ANS Part 1: cholinergic Flashcards
1
Q
homeostasis is regulated by ____ nervous system
A
autonomic
2
Q
what makes up the central nervous system
A
- brainstem
- hypothalamus
3
Q
what parts of the spinal cord are for sympathetic NS
A
thoracic and lumbar
4
Q
what parts of the spinal cord are for parasympathetic NS
A
cranial (lower brainstem and medulla) and sacral
5
Q
in the parasympathetic NS, the ganglia and post-ganglial fibers are ____ (close/far) to the organs innervated
A
close or within
6
Q
sympathetic pre-ganglion and post-ganglion length
A
- pre: short
- post: long
7
Q
parasymp pre-ganglion and post-ganglion length
A
- pre: long
- post: short
8
Q
salivary composition for symp and parasymp
A
- symp: high mucin
- parasymp: high water and electrolytes
9
Q
all pre- and post- ganglia have Ach except for ___
A
sympathetic post-ganglion: uses NE
10
Q
the NE released from symp post bind to ___ receptors
A
NE binds to adrenergic receptors
11
Q
the Ach released from parasymp post bind to ___ receptors
A
Ach binds to muscarinic receptors
12
Q
which NS innervates the adrenal medulla
A
sympathetic NS
13
Q
what receptors are found on adrenal medulla
A
nicotinic
14
Q
what does the adrenal medulla release
A
epinephrine
15
Q
adrenergic agonists are called
A
sympathomimetics
16
Q
cholinergic agonists are called
A
parasympathomimetics
17
Q
adrenergic antagonists are called
A
sympatholytics
18
Q
cholinergic antagonists are called
A
parasympatholytics
19
Q
what is the target for direct-acting agonists/antagonists
A
receptors (either pre or post synaptic)
20
Q
pre-synaptic receptors are excitatory or inhibitory or both
A
inhibitory only
21
Q
4 things that indirect acting Ag and Antag target
A
- uptake or re-uptake mechanisms
- enzyme
- storage
- exocytosis
22
Q
2 examples of indirect acting agents and their mechanism
A
- amphetamine (stim release of NE - exocytosis - indirect Ag)
- cocaine (prevent re-uptake of A/NA - indirect Ag)
23
Q
what enzyme synthesizes Ach
A
CAT
24
Q
what enzyme degrades Ach
A
acetylcholinesterase (AChE)
25
what is the rate-limiting step of Ach synthesis
availability of choline
26
choline transporter inhibition
hemicholinium
27
vesicular transport inhibition
vesamicol
28
2 examples of inhibitors for Ach exocytosis
- botulinum toxin A
| - tetanus toxin
29
example of stimulators for Ach exocytosis
black widow spider venom (alpha-latrotoxin)
30
reversible inhibitors for AchE
- physostigmine
- neostigmine
- tacrine
- edrophonium
- rivastigmine
- donepezil
31
irreversible inhibitors for AchE
- organophosphates (eg. sarin and parathion)
| - echothiophate
32
structure of nicotinic Ach receptor
ionotropic, pentameric
33
4 agonists for nicotinic Ach receptor
1. nicotine
2. lobeline
3. Ach
4. carbachol
34
antagonist for nicotinic Ach receptor
alpha-bungarotoxin
35
2 types of nicotinic Ach receptors
- neuronal (Nn)
| - muscular (Nm)
36
agonist for Neuronal nicotinic receptor (Nn)
dimethylphenyl piperazinium (DMPP)
37
3 antagonist for Neuronal nicotinic receptor (Nn)
1. hexamethonium
2. trimethaphan
3. mecamylamine
38
agonist for muscular nicotinic receptor (Nm)
phenyltrimethylammonium (PMA)
39
antagonist for muscular nicotinic receptor (Nm)
curare (d-tubocurarine)
| decamethonium
40
what subunits are sites in muscular nicotinic receptors
alpha-1 and beta-1 only!
41
4 changes that result from nicotine stimulation at ganglion
- increase heart rate
- increase blood pressure
- increase GI activity
- increase salivation
42
4 changes that result from hexamethonium stimulation at ganglion
- decrease heart rate
- decrease blood pressure
- decrease GI activity
- decrease salivation
43
drug that blocks nicotonic receptor on ganglion
trimethaphan camsylate (Arfonad)
44
which subtypes of muscarinic Ach receptors are excitatory and inhibitory
M 1,3,5 - excitatory
| M 2,4 - inhibitory
45
what type of receptors are muscarinic Ach receptors
GPCR
46
Agonist for non-selective muscarinic receptor
- muscarine
| - carbachol
47
Antag for non-selective muscarinic receptor
ATROPINE! (causes mydriasis)
48
which G protein is associated with M 1,3,5
Gq (increases IP3 and DAG)
49
Ag M1 drugs and effect
- muscarine and oxotremorine
| - increase secretory glands
50
Antag M1 drugs and effects
- atropine and pirenxipine
| - decrease gastric secretion
51
Ag M3 drugs and effects
muscarine
| -miosis (pupil constriction) and constriction of ciliary muscle, and increase secretory glands
52
Antag M3 drugs and effects
atropine (mydriasis) and 4-DAMP
53
Ag M5 drugs and effects
muscarine (endothelial cells => increase NO => vasodilation)
54
Antag M5 drugs and effects
atropine
55
2 selective antagonists on muscarinic receptors
pirenzipine and 4-DAMP
56
muscarine and carbachol is used to treat ___
urinary retention and glaucoma
57
which G proteins are involved in M2,4
G i/o, decreases adenylyl catalase and cAMP
58
M2 antagonist
gallamine (selective antagonist)
59
what does gallamine do
inhibits myocardium and smooth m
60
M4 is found in
myenteric plexus
61
what does atropine do (5 things)
- increase cardiac inotropy and chronotropy
- decrease GI motility
- blurred vision
- pupillary dilation (mydriasis)
- hot and dry skin
62
what is the endogenous ligand for direct-acting cholinergic Ag
acetylcholine
63
pilocarpine has a higher affinity for which receptor
muscarinic
64
what does pilocarpine do
increase salivation, flushing, blurred vision
65
what is pilocarpine used to treat
- xerostomia
| - glaucoma
66
what does carbachol do
miosis and decreases IOP
67
what is carbachol used to treat
- xerostomia
| - pilocarpine-resistant glaucoma
68
what class of drugs is used to treat xerostomia
sialagogues
69
what are sialagogues
drugs that promote the secretion of saliva
70
name 2 drugs used to treat xerostomia (2 sialagogues)
- pilocarpine (salagen)
| - cevimeline (evoxac)
71
cevimeline (evoxac) has a high affinity for which receptor
muscarinic receptor
72
what does cevimeline do
increase salivation
73
hexamethonium is a nicotinic Antag at the ganglion. name 6 things that it does
1. lower BP
2. blood pools in extremities
3. mydriasis
4. lower GI mobility; constipation
5. moderate bronchodilation
6. hot and dry skin
74
what can hexamethonium be used to treat
hypertension (rarely used)
75
atropine is an anticholinergic drug. what are the side effects of atropine? (saying)
- dry as a bone (dry skin)
- hot as a hare (hot skin)
- red as a beet (peripheral vasodilation)
- blind as a bat (mydriasis and blurred vision)
- mad as a hatter (disorientation, delirium)
76
which has a longer half-life: hyoscine or atropine?
hyoscine
77
what is hyoscine used to treat
- antispasmodic GI and urinary smooth m
| - prevent motion sickness
78
name 3 synthetic muscarinic antag
1. ipratropium bromide
2. benzotropine
3. darifenacine
79
ipratropium bromide tx
COPD and asthma
80
benzotropine tx
parkinson's
81
darifenacine tx
incontinence and overactive bladder
82
homatropine hydrobromide: classification and tx
- muscarinic antag
| - tx: ophthalmic admin for eye exam
83
homatropine butylbromide: classification and tx
- muscarinic antag
| - Tx: gi motility disorders
84
which of the homatropine drugs can cross the BBB
homatropine hydrobromide
85
indirect-acting drugs that inhibit AchE are considered Ag or Antag
AchE inhibitors are considered indirect-acting Ag
86
what are the clinical signs of overdose/toxicity of AchE inhibitors
```
Salivation
Lacrimation
Urination
Defecation
Gi upset
Emesis (vomiting)
-miosis
-resp/CV distress
```
87
specific cholinesterase or neuronal cholinesterase
AchE
88
non-specific or pseudo-cholinesterase
BchE
89
short-acting carbamate derivative that reversibly inhibits AchE
edrophonium
90
what two drugs are used to treat myasthenia gravis
edrophonium and neostigmine
91
3 medium-acting carbamate derivative (AchE inhibitor)
- physostigmine
- neostigmine
- rivastigmine
92
medium-acting PIPERIDINE derivative (AchE inhibitor)
donepezil
93
physostigmine Tx
glaucoma
94
neostigmine tx
myasthenia gravis
95
rivastigmine tx
alzheimer's
96
donepezil tx
alzheimer's
97
2 examples of organophosphates
- sarin (nerve gas)
| - parathion (insecticide)
98
what is the antidote for organophosphate poisoning
pralidoxime (2-PAM)
99
what are the two amino acid residues at the site on AchE
serine and histidine
100
what is echothiophate (AchE irreversible inhibitor) used to treat
glaucoma
101
how does the 2-PAM antidote work
reverses binding to enzyme and then binds to P on organophosphate which prevents binding to AchE
102
what is the irreversible stage when organophosphates bind to AchE
aged phosphorylation
