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Pharmacology > Cholinergic Drugs > Flashcards

Cholinergic Drugs Flashcards

1
Q

Acetylcholine overview

A

direct-acting cholinergic agonist
very susceptible to cholinesterase
binds to both mAChR and nAChR

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2
Q

Methacholine overview

A

direct-acting cholinergic agonist
slightly susceptible to cholinesterase
only binds to mAChR

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3
Q

Carbachol overview

A

direct-acting cholinergic agonist
not susceptible to cholinesterase
binds nAChR> mAChR

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4
Q

Bethanechol overview

A

direct-acting cholinergic agonist
not susceptible to cholinesterase
only binds to mAChR

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5
Q

Characteristics of choline esters

A

direct-acting cholinergic agonists
permanently charged
poor absorption and distribution to CNS
metabolized by acetylcholinesterase

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6
Q

Characteristics of alkaloids

A

MOA: agonists at cholinergic receptors
uncharged–> well absorbed
muscarine is charged but can cross the BBB and is highly toxic when ingested

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7
Q

Alkaloids

A

muscarine and pilocarpine –> mAChR

nicotine and lobeline–>nAChR

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8
Q

choline esters

A

ACh
methacholine
carbachol
bethanechol

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9
Q

3 groups of AChE inhibitors

A

alcohols (reversible)
carbamic acid esters (reversible but longer lasting than alchols)
organophosphates (irreversible; covalent)

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10
Q

Charged AChE inhibitors

A

insoluble in lipids –> do not cross BBB, poor PO absorption

quaternary agents

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11
Q

Neutral AChE inhibitors

A

lipid soluble–> can cross BBB and are readily absorbed

most organophosphates, tertiary agents

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12
Q

Parasympathetic effects to the eye

A

Miosis (pupillary contraction)

contraction of ciliary muscle for near vision

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13
Q

Parasympathetic effects to the heart

A

SA node- decreased chronotropy (rate)
Atria- decrease in ionotropy (contractile strength), decrease in refractory period
AV node- decrease in dromotropy (conduction velocity), increase in refractory period
ventricles- small decrease in contractile strength

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14
Q

Parasympathetic effects to the blood vessels

A

Arteries- dilation (via EDRF); constriction (high-dose direct effect)
Veins- dilation (via EDRF); constriction (high-dose direct effect)

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15
Q

Parasympathetic effects to the lungs

A

bronchial muscle-contraction (bronchoconstriction)

bronchial glands- stimulation

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16
Q

Parasympathetic effects to the GI tract

A

motility- increase
sphincters-relaxation
secretion-stimulation

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17
Q

parasympathetic effects to the urinary bladder

A

detrusor- contraction
trigone and sphincter-relaxation
voiding of urine

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18
Q

Parasympathetic effects to the glands

A

sweat, salivary, lacrimal, and nasopharyngeal- secretion

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19
Q

ACh

A

approved for intraocular use during surgery and causes miosis (reduction in pupil size)

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20
Q

Bethanechol

A

affects primarily urinary and GU tracts
can be used to treat pts with urinary retention and heartburn
little CV stimulation
may produce UTI if sphincter fails to relax

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21
Q

Carbachol

A

used for treatment of glaucoma or to produce miosis during surgery or ophthalmic exam

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22
Q

Cevimeline

A

oral tablet used to treat dry mouth (xerostomia) in pts with Sjogren syndrome

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23
Q

Pilocarpine

A

xerostomia treatment with Sjogren syndrome or head and neck cancer treatment related xerostomia (PO)
miosis during ophthalmic procedures (topical)
glaucoma (topical)

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24
Q

Varenicline

A

Chantix
SMOKING CESSATION
partial agonist that binds with high affinity and selectivity to alpha4 beta2 nAChRs

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25
Q

MOA of Varenicline

A

stimulation and subsequent moderate, sustained release of mesolimbic dopamine are though to reduce craving and withdrawal symptoms associated with smoking cessation

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26
Q

What is a common adverse effect of Varenicline?

A

nausea; serious adverse effects are neuropsychiatric symptoms–>changes in behavior, agitation, depressed mood, suicidal ideation, and suicide

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27
Q

Major uses of direct-acting cholinergic agonists

A

Diseases of the eye- glaucoma, accommodative esotropia: misalignment of the eyes caused by hypermetropic accommodative error
GI/GU disorders: postoperative ileus, congenital megacolon, urinary retention, esophageal reflux, xerostomia, Sjogren syndrome

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28
Q

Toxicity of muscarinic stimulants

A

N/V/D urinary urgency, salivation, sweating, cutaneous vasodilation, bronchial constriction, increase in glandular secretion (SLUDGE)

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29
Q

Contraindications of muscarinic stimulants

A

pts with asthma, hyperthyroidism, coronary insufficiency, acid-peptic disease

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30
Q

Toxicity of nicotinic stimulants

A

nicotine poisoning: cigarettes and insecticides
acute toxicity includes CNS stimulation ,skeletal muscle end plate depolarization, respiratory paralysis, HTN, cardiac arrhythmias

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31
Q

How do you treat toxicity with direct-acting cholinergic agonists?

A

atropine and parenteral anticonvulsants (diazepam, a benzodiazepine)

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32
Q

Clinical uses of indirect-acting cholinergic agonists

A

Glaucoma, dementia, antidote to anticholineric poisoning, reversal of neuromuscular paralysis, MG, AChE inhibitor toxicity

33
Q

Use of indirect-acting cholinergic agonists in glaucoma

A

stimulation of mAChRs on the ciliary body facilitate aqueous humor outflow and reduces intraocular pressure (replaced by beta-blockers, prostaglandins)

34
Q

Use of indirect-acting cholinergic agonists in demetia

A

Alzheimer’s and Parkinson

pts with Alzheimers have a deficiency of intact cholinergic neurons

35
Q

Use of indirect-acting cholinergic agonists as an antidote to anticholinergic poisoning

A

from atropine, antihistamines, TCAs, sleep aids, cold preparations
symptoms: cutaneous vasodilation, anhidrosis, anhydrotic hyperthermia, nonreactive mydriasis, delirium, hallucinations, reduction/elimination of the desire to urinate

36
Q

Use of indirect-acting cholinergic agonists in AChE inhibitor toxicity

A

SLUDGE symptoms, effects on NMJ

treatments include atropine, maintenance of vital signs, decontamination, pralidoxime (cholinesterase regenerator)

37
Q

Antinicotinic agents

A

NMJ (skeletal muscle relaxants)

Ganglia (rarely used)

38
Q

Antimuscarinic agents

A

CNS, nerves, heart, smooth muscle, glands, endothelium
block the effects of parasympathetic autonomic discharge
the most clinically useful cholinergic antagonists

39
Q

Prototype antimuscarinic agent

A

atropine

40
Q

Uses for anticholinergic agents

A 
motion sickness
GI disorders
ophthalmology
respiratory disorders
urinary disorders
cholinergic poisoning
movement disorders
41
Q

Drugs used for motion sickness

A

scopolamine

42
Q

Drugs used for GI disorders (anticholinergic)

A

Atropine, dicyclomine, glycopyrrolate, hyoscyamine

43
Q

Drugs used in ophthalmology (anticholinergic)

A

Atropine, cyclopentolate, homatropine, scopolamine, tropicamide

44
Q

Drugs used for respiratory disorders (anticholinergic)

A

Ipratropium

Tiotropium

45
Q

Drugs used for urinary disorders (anticholinergic)

A 
Darifenacin
oxybutynin
solifenacin
tolterodine
trospium
46
Q

Drugs used for cholinergic poisoning

A

atropine ( + pralidoxime)

47
Q

Drugs used for movement disorders (anticholinergic)

A 
benztropine
biperiden
orphenadrine
procyclidine
trihexyphenidyl
48
Q

Effects of anticholinergics on CNS

A

sedation, drowsiness, amnesia, hallucinations, tremor reduction
effects vary within class

49
Q

Effects of anticholinergics on eye

A

pupil dilation, cycloplegia (ciliary muscle paralysis), loss of accommodation, secretion reduction

50
Q

Effects of anticholinergics on cardiovascular system

A

tachycardia may occur, little effect on BP

51
Q

Effects of anticholinergics on respiratory system

A

bronchodilation and secretion reduction

52
Q

Effects of anticholinergics on GI tract

A

reduction in salivation, gastric secretion, prolonged gastric emptying time

53
Q

Effects of anticholinergics on GU tract

A

urinary retention

54
Q

Effects of anticholinergics on sweat glands

A

suppression of thermoregulatory sweating by inhibiting sympathetic cholinergic nerve fibers (NO parasympathetic innervation of sweat glands)

55
Q

Treatment for Parkinson disease

A

mAChR antagonists can reduce tremors
not as effective as standard dopaminergic therapy (used in combo)
tertiary amines benztropine, trihexyphenidyl, and procyclidine

56
Q

Atropine for anesthesia

A

given to block responses to vagal reflexes induced by surgical manipulation of visceral organs
paired with the cholinesterase inhibitor neostigmine to block its parasympathetic effects

57
Q

Neostigmine

A

cholinesterase inhibitor

58
Q

When are mAChR antagonists used for ophthalmologic disorders?

A

when cycloplegia or prolonged mydriasisi is required–>refractive eye surgery (LASIK)

59
Q

Why are mAChR antagonists not used for ophthalmologic disorders often?

A

alpha-adrenergic receptor agonists are shorter-acting and produce less adverse effects

60
Q

What two drugs are used to prevent synechia formation in uveitis and iritis (where the iris adheres to either the lens or the cornea)?

A

homatropine and atropine
long-acting agents
mydriasis may last 6 hours to 12 days and cycloplegia persists about 10 hrs to 14 days

61
Q

What two respiratory disorders use anticholinergics?

A

asthma and COPD

62
Q

What two anticholinergic medications are used for asthma and COPD?

A

ipratropium and tiotropium
inhalation mAChR antagonists
tiotropium has a longer bronchodilator action than ipratropium and can be dosed once daily

63
Q

What class of drug can be used in treatment of common diarrhea and other mild or self-limited conditions of hypermotility?

A

mAChR antagonists

often combined with an opiod antidiarrheal drug to discourage abuse of opioid agent

64
Q

Lomotil

A

combo of atropine (mAChR antagonist) and diphenoxylate (opioid)

65
Q

When are anticholinergics used for GU disorders?

A

symptomatic relief in the treatment of urinary urgency caused by minor inflammatory bladder disorders

66
Q

What receptor is common on the bladder wall and sphincter smooth muscle?

A

M3

67
Q

What is a prototype selective M3 antagonist used in GU disorders?

A

oxybutynin, but it has side effects such as dry mouth/eyes, dizziness, constipation, blurred vision

68
Q

What 3 drugs are selective for the M3 subtype and are advantageous because of their longer half-lives and reduced incidence of xerostomia and constipation?

A

darifenacin, solifenacin, and tolterodine

69
Q

What drug is given for cholinergic poisoning?

A

atropine (mAChR)

no effective treatment at nAChR (pralidoxime)

70
Q

What kind of poisoning is atropine useless in?

A

delayed-onset mushroom poisoning

N/V 6-12 hours after ingestion and causes hepatic/renal cellular injury by amatoxins that inhibit RNA polymerase

71
Q

Adverse effects of anticholinergics

A

mydriasis and cycloplegia may be adverse effects of antimuscarinic agents used to reduce GI secretion

72
Q

High systemic concentrations of anticholinergics lead to what?

A

block of parasympathetic function: dry as a bone, blind as a bat, red as a beet, mad as a hatter, hot as a hare
treat wtih AChE inhibitors

73
Q

Contraindications of anticholinergics

A

glaucoma, prostatic hyperplasia, acid-peptic disease

74
Q

Cholinesterase inhibitors-alcohols

A

edrophonium

75
Q

cholinesterase inhibitors- carbamic acid esters

A

neostigmine, pyridostigmine, physostigmine, and carbaryl

76
Q

cholinesterase inhibitors- organophosphates

A

echothiphate, parathion, malathion, (insecticides) sarin, soman, and tabun (nerve gases)

77
Q

Tertiary and uncharged AChE inhibitors

A 
physostigmine
donepezil
tacrin
rivastigmine
galantamine
78
Q

Quaternary and charged AChE inhibitors

A 
neiostigmine
pyridostigmin
edrophonium
echothiophate
ambenonium

Pharmacology (3 decks)

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