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Flashcards in Autonomic Drugs Deck (37):
1

How are anti-cholinesterase agents classified?

based on duration of enzyme inhibition; related to the speed with which inhibitor dissociates from the esteric site of AChE

2

What receptors does norepinephrine not interact with in the ANS?

Beta 2

3

Cholinergic stimulation causes smooth muscle to _________

Contract

4

Five clinical signs you expect to see when using anti-cholinesterase agents

  1. Constriction of pupils
  2. Increased secretion of sweat, saliva, tears
  3. Slow heart rate
  4. Mucus secretion in the resp tract
  5. Constriction of bronchioles

5

Stronger beta2 agonist: 

isoproterenol, epinephrine, or norepinephrine?

Iso > Epi >>Norepi

6

What happens if you activate Gi in a smooth muscle cell?

Contraction

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7

mAChR activation promotes/inhibits urination?

promotes

  • contracts detrusor mm
  • relaxes sphincter mm
  • increases peristalsis in ureters

 

8

What enzyme breaks down ACh in the synaptic cleft?

acetylcholinesterase

9

mAChR activation has what two effects on the eye?

  1. contraction of sphincter muscle > miosis (pupil constriction)
  2. contraction of ciliary muscle > incr curvature of lens

10

If you use a cholinergic agonist with high muscarinic receptor activity, what effect do you need to be concerned about on the heart?

Bradycardia

11

Stronger alpha1 agonist: 

isoproterenol, epinephrine, or norepinephrine?

Norepi > Epi >> Iso

12

Descrbie muscarinic receptors

  • stimulated by natural alkaloid - muscarine
  • 5 subtypes
  • tx drugs exhibit little/no subtype selectivity

13

What is the MOI of organophosphates, such as sarin?

Anticholinesterase

14

What type of GI tract disorder would anticholinergic drugs be used to treat?

GI spasms; these are called "spasmolytics" or "antispasmotics"

15

Stronger alpha2 agonist: 

isoproterenol, epinephrine, or norepinephrine?

Epi = Norepi >> Iso 

16

M1, M2 and M3 receptors  couple with what G-protein?

Gq

17

Why do anticholinergic drugs disrupt sweating?

Because sympathetic neurons use acetylcholine for sweat gland neurons

18

What happens if you activate Gi in a cardiac muscle cell?

Decreased contraction

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19

5 Therapeutic Uses for Anti-Cholinergic Agents

  1. Reduce smooth muscle spasms
  2. Antisecretory effects
  3. Ophthalmic exams
  4. Prevent heart block 
  5. Antidotes

20

What does SLUD/BLUD stand for?

Salivation/Bradycardia

Lacrimation

Urination

Defecation

21

Nictonic receptors

  • stimulated by natural plant alkaloid nicotine
  • some subtypes undergo rapid desensitization with over-stimulation - tachyphylaxis
  • tx drugs exhibit selectivity for nicotinic receptors in sk mm (muscle relaxants) vs. receptors in neural tissues 

22

Stronger beta1 agonist: 

isoproterenol, epinephrine, or norepinephrine?

Iso > Epi = Norepi

23

Explain the effects of mAChR activation on blood vessels

  • agonists cause pronounced atypical relaxation of vascular smooth muscle and fall in blood pressure
  • mAChR are located on endothelial cells 
  • mediated by nitric oxide

24

What receptors does isoproterenol not interact with in the ANS?

alpha 1 and 2

25

M2 and M4 receptors are coupled with what G-protein receptor?

Gi

26

Does mAChR activation causes bronchial smooth muscle contraction or dilation?

Contraction > bronchoconstriction

27

mAChR activation promotes/inhibits secretions from most secretory glands?

Promotes (SLUD)

28

Key differences between glycopyrrolate and atropine

  1. less CNS effects (sedation, amnesia, etc.)
  2. longer half life & more potent
  3. less tachycardia 

29

Major effects of ACh on the GI tract

  • incr motility & peristalsis
  • incr smooth muscle tone
  • incr amplitude of contractions
  • incr secretions (acid)

30

What type of GI disorder would cholinergic agonists be used to treat?

constipation/impactions; these are "prokinetic agents"

31

What happens if you activate Gq in a smooth muscle cell?

Contraction

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32

Signs of acute organophosphate poisoning

  • inhaled: ocular, respiratory
  • oral: GI, systemic signs
  • cutaneous: sweating, muscle fasciculations

33

What is acetylcholine important for in the CNS?

cognition

34

What are the parasympathetic effects on cardiac tissue mediated by?

the vagal release of ACh> activates cardiac mAChR > baroreceptor reflex > reduction in heart rate

35

Describe a typical parasympathetic pre- and post-ganglionic neuron

Two synapses; long pre-ganglionic axon, short post-ganglionic axon 

36

What is the function of the parasympathetic nervous system?

provides "vegetative" or resting control of visceral organs; excessive activity causes SLUD/BLUD syndrome

37

What happens if you activate a nicotinic receptor on a neuron, smooth muscle, or cardiac muscle cell?

  • You will increase cell activity, and thus increase probability of neurotransmitter release, as well as cause smooth muscle contraction and cardiac muscle contraction.
  • increased alertness (neurons), heart rate (cardiac muscles), and blood pressure (smooth muscle)