Autonomic Drugs: Ch. 1.1: Cholinomimetics Flashcards
1
Q
At which end-organs are M1 ACh receptors found?
A
the CNS
2
Q
Muscarinic agonists reduce intraocular pressure by causing contraction of the ciliary body, facilitating _____.
A
the outflow of aqueous humor
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
4
Q
When cholimomimetic drugs activate muscarinic receptors, they mimic the effect of _____ at end organs.
A
parasympathetic nerve discharge
5
Q
What is methacholine? What is it used to treat?
A
- a cholinomimetic
- used for asthma/pulmonary testing
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
7
Q
Muscarinic agonists reduce intraocular pressure by causing ______, facilitating the outflow of aqueous humor.
A
contraction of the ciliary body
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
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
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
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
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
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
14
Q
Muscarinic receptors are coupled to ______ that function as transducers.
A
G proteins
15
Q
____ increase the secretory and motor activity of the gut.
A
Muscarinic agonists
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
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
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
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
20
Q
Intravascular injection of ______ produce marked vasodilation.
A
muscarinic agonists
21
Q
What does ‘cholinomimetic’ mean?
A
- it mimics or modifies the affect of ACh
- aka ACh receptor agonists
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
23
Q
A _____ instigates asthma for pulmonary testing.
A
methacholine challenge
24
Q
At which end-organs are M2 ACh receptors found?
A
the heart
25
Gq receptors activate the _____ cascade, which leads to increased intracellular Ca++.
IP3/DAG
26
Cue:
* "Enjoy Acetyl-Cola" sign with a mime on it
* these drugs are ACh receptor agonists aka cholinomimetics
* mime = cholino**mime**tic
27
* M1 = G\_\_
* M2 = G\_\_\_
* M3 = G\_\_\_
* M1 = Gq
* M2 = Gi
* M3 = Gq
28
What is the major NT of the PNS?
ACh
29
Muscarinic stimulants can contract the \_\_\_\_\_\_, leading to symptoms of wheezing.
smooth muscle of the bronchial tree
30
What is Carbachol? What is it used to treat?
* a cholinomimetic
* used to treat acute angle-closure glaucoma
31
When cholimomimetic drugs activate ______ receptors, they mimic the effect of parasympathetic nerve discharge at end organs.
muscarinic
32
Where are nicotinic receptors found?
* on autonomic ganglia
* at skeletal neuromuscular junctions
* in the adrenal gland
33
In acute glaucoma, ______ can be used to treat because it activates the sphincter pupillae muscle to cause myosis and therefore relieves pressure.
pilocarpine
34
This a cholinomimetic used to treat:
* dry mouth from:
* Sjogrens
* radiation damage
* SEs from other meds
* glaucoma
Pilocarpine
35
Cue:
* a smoker near some ganglia-like transformers on a telephone pole
* smoker = nicotinic ACh receptors
* transformers = ganglia
* \*\*\* nicotinic ACh receptors are found on autonomic ganglia
36
\_\_\_\_\_\_\_ reduce intraocular pressure by causing contraction of the ciliary body, facilitating the outflow of aqueous humor.
Muscarinic agonists
37
Activation of M3 receptors leads to the release of NO from vascular endothelial cells, which causes increased cGMP and therefore ______ of the blood vessels.
relaxation
38
This drug is a partial agonist at nicotinic receptors, and as such, is used to treat smoking cessation.
varenicline
39
Cue:
* M3 motorcycle has a clogged, constricted exhaust pipe
* clogged, constricted pipe = atherosclerosis
* \*\*\* atherosclerosis --\> vascular epithelial cell damage --\> direct muscarinic receptor activation --\> vasoconstriction
40
Cue:
* man running thru the "Para-City Marathon Challenge" finish line as he drinks an Acetyl-Cola
* marathon = methacholine
* challenge = methacholine challenge = asthma testing
* Acetyl-Cola = a cholinomimetic
41
Muscarinic agonists increase the ______ and _____ of the gut.
secretory and motor activity
42
Muscarinic agonists reduce ______ by causing contraction of the ciliary body, facilitating the outflow of aqueous humor.
intraocular pressure
43
This is a cholinomimetic used to treat acute angle-closure glaucoma (only).
Carbachol
44
\_\_\_\_\_\_ eliminates M3 receptor activation and therefore causes vascular smooth muscle constriction.
Atherosclerosis
45
What is Bethanechol? What is it used to treat?
* 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
Carbachol is a ______ agonist.
nicotinic AND muscarinic
47
Name 5 cholinomimetics and which receptor they act upon.
1. bethanicol (muscarinic)
2. pilocarpine (muscarinic)
3. methacholine (muscarinic)
4. carbachol (both nicotinic AND muscarinic)
5. varenicline (nicotinic)
48
\_\_\_\_\_ receptors are transmembrane polypeptides that act as ion channels.
Nicotinic
49
Intravascular injection of muscarinic agonists produces \_\_\_\_\_\_.
marked vasodilation
50
Cue:
* fisherman with his hoodie pulled tightly around his head
* constricted hood = pupillary constriction
* \*\*\* Pilocarpine activates the sphincter pupillae muscle to cause pupillary construction (useful in acute angle-closure glaucoma).
51
Nicotinic receptors are ______ that act as ion channels.
transmembrane polypeptides
52
Cue:
* Beth the construction worker, drinking an Acetyl Cola, holding a bladder hose, standing next to a cement truck pouring cement
* Beth = Bethanechol
* Acetyl Cola = it's a cholimomimetic
* cement truck = GI motility
* bladder hose = tx for urinary retention
53
\_\_\_\_\_\_ receptors are coupled to G proteins that function as transducers.
Muscarinic
54
Atherosclerosis eliminates ____ receptor activation and therefore causes vascular smooth muscle constriction.
M3
55
Because muscarinic agonists stimulate _____ and relax \_\_\_\_\_, bethanechol can be used to treat non-obstructive urinary obstruction.
* stimulate the detrusor muscle
* relax the bladder sphincter muscles
56
Because muscarinic agonists stimulate the detrusor muscle and relax the bladder sphincter muscles, bethanechol can be used to treat \_\_\_\_\_\_.
non-obstructive urinary obstruction
57
Gi receptor activation leads to the ______ .
inhibition of cAMP production
58
What 3 pathologies can cholinomimetic exacerbate?
1. COPD
2. asthma
3. peptic ulcer disease
59
Cue:
* a pile o' carp with dripping mouths being dumped from a net with round glass floats on it held by a crane
* 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
\_\_\_\_\_ receptors activate the IP3/DAG cascade, which leads to increased intracellular Ca++.
Gq
61
Cue:
* an electrical outlet near the smoker
* outlet = motor end plate
* smoker = nicotinic receptor
* \*\*\* nicotinic ACh receptors are found on skeletal muscle motor end plates (neuromuscular junction)
62
Cue:
* "Ion Channel News" on TVs behind the smoker
Nicotinic receptors act as ion channels
63
This is a cholinomimetic used for asthma/pulmonary testing.
methacholine
64
Cue:
* motorcycle in the M2 parking space with a packed-up tent
* M2 = M2 receptor; Gi
* packed tent = inhibited cAMP
65
Cue:
* Construction sign says "Do not obstruct"
* Muscarinic agonists, like bethanechol, are used to treat non-obstructive GI dysmotility, like post-op ileus, neurogenic ileus, and congenital megacolon
66
At which end-organs are M3 ACh receptors found?
* glands
* the bladder
* the smooth muscle of the eye
67
\_\_\_\_\_\_ can contract the smooth muscle of the bronchial tree, leading to symptoms of wheezing.
Muscarinic stimulants
68
In acute glaucoma, pilocarpine can be used to treat because it activates the sphincter pupillae muscle to cause _____ and therefore relieves pressure.
myosis
69
When ______ drugs activate muscarinic receptors, they mimic the effect of parasympathetic nerve discharge at end organs.
cholimomimetic
70
What is pilocarpine? What is it used to treat?
* a cholinomimetic used to treat:
* dry mouth from:
* Sjogrens
* radiation damage
* SEs from other meds
* glaucoma
71
What is carbachol? What is it used for?
* a cholinomimetic used to treat acute angle-closure glaucoma (only)
72
Activation of ____ receptors leads to the release of NO from vascular endothelial cells, which causes increased cGMP and therefore relaxation of the blood vessels.
M3
73
What does activation of an M2 receptor in the heart cause?
* decreased HR at the SA node
* decreased contractility of the atria
* decreased conduction velocity through the AV node
74
Cue:
* 3 dogs in the sidecars of the motorcycles parked in the M1 and M3 spaces
* 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
Cue:
* Cement truck pouring cement out of a colonic-looking spot behind Beth the construction worker
Muscarinic agonists, like bethanechol, increase secretion and motor activity of the gut
76
Name 2 ACh receptor subtypes.
1. nicotinic
2. muscarinic
77
Muscarinic stimulants can contract the smooth muscle of the bronchial tree, leading to symptoms of \_\_\_\_\_\_.
wheezing
78
Gq receptors activate the IP3/DAG cascade, which leads to increased \_\_\_\_\_\_\_.
intracellular Ca++
79
\_\_\_ receptor activation leads to the inhibition of cAMP production.
Gi
80
Atherosclerosis eliminates M3 receptor activation and therefore causes \_\_\_\_\_\_.
vascular smooth muscle constriction
81
In acute glaucoma, pilocarpine can be used to treat because it activates _______ to cause myosis and therefore relieves pressure.
the sphincter pupillae muscle
82
Cue:
* M1 motorcycle rider has a brain helmet
* M1 = M1 receptor, Gs
* brain helmet = found in CNS
83
Name the receptor:
* decreased HR at the SA
* node decreased contractility of the atria
* decreased conduction velocity through the AV node
M2 in the heart
84
What is varenicline? What is it used for?
* a cholinomimetic drug
* a partial agonist at nicotinic receptors
* smoking cessation
85
Name 2 muscarinic agonists used to constrict the pupil and relieve intraocular pressure.
1. Pilocarpine
2. Carbachol
