Lecture 6 - Cholinergic Agonists

Question 1

______ receptors use ion channels

Answer 1

nicotinic

Question 2

nicotinic affects ganglion of both ___ and ___

Answer 2

SNS

PNS

Question 3

nicotinic affects _____ muscle

Answer 3

skeletal

Question 4

Muscarinic receptors are _____ mediated

Answer 4

G-protein

Question 5

What do muscarinic receptors affect ?

Answer 5

effector organs/tissues of parasympathetic

Question 6

Sweat receptors on the ____ are adrenergic

Answer 6

palms

Question 7

Sweat receptors everywhere else are ____

Answer 7

cholinergic (but still part of sympathetic system)

Question 8

All preganglionic synapses are _____

Answer 8

cholinergic

Question 9

Skeletal muscle works through ___ receptors

Answer 9

ACh

Question 10

Does ACh cross the BBB

Answer 10

NO

-so there are no psychological effects

Question 11

What does ACh activate?

Answer 11

• all autonomic ganglia (sympathetic and parasympathetic)

- skeletal muscle receptors

Question 12

What does Pilocarpine do?

Answer 12

-very similar to ACh but it CAN penetrate BBB

Question 13

What is pilocarpine the drug of choice for?

Answer 13

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

-also used for fixed focus

Question 14

What does AChE do? (acetylcholinesterase)

Answer 14

degrades Ach in the synapse

Question 15

What will inhibition of AChE do?

Answer 15

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

Question 16

What is myasthenia gravis?

Answer 16

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

Question 17

What type of drugs can help with myasthenia gravis?

Answer 17

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

Question 18

What is alzheimer’s disease?

Answer 18

cholinergic neurons in brain undergo reduced activity and then die

Question 19

How can you treat alzheimer’s disease?

Answer 19

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

Question 20

Neostigmine is a ??

Answer 20

AChE inhibitor

Question 21

How does neostigmine work?

Answer 21

• 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)

Question 22

Donepazil (Aricept) is a ?

Answer 22

AChE inhibitor

Question 23

How does Donepazil (Aricept) work?

Answer 23

stimulates cholinergic neurons in brain

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

Question 24

Atropine is a ??

Answer 24

cholinergic antagonist

an antagonist of the parasympathetic nervous system

Question 25

Atropine = ____

Answer 25

belladonna (beautiful woman) | -pupil dilation

Question 26

Atropine does what?

Answer 26

-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

Question 27

Neocitran is a ??

Answer 27

- antihistamine | - sympathomimetic

Question 28

Neocitran is an antihistamine and therefore ?

Answer 28

decreases parasympathetic nerve activity

Question 29

What are a few side effects of antihistamine?

Answer 29

-sedation and drying (atropinic)

Question 30

What does a sympathomimetic do?

Answer 30

obvs increase sympathetic receptor activity

Question 31

Who should not be taking Neocitran?

Answer 31

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

Question 32

Scopolamine

Answer 32

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

Question 33

Tiotropium

Answer 33

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

Question 34

What are some overdose/side effects of blocking cholinergic system

Answer 34

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

Question 35

SLUDS

Answer 35

``` salivation lacrimation urination defecation sweat ```

Question 36

Jimson weed | datura stramonium

Answer 36

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

Question 37

What are NMJ blockers used for?

Answer 37

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

Question 38

What is the order of muscular paralysis?

Answer 38

eyes, face, fingers, limbs, trunk, diaphragm

Question 39

Order of recovery from muscular paralysis?

Answer 39

diaphragm, trunk, limbs, fingers, face, eyes

Question 40

NMJ blockers can be...?

Answer 40

non-depolarizing or depolarizing

Question 41

How can NMJ blockers cause paralysis?

Answer 41

it desensitizes | -therefore a risk of paralysis

Question 42

Curare is ??

Answer 42

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

Question 43

Is curare non-depolarizing or depolarizing?

Answer 43

non-depolarizing

Question 44

Succinylcholine is ??

Answer 44

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

Question 45

Is succinylcholine non-depolarizing or depolarizing?

Answer 45

depolarizing | *only depolarizing NMJ used