(9.1) Intro to Cholinergic drugs (Kruse) Flashcards

1
Q

What system does the cholinergic system act on?

A

Parasympathetic

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

What are the neurotransmitters and receptors for the parasympathetic system?

A

Neurotransmitters: ACh

Receptors : nAChR, mAChR

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

Subtypes and characteristics of AChRs

Receptor type: M1

Location:

Structural features:

Mechanism:

A

Location: Nerves

Structural features: GPCR, Gq/11

Mechanism: IP3 , DAG cascade

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

Subtypes and characteristics of AChRs

Receptor type: M2

Location:

Structural features:

Mechanism:

A

Location: Heart, nerves, smooth muscle

Structural features: GPCR, Gi/o

Mechanism: Inhibition of cAMP production, activation of K+ channels

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

Subtypes and characteristics of AChRs

Receptor type: M3

Location:

Structural features:

Mechanism:

A

Location: Glands, smooth muscle, endothelium

Structural features: GPCR, Gq/11

Mechanism: IP3, DAG cascade

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

Subtypes and characteristics of AChRs

Receptor type: M4

Location:

Structural features:

Mechanism:

A

Location: CNS

Structural features: GPCR, Gi/o

Mechanism: Inhibition of cAMP production

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

Subtypes and characteristics of AChRs

Receptor type: M5

Location:

Structural features:

Mechanism:

A

Location: CNS

Structural features: GPCR, Gq/11

Mechanism: IP3 , DAG cascade

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

Subtypes and characteristics of AChRs

Receptor type: Nn

Location:

Structural features:

Mechanism:

A

Location: Postganglionic cell body, dendrites, CNS

Structural features: alpha and beta only

Mechanism: Na+, K+ depolarizing ion channel

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

General rules to follow with organs and mAChR receptors:

GENERALLY…

In most organs _____ is predominant

A

M3

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

General rules to follow with organs and mAChR receptors:

GENERALLY…

____ predominates in the heart

A

M2

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

General rules to follow with organs and mAChR receptors:

GENERALLY…

Smooth muscle is predominated by _____ and ______

A

M2, M3

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

Define:

Cholinergic agonist

A

Mimic the actions of ACh on nAChRs and mAChRs

They are classified based on their MOA

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

Direct acting cholinergic agonists:

Choline esters

MOA?

Examples?

A

MOA = agonists at cholinergic receptors

Acetylcholine, Methacholine, Carbachol, Bethanechol

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

What are the three groups of AChE inhibitors?

A
  1. Alcohols (reversible)
  2. Carbamic acid esters (reversible but longer lasting than alcohols)
  3. Organophosphates (irreversible)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

General rule for actions of cholinergic agonists?

A

Rest and digest

Pupillary constriction (near vision), salivation, constriction/secretion of bronchi, slowing heart rate, gastric secretion, voiding of urine

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

—-DIDN”T ADD SPECIFICS FOR DRUGS; NEED TO COMPARE TO DRUG TABLE

A