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SBL > Cholinergics > Flashcards

Cholinergics Flashcards

1
Q

Acetylcholine MOA

A

Direct-acting cholinomimetic

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2
Q

Bethanechol MOA

A

Direct-acting cholinomimetic

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3
Q

Carbachol MOA

A

Direct-acting cholinomimetic

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4
Q

Methacholine MOA

A

Direct-acting cholinomimetic

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5
Q

Cevimeline MOA

A

Direct-acting cholinomimetic

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6
Q

Pilocarpine MOA

A

Direct-acting cholinomimetic

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7
Q

Varenicline MOA and generic name

A

Chantix, Direct-acting cholinomimetic

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8
Q

Ambenonium MOA

A

Cholinesterase inhibitor

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9
Q

Donepezil MOA

A

Cholinesterase inhibitor

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10
Q

Echothiophate MOA

A

Cholinesterase inhibitor

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11
Q

Edrophonium MOA

A

Cholinesterase inhibitor

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12
Q

Galantamine MOA

A

Cholinesterase inhibitor

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13
Q

Neostigmine MOA

A

Cholinesterase inhibitor

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14
Q

Physostigmine MOA

A

Cholinesterase inhibitor

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15
Q

Pyridostigmine MOA

A

Cholinesterase inhibitor

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16
Q

Rivastigmine MOA

A

Cholinesterase inhibitor

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17
Q

Tacrine MOA

A

Cholinesterase inhibitor

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18
Q

Pralidoxime MOA

A

Cholinesterase regenerator

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19
Q

Scopolamine MOA and clinical use

A

antimuscarinic, motion sickness and ophthalmology

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20
Q

Atropine MOA and clinical use

A

antimuscarinic, GI disorders and ophthalmology, cholinergic poisoning

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21
Q

Dicyclomine MOA and clinical use

A

antimuscarinic, GI disorders

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22
Q

Glycopyrrolate MOA and clinical use

A

antimuscarinic, GI disorders

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23
Q

Hyoscyamine MOA and clinical use

A

antimuscarinic, GI disorders

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24
Q

Cyclopentolate MOA and clinical use

A

antimuscarinic, ophthalmology

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25
Q

Homatropine MOA and clinical use

A

antimuscarinic, ophthalmology

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26
Q

Tropicamide MOA and clinical use

A

antimuscarinic, ophthalmology

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27
Q

Ipratropium MOA and clinical use

A

antimuscarinic, resp disorders

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28
Q

Tiotropium MOA and clinical use

A

antimuscarinic, resp disorders

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29
Q

Darifenacin MOA and clinical use

A

antimuscarinic, urinary disorders

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30
Q

Fesoterodine MOA and clinical use

A

antimuscarinic, urinary disorders

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31
Q

Oxybutynin MOA and clinical use

A

antimuscarinic, urinary disorders

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32
Q

Solifenacin MOA and clinical use

A

antimuscarinic, urinary disorders

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33
Q

Tolterodine MOA and clinical use

A

antimuscarinic, urinary disorders

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34
Q

Trospium MOA and clinical use

A

antimuscarinic, urinary disorders

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35
Q

Benztropine MOA and clinical use

A

antimuscarinic, movement disorders

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36
Q

Biperiden MOA and clinical use

A

antimuscarinic, movement disorders

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37
Q

Orphenadrine MOA and clinical use

A

antimuscarinic, movement disorders

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38
Q

Procyclidine MOA and clinical use

A

antimuscarinic, movement disorders

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39
Q

Trihexyphenidyl MOA and clinical use

A

antimuscarinic, movement disorders

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40
Q

Mecamylamine MOA

A

ganglion blockers

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41
Q

MOA of Ach mimetics

A

mimic actions of ACh on nicotinic and muscarinic acetylcholine receptors

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42
Q

M1 receptor location and mechanism

A

nerves, GPCR - Gq

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43
Q

M2 receptor location and mechanism

A

heart, nerves, smooth muscle; GPCR - Gi

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44
Q

M3 receptor location and mechanism

A

glands, smooth muscle, endothelium; GPCR - Gq

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45
Q

M4 receptor location and mechanism

A

CNS, GPCR - Gi

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46
Q

M5 receptor location and mechanism

A

CNS, GPCR - Gq

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47
Q

Nm receptor location and mechanism

A

skeletal muscle, NMJ; pentamer - Na, K depolarizing ion channel

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48
Q

Nn receptor location and mechanism

A

Postganglionic cell body, dendrites, CNS; alpha and beta, depolarizing ion channel

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49
Q

Effects of direct-acting cholinergic agonists on skeletal muscle

A

nAChRs will cause muscle contraction, prolonged agonist will cause flaccid paralysis

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50
Q

Effects of direct-acting cholinergic agonists on parasympathetics

A

miosis, negative inotropy and chronotropy, dilation of vessels, bronchoconstriction, increased GI motility, detrusor contraction, secretion from glands increases

51
Q

Effects of direct-acting cholinergics on eye

A

contraction of iris and ciliary muscle, increasing aqueous humor outflow

52
Q

Effects of direct-acting cholinergics on CV system

A

reduce PVR and changes heart rate, endothelium-derived relaxing factor is released and relaxes smooth muscle

53
Q

Effects of direct-acting cholinergics on GI and GU

A

increase in glandular secretions, smooth muscle contraction and smooth muscle relaxation

54
Q

Effects of direct-acting cholinergics on CNS

A

moderate doses cause an increase in cognitive function, higher concentrations can cause tremors and analgesia

55
Q

Effects of direct-acting cholinergics on PNS

A

activation of autonomic ganglia, sympathomimetic on CV system and parasympathomimetic on GI/GU

56
Q

Clinical uses of direct-acting cholinergic agonists

A

Glaucoma, esotropia, GI/GU disorders

57
Q

Direct-acting cholinergic agonists in glaucoma

A

contraction of ciliary body, facilitating aqueous humor outflow

58
Q

Direct-acting cholinergic agonists in GI/GU disorders

A

Bethanechol used for postoperative ileus, megacolon, urinary retention; pilocarpine and cevimeline increase salivary secretion

59
Q

Toxicity of muscarinic direct-acting choliniomimetics

A

nausea, vomiting, diarrhea, urinary urgency, salivation, sweating, bronchoconstriction

60
Q

Major contraindications of mAChR agonists

A

asthma, hyperthyroidism, coronary insufficiency, acid-peptic disease

61
Q

Acute toxicity of nicotinic stimulants

A

CNS stimulation, NMJ depolarization leading to resp paralysis, hypertension, cardiac arrhythmias

62
Q

Chronic toxicity of nicotinic stimulants

A

increased risk of vascular disease, sudden coronary death, ulcer recurrences

63
Q

Acetylcholine clinical use

A

causes miosis

64
Q

Methacholine clinical use

A

bronchial airway hyperreactivity

65
Q

Bethanechol clinical use

A

urinary retention and heartburn

66
Q

Carbachol clinical use

A

glaucoma, produce miosis during surgery

67
Q

Cevimeline clinical use

A

xerostomia in pts with Sjogrens

68
Q

Pilocarpine clinical use

A

xerostomia, miosis during ophthalmic procedures, glaucoma

69
Q

Varenicline clinical use

A

smoking cessation

70
Q

Varenicline intrinsic activity

A

partial agonist that binds to a4B2 nicotinic receptors

71
Q

Varenicline causes the release of what NT?

A

dopamine - stimulating reward pathway

72
Q

AE of varenicline

A

neuropsych sxs such as agitation, depression, suicide ideation

73
Q

Chemical subgroups of AChE inhibitors

A

alcohols and carbamic acid esters, which reversibly bind to AChE; organophosphates, which irreversibly bind to AChE

74
Q

MOA of AChE Inhibitors

A

inhibition of AChE, resulting in ACh accumulation throughout the body and activation of nAChRs and mAChRs

75
Q

Duration of action of AChE Inhibitors

A

alcohols and carbamic acid esters - short duration of action due to noncovalent bonds; organophosphates - very long duration, forms a very stable bond

76
Q

Organ systems effected by AChE inhibitors

A

stimulate autonomic effector organs, stimulate CNS, depression after stimulation of CNS

77
Q

Effects of AChE inhibitors on CV system

A

bradycardia, decrease in cardiac output, modest increase in BP

78
Q

Therapeutic uses of AChE inhibitors

A

diseases of eye, GI and GU disorders, NMJ, heart, and Alzheimer’s

79
Q

AChE toxicity

A

cutaneous vasodilation, anhidrosis, anhydrotic hyperthermia, nonreactive mydriasis, delirium, hallucination

80
Q

Common antidote for AChE Inhibitors

A

physostigmine

81
Q

AChE Inhibitor interaction with succinylcholine

A

enhance phase 1 block, antagonize phase 2 block

82
Q

AChE inhibitor interaction with nondepolarizing NMBA

A

diminish neuromuscular blockade

83
Q

AChE inhibitor interaction with cholinergic agonists

A

enhance effects of cholinergic agnoists

84
Q

AChE inhibitor interaction with B-blockers

A

enhance bradycardic effects

85
Q

AChE inhibitor interaction with systemic corticosteroids

A

enhance muscle weakness

86
Q

Acute intoxication of AChE inhibitors

A

miosis, salivation, sweating, bronchial constriction, vomiting, diarrhea; CNS involvement may follow rapidly

87
Q

Antidote for AChE Inhibitor poisoning

A

atropine, cholinesterase regenerator

88
Q

Cholinesterase regenerator MOA

A

regenerate active enzyme from organophosphorus-cholinesterase complex via removal of phosphorous group

89
Q

Prophylactic agent for AChE inhibitor

A

pyridostigmine

90
Q

Pyridostigmine side effects

A

stomach cramps, diarrhea, nausea, frequent urination, HA, dizziness, SOB, peptic ulcer, blurred vision, watery eyes

91
Q

MOA of mAChR blockers

A

parasympatholytic, block effects of PS autonomic discharge

92
Q

Clinical use of tertiary amines - mAChR-blockers

A

eye or CNS

93
Q

Clinical use of quaternary amines - mAChR-blockers

A

peripheral nervous system

94
Q

Half life and excretion of atropine

A

2 hours; 60% excreted in urine, 40% eliminated by phase I and II reactions

95
Q

Intrinsic activity of atropine

A

reversible antagonist

96
Q

Tissues most sensitive to atropine

A

salivary, bronchial, sweat glands

97
Q

mAChR blockers on CNS

A

longer lasting sedative effect, can reduce tremor associated with Parkinson’s disease, prevents motion sickness

98
Q

mAChR blockers on eye

A

block papillary constrictor muscle resulting in dilation, weaken contraction of ciliary muscle which prevents accommodation, and reduces lacrimal secretion

99
Q

mAChR blockers on CV system

A

tachycardia may occur, no significant changes

100
Q

mAChR blockers on respiratory

A

bronchodilation and reduced secretion

101
Q

mAChR blockers on GI

A

decrease salivary secretion, other GI secretions are most unaffected, gastric emptying is prolonged, smooth muscle relaxation

102
Q

mAChR blockers on GU

A

relax smooth m. of ureters and bladder to slow voiding

103
Q

mAChR blockers on sweat glands

A

suppression of thermoregulatory sweating, inhibits sympathetic cholinergic nerve fibers

104
Q

Cholinergic antagonists for parkinson disease

A

reduce tremor, benzotropine and trihexyphenidyl

105
Q

Cholinergic antagonists for motion sickness

A

vestibular disorders, scopolamine

106
Q

Cholinergic antagonists for anesthesia

A

atropine blocks vagal reflexes

107
Q

Cholinergic antagonists for ophthalmologic disorders

A

retina examination facilitated by mydriasis

108
Q

Cholinergic antagonists for respiratory disorders

A

ipratropium used as first-line therapy, tiotropium may also be used

109
Q

Cholinergic antagonists in CV disorders

A

atropine used for symptomatic bradycardia and hyperactive carotid sinus reflexes

110
Q

Cholinergic antagonists in GI disorders

A

travelers diarrhea, conditions of hypermotility

111
Q

Cholinergic antagonists in urinary disorders

A

relief of urinary urgency; generally will be selective for M3 receptor

112
Q

cholinergic poisoning antidote

A

pralidoxime

113
Q

AE of mAChR antagonists

A

block of parasympathetic function, hyperthermic effects

114
Q

Contraindication of mAChR antagonists

A

glaucoma, men with prostatic hyperplasia, acid-peptic diseases (can slow gastric emptying)

115
Q

Pirenzepine selectivity and MOA

A

M1, inhibits gastric secretion by acting at the ganaglia

116
Q

Chemistry of ganglion-blocking drugs

A

synthetic amines

117
Q

MOA Ganglion-blocking drugs

A

block action of ACh and similar agonists at nAChRs of both parasympathetic and sympathetic autonomic ganglia, block autonomic outflow

118
Q

Nerve effects of ganglion-blocking drugs

A

enhance sympathetic tone, sedation, tremor, choreiform movements, mental aberrations

119
Q

Eye effects of ganglion-blocking drugs

A

cycloplegia with loss of accommodation, moderate dilation of pupil

120
Q

CV system effects of ganglion blocking drugs

A

decrease in vascular tone, decrease in BP, diminished contractility, moderate tachycardia

121
Q

GI effect of ganglion blocking drugs

A

reduced secretion and inhibited motility

122
Q

GU effect of ganglion blocking drugs

A

urination retention or hesitancy, erection may be prevented

123
Q

Clinical applications of ganglion blocking drugs

A

may be used for hypertension, but patients are not typically willing to use them due to toxicity

SBL (21 decks)

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