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Pharmacology > 2. Cholinergic Agonists and Muscarinic Antagonists > Flashcards

2. Cholinergic Agonists and Muscarinic Antagonists Flashcards

1
Q

What is the primary NT innervating SKM?

A

ACh

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2
Q

Which muscarinic receptor subtypes are excitatory? what is there signaling?

A

M1, 3, 5

  • Inc IP3
  • Inc Ca2+
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3
Q

Which muscarinic receptor subtypes are inhibitory? What is their signaling?

A

M2, 4

  • Dec cAMP
  • Inc K+ conductance
  • Also function as auto-receptors, that can be located pre-synaptically and self-regulate ACh release
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4
Q

What are the muscarinic agonist effects on the eye?

A
  • Constriction of pupil
    • Focusing for near vision
  • Allows for drainage of vitreous humor, helping to reduce intra-ocular pressure
    • Tx for glaucoma - pilocarpine
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5
Q

What are the muscarinic agonist effects on the heart?

A
  • Decreased:
    • HR
    • Contractility
    • Conduction Rate
  • Impact has variability b/c may be compensated by SNS - baroreceptors activation of the SNS to regulate BP
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6
Q

What are the muscarinic agonist effects on the vascular smooth muscle?

A
  • Blood Vessel Dilation
  • Stimulation of Secretory Glands
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7
Q

How is vascular smooth muscle dilated via a muscarinic agonist?

A
  • Release of NO through direct activation of local M3 receptors on the endothelium, which leads to:
    1. Increased cGMP
    2. Reduces intracellular Ca2
    3. Which reduces phosphorylation of myosin
    4. Allows muscles to relax
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8
Q

What are the muscarinic agonist effects on the urinary tract? What are they used to treat?

A
  • Relaxes bladder:
    • Constricts detrusor
    • Relaxes trigone
    • Relaxes sphincter muscle
  • Tx for Urinary Retention - bethanecol
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9
Q

What are the muscarinic agonist effects on the secretory glands in the bronchus? What are they used to tx?

A
  • Bronchoconstriction and increased mucous secretions
  • Used to test for Asthma (hyperactive airway), by giving the pt methacholine to stimulate bronchoconstriction
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10
Q

What can be used as bronchodilators?

A

Anti-cholinergics

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11
Q

What are the muscarinic agonist effects on intestinal function? What are they used to tx?

A
  • Increased motility and secretions
  • Decreased sphincter tone​
  • Tx of cessation of intestinal function that can occur post-op
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12
Q

What do you use to tx xerostomia?

A

muscarinic agonist

cevimeline

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13
Q

What pts are at an increased risk for adverse effects from muscarinic receptor activation?

A
  • Asthma
  • CVD
  • Peptic ulcers
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14
Q

Which classification of AChE Inhibitors/Anticholinesterases has therapeutic value?

A

Reversible AChE Inhibitors

  • neostigmine
    • Tx of myasthenia gravis, reversal of nondepolarizing muscle relaxants
  • physostygmine
    • ​Tx of gluacoma
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15
Q

What are Irreversible AChE Inhibitors used for?

A

Insecticides - organophosphates

Binds to and damages AChE

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16
Q

Which receptor does Acetylcholine have a greater affinity for?

A

muscarinic

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17
Q

How does atropine treat insecticide poisoning from organophosphates?

A
  • It is a muscarinic receptor antagonist that alleviates CNS and parasympathetic stimulation
  • Solves immediate problem
    • But have to wait 2wks for AChE to reload
18
Q

What is another drug besides atropine that is used to treat insecticide poisoning from organophosphates? How does it work?

A

pralidoxime

  • Can bind to site within AChE
    • Interacts with phosphoryl group left by organophosphate
    • Can sequester phophoryl group and reactivate AChE
19
Q

What are the therapuetic cholinergic agonists used to tx Glaucoma?

A
  • Beta blockers
  • Prostaglandins
20
Q

What are the therapuetic cholinergic agonists used to tx xerostomia?

A

Direct Agonists

  • Pilocarpine
  • Cevimeline
21
Q

What are the therapuetic cholinergic agonists used to tx reversal of neuromuscular block?

A

Indirect agonists

  • Competitive inhibition of nicotinic receptors
22
Q

What are the therapuetic cholinergic agonists used to tx myasthenia gravis (AI disorder that attacks ACh receptors)?

A

Indirect agonists

  • Inc amounts of ACh within signaling to help tx
23
Q

What are the therapuetic cholinergic agonists used to tx atropine poisoning?

A

Physostigmine

  • CNS availability (indirect agonists)
24
Q

What are the therapuetic cholinergic agonists used to tx paralytic ileus?

A

Bethanecol

  • Direct agonist
25
Q

What are the therapuetic cholinergic agonists used to tx bladder atony?

A

Bethanecol

  • Direct agonist
26
Q

What is used to tx Alzheimer type dementias?

A

therapuetic cholinergic agonists

27
Q

What organs does atropine have a larger effect on?

A
  • Lungs
  • GI
  • Heart
28
Q

What organs does scopolamine have a larger effect on?

A
  • Eye
  • Secretory Glands
  • CNS
29
Q

What are the effects of muscarinic antagonists on the eye?

A
  • Paralysis of accommdation
  • Intraocular pressure is only impacted in narrow-angle glaucoma
30
Q

What are the effects of low dose muscarinic antagonists on the cardiovascular system?

A

mild bradycardia

31
Q

What are the effects of higher dose muscarinic antagonists on the cardiovascular system?

A

tachycardia

32
Q

What are the effects of muscarinic antagonists on the Genitourinary tract?

A

urinary retention

33
Q

What are the effects of muscarinic antagonists on body temp?

A

Inhibition of sweating can cause increase in body temp

34
Q

What muscarinic antagonist is more effective at the medulla and higher cerebral centers?

A

Scopolamine

  • Can cause:
    • Drowsiness, Sedation
    • Euphoria
    • Amnesia, Delirium, Hallucinations
35
Q

What is Parkinson’s Disease related to in the CNS?

A

Loss of balance between cholinergic and dopamine signaling in the striatum

36
Q

What is motion sickness related to in the CNS?

A

Acetylcholine acts as a neuromodulator in the vestibular system increasing responsiveness

37
Q

What is an adverse affect of muscarinic antagonists in children treated with physostygmine?

A

Atropine poisoning

38
Q

What is an adverse affect of muscarinic antagonists for pts with narrow-angle glaucoma?

A

increased intraocular pressure

39
Q

What is an adverse affect of muscarinic antagonists in pts with prostatic hypertrophy?

A

urinary retention

40
Q

Why do synthetic quaternary ammonia muscarinic antagonists have no CNS effects?

A

Does not cross BBB

Pharmacology (18 decks)

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