Lecture 6 - Cholinergic Agonists Flashcards

1
Q

______ receptors use ion channels

A

nicotinic

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2
Q

nicotinic affects ganglion of both ___ and ___

A

SNS

PNS

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3
Q

nicotinic affects _____ muscle

A

skeletal

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4
Q

Muscarinic receptors are _____ mediated

A

G-protein

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5
Q

What do muscarinic receptors affect ?

A

effector organs/tissues of parasympathetic

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6
Q

Sweat receptors on the ____ are adrenergic

A

palms

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7
Q

Sweat receptors everywhere else are ____

A

cholinergic (but still part of sympathetic system)

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8
Q

All preganglionic synapses are _____

A

cholinergic

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9
Q

Skeletal muscle works through ___ receptors

A

ACh

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10
Q

Does ACh cross the BBB

A

NO

-so there are no psychological effects

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11
Q

What does ACh activate?

A
  • all autonomic ganglia (sympathetic and parasympathetic)

- skeletal muscle receptors

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12
Q

What does Pilocarpine do?

A

-very similar to ACh but it CAN penetrate BBB

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13
Q

What is pilocarpine the drug of choice for?

A

severe acute glaucoma (intraocular pressure)
-it causes immediate opening of drainage system of the eye

-also used for fixed focus

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14
Q

What does AChE do? (acetylcholinesterase)

A

degrades Ach in the synapse

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15
Q

What will inhibition of AChE do?

A

It will increase the activity of ACh in the synapse

i. e. it will have a cholinergic agonist effect
- increased activation of the parasympathetic NS

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16
Q

What is myasthenia gravis?

A

it is autoimmune destruction of Ach receptors at NMJ (neuromuscular junction)

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17
Q

What type of drugs can help with myasthenia gravis?

A

drugs which increase ACh activity can aid the symptoms
(no underlying pathology)

  • this is a short term solution because you are only increase Ach of the receptors that are left
  • eventually all receptors will die because that is a characteristic of this condition
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18
Q

What is alzheimer’s disease?

A

cholinergic neurons in brain undergo reduced activity and then die

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19
Q

How can you treat alzheimer’s disease?

A

You can administer drugs which can increase ACh activity in the brain can therefore treat some symptoms of AD, but not underlying pathology

20
Q

Neostigmine is a ??

A

AChE inhibitor

21
Q

How does neostigmine work?

A
  • stimulates the bladder and GI tract (used for urinary bladder disease and constipation)
  • it can also aid in symptoms of myasthenia gravis (it increases muscular strength and response)
22
Q

Donepazil (Aricept) is a ?

A

AChE inhibitor

23
Q

How does Donepazil (Aricept) work?

A

stimulates cholinergic neurons in brain

-can be used to treat symptoms of alzheimer’s disease

24
Q

Atropine is a ??

A

cholinergic antagonist

an antagonist of the parasympathetic nervous system

25
Q

Atropine = ____

A

belladonna (beautiful woman)

-pupil dilation

26
Q

Atropine does what?

A

-decreases CV response to parasympathetic stimulation
(heart rate increases and BP rises)
-bronchodilation and decreased respiratory sections
-antispasmodic effect on GI tract and other smooth muscles
-PUPIL DILATION

27
Q

Neocitran is a ??

A
  • antihistamine

- sympathomimetic

28
Q

Neocitran is an antihistamine and therefore ?

A

decreases parasympathetic nerve activity

29
Q

What are a few side effects of antihistamine?

A

-sedation and drying (atropinic)

30
Q

What does a sympathomimetic do?

A

obvs increase sympathetic receptor activity

31
Q

Who should not be taking Neocitran?

A

elderly people

  • can cause cardiovasculation issues (hypertension, MI)
  • can cause GI and GU issues (constipation and urinary retention)
32
Q

Scopolamine

A
  • strong CNS effect

- most-effective anti-nausea drug

33
Q

Tiotropium

A
  • derived from atropine

- inhaled bronchodilators (long-term effect)

34
Q

What are some overdose/side effects of blocking cholinergic system

A

Eyes:

  • sandy eye syndrome
  • loss of near vision

Mouth:
-dry pasty saliva

Gut:
-no movement, but sustained acid - causes nausea, vomiting, constipation, pain

No Sweat:

Bladder: flaccid bladder, constricted sphincter

But you won’t care - cause you’re paralyzed

35
Q

SLUDS

A
salivation
lacrimation
urination
defecation
sweat
36
Q

Jimson weed

datura stramonium

A

Main ingredients: belladonna alkaloids, atropine, scopolamine

  • anticholinergic
  • extracts of it used in treating asthma, intestinal cramps, diarrhea and bed-wetting

red as a beet
dry as a bone
blind as a bad
mad as a hatter

37
Q

What are NMJ blockers used for?

A

used in surgery
-it reduces the amount of anesthesia needed, allows rapid recovery of senses

-they are injected IV

38
Q

What is the order of muscular paralysis?

A

eyes, face, fingers, limbs, trunk, diaphragm

39
Q

Order of recovery from muscular paralysis?

A

diaphragm, trunk, limbs, fingers, face, eyes

40
Q

NMJ blockers can be…?

A

non-depolarizing or depolarizing

41
Q

How can NMJ blockers cause paralysis?

A

it desensitizes

-therefore a risk of paralysis

42
Q

Curare is ??

A

an NMJ blocker

  • it is amazonian poison
  • no longer used
43
Q

Is curare non-depolarizing or depolarizing?

A

non-depolarizing

44
Q

Succinylcholine is ??

A

an NMJ blocker

-causes twitching and fasciculation at first (from depolarization) but then flaccid paralysis

45
Q

Is succinylcholine non-depolarizing or depolarizing?

A

depolarizing

*only depolarizing NMJ used