Cholinomimetics (direct acting cholinergics) Flashcards

1
Q

What is methacholine?

Which receptors is it selective for?

What is its effect on the receptor?

Is it able to cross the BBB?

A

Selective mAChR agonist

polar; unable to cross BBB

*test for asthma (induce bronchoconstriction)

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2
Q

What is carbachol?

Which receptors is it selective for?

What is its effect on the receptor?

Is it able to cross the BBB?

A

Non-selective cholinergic agonist

polar; unable to cross BBB

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3
Q

What is bethanechol?

Which receptors is it selective for?

What is its effect on the receptor?

Is it able to cross the BBB?

A

Selective mAChR agonist

polar; unable to cross BBB

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4
Q

What is cevimeline?

Which receptors is it selective for?

What is its effect on the receptor?

A

Selective mAChR agonist

*xerostomia

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5
Q

What is pilocarpine?

Which receptors is it selective for?

What is its effect on the receptor?

A

Selective mAChR agonist

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6
Q

What is varenicline?

Which receptors is it selective for?

What is its effect on the receptor?

Is it able to cross the BBB?

A

Selective nAChR agonist

nonpolar; able to cross BBB

*chantix - smoking cessation

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7
Q

What cholinergics would be most effective in treating xerostomia in Sjögrens syndrome?

A
  • cevimeline
  • pilocarpine
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8
Q

What cholinergics would be most effective in treating non-obstructive GI disorders?

A

-bethanechol

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9
Q

What cholinergics would be most effective in treating urinary retention?

A

-bethanechol

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10
Q

What cholinergics would be most effective in treating glaucoma?

A
  • carbachol
  • pilocarpine
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11
Q

What cholinergics would be most effective in producing miosis?

A
  • acetylcholine
  • carbachol
  • pilocarpine
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12
Q

What cholinergics would be most effective in stimulating/testing for asthma?

A

-methacholine

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13
Q

What cholinergics would be most effective in smoking cessation?

A

-varenicline

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14
Q

What are the major clinical uses of cholinergics?

A
  • glaucoma
  • accomdative esotropia
  • non-obsrtuctive GI disorders
  • xerostomia in Sjögrens
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15
Q

What are the side effects of muscarinic agonist toxicity?

A

BM SLUDGE

  • miosis
  • bronchoconstriction
  • salivation
  • lacrimation
  • urination
  • diarrhea
  • GI pain
  • emesis
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16
Q

What are the side effects of nicotinic agonist toxicity?

A

*only caused by nicotine*

  • convulsions (CNS stimulation) followed by paralysis (end plate depolarization blockade)
  • respiratory paralysis
  • hypertension followed by hypotension
  • tachycardia followed by bradycardia