Chapter 7-8: Cholinoceptor Drugs Flashcards

Test 2

1
Q

Where are mAch-R?

A

Nerves
Heart/smooth muscle
Glands/endothelium

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Where are nAch-R?

A

NMJ
Autonomic ganglion

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Muscarine mimics effects of what NS?

A

PNS

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

What can bind to the cholinoceptors?

A

Choline esters and Alkaloids

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

What is Mycetism?

A

Toxicity of Muscarinic agonism
Brightly colored mushrooms

Vomiting, diarrhea, drooling, decreased HR/RR/BP, shock

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

What is Tx for Mycetism?

A

Antimuscarinic:

2mg Atropine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

T/F: Nicotine only binds to nAch-R?

A

T

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Why do you see tremors when smoking?

A

Nicotine at the NMJ binds to the nAch-R causing small contractions

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What does the M1,3,5 receptors do?

A

Stimulatory
Increase phospholipase C

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

What does M2,4 receptors do?

A

Inhibitory
inhibits adenylyl cyclase

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

List the major clinical uses of cholinomimetic agonists

A
  • Tx of Glaucoma: Carbachol/pilocarpine - reduce intraocular pressure with glaucoma
  • MG: neostigmine/pyridostigmine- improve muscle strength by increasing acetylcholine levels at NMJ

-Alzheimer’s: Cholinesterase INHIBITOR donepezil - manage symptoms by enhancing cholinergic function in the brain

-Postoperative Ileus and Urinary Retention: Bethanechol- stimulate bowel and bladder function

-Xerostomia (Dry Mouth): Pilocarpine and cevimeline- stimulate salivary secretion in patients with dry mouth, often due to Sjögren’s syndrome or radiation therapy.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Tx of Glaucoma

A

Carbachol/pilocarpine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Management of MG:

A

-stigmine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Management of Alzheimers

A

donepezil

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Postoperative Ileus and Urinary Retention Tx

A

Bethanechol

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Dry mouth Tx:

A

“Xerostomia”

Pilocarpine
cevimeline

17
Q

T/F: Esters of Choline cross barriers easily

A

F

Large and charged. insoluble in lipids and doesnt cross barriers easily

18
Q

Describe the Pharmacokinetics for Esters of Choline

A

A: poor
D: poor
M: -Ach: rapid (5-20 secs)
- Methacholine: 3x longer
- Carbachol/Bethanechol - resistant to hydrolysis: 4 min to hours

19
Q

What is the Betel nut?

A

Arecoline Alkaloid

similar effects to nicotine

used alot in various places in the world and has a red color

20
Q

Nicotine is very ____ soluble

A

lipid

21
Q

Nicotine stimulates _______ NS

A

ALL OF THE

22
Q

Which NS responses dominate the others in response to nicotine?

A

Sympathetic

23
Q

Describe Pharmacokinetics with Alkaloids

A

A: Pilocarpine, Nicotine, Lobeline
(-INE)!!!!!!!!! - well
-Muscarine - charged so less well
E: Kidneys- enhanced by acidification of urine

24
Q

T/F: Atropine in Open Angle glaucoma is contraindicated and is a medical emergency

A

F

Closed-angle (Narrow angle)

25
Q

What is glaucoma?

A

excess intraocular fluid

26
Q

cholinomimetics Organ effects: Eye

A

Constriction of pupil “miosis”

Increases intraocular drainage

27
Q

cholinomimetics Organ effects: CVS

A

-Reduction in peripheral vascular resistance
-vasodilation
-decrease BP
-reflex tachycardia
large doses bradycardia

28
Q

cholinomimetics Organ effects: Respiratory

A

bronchials contract
secretions increased

29
Q

cholinomimetics Organ effects: GI

A

Increased GI activity
relaxed sphincter

30
Q

cholinomimetics Organ effects: CNS

A

release dopamine, serotonin, GABA, NE

enhance cognitive functions

31
Q

Define the different types of glaucoma and the use of cholinomimetics

A

Open angled: cholinomimetic drugs like pilocarpine can constrict the pupil and increase drainage through the canal of Schlemm.

Closed angled: the iris is pushed forward, cholinomimetics can worsen the condition by further constricting the angle and impeding drainage. This can lead to a medical emergency.

32
Q

cholinomimetics Organ effects: NMJ

A

immediate depolarization of end plate
muscle contraction

33
Q

What is depolarization blockade?

A

When the cell is continuously being depolarized and cant repolarize causing flaccid paralysis

Ex) Succs

34
Q
A