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Autonomic Nervous System / Cholinergic Transmission Flashcards

1
Q

What are the featurse of the autonomic nervous system?

A
  • involuntary
  • sympathic and parasympathetic
  • handles visceral functions
  • 2 neurons in series (pre and post ganglionic)
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2
Q

All preganglionic fibers of the autonomic nervous system release…

A

ACh

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3
Q

What are the functions of the sympathic nervous system?

A
  • fight or flight
  • runs on norepinerphrine
  • increases CO, BP, RR, Blood Flow, BG
  • decreases RBF, digestive processes
  • fires at once
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4
Q

In the sympathic nervous system, there is ______ preganglions and _______ postganglions

A

short
long

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5
Q

What are the functions of the parasympathic nervous system?

A
  • normal maintenance and anabolic metabolism
  • incremental activation
  • vagal stimulation
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6
Q

In the sympathic nervous system, there is ______ preganglions and _______ postganglions

A

long
short

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7
Q

What are the functions of the somatic nervous system?

A
  • voluntary
  • controls movement, respiration, and posture
  • always excitatory
  • no ganglia
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8
Q

What do cholinergic fibers release?

A

ACh

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9
Q

All preganglionic efferent and somatic motor fibers to skeletal muscle are ____________________ fibers

A

cholinergic

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10
Q

Most parasympathetic postganglionic fibers are…

A

cholinergic

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11
Q

Adrenergic fibers release…

A

norepinephrine

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12
Q

Most sympathetic post ganglionic fibers are…

A

adrenergic

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13
Q

What are the steps of cholinergic transmission?

A
  • Acetyl CoA + choline = ACh
  • Transported to cytoplasm, prepped for release
  • Calcium triggers release
  • Binds to cholinergic receptor
  • Acetylcholinesterase breaks up the party: choline + acetate
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14
Q

What are the types of autonomic receptors?

A

Cholinergic receptors
Nicotinic (ganglionic)
Muscarinic
Adrenergic receptors
Alpha
Beta
Dopamine

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15
Q

What are the three main classes of nicotinic receptors?

A
  • muscle
  • ganglionic
  • CNS
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16
Q

Are nicotinic receptors excitatory or inhibitory?

A

excitatory

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17
Q

What are the types of muscarinic receptors?

A
  • M1: neural
  • M2: atrial
  • M3: glandular/smooth muscle
  • M4 and M4: CNS
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18
Q

What is the function of M1 receptors?

A

Neural
- CNS excitation, gastric secretion

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19
Q

What is the function of M2 receptors?

A

Atrial
- cardiac and neural inhibition

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20
Q

What is the function of M3 receptors?

A

Glandular/Smooth Muscle
- gastric acid, salivary secretions, GI contraction, ocular accommodation, vasodilation

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21
Q

What are the types of adrenergic receptors and where are they located?

A
  • Α1, Α2
  • Β1, Β2, Β3
  • DOPAMINE
  • post-ganglionic sympathetic system only
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22
Q

What is another name fo muscarinic agonists?

A

cholinergics

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23
Q

What is the main function of cholinergic drugs?

A

parasympathomimetic

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24
Q

What are the types of cholinergic drugs?

A
  • direct acting
    — binds directly to NACH(OS) and MACH(OS)
  • indirect acting
    — inhibits acetylcholinesterase
    — amplifiers of endogenous ACh
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25
What are the examples of direct acting cholinergics?
- Pilocarpine (salagen) - Bethanechol (urecholine) - Cevimiline (evoxac)
26
# direct acting cholinergic What is the function of pilocarpine (salagen)?
- glaucoma TX - causes mitosis, lowers IOP - dental use - radiation-induced **xerostomia**
27
# direct acting cholinergic What is the function of bethanechol (urecholine)?
- post-operative urinary retention - most resistant to cholinersterase
28
# direct acting cholinergic What is the function of cevimiline (evoxac)?
- selective for **M3** - more selective for exocrine glands - radiation-induced **xerostomia** - **sjogren's syndrome**
29
What are the types of indirect acting cholinergic drugs?
- reversible --- stigmine agents, donepezil (aricept), galantamine (razadyne) - irreversible --- organophosphates
30
What is the main function of indirect acting cholinergic drugs?
acetylcholinesterase inhibitors
31
Indirect acting cholinergics are used for treatment of...
- myasthenia gravis - glaucoma - GI motility - reversal of neuromuscular blockade - anticholinergic toxicity - alzheimers
32
What are the different types of reversible ACHE inhibitors?
- Pyridostigmine (Regonol®) - Neostigmine (Prostigmin®) - Physostigmine (Antilirium®) - Edrophonium (Tensilon®) - Galantamine, rivastigmine, donepezil
33
Pyridostigmine (Regonol®) is used for...
*Myasthenia gravis *Nerve agent prophylaxis | 1st line for MG
34
Neostigmine (Prostigmin®) is used for...
*Myasthenia gravis *Post-op ileus / urinary retention *Neuromuscular blockade reversal | Doesn’t enter CNS (quaternary amine)
35
Physostigmine (Antilirium®) is used for...
*Anticholinergic toxicity | Enters CNS (tertiary amine); not routinely used
36
Edrophonium (Tensilon®) is used for...
*Diagnosis of myasthenia gravis | Doesn’t enter CNS (quaternary amine); Not routinely used
37
Galantamine, rivastigmine, donepezil is used for...
*Mild-to-moderate Alzheimer’s disease
38
What are the featurs of organophosphates?
- Irreversible AChE - Long lasting | bad!
39
What are examples of organophosphates?
- Insecticides --- Parathion, malathion - Nerve agents ---Sarin, soman, tabun, VX - Novichok Agents
40
What is the mechanism behind organophosphates?
- Phosphorous (+) attracted to serine (-) - OP attaches to AChE, prevents ACh binding - Cholinesterase is now blocked - AChE is now permanently out of commission (unless hydrolyzed or regenerated)
41
When an organophosphate blocks cholinesterase what happens?
1 of 3 things... 1. Hydrolyze to original state (slow) 2. Regenerate with an oxime (fast) 3. Age (cannot regenerate)
42
What are the muscarinic symptoms of cholinergic toxicity?
Salivation Lacrimation Urination Diarrhea GI discomfort Emesis Miosis/muscles weak Bronchorrhea Bradycardia Salivation/sweating
43
What are the nicotinic symptoms of cholinergic toxicity?
Muscle cramps Tachycardia Weakness Twitching Fasciculations
44
How much time do you have to be treated after exposure to nerve agents (organophosphates)?
Depends but anywhere from 2 minutes to 40 hours
45
What drugs can you treat an exposure to organophosphates?
- Pralidoxime (2-PAM; regenerates AChE) - Atrophine (muscarinic only; requires huge amounts) - Pyridostigmine (prophylaxis only)
46
What is another word for muscarinic antagonists?
anticholinergics
47
What is the function of anticholinergics?
binds muscarinic receptors, blocks ACh
48
What are the types of anticholinergics?
- tertiary amines (central effects) --- atrophine, scopolamine (scopace), benztropine (cogentin), dicyclomine (bentyl) - quaternary amines (peripheral effects) --- glycopyrrolate (robinul), tiotropium (spiriva)
49
What are the uses of atropine? | prototypical anticholinergic
- muscarinic selectivity - No effect S/P heart transplant - Indictions --- bradycardia --- OP toxicity
50
Why should you not used <0.5 mg of atropine in adults?
paradoxical bradycardia
51
# anticholinergic What are the uses of scopolamine?
- found in hyoscyamus niger (henbane) - teritary amine - use in --- motion sickness --- voodoo zombification
52
# anticholinergic What are the uses of glycopyrrolate?
- used to dry secretions --- surgery --- ketamine treatment - adjunct for reversal of neuromucsular blockers | quaternary amine; fever central effects
53
What negative effects do anticholinergics have on the CNS?
Drowsiness, amnesia, agitation, hallucinations, coma
53
What are the many uses for anticholinergics?
- ophthalmology --- mydriasis, cycloplegia, increased IOP - GI/GU --- antispasmodic, antidiarrheal, urinary incontinence - Cardio --- vagolytic (increase heart rate) - Secretions --- decrease all - Antidote --- reversal of cholinergic toxicity (organophosphates) - Pulomonary --- COPD, Asthma
54
What negative effects do anticholinergics have on the eyes?
Mydriasis, cycloplegia, reduced lacrimal secretion
55
What negative effects do anticholinergics have on the CV system?
Tachycardia (vagal inhibition)
56
What negative effects do anticholinergics have on the respiratory system?
Bronchodilation, reduced airway secretions
57
What negative effects do anticholinergics have on the GI system?
Decreased motility, xerostomia
58
What is another name for ganglion stimulating drugs?
nicotinic drugs
59
What is an example of a nicotinic drug?
varenicline (chantix)
60
# nicotinic drug What are the functions of varenicline (chantix)?
- inhibits --- nicotine binding --- withdrawal symptoms --- dopamine release - partial agonist/antagnoist - long half-life and high affinity for NACH(OS)
61
What are the depolarizing neuromuscular blockers?
succinylcholine
62
What are the polarizing neuromuscular blockers?
- rocuronium - vecuronium - pancuronium (causes tachycardia) - cisatricurium
63
What is the function of a neuromuscular blocker?
- inhibit binding of ACh and NMJ
64
# depolarizing neuromuscular blocker What is the use of succinylcholine?
- open sodium channels - onset = 60 seconds - duration = 5 minutes - 1.5 mg/kg IV
65
Why do you need to be careful with succinylcholine?
hyperkalemia - denervation supersensitivity
66
# polarizing neuromuscular blocker What is the use of rocuronium?
- no significatn ADR - reversal agent - onset = 60 seconds - duration = 45 minutes - 0.6-1.2 mg/kg

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