Autonomic Drugs Flashcards

1
Q

How are anti-cholinesterase agents classified?

A

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

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2
Q

What receptors does norepinephrine not interact with in the ANS?

A

Beta 2

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3
Q

Cholinergic stimulation causes smooth muscle to _________

A

Contract

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4
Q

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

A
  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
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5
Q

Stronger beta2 agonist:

isoproterenol, epinephrine, or norepinephrine?

A

Iso > Epi >>Norepi

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6
Q

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

A

Contraction

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7
Q

mAChR activation promotes/inhibits urination?

A

promotes

  • contracts detrusor mm
  • relaxes sphincter mm
  • increases peristalsis in ureters
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8
Q

What enzyme breaks down ACh in the synaptic cleft?

A

acetylcholinesterase

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9
Q

mAChR activation has what two effects on the eye?

A
  1. contraction of sphincter muscle > miosis (pupil constriction)
  2. contraction of ciliary muscle > incr curvature of lens
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10
Q

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

A

Bradycardia

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11
Q

Stronger alpha1 agonist:

isoproterenol, epinephrine, or norepinephrine?

A

Norepi > Epi >> Iso

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12
Q

Descrbie muscarinic receptors

A
  • stimulated by natural alkaloid - muscarine
  • 5 subtypes
  • tx drugs exhibit little/no subtype selectivity
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13
Q

What is the MOI of organophosphates, such as sarin?

A

Anticholinesterase

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14
Q

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

A

GI spasms; these are called “spasmolytics” or “antispasmotics”

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15
Q

Stronger alpha2 agonist:

isoproterenol, epinephrine, or norepinephrine?

A

Epi = Norepi >> Iso

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16
Q

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

A

Gq

17
Q

Why do anticholinergic drugs disrupt sweating?

A

Because sympathetic neurons use acetylcholine for sweat gland neurons

18
Q

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

A

Decreased contraction

19
Q

5 Therapeutic Uses for Anti-Cholinergic Agents

A
  1. Reduce smooth muscle spasms
  2. Antisecretory effects
  3. Ophthalmic exams
  4. Prevent heart block
  5. Antidotes
20
Q

What does SLUD/BLUD stand for?

A

Salivation/Bradycardia

Lacrimation

Urination

Defecation

21
Q

Nictonic receptors

A
  • 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
Q

Stronger beta1 agonist:

isoproterenol, epinephrine, or norepinephrine?

A

Iso > Epi = Norepi

23
Q

Explain the effects of mAChR activation on blood vessels

A
  • 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
Q

What receptors does isoproterenol not interact with in the ANS?

A

alpha 1 and 2

25
Q

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

A

Gi

26
Q

Does mAChR activation causes bronchial smooth muscle contraction or dilation?

A

Contraction > bronchoconstriction

27
Q

mAChR activation promotes/inhibits secretions from most secretory glands?

A

Promotes (SLUD)

28
Q

Key differences between glycopyrrolate and atropine

A
  1. less CNS effects (sedation, amnesia, etc.)
  2. longer half life & more potent
  3. less tachycardia
29
Q

Major effects of ACh on the GI tract

A
  • incr motility & peristalsis
  • incr smooth muscle tone
  • incr amplitude of contractions
  • incr secretions (acid)
30
Q

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

A

constipation/impactions; these are “prokinetic agents”

31
Q

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

A

Contraction

32
Q

Signs of acute organophosphate poisoning

A
  • inhaled: ocular, respiratory
  • oral: GI, systemic signs
  • cutaneous: sweating, muscle fasciculations
33
Q

What is acetylcholine important for in the CNS?

A

cognition

34
Q

What are the parasympathetic effects on cardiac tissue mediated by?

A

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

35
Q

Describe a typical parasympathetic pre- and post-ganglionic neuron

A

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

36
Q

What is the function of the parasympathetic nervous system?

A

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

37
Q

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

A
  • 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)