomyolysis w/ hyperkalemia w/ ventricular dysrhythmias
cardiac arrest
death if given to peeps with undiagnosed myopathy

118
Q

Succinylcholine route

A

IV

119
Q

succinylcholine contraindication

A

patient lacking AChE

120
Q

succinylcholine caveat

A

can’t be reversed

121
Q

Tubocurarine description

A

Benzylisoquinoline Non depolarizing Nm NMJ blocker –reversible

122
Q

Tubocurarine actions

A

blocks Nm receptor and leads to flaccid skeletal paralysis

123
Q

Tubocurarine indications

A

muscle relaxation for surgery

124
Q

Tubocurarine roxicity

6

A 
respiratory failure
paralysis in fully conscious
tachy
hypertension
histmaine release
ganglionic and muscarinic side effects
125
Q

Tubocurarine duration

A

30-60 minutes

126
Q

What drug is primarily used to reverse nondepolarizing nicotinic NMJ receptor blockers

A

neostigmine

127
Q

Pancuronium description

A

aminosteroid nondepolarizing nicotinic NMJ receptor blocker

128
Q

Vercuronium Description

A

aminosteroid nicotnic NMJ blocker, reversible

129
Q

Vercuronium actions

A

flaccid paralysis

130
Q

Vercuronium indication (2)

A

muscle relaxer for surgery

used for executions

131
Q

Vercuronium toxicity (6)

A 
special training required for admin
respiratory failure
paralysis in awake individual 
tachycardia 
HTN
histamine release
ganglionic and muscarinic side effects
132
Q

Vercuronium duration

A

30-60 minutes

133
Q

Vercuronium caveat

A

caution with hepatic impairment

134
Q

aminosteroids are what class of cholinergic

A

non depolarizing nicotinic NMJ blocker

135
Q

Benzylisoquinolines are what class of cholinergic?

A

non depolarizing nicotinic NMJ blocker

136
Q

Cisatracurium brand name

A

nimbex

137
Q

Cisatracurium descrption

A

Benzylisoquinoline Nm NMJ blocker–reversible

138
Q

Cisatracurium actions

A

blocks receptors and leads to flaccid skeletal muscle paralysis

139
Q

Cisatracuriumindications

A

muscle relaxation for surgery

140
Q

Cisatracurium toxicity

A 
respiratory failure
paralysis in fully conscious patients
tachycardia
HTN
histamine release
ganglion and muscarinic effects
141
Q

Cisatracurium duration

A

30-60 minutes

142
Q

Rocuronium description

A

aminosteroid nondepolarizing nicotinic NMJ receptor blocker

143
Q

Trimethaphan description

A

Nn ganglionic blocker –reversible

144
Q

Trimethaphan brand name

A

arfonad

145
Q

Tubocurarine brand name

A

curare

146
Q

Trimethaphan indications

A

rarely used in hyertensive crisis or dissecting aortic aneurysm

147
Q

Botox descrption

A

inhibitor of ACh release

148
Q

Botox Actions

A

interferes w/ vesicle docking proteins on interior of nerve membrane , so ACh can’t be released

149
Q

Botox indications

A 
wrinkles
muscle weakness
diplopia
blurred vision
ptosis
dysphagia 
dysphonia
dysarthria
urinary incontinence
breathing difficulties
150
Q

M1 receptors

  • located where
  • mechanism
  • 2nd messenger
  • Action
A

nerve endings
Gq
increased IP3 and DAG cascade
activate myenteric plexus

151
Q

M2 receptors

  • located where
  • mechanism
  • 2nd messenger
  • Action
A

heart
Gi
decreased CAMP, activate K channels
slows SA Node/ HR

152
Q

M3 receptors

  • located where
  • mechanism
  • 2nd messenger
  • Action
A

smooth muscles, glands, endothelium
Gq
increased IP3, DAG
contract detrusor muscle, increase secretions

153
Q

Nn

  • located where
  • mechanism
  • 2nd messenger
  • Action
A

ANS ganglia
N-K ion channel
Na
depolarizes postganglionic fiber and evokes AP

154
Q

Nm

  • located where
  • mechanism
  • 2nd messenger
  • Action
A

NMJ
Na-K ion channel
Na
depolarizes muscle cell–leads to contraction

155
Q

DUMBBEELSS for acetylcholine overdose stands for

A 
diarrhea
urination
miosis
bronchorrhea
bradycardia
excitation of skeletal muscles
emesis
salivation
sweating
156
Q

What are signs of anticholinergic overdose?

A 
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

Pharmacology (9 decks)

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