Cholinergics:Acetylcholinesterase inhibitors Flashcards Preview

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Flashcards in Cholinergics:Acetylcholinesterase inhibitors Deck (38)
1

agents that enhance the effects of endogenously released acetylcholine by blocking its natural breakdown by the enzyme acetylcholinesterase

Acetycholinesterase inhibitors

2

Sites of action of acetylcholinesterase activity

Post-ganglionic parasympathetic neuroeffector junctions
- Sympathetic and parasympathetic ganglia
- Skeletal neuromuscular junction
- CNS (if penetrate into the CNS)

3

Sites of action of acetylcholinesterase activity
is it sympathetic, parasympathetic or neither or both
ganglia

both

4

Sites of action of acetylcholinesterase activity: is it in CNS?

if it can penetrate the CNS but must be lipophilic

5

During breakdown of Ach, Ach is temporarily _____ and then acetate is removed via:

acetylated
removed via hydrolysis

6

Edrophonium is

Non-substrate reversible AchE inhibitors

7

Edrophonium acts by:

reversibly, competitive inhibitors for the substrate binding domain

8

Edrophonium is truly reversible competitive enZ inhibitor and non-covalent or covalent binding

covalent

9

Onset of Edrophonium is delayed/rapid onset

rapid onset

10

Duration of action of Edrophonium

and short duration of action (minutes)

11

Administration route of Edrophonium

- not orally active; i.v. administration

12

Uses of Physostigmine

1) treatment of chronic wide angle glaucoma (ophthalmic application)
2) toxicity by antimuscarinic drug poisoning (i.v.; penetrates into the CNS and can treat CNS toxicity by these agents)

13

Physostigmine is slowly/rapidly reversible

slowly

14

Physostigmine is a tertiary amine (lipophilic) which can penetrate cell membranes and thus can have

CNS effects

15

Neostigmine: type of drug

“Reversible” substrate inhibitors of acetylcholinesterase

16

Neostigmine is rapidly/slowly reversible

slowly

17

Neostigmine has no CNS affects because

it's a quarternary amines thus positively charged

18

treatment of myasthenia gravis

Neostigmine

19

prevention and treatment of post-operative atony of gut and bladder (oral)

Neostigmine

20

Delivery of neostigmine for prevention and treatment of post-operative atony of gut and bladder

(oral)

21

reversal of paralysis by competitive neuromuscular blocking drugs (i.v.)

Neostigmine

22

reversal of paralysis by competitive neuromuscular blocking drugs by Neostigmine; delivery method:

IV

23

During breakdown of Ach, the Ach is temporararily
__________ and then _______ is removed by hyrdolysis

acetylated
acetate

24

process of Ach breakdown is

rapid

25

Non-substrate reversible AchE inhibitors

Edrophonium

26

Can edrophonium enter CNS?
why or why not?

nope
has charged amine

27

Two types of reversibe AcheE substrate inhibitors

Neostigmine
Physostigmine

28

Difference of delievery between neostigmine and physostigmine?

Neostigmine is quartanary amine so no CNS penetration

29

Drug promotes signaling at neuromuscluar jnx and prevents muscle weakness that you get form Myasthia Gravis

Neostigmine--given orally

30

Reversible Acetylcholinesterase used to treat wide eyed glaucoma

Physostigmine

31

If you are suffering from toxicity by antimuscarinic drug poisoning (penetrates into the CNS and can tx CNS toxicity)

Physostigmine

32

Neostigmine works by nesting in the AchE and get degraded so it slowly breaks down: how does this affect muscle contraction?

Ach stays in post cleft longer thus greater muscle contraction.

33

Side affects of reversible AchE inhibitors

SLUDGE, hypotension, bradycardia, blurred vision

34

What does SLUDGE stand for

salivation
lacrimation
urination
defication
GI issues
emisis = vomitting

35

Why do we get blurred vision from reversible AchE inhibitors?

bc we are promoting PNS activity in cliliary msl so get lots of contraction of ciliary msl

36

Used to diagnose myasthenia gravis
used to treat myastenia gravis

edrophonium
neostigmine

37

used to distinguish cholinergic from mysthenic crisis

edrophonium

38

Drug used to reverse paralysis by competitive neuromuscular blocking agents

edrophonium