Muscarinic antagonist Flashcards

1
Q

What are muscarinic antagonist drugs?

A
  • those that inhibit muscarinic receptors
  • M1 = Gaq
  • M2 = Gai
  • M3 = Gaq
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2
Q

What do muscarinic antagonist drugs do to the parasympathetic activity?

A
  • reduce the activity
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3
Q

Why are muscarinic antagonist drugs commonly called anti-cholinergic?

A
  • muscarinic receptors are a form of cholinergic receptor
  • inhibit muscarinic means anti-cholinergic
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4
Q

What is one of the most commonly prescribed muscarinic antagonist drugs?

A
  • atropine
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5
Q

What is atropine used for in the heart?

A
  • treat people with bradycardia
  • patients have low HR
  • patients may have lower CO
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6
Q

What is the mechanism of action of atropine?

A
  • competitive antagonist
  • inhibits acetylcholine and therefore muscarinic receptors
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7
Q

In a normal physiological response what does the muscarinic receptor M2 do to the heart?

A
  • inhibit adenylyl cyclase (AC) as part of Gai
  • ⬇️ AC = ⬇️ HR and inotropic contraction
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8
Q

Atropine is a non selective competitive antagonist, meaning it can compete with acetylcholine and inhibit its activity when binding to muscarinic receptors. Although it has a wide range of effects, what does atropine do to the heart in patients with bradycardia?

A
  • does not inhibit adenylyl cyclase (AC) in Gas
  • ⬆️ activation of SA node = ⬆️ HR
  • ⬆️ inotropic contraction
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