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Block 3 Pharm > cholinergic neurons > Flashcards

cholinergic neurons Flashcards

1
Q

Acetylcholine (ACh) is a common ____

A

neurotransmitter

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2
Q

_____neurons are those that utilize ACh

A

Cholinergic

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3
Q

Neurotransmission Six sequential steps:

A 
Synthesis
Storage
Release
Binding of ACh to receptor
Degradation in synaptic cleft
Recycling of choline and acetate
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4
Q

Black widow spider venom causes all ACh stored in synaptic vesicles to ____

A

empty

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5
Q

ACh ____ inhibitors will block the degradation and increase time ACh is acting on postsynaptic receptors

A

esterase

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6
Q

______ toxin blocks release of vesicle content (ACh)

A

Botulinum

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7
Q

Two families distinguished on basis of their different affinities for agents that mimic the action of ACh (parasympathomimetics):
what are they?

A

Nicotinic

Muscarinic

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8
Q

this cholinergic receptor is ligand-gated ion channels whose activation causes a rapid (millisecond) increase in cellular permeability to Na+ and Ca++, depolarization, and excitation

A

Nicotinic

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9
Q

this cholinergic receptor is GPCRs with slower (still few seconds to minutes) responses

A

Muscarinic

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10
Q

muscarinic receptors may be either excitatory or inhibitory, and they are not necessarily linked to changes in _____

A

ion permeability

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11
Q

muscarinic receptors are Located primarily (but not exclusively) at the ________ of the parasympathetic nervous system

A

neuroeffector junction

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12
Q

muscarinic receptors: Five subclasses: M1-5 but only 3 have been functionally characterized
what are first three?

A

M1: gastric parietal cells
M2: cardiac cells and smooth muscle
M3: bladder, exocrine glands, smooth muscle

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13
Q

for muscarinic receptors what do you need to recognize to identify it

A

Recognize muscarine (alkaloid present in certain poisonous mushrooms)

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14
Q

for nicotinic receptors what do you need to recognize to identify it

A

Recognize nicotine

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15
Q

Nicotine at ____stimulates

A

[low]

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16
Q

Nicotine at _____ inhibits

A

[high]

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17
Q

Nicotine at [low] stimulates and at [high] inhibits, due to _______

A

desensitization

18
Q

nicotinic receptors locations

A

CNS
Adrenal medulla
Autonomic ganglia
NMJ

19
Q

Direct-Acting Cholinergic Agonists are also known as ____.

A

parasympathomimetics

20
Q

what do Cholinergic Agonists do?

A

Mimic the effects of ACh by binding directly to cholinergic receptors

21
Q

Some drugs preferentially bind to muscarinic receptors and are termed ______

A

muscarinic agents

22
Q

As a group, Cholinergic Agonist show little _____ so their use is limited

A

specificity

23
Q

Indirect-Acting Cholinergic Agonists Inhibit _______ which degrades ACh

A

acetylcholinesterase (AChE)

24
Q

Indirect-Acting Cholinergic Agonists Subtypes are______ and are used as nerve agents and pesticides

A

organophosphates

25
Q

Cholinergic Agonists Effects

DUMBBELSS

A 
Diarrhea
Urination
Miosis
Bronchorrhea**
Bradycardia**
Emesis
Lacrimation
Sweating
Salivation**
26
Q

Cholinergic Agonists Effects

SLUDGEMM

A 
Salivation
Lacrimation
Urination
Diarrhea
GI upset**
Emesis
Miosis
Muscle spasms**
27
Q

Cholinergic Antagonists are also known as?

A

cholinergic blockers, parasympatholytics, or anticholinergics

28
Q

what do Cholinergic Antagonists do?

A

Bind to ACh receptors but do NOT trigger the usual receptor-mediated response

29
Q

Compared to cholinergic agonists, Cholinergic Antagonists have many more ______.

A

therapeutic applications

30
Q

Cholinergic Antagonists- Three main groups/uses based on specific site of action:

A
  1. Muscarinic receptors of the parasympathetic nerves (aka: antimuscarinic agents)
  2. Nicotinic receptors of the sympathetic and parasympathetic ganglia
  3. Nicotinic receptor on skeletal muscle (aka: neuromuscular blockers)
31
Q

____ Cause inhibition of all muscarinic functions

A

Antimuscarinic Agents

32
Q

Antimuscarinic Agents, Also block the few sympathetic neurons that are_______ (i.e., sweat and salivary glands)

A

cholinergic

33
Q

Antimuscarinic Agents Have little to no action at _______ (i.e., lack NMJ and autonomic ganglion activity)

A

nicotinic receptors

34
Q

ABCDs of anticholinergic effects

A 
Anorexia
Blurry vision
Constipation/
Confusion
Dry Mouth
Sedation/
Stasis of urine
35
Q

Anticholinergic Effects

A
  1. Hot as a hare: increased body temperature
  2. Blind as a bat: mydriasis (dilated pupils), blurred vision
  3. Dry as a bone: dry mouth, dry eyes, decreased sweat, constipation, urinary retention
  4. Red as a beet: flushed face
  5. Mad as a hatter: confusion/delirium/euphoria
  6. Bloated as a toad: constipation, urinary retention, ileus
  7. And the heart runs alone: tachycardia
36
Q

MANY drugs have anticholinergic effects that are not the main ____

A

MOA

37
Q

MANY drugs have anticholinergic effects that are not the main MOA, examples?

A

antihistamines, opioid analgesics, antipsychotics, antidepressants, antiemetics, muscle relaxants

38
Q

this is Often considered the prototype anticholinergic drug

A

Atropine

39
Q

Atropine CV uses

A

Bradycardia: blocks parasympathetic activity which leads to an increased HR (dose-dependent action)

40
Q

Atropine uses

A

Bradycardia
OP Poisoning
Secretions: pre-anesthesia drying of secretions
Eye: results in persistent mydriasis, unresponsiveness to light, cycloplegia

41
Q

Atropine ADR

A

in general think anti-SLUDGE

Block 3 Pharm (6 decks)

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