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RENAL II EXAM 1 > Introduction to Cholinergic agonists and antagonists - through slide 39 - SRS > Flashcards

Introduction to Cholinergic agonists and antagonists - through slide 39 - SRS Flashcards

1
Q

Describe cholinergic transmission from synthesis to termination

A
  1. CHT transporter brings in hemicholiniums
  2. ChAT synthesizes ACh from choline and AcCoA
  3. ACh is packaged in vesicles by VAT
  4. VAMPS engage synaptic vesicles and lead to exocytosis of the ACh
  5. ACh interacts with muscarinic (G proteins) and nicotinic receptors
  6. ACh destroyed by AChE
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2
Q

Describe adrenergic transmission from synthesis to termination

A
  1. Tyrosine hydroxylase converts tyrosine to dopa to dopamine to NE
  2. VMAT packages the NE in synaptic vesicles
  3. CA++ channels open and lead VAMPS to engage vesicles, exocytosing NE
  4. NET takes up NE from the synaptic cleft
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3
Q

What is the parasympathetic NT?

A

ACh

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4
Q

What are the parasympathetic receptors?

A

•nAChR, mAChR

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5
Q

What are the sympathetic NTs?

A

•NE > Epi (DA); ACh

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6
Q

What are the receptors for the sympathetic system?

A

•α, β, (D), nAChR, mAChR

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7
Q

What type of receptors are the muscarinics?

A

GPCRs

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8
Q

Which muscarinic receptors are what kind of G’s (s, i, q)?

A

Odds are Stimulatory via Gq (M1,3,5)

Evens are inhibitory via Gi (G2,4)

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9
Q

Where are M1s?

A

CNS and ganglia

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10
Q

Where are M2s?

A

Heart, nerves, smooth muscle

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11
Q

Where are M3s?

A

Glands, smooth muscle, endothelium

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12
Q

In most organs what mAChR are predominant?

A

M3

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13
Q

What muscarinic receptor predominates in the heart?

A

M2

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14
Q

What muscarinic receptors are predominant in smooth muscle?

A

M3, M2

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15
Q

What are the types of agonists for cholinergic drugs?

A

Direct-acting

indirect-acting`

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16
Q

What is the class of indirect-acting cholinergic drugs?

A

AChE inhibitors

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17
Q

What are the types of cholinergic antagonists?

A

Antinicotinic agents

antimuscarinic agents

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18
Q

What types of antinicotinic agents are there? What is the problem with these?

A

Neuromuscular blockers

ganglion blockers

Tend to have many side effects due to the abundance of nicotinic receptors through the body.

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19
Q

What is the prototype antimuscarinic agent?

A

Atropine

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20
Q

What are the impacts of cholinergic agonists on the following:

Eye

Salivary gland

bronchi

heart

GI tract

Bladder

A
  1. Eye - pupil constriction, near vision
  2. Salivary gland - salivation
  3. bronchi - constriction and secretion
  4. heart - slowing
  5. GI tract - gastric secretion increased, colic, diarrhea
  6. Bladder - Void urine
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21
Q

What are direct-acting cholinergic drugs?

A

Choline esters, alkaloids

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22
Q

What are the problems for the direct acting cholinergic agonists?

What is the typical approach to using these drugs?

A

Poor absorption, susceptible to AChE

Used locally, such as topical application - eye drops

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23
Q

What are the four choline esters we covered?

A

Acetylcholine

methacholine

carbachol

bethanechol

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24
Q

What are the cholinomimetic alkaloids we covered?

A

Muscarinic - Muscarine and pilocarpine

Nicotinic - nicotine and lobeline

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25
Q

Muscarine is charged, but capable of…

A

Crossing BBB, thus highly toxic when ingested

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26
Q

What are the two major uses for direct-acting cholinergics?

A

Diseases of the eye

  • glaucoma
  • accomodative esotropia

GI/GU disorders

  • Postoperative ileus
  • Congenital megacolon
  • Urinary retention
  • Esophageal reflux
  • Xerostomia, Sjögren syndrome
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27
Q

Name 6 direct acting cholinergic agonists

A
  1. Acetylcholine
  2. bethanechol
  3. carbachol
  4. cevimeline
  5. methacholine
  6. pilocarpine
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28
Q

What is the approved use for acetylcholine we covered?

A

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

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29
Q

Bethanechol is a selective mAChR agonist that primarily affects what systems?

What can it be used for?

Risk associated with this?

A

Urinary and GU tracts

treats urinary retention and heartburn

UTI if sphincter fails to relax

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30
Q

Carbachol is a nonspecific cholinergic agonist that is used for treatment of?

A

Glaucoma

produce miosis during surgery or opthalmic exam

31
Q

What is cevimeline used for?

A

Treat xerostomia in Sjogrens patients`

32
Q

What is methacholine used for?

A

Used in diagnosis of bronchial airway hyperreactivity

33
Q

What is pilocarpine useful for?

A

Xerostomia, miosis

34
Q

What is the trade name of varenicline?

A

Chantix

35
Q

What is varenicline used for?

What is its target?

A

Smoking cessation

binds with high affinity and selectivity to α4β2 nAChRs (NN)

36
Q

What type of drug is varenicline?

A

Partial agonist -
•stimulation and subsequent moderate, sustained release of mesolimbic dopamine are thought to reduce craving and withdrawal symptoms associated with smoking cessation

37
Q

Who should not have varenicline?

A

People with a history of depression or suicidal ideation

38
Q

Muscarinic stimulants produce the slude toxicity effects, what is the approach to mitigating this?

A

Atropine used for muscarinic effects

39
Q

Nicotine poisoning can occur via cigarettes and insecticides, what are the toxiticy effects? (5)

A
  1. CNS stimulation,
  2. skeletal muscle end plate depolarization,
  3. respiratory paralysis,
  4. hypertension,
  5. cardiac arrhythmias
40
Q

What are the three chemical groups of AChE inhibitors?

A

Alcohols

carbamates

organophosphates

41
Q

What are some clinical uses of AChE inhibitors?

(6)

A
  1. Mysathenia gravis
  2. reversal of neuromuscular blockade during anesthesia
  3. alzheimers
  4. parkinsons
  5. antidote for anticholinergic poisioning
  6. Sarin gas
42
Q

What are the effects of AChE inhibitor toxicity?

A

SLUDGEM

  • Salivation, Lacrimation, Urination, Defecation, Gastrointestinal, Emesis
  • Also NMJ effects: muscle fasciculations followed by paralysis
43
Q

If treating alzheimers or parkinsons would you use a charged or uncharged AChE inhibitors?

A

Uncharged

44
Q

What is the alcohol AChE inhibitor? What are its lipid solubility and charge profiles?

A

Edrophonium

lipid sol - low

Charged

45
Q

What are the carbamates we looked at?

What are their lipid solubilities and charges like?

A

neostigmine, low lipid sol. and charged

pyridostigmine, low lipid sol. and charged

physostigmine, high lipid sol. and uncharged

46
Q

What is the organophosphate AChE inhibitor we covered? Lipid sol? Charge?

A

Echotiophate - low lipid sol. and charged

47
Q

What are the cholinergic antagonist subgroups?

A

Antinicotinic

antimuscarinic

48
Q

What are the antinicotinic agents?

A

neuromuscular junction - skeletal m.

ganglia (rarely used)

49
Q

What organs are the antimuscarinics used for?

A

CNS, nerves, heart, s. muscle, glands, endothelium

block autonomic discharge

50
Q

What drug is used for motion sickness? What type of drug is it?

A

Scopolamine - antimuscarinic

51
Q

What antimuscarinics are used for respiratory disorders?

A

Ipratropium

Tiotropium

52
Q

What are the antimuscarinic agents used for GI disorders?

A

Atropine

dicyclomine

glycopyrrolate

hyoscyamine

53
Q

What antimuscarinic drugs are used for movement disorders?

Are these likely charged or uncharged?

A
  • Benztropine
  • Biperiden
  • Orphenadrine
  • Procyclidine
  • Trihexyphenidyl

likely uncharged so as to reach CNS

54
Q

What are the antimuscarinics used in opthalmology?

A
  • Atropine
  • Cyclopentolate
  • Homatropine
  • Scopolamine
  • Tropicamide
55
Q

What antimuscarinics are used for urinary disorders?

A
  1. Darifenacin
  2. Oxybutynin
  3. Solifenacin
  4. Tolterodine
  5. Trospium
56
Q

What drugs are used for cholinergic poisoning?

A

Atropine + pralidoxime

57
Q

What are the effects of antimuscarinics on the CNS?

A
  1. Sedation
  2. drowsiness
  3. amnesia
  4. hallucinations
  5. tremor reduction
58
Q

What are the effects of antimuscarinics on the eye?

A
  1. Pupil dilation
  2. cycloplegia (ciliary muscle paralysis)
  3. Loss of accomodation
  4. Secretion reduction
59
Q

What are the effects of antimuscarinics on the cardiovascular system?

A

Tachycardia

(small effect on blood pressure)

60
Q

What would an antimuscarinic do to the respiratory system?

A

Bronchodilation

secretion reduction

61
Q

What are the effects of antimuscarinics on the GI tract?

A
  1. Reduction in salivation
  2. gastric secretion
  3. prolonged gastric emptying time
62
Q

What effects do antimuscarinics have on the GU tract?

A

urinary retention

63
Q

What effect do antimuscarinics have on sweat glands?

A

Suppression of thermoregulatory sweating by inhibiting sympathetic cholinergic nerve fibers (no parasympathetic innervation of sweat glands)

64
Q

What is the target for anticholinergic treatment for Parkinsons? What are the drugs we covered for this?

A

mAChR antagonists can reduce tremors

Tertiary amines:

  • benztropine
  • trihexyphenidyl
  • procycline
65
Q

Scopolamine is used for motion sickness, what are the routes of administration?

A

PO, injection, transdermal

66
Q

Atropine can be used for anesthesia, how/when?

A
  1. Given to block responses to vagal reflexes induced by surgical manipulation of visceral organs.
  2. Atropine (or glycopyrrolate) is paired with the cholinesterase inhibitor neostigmine, to block its parasympathetic effects during reversal of neuromuscular blockade.
67
Q

When performing eye surgery what kinds of drugs would you want?

A

mAChR antagonists - to induce cycloplegia or mydriasis

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

68
Q

What are two drugs used to prevent synechia formation in uveitis and iritis?

A

homatropine and atropine

(produce long lasting mydriasis and cycloplegia)

69
Q

Asthma and COPD can be treated with anticholinergics, what are they? Which can be used once a day?

A

Ipratropium

Tiotropium - longer bronchodilation = 1 dose per day

70
Q

anticholinergics can be used to treat GI disorders, what are these often combined with and why?

A
  • Often combined with an opioid antidiarrheal drug to discourage abuse of the opioid agent
  • Example: Lomotil - combination of atropine and diphenoxylate
71
Q

Anticholinergics can be used to treat GU disorders, what receptor do we want these to be selective for?

What are four drugs that are options for this?

A

Selectivity to M3 subtype of of mAChr - predominate in bladder wall and sphincter smooth muscle

  1. Darifenacin
  2. silifenacin
  3. tolterodine
  4. Oxybutynin - not preferred d/t short half life and significant side effects (xerostomia, dizziness, constipation, blurred vision)
72
Q

What are examples of poisoning events that anticholinergics are useful for?

A
  1. AChE inhibitor overdose
  2. Sarin gas
  3. Organophosphate insecticides
73
Q

What are two examples of poisonings that anticholinergics are not good for?

A
  1. Poisoning at the nAChR - must use plaidoxime to regenerate the nAChRs
  2. Delayed-onset mushroom poisoning
74
Q

What are three contraindications for anticholinergics?

A
  1. Glaucoma
  2. Prostatic hyperplasia
  3. Acid-peptic disease

RENAL II EXAM 1 (8 decks)

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