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Sketchy Pharm- ANS drugs- LAH > Autonomic Drugs: Ch. 1.1: Cholinomimetics > Flashcards

Autonomic Drugs: Ch. 1.1: Cholinomimetics Flashcards

1
Q

At which end-organs are M1 ACh receptors found?

A

the CNS

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2
Q

Muscarinic agonists reduce intraocular pressure by causing contraction of the ciliary body, facilitating _____.

A

the outflow of aqueous humor

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3
Q

In _____, pilocarpine can be used to treat because it activates the sphincter pupillae muscle to cause myosis and therefore relieves pressure.

A

acute glaucoma

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4
Q

When cholimomimetic drugs activate muscarinic receptors, they mimic the effect of _____ at end organs.

A

parasympathetic nerve discharge

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5
Q

What is methacholine? What is it used to treat?

A
  • a cholinomimetic
  • used for asthma/pulmonary testing
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6
Q

Activation of M3 receptors leads to the release of NO from vascular endothelial cells, which causes _____ and therefore relaxation of the blood vessels.

A

increased cGMP

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7
Q

Muscarinic agonists reduce intraocular pressure by causing ______, facilitating the outflow of aqueous humor.

A

contraction of the ciliary body

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8
Q

Because _____ stimulate the detrusor muscle and relax the bladder sphincter muscles, bethanechol can be used to treat non-obstructive urinary obstruction.

A

muscarinic agonists

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9
Q

Cue:

  • 3 motorcycle parking spots, labeled M1, M2, and M3, in front of the “QIQ Mart”
A
  • M1, M2, M3 = muscarinic ACh receptors
  • QIQ = receptors are coupled to Gq, Gi, Gq, respectively
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10
Q

Cue:

  • M2 motorcycle rider has a torn heart jacket showing only atria and jewels
A
  • M2 = M2 receptor, Gi
  • heart = activation in heart leads to:
    • decreased HR at the SA node
    • decreased contractility of the atria
    • decreased conduction velocity through the AV node
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11
Q

Cue:

  • adrenal-gland-looking beanie hat on the smoker
A
  • smoker = nicotinic receptor
  • beanie = adrenal gland
  • *** Nicotinic ACh receptors are found on the adrenal gland
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12
Q

Because muscarinic agonists stimulate the detrusor muscle and relax the bladder sphincter muscles, _____ can be used to treat non-obstructive urinary obstruction.

A

bethanechol

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13
Q

Cue:

  • flyer for quitting smoking says to “Call 1-800-VERY-CLEAN”
A
  • 1-800-VERY-CLEAN = varenicline
  • smoking = nicotinic receptor agonist
  • quitting = smoking cessation
  • *** Varenicline is a nicotinic receptor agonist used for smoking cessation
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14
Q

Muscarinic receptors are coupled to ______ that function as transducers.

A

G proteins

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15
Q

____ increase the secretory and motor activity of the gut.

A

Muscarinic agonists

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16
Q

Cue:

  • a man in an apt window with his hoodie pulled tightly around his head to avoid carbon fumes rising from the smoker below
A
  • carbon fumes = Carbachol; both a muscarinic and nicotinic agonist
  • constricted hood = pupillary constriction
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17
Q

Activation of M3 receptors leads to the release of ___ from vascular endothelial cells, which causes increased cGMP and therefore relaxation of the blood vessels.

A

NO

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18
Q

Cue:

  • M3 motorcycle has a dilated nitric oxide exhaust pipe
A
  • M3 = M3 receptor; Gs
  • *** M3 receptor activation –> NO release in vascular smooth muscle cells –> increased cGMP –> vasodilation
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19
Q

This is a cholimomimetic used to treat:

  • non-obstructive GI disorders:
    • post-op ileus
    • neurogenic ileus
    • congenital megacolon
  • non-obstructive urinary retention:
    • post-op
    • post-partum
    • neurogenic bladder from spinal cord injury
A

bethanechol

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20
Q

Intravascular injection of ______ produce marked vasodilation.

A

muscarinic agonists

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21
Q

What does ‘cholinomimetic’ mean?

A
  • it mimics or modifies the affect of ACh
    • aka ACh receptor agonists
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22
Q

Cue:

  • M3 motorcycle rider holding a sponge and giving an Acetyl Cola toast, sitting on his bike that is painted like smooth muscle
A
  • M3 = M3 receptor, Gs
  • sponge = glands
  • smooth muscle = smooth muscle organs
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23
Q

A _____ instigates asthma for pulmonary testing.

A

methacholine challenge

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24
Q

At which end-organs are M2 ACh receptors found?

A

the heart

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25
Q

Gq receptors activate the _____ cascade, which leads to increased intracellular Ca++.

A

IP3/DAG

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26
Q

Cue:

  • “Enjoy Acetyl-Cola” sign with a mime on it
A
  • these drugs are ACh receptor agonists aka cholinomimetics
  • mime = cholinomimetic
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27
Q
  • M1 = G__
  • M2 = G___
  • M3 = G___
A
  • M1 = Gq
  • M2 = Gi
  • M3 = Gq
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28
Q

What is the major NT of the PNS?

A

ACh

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29
Q

Muscarinic stimulants can contract the ______, leading to symptoms of wheezing.

A

smooth muscle of the bronchial tree

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30
Q

What is Carbachol? What is it used to treat?

A
  • a cholinomimetic
  • used to treat acute angle-closure glaucoma
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31
Q

When cholimomimetic drugs activate ______ receptors, they mimic the effect of parasympathetic nerve discharge at end organs.

A

muscarinic

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32
Q

Where are nicotinic receptors found?

A
  • on autonomic ganglia
  • at skeletal neuromuscular junctions
  • in the adrenal gland
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33
Q

In acute glaucoma, ______ can be used to treat because it activates the sphincter pupillae muscle to cause myosis and therefore relieves pressure.

A

pilocarpine

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34
Q

This a cholinomimetic used to treat:

  • dry mouth from:
    • Sjogrens
    • radiation damage
    • SEs from other meds
  • glaucoma
A

Pilocarpine

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35
Q

Cue:

  • a smoker near some ganglia-like transformers on a telephone pole
A
  • smoker = nicotinic ACh receptors
  • transformers = ganglia
  • *** nicotinic ACh receptors are found on autonomic ganglia
36
Q

_______ reduce intraocular pressure by causing contraction of the ciliary body, facilitating the outflow of aqueous humor.

A

Muscarinic agonists

37
Q

Activation of M3 receptors leads to the release of NO from vascular endothelial cells, which causes increased cGMP and therefore ______ of the blood vessels.

A

relaxation

38
Q

This drug is a partial agonist at nicotinic receptors, and as such, is used to treat smoking cessation.

A

varenicline

39
Q

Cue:

  • M3 motorcycle has a clogged, constricted exhaust pipe
A
  • clogged, constricted pipe = atherosclerosis
  • *** atherosclerosis –> vascular epithelial cell damage –> direct muscarinic receptor activation –> vasoconstriction
40
Q

Cue:

  • man running thru the “Para-City Marathon Challenge” finish line as he drinks an Acetyl-Cola
A
  • marathon = methacholine
  • challenge = methacholine challenge = asthma testing
  • Acetyl-Cola = a cholinomimetic
41
Q

Muscarinic agonists increase the ______ and _____ of the gut.

A

secretory and motor activity

42
Q

Muscarinic agonists reduce ______ by causing contraction of the ciliary body, facilitating the outflow of aqueous humor.

A

intraocular pressure

43
Q

This is a cholinomimetic used to treat acute angle-closure glaucoma (only).

A

Carbachol

44
Q

______ eliminates M3 receptor activation and therefore causes vascular smooth muscle constriction.

A

Atherosclerosis

45
Q

What is Bethanechol? What is it used to treat?

A
  • a cholimomimetic used to treat:
    • non-obstructive GI orders:
      • post-op ileus
      • neurogenic ileus
      • congenital megacolon
    • non-obstructive urinary retention:
      • post-op
      • post-partum
      • neurogenic bladder from spinal cord injury
46
Q

Carbachol is a ______ agonist.

A

nicotinic AND muscarinic

47
Q

Name 5 cholinomimetics and which receptor they act upon.

A
  1. bethanicol (muscarinic)
  2. pilocarpine (muscarinic)
  3. methacholine (muscarinic)
  4. carbachol (both nicotinic AND muscarinic)
  5. varenicline (nicotinic)
48
Q

_____ receptors are transmembrane polypeptides that act as ion channels.

A

Nicotinic

49
Q

Intravascular injection of muscarinic agonists produces ______.

A

marked vasodilation

50
Q

Cue:

  • fisherman with his hoodie pulled tightly around his head
A
  • constricted hood = pupillary constriction
  • *** Pilocarpine activates the sphincter pupillae muscle to cause pupillary construction (useful in acute angle-closure glaucoma).
51
Q

Nicotinic receptors are ______ that act as ion channels.

A

transmembrane polypeptides

52
Q

Cue:

  • Beth the construction worker, drinking an Acetyl Cola, holding a bladder hose, standing next to a cement truck pouring cement
A
  • Beth = Bethanechol
  • Acetyl Cola = it’s a cholimomimetic
  • cement truck = GI motility
  • bladder hose = tx for urinary retention
53
Q

______ receptors are coupled to G proteins that function as transducers.

A

Muscarinic

54
Q

Atherosclerosis eliminates ____ receptor activation and therefore causes vascular smooth muscle constriction.

A

M3

55
Q

Because muscarinic agonists stimulate _____ and relax _____, bethanechol can be used to treat non-obstructive urinary obstruction.

A
  • stimulate the detrusor muscle
  • relax the bladder sphincter muscles
56
Q

Because muscarinic agonists stimulate the detrusor muscle and relax the bladder sphincter muscles, bethanechol can be used to treat ______.

A

non-obstructive urinary obstruction

57
Q

Gi receptor activation leads to the ______ .

A

inhibition of cAMP production

58
Q

What 3 pathologies can cholinomimetic exacerbate?

A
  1. COPD
  2. asthma
  3. peptic ulcer disease
59
Q

Cue:

  • a pile o’ carp with dripping mouths being dumped from a net with round glass floats on it held by a crane
A
  • pile-o-carp = pilocarpine
  • dripping mouths = increases salivation
  • net = zonular fibers of the eye
  • round glass floats = accommodated lens (ciliary body contraction)
  • crane = smooth muscle cells of ciliary muscle
60
Q

_____ receptors activate the IP3/DAG cascade, which leads to increased intracellular Ca++.

A

Gq

61
Q

Cue:

  • an electrical outlet near the smoker
A
  • outlet = motor end plate
  • smoker = nicotinic receptor
  • *** nicotinic ACh receptors are found on skeletal muscle motor end plates (neuromuscular junction)
62
Q

Cue:

  • “Ion Channel News” on TVs behind the smoker
A

Nicotinic receptors act as ion channels

63
Q

This is a cholinomimetic used for asthma/pulmonary testing.

A

methacholine

64
Q

Cue:

  • motorcycle in the M2 parking space with a packed-up tent
A
  • M2 = M2 receptor; Gi
  • packed tent = inhibited cAMP
65
Q

Cue:

  • Construction sign says “Do not obstruct”
A
  • Muscarinic agonists, like bethanechol, are used to treat non-obstructive GI dysmotility, like post-op ileus, neurogenic ileus, and congenital megacolon
66
Q

At which end-organs are M3 ACh receptors found?

A
  • glands
  • the bladder
  • the smooth muscle of the eye
67
Q

______ can contract the smooth muscle of the bronchial tree, leading to symptoms of wheezing.

A

Muscarinic stimulants

68
Q

In acute glaucoma, pilocarpine can be used to treat because it activates the sphincter pupillae muscle to cause _____ and therefore relieves pressure.

A

myosis

69
Q

When ______ drugs activate muscarinic receptors, they mimic the effect of parasympathetic nerve discharge at end organs.

A

cholimomimetic

70
Q

What is pilocarpine? What is it used to treat?

A
  • a cholinomimetic used to treat:
    • dry mouth from:
      • Sjogrens
      • radiation damage
      • SEs from other meds
    • glaucoma
71
Q

What is carbachol? What is it used for?

A
  • a cholinomimetic used to treat acute angle-closure glaucoma (only)
72
Q

Activation of ____ receptors leads to the release of NO from vascular endothelial cells, which causes increased cGMP and therefore relaxation of the blood vessels.

A

M3

73
Q

What does activation of an M2 receptor in the heart cause?

A
  • decreased HR at the SA node
  • decreased contractility of the atria
  • decreased conduction velocity through the AV node
74
Q

Cue:

  • 3 dogs in the sidecars of the motorcycles parked in the M1 and M3 spaces
A
  • 3 dogs = 3 “dags” for DAG
  • M1 = M1 receptor; Gq
  • M3 = M3 receptor; Gq
  • *** M1 and M3 are coupled to Gq proteins which activate IP3-DAG cascade
75
Q

Cue:

  • Cement truck pouring cement out of a colonic-looking spot behind Beth the construction worker
A

Muscarinic agonists, like bethanechol, increase secretion and motor activity of the gut

76
Q

Name 2 ACh receptor subtypes.

A
  1. nicotinic
  2. muscarinic
77
Q

Muscarinic stimulants can contract the smooth muscle of the bronchial tree, leading to symptoms of ______.

A

wheezing

78
Q

Gq receptors activate the IP3/DAG cascade, which leads to increased _______.

A

intracellular Ca++

79
Q

___ receptor activation leads to the inhibition of cAMP production.

A

Gi

80
Q

Atherosclerosis eliminates M3 receptor activation and therefore causes ______.

A

vascular smooth muscle constriction

81
Q

In acute glaucoma, pilocarpine can be used to treat because it activates _______ to cause myosis and therefore relieves pressure.

A

the sphincter pupillae muscle

82
Q

Cue:

  • M1 motorcycle rider has a brain helmet
A
  • M1 = M1 receptor, Gs
  • brain helmet = found in CNS
83
Q

Name the receptor:

  • decreased HR at the SA
  • node decreased contractility of the atria
  • decreased conduction velocity through the AV node
A

M2 in the heart

84
Q

What is varenicline? What is it used for?

A
  • a cholinomimetic drug
    • a partial agonist at nicotinic receptors
  • smoking cessation
85
Q

Name 2 muscarinic agonists used to constrict the pupil and relieve intraocular pressure.

A
  1. Pilocarpine
  2. Carbachol

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