L11: Cholinergic Agonists Flashcards

(31 cards)

1
Q

what is ACh synthesized from

A

choline + Acetyl CoA

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

ACh is released in response to ______ which increases the _______ influx

A

depolarization
Ca+

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

the release of ACh sitmulates what receptors

A

nicotinic or muscarinic

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

how is ACh inactivated?

A
  • gets hydrolyzed by acetylcholinesterase (AChE)
  • choline gets endocytosed into terminal
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

all use of Bethanecol is considered

A

extra label

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

what are the indications of Bethanecol

A
  • decreases bladder contractility in dogs/cats
  • potential GI indications…cecal displacement/dislocation in cows; equine gastric ulcer syndrome
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

why is Bethanecol not a slay choice drug for large animals

A

REQUIRES COMPOUNDING
& fucks up GI
- cecal displacement/dislocation in cows
- equine gastric ulcer syndrome

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

pharmacodynamics of Bethanecol (what systems does it affect most)

A

affects GI and urinary most strongly

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

administration method of Bethanecol

A

PO in dogs
SC in large animals

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

adverse effects of Bethanecol

A

overextension of therapeutic effect
particularly colic in horses

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

contradictions of Bethanecol

A
  • Obstruction - GI impaction, torsion, blocked urethra
  • gastric ulcers (small animals)
  • hyperthyroidism
  • hypotension, bradycardia
  • any animal with asthma b/c risk of bronchoconstriction
  • epilepsy
  • hypersensitivity
  • recent GI surgery
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

motor nerves release ACh onto ____ receptors of the skeletal muscle neuromuscular joints

A

Nm

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

explain the signaling at neuromuscular junction

A
  • motor neurons release ACh onto Nm receptors
  • Na channels open and depolarize the end plate
  • magnitude of voltage chance is proportional to the amount of ACh released
  • once threshold is reached adjacent V-gated Na channels open, transmitting the AP along the muscle fiber and causing contraction
  • ACh is broken down and Na+ channels reset
  • if ACh is present in the neuromuscular junction for too long, receptors will depolarize
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Myasthenia like syndrome is an _____ attack against ______ receptors

A

autoimmune
Nm

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

what is myasthenia like syndrome treated with

A

methimazole

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

T/F: myasthenia like syndrome is congenital

17
Q

indications for Neostigmine use

A

treatment of GI or bladder atony (not moving), esp. following Sx
Reversal of neuromuscular blockade

18
Q

Neostigmine is labeled for use in what animals

A

sheep, swine, cattle, horses

19
Q

what is the extra label use of neostigmine

A

diagnosis and treatment of myasthenia like syndrome

20
Q

Neostigmine ROI

21
Q

metabolism of Neostigmine

A

plasma cholinesterases and liver

22
Q

OD of what drug may cause a “cholinergic crisis”

23
Q

elimination of neostigmine

A

primarily urinary, half life is ~40 seconds

24
Q

labeled use of Pyridostigmine bromide

A

cases w/ canine myasthenia like syndrome
extra label use in cats

25
ROI pyridostigmine bromide
PO
26
metabolism of pyridostigmine bromide
plasma cholinesterases and liver
27
elimination of pyridostigmine bromide
primarily urinary half life about 2 min
28
adverse effects of pyridostigmine bromide
* **intussusception** * tolerance due to downregulation of Nm receptors
29
what are the cholinesterase inhibitors
* neostigmine * pyridostigmine
30
what drug is a direct acting cholinergic agonist
bethanechol
31