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Medical Pharmacology Exam 1 > Cholinergics I > Flashcards

Cholinergics I Flashcards

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USMLE® Step 1 flashcards
1
Q

What is the major difference between the muscarinic and nicotinic cholinoreceptors?

A

The muscarinics are GPCRs while the nicotinics are ion channels

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2
Q

There are 3 types of muscarinic receptors, M1, M2 and M3. Where are they found?

A

M1 - Postganglionic neurons
M2- Cardiac, smooth muscle
M3 - Glands, smooth muscles, endothelium

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3
Q

There are 2 types of nicotinic cholinoreceptors (N1/N2) Where are they found?

A

N1 / Nn - Postganglionic autonomic (symp and parasymp) neurons
N2/ Nm - Skeletal muscle neuromuscular junction

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4
Q

What is the mechanism of action of the nicotinic cholinoreceptors?

A

Cause depolarization by activating sodium and potassium channels

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5
Q

The nicotinic receptor is activated by _ molecules of Ach. It causes _

A

2 molecules

Sodium channel opening, excitatory post-synap. potential

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6
Q

In addition to the sympathetic and parasymp ganglia, the adrenal medulla contains what subtype of nicotinic receptor?

A

The N1/Nn subtype

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7
Q

What is the effect of cholinergics on the parasympathetic NS?

A

Activation, cholinergics are parasympathomimetics

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8
Q

Acetylcholine, bethanechol, carbachol and methacholine are all AchR agonist. How are the latter 3 related to Ach?

A

The latter 3 are synthetic Ach derivatives that are more selective and have longer duration of action

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9
Q

Muscarine and pilocarpine are _

A

Cholinergics that are selective for the muscarinic type AchR

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10
Q

Nicotine and varenicline are _

A

Cholinergics that are selective for the nicotinic type AchR

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11
Q

Muscarine, pilocarpine, varenicline and nicotine all fall under the class of _

A

Natural alkaloids

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12
Q

When AchR agonists mimic the parasymp NS, this is accomplished by activating what type of receptor? Where are these receptors located (3)

A

The muscarinic receptors

Smooth muscle, glands, heart

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13
Q

What is the effect of muscarinic receptor activation of the lung?

A

Broncho-constriction

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14
Q

The major factor determining the synthesis of Ach is _. What type of co-transporter is this?

A

Choline uptake

Sodium - choline

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15
Q

What is the enzyme that catalyzes the synthesis of Ach?

A

Choline acetyl-transferase

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16
Q

Methacholine is an Ach derivative that has a methyl group. What is the significance of this group?

A

It has greater selectivity for muscarinic type receptors

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17
Q

Carbachol is an Ach derivative that has an amino (NH2) group. What is the significance of this group?

A

It has a longer duration of action as it binds poorly to AchE and pseudoAchE

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18
Q

Bethanechol is an Ach derivative that has a methyl group and an amino group. What is the significance of these groups?

A

It is long lasting and it is selective for the muscarinic type receptor

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19
Q

The 2 major enzymes that hydrolyze Ach are _

A

Acetylcholinesterase and plasma cholinesterase (aka pseudocholinesterase and butyrylcholinesterase)

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20
Q

What are the major locations of acetylcholinesterase (3)?

A

Cholinergic synapses
Neuromuscular junctions
RBCs

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21
Q

What are the major locations of plasma cholinesterase (2)? What are 2 major functions?

A

Plasma and Liver

  • Hydrolyze escaped ACh
  • Hydrolyze ingested plant esters
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22
Q

Succinylcholine, a neuromuscular blocker is inactivated by _

A

Plasmacholinesterase

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23
Q

Organophosphate insecticides are more likely to react with _ while organophosphate nerve gases are more likely to react with _

A

Plasma cholinesterase

AchE

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24
Q

What is the net effect of AchE inhibitors?

A

They (indirectly) stimulate the parasymp NS, same as the cholinergic drugs

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25
Q

The 4 examples of AchE inhibitors provided are _

A

– edrophonium
– neostigmine
– pyridostigmine
– physostigmine

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26
Q

Edrophonium, neostigmine, pyridostigmine and physostigmine are all [long/short] acting. Their main function is as _

A

Short acting, reversible

competitive inhibitors of AchE

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27
Q

Organophosphate derivative, nerve gases and insecticides are all examples of _

A

Non-competitive inhibitors of AchE

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28
Q

Edrophonium and ambemonium are both _

A

Reversible short acting inhibitors of AchE

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29
Q

Neostigmine, physostigmine and pyridostigmine are all _

A

Reversible short acting inhibitors of AchE

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30
Q

Sarin, soman and VX are all examples of _. They function as _

A

Nerve gases

Irreversible inhibitors of AchE

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31
Q

Carbaryl and tetraethylpyrophosphate are both examples of _. They function as _

A

Insecticides

Irreversible inhibitors of AchE

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32
Q

Malathion and parathion are both examples of _. They function as _

A

Insecticides

Irreversible inhibitors of AchE

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33
Q

Di-isopropylfluorophosphate (DFP) and echothiophosphate are both examples of _. They function as _

A

Organophosphate derivatives

Irreversible inhibitors of AchE

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34
Q

AchE inhibitors fall into 3 groups (alcohols, carbamates and organophosphates). Edrophonium is a _. It crosses the BBB [true/false]. Why?

A

Simple alcohol
False
It has a quaternary ammonium group (charged)

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35
Q

AchE inhibitors fall into 3 groups (alcohols, carbamates and organophosphates). Neostigmine, physostigmine, carbaryl and pyridostigmine are all _. Which crosses the BBB?

A

Carbamates

Physostigmine

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36
Q

AchE inhibitors fall into 3 groups (alcohols, carbamates and organophosphates). Di-isopropylfluorophosphate (DFP) and echothiophosphate are both _

A

Organophosphates

37
Q

Ach is hydrolyzed by AchE in _ steps. The intermediates of this reaction are _ (2). The final product is AchE and _

A

Two
Choline (free) and Acetylated AchE
Acetate and AchE

38
Q

The AchE intermediate from the hydrolysis of neostigmine is _. How long does this take compared to Ach hydrolysis?

A 
Carbamylated AchE (more resistant to hydration)
0.5 - 2 hrs 
Much longer than Ach (100 microseconds)
39
Q

Di-isopropylfluorophosphate (DFP) can interact with AchE to form _. This is “rescue-able” until the formation of _

A

Phosphoryl AchE

Aged AchE

40
Q

Edrophonium, neostigmine, pyridostigmine and ambemonium can all be used for the treatment of which disease? They are all intermediate in duration except for _ which is very short acting?

A

Myesthenia gravis

Edrophonium

41
Q

Edrophonium and neostigmine are both used for the treatment of _. Which is longer in duration?

A

Ileus

Neostigmine

42
Q

In addition to myesthenia gravis and ileus, what type of heart condition can edrophonium be used for?

A

Arrythmias

43
Q

Physostigmine, demecarium and echothiophate can all be used for the treatment of what eye disease? Which of this is of long duration?

A

Glaucoma

Echothiophosphate

44
Q

Organophosphates like herbicides and insecticides are lipid soluble drugs that act as _. What are the major routes involved in O-P poisoning?

A

AchE inhibitors

Dermal and Pulmonary

45
Q

The clinical marker for degree of organophosphate intoxication is _. What is the acronym?

A

Parasymp. stimulation

SLUD

46
Q

If organophosphate intoxication first results in occular and respiratory symptoms, what is the most likely route of intoxication?

A

Respiratory

47
Q

If organophosphate intoxication first results in GI symptoms, what is the most likely route of intoxication?

A

Oral

48
Q

The 2 drugs used for the treatment of organophosphate poisoning are _

A

Atropine and Pralidoxime (2-PAM)

49
Q

What are the effects of atropine? Why is it administered in large doses at first?

A

Atropine competitively binds muscarinic receptors (blocks parasymp symptoms)
High doses help cross BBB

50
Q

What are the effect of pralidoxime (2-PAM)? What is the temporal consideration for its administration? Where is it most effective?

A

It is an AchE reactivator (removes phosphoryl group)
It has to be administered before aging
Neuromuscular synapses

51
Q

Acute closed angle glaucoma (vs. chronic) is a medical emergency. What two drugs are usually administered to treat this? What are their mechanism of action?

A

Pilocarpine (muscarinic agonist)
Physostigmine (AchE inhibitor)
Cause ciliary body ctx, opens canal of schlemm

52
Q

Postoperative ileus, congenital megacolon, urinary retention and reflux esophagitis are treated using _ (2)

A

Bethanechol and neostigmine

53
Q

Salivary secretions can be increased using _, while dry mouth assoc. with Sjogren syndrome can be treated using _

A

Pilocarpine

Cevimeline

54
Q

For the treatment of myesthenia gravis, what 4 AchE inhibitors are usually employed?

A 
MG - NAPE
Neostigmine
Ambemonium
Pyridostigmine
Edrophonium
55
Q

Why are cholinergic agonists not administered IV or IM?

A

Increased toxicity, loss of selectivity

56
Q

Cholinergic agonists used for the treatment of occular conditions are usually [secondary, tertiary or quaternary] compounds

A

Tertiary

57
Q

Four conditions contraindicated for the use of cholinergic agonists are _

A

Asthma
Coronary insufficiency
Hyperthyroidism
Peptic acid disease

58
Q

Flushing, sweating, cramping, belching, urinary bladder tightness, reduced visual accomodation, headache and salivation are all _

A

Side effects of cholinergic agonists

59
Q

Atropine and homatropine are selective for _

A

muscarinic selective antagonists

60
Q

Scopolamine and methscopolamine are selective for _. Which is a quaternary amine?

A

muscarinic selective antagonists

Methscopolamine

61
Q

Trihexyphenidyl, Cyclopentolate and tropicamide are selective for _

A

muscarinic selective antagonists

62
Q

Ipratropium and tiotropium are selective for _

A

muscarinic selective antagonists

63
Q

Darifenacin, solifenacin and tolterodine are examples of _

A

M3 selective cholinergic antagonists

64
Q

Mecamylamine and trimethaphan are examples of _

A

Nicotinic selective cholinergic antagonists

65
Q

The example of depolarizing cholinergic nicotine selective drug provided is _ This is metabolized by _

A

Succinylcholine

Pseudocholinesterase

66
Q

Curare is an example of _. It causes _

A

non-depolarizing nicotine specific cholinergic antagonist

Paralysis

67
Q

Atracurium, cisatracurium and mivacurium are all examples of _

A

non-depolarizing nicotine specific cholinergic antagonist

68
Q

Pancuronium and vecuronium are examples of _

A

non-depolarizing nicotine specific cholinergic antagonist

69
Q

What are the direct and indirect means by which muscarinic receptors mimic parasymp NS?

A

Direct - AchR agonist

Indirect - AchE antagonists

70
Q

Quaternary alcohol, carbamates and organophosphate derivative are [competitive/noncompetitive] cholinesterase inhibitors

A

Alcohols and carbamates - competitive

OP - non-competitive

71
Q

Among organophosphates, the only one with clinical use us _. It is used for treatment of _

A

Malathion

Head lice

72
Q

To stimulate smooth muscle post-op (increase GI motil, increase bladder emptying, increase saliva) you would use _. It acts as a _

A

Bethanechol

Muscarinic agonist

73
Q

To test the function of muscarinicreceptors, slow the heart and test for bronchial hyperactivity, you would use _

A

Methacholine

74
Q

Corneal application of _ and _ are used in acute wide angle glaucoma

A

Pilocarpine and carbachol

75
Q

To increase GI motility and bladder emptying following surgery, and to reverse neuromuscular blockade (curare), you’d use _

A

Neostigmine

76
Q

To treat mysethenia gravis, block effect of nerve gases, reverse neuromuscular blocade you’d use _

A

Pyridostigmine

77
Q

The N1 or Nn subtype of nicotinic receptor is usually found in synapses between _

A

Nerve and Nerve - Think peipheral ganglia of autonomics

78
Q

The N2 or Nm subtype of nicotinic receptor is usually found in synapses between _

A

Nerve and muscle - Think neuromuscular junction of somatic NS

79
Q

What are the 2 broad categories of cholinergic drugs that mimic the parasympathetics via muscarinic receptors?

A 
ACh and synthetic choline esters (analogues of ACh)
Natural Alkaloids (more selective for muscarinic receptors)
80
Q

What are the 4 muscarinic receptor agonists that directly stimulate the parasympathetic NS? Which 2 are muscarinic selective?

A

Acetylcholine
Methacholine (Selective)
Carbachol
Bethanechol (Selective)

81
Q

What are the 2 AChE inhibitors that are also quaternary ammoniums?

A

Edrophonium

Neostigmine

82
Q

Atropine is a great first drug for the treatment of _. What will it not affect / rescue? Why?

A

organophosphate intoxication
Neuromuscular synapse hyperactivity and resulting paralysis
It is a muscarinic (not nicotinic) blocker

83
Q

In situations of cholinergic agonist overdose, what 2 drugs can be used?

A

Atropine

Norepinephrine

84
Q

Effector sites of the muscarinic receptor antagonists include (4) _

A

Smooth muscle
Cardiac muscle
Glands
CNS

85
Q

Under what conditions will muscarinic antagonists cause partial blockade at the autonomic ganglia or neuromuscular junctions?

A

Extremely high doses

86
Q

When Mydriasis and cycloplegia are both required for an eye exam, what 5 antimuscarinic drugs can be used? (in order of desending duration of action)

A 
ASHCT
Atropine 
Scopolamine
Homatropine
Cyclopenolate
Tropicamide
87
Q

In cases of myocardial infarct, what is the use of muscarinic antagonists? Which one specifically?

A

MI causes reflex slowing of the heart because of vagal inputs
Atropine can block this slowing. Only used in ICU

88
Q

What are the 2 effects of the antimuscarinic drugs on the airway? Which is not beneficial? Why?

A

Bronchodilation and decreased secretions

Decreased secretion - increased microbe stasis and growth

89
Q

What 2 antimuscarinic drugs are essentially topical agents that can be used to elicit bronchodilation without decreased secretion? Why? What disease can they be used for?

A

Ipratropium and Tiotropium
Quaternary amine, don’t cross the mucus membranes to get systemic to cause decreased secretion
COPD

Medical Pharmacology Exam 1 (15 decks)

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