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Pharm Exam2 > Cholinergic Agonists > Flashcards

Cholinergic Agonists Flashcards

1
Q

Choline esters - name 3.

A

Methancol
Carbachol
Bethanecol

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2
Q

Bethanechol - what is the action?

A

“Beth - call me to activate your BOWEL and BLADDER”

activates bowel and bladder via Muscarinic receptors
resistant to AChE

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3
Q

Carbachol

A

“A carbon copy of ACh”
stimulates nicotinic and muscarinic
pupillary constriction, relieves intraoccular pressure

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4
Q

Methacholine

A

Stimulates muscarinic receptors in airway when inhaled

Use as challenge test for asthma ddx.

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5
Q

Alkaloids - give several examples

A

Muscarine
Pilocarpine
Oxotremorine
Nicotine

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6
Q

What occurs with muscarinic stimulation of the eye?

A

Constricts pupil
Facilitates NEAR vision
decreases intra ocular pressure
Think: GLAUCOMA - pilocarpine given

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7
Q

What occurs with muscarinic stimulation of the heart?

A

Muscarinic stim –> vagal stimulation = BRADYCARDIA!
Atrial and SA nodes effected
AV NODE IS SLOWED

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8
Q

Blood vessels have what type of receptors?

A

M3

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9
Q

Stimulation of M3 receptors on BV leads to what?

A

Dilation of vessels via NO release.

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10
Q

Muscarinic agonists do what to the lungs?

A

Bronchoconstrict
Increase bronchiole secretions

This is why we give methacholine to challenge asthma ddx.

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11
Q

Name a muscarinic agonist that increases cholingergic effect and has a STRANGE side effect.

A

Arecoline –> causes red saliva

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12
Q

When treating glaucoma, what do we use?

A

Drops into eye to open angle.

Use with atropine to break adhesions between iris and lens.

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13
Q

What is a side effect of treating with pilocarpine?

A

Salivation, sweating.

2-3L sometimes.

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14
Q

What is cevimeline?

A

A selective M3 agonist.
Less side effects, longer action.
Less sweater.

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15
Q

Side effects from muscarinic side effects?

A 
Sweat
increased gut activity
drooling
bronchospasm
tears
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16
Q

Why is poisoning with mushrooms a concern? What do we treat with?

A

Mushrooms are muscarine agonists.

Treat with atropine (ANTAGONIST) and Epi.

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17
Q

Which receptors sensitize rapidly?

A

Nicotinic

18
Q

Compare low dose nicotinic stimulation in brain to high dose stimulation?

A

Low dose:
increased alertness and attention

High Dose
tremor, emesis, increased RR

Toxicity:
convulsions

19
Q

Does Nicotine activate PSNS or SNS?

A

Both!

20
Q

What are some effects of Nicotine toxicity?

A

vomiting
CNS overstim (convulsions, coma, respiratory arrest)
Skeletal mm depol (blocks NMJ and get paralysis)
Cardio: HTN and arrhythmia

21
Q

How to treat nicotine poisoning?

A

Atropine blocks M receptors
Anticonvulsant
Assist Respiration

22
Q

What does Chantix do?

A

partial agonist on nicotine receptor in brain
prevents cravings
blocks effect of nicotine if smoke

23
Q

Name some cholinesterase inhibitors?

A

“-stigmines” and “-phoniums”

Neostigmine (myasthenia gravis)
Physostigmine
Donezipil
Edrophonium (myasthenia gravis)

24
Q

What is one toxic substance that works as a cholinesterase inhibitor?

A

Organophosphates

25
Q

What’s are some concerns with Neostigmine?

A

Use post op to remove neuromuscular blockade (NMB), but has poor oral absorption and doesn’t enter CNS.

Use to increase bladder motility, treat MG, and reverse NMB

26
Q

What cholinesterase inhibitors enter the CNS?

A

Physostigmine
Think it “phyxs” an atropine overdose

Give in the eye

27
Q

Endrophonium - what is it good for?

A

Cholinesterase inhibitor

reversible, short acting

28
Q

What can we use against organophosphate poisoning?

A

2PAM - but not for carbamates!

29
Q

What is 2PAM?

A

binds and inhibits AChE
most effective at NMJ
does not enter CNS

30
Q

Some effects of AChE inhibitors?

A

CNS - improved alertness and memory
Eye - meiosis
GI, Bladder stim
Respiratory- salivation, secretion, bronchoconstric

31
Q

Cardio effects of AChE inhibitors?

A

Sympathetics dominated by Nicotine

So - see heart with bradycardia, decreased force
BP has little effect - no cholinergic innervation

32
Q

What is Donezipil often used for?

A

Donezipil = aricept
AChE inhibitor that penetrates CNS

Also could be
Aricept, Exelon, Reminyl, Cognex

33
Q

How does Echothiophate work? What do we use it for?

A

Organophosphate AChE inhibitor

IRREVERSIBLE inhibition of AChE

use topically to produce long lasting decrease in Pressure

34
Q

What is DFP? Why is it dangerous?

A

organophosphate
irreversibly binds AChE

lipid soluble, penetrates CNS

35
Q

How do soman, sarin, and tabun work?

A

neve gases

organophosphates

36
Q

How should we treat glaucoma?

A

Direct agonist:
pilocarpine or carbachol (lowers P)
Cholinesterase Inhib
also could be used

37
Q

Two possible drugs for GI/Urinary?

A

Bethanechol more common

Used to also be neostigmine

38
Q

Name the TOXICITIES For AChE

A 
SLUDGE
salivation
    lacrimation
        urination
            defecation
                  gastric distress
                       emesis
39
Q

What do we give for organophosphate AChE inhibitor poisoning?

A

atropine
2-Pam if w/in 3-4hrs of exposure
Diazepam for seizures

40
Q

What can cause carbamate AChE poisoning?

A

Sevin
Baygon
Temik

Pharm Exam2 (4 decks)

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