Lecture 6 - Cholinergic Agonists Flashcards Preview

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Flashcards in Lecture 6 - Cholinergic Agonists Deck (45)
1

______ receptors use ion channels

nicotinic

2

nicotinic affects ganglion of both ___ and ___

SNS
PNS

3

nicotinic affects _____ muscle

skeletal

4

Muscarinic receptors are _____ mediated

G-protein

5

What do muscarinic receptors affect ?

effector organs/tissues of parasympathetic

6

Sweat receptors on the ____ are adrenergic

palms

7

Sweat receptors everywhere else are ____

cholinergic (but still part of sympathetic system)

8

All preganglionic synapses are _____

cholinergic

9

Skeletal muscle works through ___ receptors

ACh

10

Does ACh cross the BBB

NO
-so there are no psychological effects

11

What does ACh activate?

-all autonomic ganglia (sympathetic and parasympathetic)
-skeletal muscle receptors

12

What does Pilocarpine do?

-very similar to ACh but it CAN penetrate BBB

13

What is pilocarpine the drug of choice for?

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

-also used for fixed focus

14

What does AChE do? (acetylcholinesterase)

degrades Ach in the synapse

15

What will inhibition of AChE do?

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

16

What is myasthenia gravis?

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

17

What type of drugs can help with myasthenia gravis?

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

18

What is alzheimer's disease?

cholinergic neurons in brain undergo reduced activity and then die

19

How can you treat alzheimer's disease?

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

20

Neostigmine is a ??

AChE inhibitor

21

How does neostigmine work?

-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

Donepazil (Aricept) is a ?

AChE inhibitor

23

How does Donepazil (Aricept) work?

stimulates cholinergic neurons in brain
-can be used to treat symptoms of alzheimer's disease

24

Atropine is a ??

cholinergic antagonist
(an antagonist of the parasympathetic nervous system)

25

Atropine = ____

belladonna (beautiful woman)
-pupil dilation

26

Atropine does what?

-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

Neocitran is a ??

-antihistamine
-sympathomimetic

28

Neocitran is an antihistamine and therefore ?

decreases parasympathetic nerve activity

29

What are a few side effects of antihistamine?

-sedation and drying (atropinic)

30

What does a sympathomimetic do?

obvs increase sympathetic receptor activity

31

Who should not be taking Neocitran?

elderly people

-can cause cardiovasculation issues (hypertension, MI)
-can cause GI and GU issues (constipation and urinary retention)

32

Scopolamine

-strong CNS effect
-most-effective anti-nausea drug

33

Tiotropium

-derived from atropine
-inhaled bronchodilators (long-term effect)

34

What are some overdose/side effects of blocking cholinergic system

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

SLUDS

salivation
lacrimation
urination
defecation
sweat

36

Jimson weed
(datura stramonium)

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

What are NMJ blockers used for?

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

-they are injected IV

38

What is the order of muscular paralysis?

eyes, face, fingers, limbs, trunk, diaphragm

39

Order of recovery from muscular paralysis?

diaphragm, trunk, limbs, fingers, face, eyes

40

NMJ blockers can be...?

non-depolarizing or depolarizing

41

How can NMJ blockers cause paralysis?

it desensitizes
-therefore a risk of paralysis

42

Curare is ??

an NMJ blocker
-it is amazonian poison
-no longer used

43

Is curare non-depolarizing or depolarizing?

non-depolarizing

44

Succinylcholine is ??

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

45

Is succinylcholine non-depolarizing or depolarizing?

depolarizing
*only depolarizing NMJ used