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PHRM 825 > PHRM 825: Pharmacologic Manipulations of the Cholinergic System > Flashcards

PHRM 825: Pharmacologic Manipulations of the Cholinergic System Flashcards

1
Q

What causes botulism and where is it present?

A

Bacterium clostridium botulinum; soil and water

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2
Q

How does clostridium botulinum cause botulism?

A

Inhibits release of Ach

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3
Q

What are symptoms of botulism?

A
  • Weakness
  • Trouble seeing
  • Feeling tired
  • Trouble speaking
  • NOT NECESSARILY FEVER*
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4
Q

What is the most fatal symptom of neuropathy of the ANS?

A

Silent ischemic events (painless event)

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5
Q

What are 2 approaches to increase cholinergic stimulation?

A

Increase endogenous stimulation and use exogenous stimulation

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6
Q

What can reduce symptoms of neuropathic ANS disorders?

A

Cholinergic stimulation

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7
Q

Would an AchE inhibitor help botulism patients?

A

No. Patient’s don’t release Ach

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8
Q

What are the 2 types of cholinesterases?

A

Acetylcholinesterase (AchE) and plasmacholinesterase (Butyrylcholinesterase (BuChE)

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9
Q

Where is AchE located?

A

In nerve synapses

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10
Q

Where is butyrylcholinesterase (BuChE) located?

A

In plasma and many organs (liver, skin, GI tract, brain)

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11
Q

What does BuChE metabolize?

A

Succinylcholine

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12
Q

Where do acetylcholinesterase inhibitors bind?

A

The same site as acetylcholine

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13
Q

What are the 3 classes of AchE inhibitors?

A

Quaternary ammonium alcohols, carbamates, and organophosphates

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14
Q

What drug is a tertiary amine that can enter the CNS?

A

Physostigmine

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15
Q

What can physostigmine be used to treat?

A

glaucoma and Alzheimer’s disease, and atropine overdose

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16
Q

What is neostigmine used to treat?

A

myasthenia gravis, reversal of neuromuscular blockers and post-operative ileus

17
Q

What is pyridostigmine use to treat?

A

myasthenia gravis, reversal of neuromuscular blockers and post-operative ileus

18
Q

What is an irreversible, covalent binding AchE inhibitor?

A

Organophosphates

19
Q

What are organophosphates used to treat?

A

Glaucoma (not commonly used)

20
Q

What are symptoms of acetylcholinesterase inhibitor poisoning?

A 
DUMBBELLSS
(all of these are M3 except Bradycardia)
-Diarrhea
-Urination
-Miosis
-Bronchospasms
-Bradycardia (M2)
-Excitation of skeletal muscles and CNS
-Lacrimation
-Sweating
-Salivation
21
Q

What can be given to treat AchE “poisoning”?

A

Pralidoxime chloride (2-PAM) and/or Atropine

22
Q

What drug is usually used for diagnosis of myasthenia gravis?

A

Edrophonium (tensilon)

23
Q

Symptoms of myasthenia gravis

A
  • Muscle weakness (visible in eye)
  • Trouble chewing/swallowing
  • Hard to talk/nasal sound
  • Reduced facial expression
24
Q

What causes myasthenia gravis?

A

Auto-antibodies that block nicotinic acetylcholine receptors at the postsynaptic neuromuscualr junction

25
Q

What are the 2 cholinergic centers in the CNS?

A
  • Nucleus Basalis of Meynert and medial septal nuclei (basal forebrain)
  • Mesopontine tegmentum (brain stem)
26
Q

What reversible AchE inhibitors are used in managing symptoms of Alzheimer’s Disease?

A
  • Donepezil
  • Rivastigmine
  • Tacrine
  • Galantamine
27
Q

What was the first parasympathomimetic discovered?

A

Muscarine

28
Q

Why is clinical use of muscarine not recommended?

A

It can cross the BBB and cause convulsions

29
Q

What is methacholine used for?

A

To diagnose bronchial hyperreactivity in Asthma and COPD

30
Q

How is open angle glaucoma treated?

A

M3 muscarinic agonist

31
Q

How is closed angle glaucoma treated?

A

iridectomy; medical emergency

32
Q

What muscarinic agonists are used to treat glaucoma?

A

Carbachol and pilocarpine

33
Q

CNS effects are mainly mediated by what receptors?

A

M1

34
Q

What are therapeutic effects of muscarinic agonists?

A
  • Arousal and attention

- Improve cognitive function

35
Q

Side effects of muscarinic agonists

A

Tremors and hypothermia

PHRM 825 (36 decks)

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