cholinergic neurons

Question 1

Acetylcholine (ACh) is a common ____

Answer 1

neurotransmitter

Question 2

_____neurons are those that utilize ACh

Answer 2

Cholinergic

Question 3

Neurotransmission Six sequential steps:

Answer 3

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

Question 4

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

Answer 4

empty

Question 5

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

Answer 5

esterase

Question 6

______ toxin blocks release of vesicle content (ACh)

Answer 6

Botulinum

Question 7

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

Answer 7

Nicotinic

Muscarinic

Question 8

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

Answer 8

Nicotinic

Question 9

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

Answer 9

Muscarinic

Question 10

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

Answer 10

ion permeability

Question 11

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

Answer 11

neuroeffector junction

Question 12

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

Answer 12

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

Question 13

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

Answer 13

Recognize muscarine (alkaloid present in certain poisonous mushrooms)

Question 14

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

Answer 14

Recognize nicotine

Question 15

Nicotine at ____stimulates

Answer 15

[low]

Question 16

Nicotine at _____ inhibits

Answer 16

[high]

Question 17

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

Answer 17

desensitization

Question 18

nicotinic receptors locations

Answer 18

CNS
Adrenal medulla
Autonomic ganglia
NMJ

Question 19

Direct-Acting Cholinergic Agonists are also known as ____.

Answer 19

parasympathomimetics

Question 20

what do Cholinergic Agonists do?

Answer 20

Mimic the effects of ACh by binding directly to cholinergic receptors

Question 21

Some drugs preferentially bind to muscarinic receptors and are termed ______

Answer 21

muscarinic agents

Question 22

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

Answer 22

specificity

Question 23

Indirect-Acting Cholinergic Agonists Inhibit _______ which degrades ACh

Answer 23

acetylcholinesterase (AChE)

Question 24

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

Answer 24

organophosphates

Question 25

Cholinergic Agonists Effects | DUMBBELSS

Answer 25

``` Diarrhea Urination Miosis Bronchorrhea** Bradycardia** Emesis Lacrimation Sweating Salivation** ```

Question 26

Cholinergic Agonists Effects | SLUDGEMM

Answer 26

``` Salivation Lacrimation Urination Diarrhea GI upset** Emesis Miosis Muscle spasms** ```

Question 27

Cholinergic Antagonists are also known as?

Answer 27

cholinergic blockers, parasympatholytics, or anticholinergics

Question 28

what do Cholinergic Antagonists do?

Answer 28

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

Question 29

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

Answer 29

therapeutic applications

Question 30

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

Answer 30

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)

Question 31

____ Cause inhibition of all muscarinic functions

Answer 31

Antimuscarinic Agents

Question 32

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

Answer 32

cholinergic

Question 33

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

Answer 33

nicotinic receptors

Question 34

ABCDs of anticholinergic effects

Answer 34

``` Anorexia Blurry vision Constipation/ Confusion Dry Mouth Sedation/ Stasis of urine ```

Question 35

Anticholinergic Effects

Answer 35

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

Question 36

MANY drugs have anticholinergic effects that are not the main ____

Answer 36

MOA

Question 37

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

Answer 37

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

Question 38

this is Often considered the prototype anticholinergic drug

Answer 38

Atropine

Question 39

Atropine CV uses

Answer 39

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

Question 40

Atropine uses

Answer 40

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

Question 41

Atropine ADR

Answer 41

in general think anti-SLUDGE