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Pharmacology I > Autonomic System and Cholinergic Transmission > Flashcards

Autonomic System and Cholinergic Transmission Flashcards

1
Q

Describe the autonomic nervous system, the divisions and the function

A
  • involuntary
  • sympathetic and parasympathetic
  • handles visceral functions
  • 2 neurons in series: pre and post ganglionic
  • all preganglionic fibers release Ach
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2
Q

describe the sympathetic nervous systm

A
  • fight or flight
  • runs on norepinephrine
  • increases CO, BP, RR, blood flow and BG
  • decreases RBF, digestive process
  • fires at once
  • short pre and lost post
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3
Q

describe parasympathetic nervous system

A
  • normal maintenance and anabolic metabolism
  • incremental activation
  • vagal stimulation
  • long pre and short post
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4
Q

describe the somatic nervous system and its function

A
  • voluntary
  • controls movement, respiration and posture
  • always excitatory
  • no ganglia
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5
Q

describe cholinergic fibers and what they do

A
  • synthesize and release Ach
  • all preganglionic efferent and somatic motor fibers to skeletal muscle
  • most parasympathetic postganglionic fibers
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6
Q

what do adrenergic fibers do and what fibers are these

A
  • release NE
  • most sympathetic postganglionic fibers
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7
Q

what NT is released in the somatic nervous system and what is the effector organ and effect

A
  • Ach
  • skeletal muscle
  • stimulatory
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8
Q

what NT is released in sympathetic nervous system

A

NE

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9
Q

what NT is released in parasympathetic nervous system

A

Ach

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10
Q

what is the difference between a neurotransmitter and a neurohormone

A

a NT is released at the effector organ. a neurohormone is released into the blood that is then carrier to the effector organ

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11
Q

what is an example of a neurohormone in the sympathetic nervous system

A

the adrenal medulla releasing epi and NE into blood stresm

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12
Q

the effect from the autonomic nervous system depends on:

A

NT and receptors on effector organs

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13
Q

what are the steps to cholinergic transmission

A
  • acetyl CoA + choline = ACh
  • transported to cytoplasm, prepped for release
  • calcium triggers release of Ach
  • Ach binds to cholinergic receptor
  • acetylcholinesterase degrades Ach into choline and acetate
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14
Q

what is the mechanism of adrenergic transmission

A

tyrosine gets converted to dopamine which gets converted to NE
- calcium induces NE release

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15
Q

does NE get broken down by acetylcholinesterase

A

no

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16
Q

what are the autonomic receptors

A

-cholinergic receptors
- adrenergic receptors

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17
Q

what are the cholinergic receptors

A
  • nicotinic (ganglionic)
  • muscarinic
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18
Q

what are the adrenergic receptors

A

-alpha
- beta
- dopamine

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19
Q

what are the 3 main classes of nicotinic receptors

A
  • muscle
  • ganglionic
  • CNS
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20
Q

what is the effect of nicotinic receptors

A

excitatory

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21
Q

what is the mechanism of action in nicotinic receptors

A

sodium influx causes activation

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22
Q

what are the muscarinic receptors and what do each do

A
  • M1- neural: CNS excitation, gastric secretion
  • M2- atrial: cardiac and neural inhibition, decrease in HR and inotropy
  • M3: glandular/smooth muscle: increased gastric acid, salivary secretion, GI contraction, ocular accomodation, vasodilation
    -M4 and M5- CNS
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23
Q

which division of the autonomic nervous system causes pupil dilation (mydriasis)

A

sympathetic

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24
Q

what is another name for cholinergics

A

muscarinic agonists

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25
describe cholinergic drugs and the 2 types
- parasympathomimetic - direct acting: binds directly to nicotinic Ach receptor and muscarinic receptor - indirect acting: inhibits acetylcholinesterase. amplifiers of endogenous Ach
26
what are the direct acting cholinergics
- pilocarpine (salagen) - bethanechol (urecholine) - cevimiline (evoxac)
27
what does pilocarpine (salagen) do
- glaucoma tx - causes miosis, lowers IOP - dental use- radiation induced xerostomia
28
what is bethanechol (urecholine) used for
post operative urinary retention - used in sx to decrease secretions for a clear field
29
which direct acting cholinergic is most resistant to cholinesterase
bethanechol (urecholine)
30
what is cevimiline (evoxac)
- selective for M3 - more selective for exocrine glands - chronic dry mouth use - radiation induced xerostomia; sjogrens syndrom
31
what are the indirect acting cholinergics
- acetylcholinesterase inhibitors - reversible: stigmine agents, donepezil (aricept), galantamine (razadyne) - irreversible: organophosphates
32
indirect acting cholinergics used for the treatment of:
- myasthenia gravis - glaucoma - GI motility - reversal of neuromuscular blockade -anticholinergic toxicity - alzheimers
33
what are the reversible ACHE inhibitors
- pyridostigmine (Regonol) - neostigmine (Prostigmin) - physostigmine (antilirium) - edrophonium (tensilon) - galantamine, rivastigmine, donepezil
34
what are the indications for and the duration of pyridostigmine
- myasthenia gravis- 1st line - nerve agent prophylaxis - 4-6h duration
35
what are the indications for neostigmine and what type of amine is it
- myasthenia gravis - post op ileus/urinary retention - neuromuscular blockade reversal - quaternary amine
36
what are the indications for physostigmine, what type of amine is it and why isnt it routinely used
- anticholinergic activity - tertiary amine - not used due to CNS activity
37
what is the indication for edrophonium, what type of amine is it and why isnt it routinely used
- diagnosis of myasthenia gravis - quaternary amine - not used for tx because short half life of 5 minutes
38
what is the indication for galantamine, rivastigmine, and donepezil
- mild to moderate alzheimers disease - more selective ACHe for management of cognitive dysfunction - modest clinical benefits
39
describe organophosphates and the kinds
- irreversible Ache - long lasting - insecticides: parathion, malathion - nerve agents: sarin, soman tabun, VX - Novichok agents
40
what is the mechanism of ACHe
breaks down acetylcholine and binds at the esteric site - phosphorus binds irreversible to serine at the esteric site - OP attached to ACHe preventing Ach binding
41
when cholinesterase is blocked by organophosphates what 3 things can happen
- hydrolyze to original state (slow) - regenerate with an oxime (fast) - age (cannot regenerate)
42
what are the muscarinic symptoms using the acronym SLUDGE in cholinergic toxicity
- Salivation - Lacrimation -Urination - Diarrhea - GI discomfort - Emesis
43
what are the muscarinic symptoms using the acronym DUMBBELS for cholinergic toxicity
- Diarrhea - Urination - Miosis/muscles wek -Bronchorrhea -Bradycardia -Emesis -Lacrimation -Salivation/Sweating
44
what are the nicotinic symptoms of cholinergic toxicity
- Muscle cramps -Tachycardia -Weakness -Twitching -Fasciculations
45
what is the synonym and aging half life for sarin
- GB - 5 hours
46
what is the synonym and aging half life for soman
- GD - 2 minutes
47
what is the synonym and aging half life for tabun
- GA - more than 40 hours
48
what is the synonym and aging half life for VX
- none - over 40 hours
49
what can you adminster in cholinergic toxicity and what does each do
- pralidoxime (2-pam): regenerates ACHE - atropine: muscarinic antagonism only, wont correct nicotinic symptoms like paralysis - pyridostigmine: prophylaxis only
50
what is the problem with atropine
it requires a really large dose
51
what is another name for anticholinergics
muscarinic antagonists
52
what do anticholinergics do
binds muscarinic receptors, blocks Ach
53
what are the types of anticholinergics and what does each do
- tertiary amines: have central effects and get into CNS easier - quaternary amines: peripheral effects
54
what drugs are examples of tertiary amines
- atropine - scopolamine, benzotropine, dicyclomine
55
what drugs are examples of quaternary amines
- glycopyrrolate -titotropium
56
describe atropine
- prototypical anticholinergic - muscarinic selectivity - no effect on S/P heart transplant
57
what are the indications for atropine
- bradycardia - OP toxicity
58
what is the minimum dose of atropine and why
0.5mg because it can cause paradoxical bradycardia
59
what is atropine derived from
jimson weed and deadly nightshade
60
what is the mechanism of atropine
- binds M2 receptor and blocks AcH so it reduces ACH effect on the heart thus increasing HR
61
where is scopolamine found, what type of amine it is and what are its indications
- found in hyoscyamus niger (henbane) - tertiary amine - uses: motion sickness and voodoo zombification - blocks short term memory
62
what type of amine is glycopyrrolate and what is it used for
- quaternary amine, fewer central effects - used to dry secretions in surgery and ketamine treatment - adjunct for reversal of neuromuscular blockers
63
what are the uses of anticholinergic drugs
- opthalmology: mydriasis, cycloplegia, increased IOP - GI/GU: antispasmodic, antidiarrheal, urinary incontinence - cardiovascular: vagolytic ( increases HR) - secretions: decreases all, surgery and dental use - antidote: reversal of cholinergic toxicity in OP poisoning - pulmonary: COPD/ asthma treatment (bronchodilation)
64
what are the anticholinergic effects
- CNS: drowsiness, amnesia, agitation, hallucinations, coma. scopolamine > atropine - Eye: mydriasis, cycloplegia, reduced lacrimal secretion - CV: tachycardia (vagal inhibition) - respiratory: bronchodilation, reduced airway secretions - GI: decreased motility, xerostomia
65
what is another name for nicotinic drugs
ganglion stimulating drugs
66
what are the effects of too much nicotine
- seizure - respiratory arrest - coma - paralysis
67
how much nicotine can be fatal
1 drop of pure liquid = 40mg
68
what type of drug is varenicline (chantix)
a nicotinic drug
69
describe varenicline
- partial agonist/antagonist -long half life and high affinity for nicotinic acetylcholine receptors - inhibits nicotine binding, withdrawal symptoms and dopamine release
70
what are the two types of neuromuscular blockers
- depolarizing - nondepolarizing
71
what are the depolarizing neuromuscular blockers
succinylcholine
72
what are the nondepolarzing neuromuscular blockers
- rocuronium - vecuronium - pancuronium - cisatricurium
73
what do neuromuscular blockers do
inhibit binding of ACH at NMJ
74
what does succinylcholine do, what is the onset, duration and dose
- opens sodium channels - onset of 60 seconds - duration of 5 minutes - 1.5mg/KG IV - give more is hypotensive
75
what is the caution with succinylcholine
- hyperkalemia - denervation supersensitivity
76
what happens in denervation supersensitivity
- potassium increase of 5-10 mEq/L - takes 3-5 days
77
what does rocuronium do, what is the onset, duration and dose
- nondepolarizing - reversal agent with no ADR - onset 60 seconds - duration 45 minutes - 0.6-1.2MG/KG
78
which nondepolarizing NMDs are not frequently used and why
- vecuronium, pancuronium and cisatracurium because they have slow onset
79
what can pancuronium cause
tachycardia
80
what is cisatracurium used for
therapeutic temperature management
81
what is rocuronium used for
- excellent intubating conditions
82

Pharmacology I (12 decks)

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