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Pharmacology > ANS Part 1: cholinergic > Flashcards

ANS Part 1: cholinergic Flashcards

1
Q

homeostasis is regulated by ____ nervous system

A

autonomic

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2
Q

what makes up the central nervous system

A
  • brainstem

- hypothalamus

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3
Q

what parts of the spinal cord are for sympathetic NS

A

thoracic and lumbar

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4
Q

what parts of the spinal cord are for parasympathetic NS

A

cranial (lower brainstem and medulla) and sacral

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5
Q

in the parasympathetic NS, the ganglia and post-ganglial fibers are ____ (close/far) to the organs innervated

A

close or within

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6
Q

sympathetic pre-ganglion and post-ganglion length

A
  • pre: short

- post: long

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7
Q

parasymp pre-ganglion and post-ganglion length

A
  • pre: long

- post: short

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8
Q

salivary composition for symp and parasymp

A
  • symp: high mucin

- parasymp: high water and electrolytes

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9
Q

all pre- and post- ganglia have Ach except for ___

A

sympathetic post-ganglion: uses NE

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10
Q

the NE released from symp post bind to ___ receptors

A

NE binds to adrenergic receptors

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11
Q

the Ach released from parasymp post bind to ___ receptors

A

Ach binds to muscarinic receptors

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12
Q

which NS innervates the adrenal medulla

A

sympathetic NS

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13
Q

what receptors are found on adrenal medulla

A

nicotinic

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14
Q

what does the adrenal medulla release

A

epinephrine

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15
Q

adrenergic agonists are called

A

sympathomimetics

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16
Q

cholinergic agonists are called

A

parasympathomimetics

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17
Q

adrenergic antagonists are called

A

sympatholytics

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18
Q

cholinergic antagonists are called

A

parasympatholytics

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19
Q

what is the target for direct-acting agonists/antagonists

A

receptors (either pre or post synaptic)

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20
Q

pre-synaptic receptors are excitatory or inhibitory or both

A

inhibitory only

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21
Q

4 things that indirect acting Ag and Antag target

A
  1. uptake or re-uptake mechanisms
  2. enzyme
  3. storage
  4. exocytosis
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22
Q

2 examples of indirect acting agents and their mechanism

A
  1. amphetamine (stim release of NE - exocytosis - indirect Ag)
  2. cocaine (prevent re-uptake of A/NA - indirect Ag)
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23
Q

what enzyme synthesizes Ach

A

CAT

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24
Q

what enzyme degrades Ach

A

acetylcholinesterase (AChE)

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25
Q

what is the rate-limiting step of Ach synthesis

A

availability of choline

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26
Q

choline transporter inhibition

A

hemicholinium

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27
Q

vesicular transport inhibition

A

vesamicol

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28
Q

2 examples of inhibitors for Ach exocytosis

A
  • botulinum toxin A

- tetanus toxin

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29
Q

example of stimulators for Ach exocytosis

A

black widow spider venom (alpha-latrotoxin)

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30
Q

reversible inhibitors for AchE

A
  • physostigmine
  • neostigmine
  • tacrine
  • edrophonium
  • rivastigmine
  • donepezil
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31
Q

irreversible inhibitors for AchE

A
  • organophosphates (eg. sarin and parathion)

- echothiophate

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32
Q

structure of nicotinic Ach receptor

A

ionotropic, pentameric

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33
Q

4 agonists for nicotinic Ach receptor

A
  1. nicotine
  2. lobeline
  3. Ach
  4. carbachol
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34
Q

antagonist for nicotinic Ach receptor

A

alpha-bungarotoxin

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35
Q

2 types of nicotinic Ach receptors

A
  • neuronal (Nn)

- muscular (Nm)

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36
Q

agonist for Neuronal nicotinic receptor (Nn)

A

dimethylphenyl piperazinium (DMPP)

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37
Q

3 antagonist for Neuronal nicotinic receptor (Nn)

A
  1. hexamethonium
  2. trimethaphan
  3. mecamylamine
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38
Q

agonist for muscular nicotinic receptor (Nm)

A

phenyltrimethylammonium (PMA)

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39
Q

antagonist for muscular nicotinic receptor (Nm)

A

curare (d-tubocurarine)

decamethonium

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40
Q

what subunits are sites in muscular nicotinic receptors

A

alpha-1 and beta-1 only!

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41
Q

4 changes that result from nicotine stimulation at ganglion

A
  • increase heart rate
  • increase blood pressure
  • increase GI activity
  • increase salivation
42
Q

4 changes that result from hexamethonium stimulation at ganglion

A
  • decrease heart rate
  • decrease blood pressure
  • decrease GI activity
  • decrease salivation
43
Q

drug that blocks nicotonic receptor on ganglion

A

trimethaphan camsylate (Arfonad)

44
Q

which subtypes of muscarinic Ach receptors are excitatory and inhibitory

A

M 1,3,5 - excitatory

M 2,4 - inhibitory

45
Q

what type of receptors are muscarinic Ach receptors

A

GPCR

46
Q

Agonist for non-selective muscarinic receptor

A
  • muscarine

- carbachol

47
Q

Antag for non-selective muscarinic receptor

A

ATROPINE! (causes mydriasis)

48
Q

which G protein is associated with M 1,3,5

A

Gq (increases IP3 and DAG)

49
Q

Ag M1 drugs and effect

A
  • muscarine and oxotremorine

- increase secretory glands

50
Q

Antag M1 drugs and effects

A
  • atropine and pirenxipine

- decrease gastric secretion

51
Q

Ag M3 drugs and effects

A

muscarine

-miosis (pupil constriction) and constriction of ciliary muscle, and increase secretory glands

52
Q

Antag M3 drugs and effects

A

atropine (mydriasis) and 4-DAMP

53
Q

Ag M5 drugs and effects

A

muscarine (endothelial cells => increase NO => vasodilation)

54
Q

Antag M5 drugs and effects

A

atropine

55
Q

2 selective antagonists on muscarinic receptors

A

pirenzipine and 4-DAMP

56
Q

muscarine and carbachol is used to treat ___

A

urinary retention and glaucoma

57
Q

which G proteins are involved in M2,4

A

G i/o, decreases adenylyl catalase and cAMP

58
Q

M2 antagonist

A

gallamine (selective antagonist)

59
Q

what does gallamine do

A

inhibits myocardium and smooth m

60
Q

M4 is found in

A

myenteric plexus

61
Q

what does atropine do (5 things)

A
  • increase cardiac inotropy and chronotropy
  • decrease GI motility
  • blurred vision
  • pupillary dilation (mydriasis)
  • hot and dry skin
62
Q

what is the endogenous ligand for direct-acting cholinergic Ag

A

acetylcholine

63
Q

pilocarpine has a higher affinity for which receptor

A

muscarinic

64
Q

what does pilocarpine do

A

increase salivation, flushing, blurred vision

65
Q

what is pilocarpine used to treat

A
  • xerostomia

- glaucoma

66
Q

what does carbachol do

A

miosis and decreases IOP

67
Q

what is carbachol used to treat

A
  • xerostomia

- pilocarpine-resistant glaucoma

68
Q

what class of drugs is used to treat xerostomia

A

sialagogues

69
Q

what are sialagogues

A

drugs that promote the secretion of saliva

70
Q

name 2 drugs used to treat xerostomia (2 sialagogues)

A
  • pilocarpine (salagen)

- cevimeline (evoxac)

71
Q

cevimeline (evoxac) has a high affinity for which receptor

A

muscarinic receptor

72
Q

what does cevimeline do

A

increase salivation

73
Q

hexamethonium is a nicotinic Antag at the ganglion. name 6 things that it does

A
  1. lower BP
  2. blood pools in extremities
  3. mydriasis
  4. lower GI mobility; constipation
  5. moderate bronchodilation
  6. hot and dry skin
74
Q

what can hexamethonium be used to treat

A

hypertension (rarely used)

75
Q

atropine is an anticholinergic drug. what are the side effects of atropine? (saying)

A
  • 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
Q

which has a longer half-life: hyoscine or atropine?

A

hyoscine

77
Q

what is hyoscine used to treat

A
  • antispasmodic GI and urinary smooth m

- prevent motion sickness

78
Q

name 3 synthetic muscarinic antag

A
  1. ipratropium bromide
  2. benzotropine
  3. darifenacine
79
Q

ipratropium bromide tx

A

COPD and asthma

80
Q

benzotropine tx

A

parkinson’s

81
Q

darifenacine tx

A

incontinence and overactive bladder

82
Q

homatropine hydrobromide: classification and tx

A
  • muscarinic antag

- tx: ophthalmic admin for eye exam

83
Q

homatropine butylbromide: classification and tx

A
  • muscarinic antag

- Tx: gi motility disorders

84
Q

which of the homatropine drugs can cross the BBB

A

homatropine hydrobromide

85
Q

indirect-acting drugs that inhibit AchE are considered Ag or Antag

A

AchE inhibitors are considered indirect-acting Ag

86
Q

what are the clinical signs of overdose/toxicity of AchE inhibitors

A 
Salivation
Lacrimation
Urination
Defecation
Gi upset
Emesis (vomiting)
-miosis
-resp/CV distress
87
Q

specific cholinesterase or neuronal cholinesterase

A

AchE

88
Q

non-specific or pseudo-cholinesterase

A

BchE

89
Q

short-acting carbamate derivative that reversibly inhibits AchE

A

edrophonium

90
Q

what two drugs are used to treat myasthenia gravis

A

edrophonium and neostigmine

91
Q

3 medium-acting carbamate derivative (AchE inhibitor)

A
  • physostigmine
  • neostigmine
  • rivastigmine
92
Q

medium-acting PIPERIDINE derivative (AchE inhibitor)

A

donepezil

93
Q

physostigmine Tx

A

glaucoma

94
Q

neostigmine tx

A

myasthenia gravis

95
Q

rivastigmine tx

A

alzheimer’s

96
Q

donepezil tx

A

alzheimer’s

97
Q

2 examples of organophosphates

A
  • sarin (nerve gas)

- parathion (insecticide)

98
Q

what is the antidote for organophosphate poisoning

A

pralidoxime (2-PAM)

99
Q

what are the two amino acid residues at the site on AchE

A

serine and histidine

100
Q

what is echothiophate (AchE irreversible inhibitor) used to treat

A

glaucoma

101
Q

how does the 2-PAM antidote work

A

reverses binding to enzyme and then binds to P on organophosphate which prevents binding to AchE

102
Q

what is the irreversible stage when organophosphates bind to AchE

A

aged phosphorylation

Pharmacology (17 decks)

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