Cholinergics:Acetylcholinesterase inhibitors Flashcards Preview

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Flashcards in Cholinergics:Acetylcholinesterase inhibitors Deck (38)
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1
Q

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

A

Acetycholinesterase inhibitors

2
Q

Sites of action of acetylcholinesterase activity

A

Post-ganglionic parasympathetic neuroeffector junctions

  • Sympathetic and parasympathetic ganglia
  • Skeletal neuromuscular junction
  • CNS (if penetrate into the CNS)
3
Q

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

A

both

4
Q

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

A

if it can penetrate the CNS but must be lipophilic

5
Q

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

A

acetylated

removed via hydrolysis

6
Q

Edrophonium is

A

Non-substrate reversible AchE inhibitors

7
Q

Edrophonium acts by:

A

reversibly, competitive inhibitors for the substrate binding domain

8
Q

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

A

covalent

9
Q

Onset of Edrophonium is delayed/rapid onset

A

rapid onset

10
Q

Duration of action of Edrophonium

A

and short duration of action (minutes)

11
Q

Administration route of Edrophonium

A
  • not orally active; i.v. administration
12
Q

Uses of Physostigmine

A

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
Q

Physostigmine is slowly/rapidly reversible

A

slowly

14
Q

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

A

CNS effects

15
Q

Neostigmine: type of drug

A

“Reversible” substrate inhibitors of acetylcholinesterase

16
Q

Neostigmine is rapidly/slowly reversible

A

slowly

17
Q

Neostigmine has no CNS affects because

A

it’s a quarternary amines thus positively charged

18
Q

treatment of myasthenia gravis

A

Neostigmine

19
Q

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

A

Neostigmine

20
Q

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

A

(oral)

21
Q

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

A

Neostigmine

22
Q

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

A

IV

23
Q

During breakdown of Ach, the Ach is temporararily

__________ and then _______ is removed by hyrdolysis

A

acetylated

acetate

24
Q

process of Ach breakdown is

A

rapid

25
Q

Non-substrate reversible AchE inhibitors

A

Edrophonium

26
Q

Can edrophonium enter CNS?

why or why not?

A

nope

has charged amine

27
Q

Two types of reversibe AcheE substrate inhibitors

A

Neostigmine

Physostigmine

28
Q

Difference of delievery between neostigmine and physostigmine?

A

Neostigmine is quartanary amine so no CNS penetration

29
Q

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

A

Neostigmine–given orally

30
Q

Reversible Acetylcholinesterase used to treat wide eyed glaucoma

A

Physostigmine

31
Q

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

A

Physostigmine

32
Q

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

A

Ach stays in post cleft longer thus greater muscle contraction.

33
Q

Side affects of reversible AchE inhibitors

A

SLUDGE, hypotension, bradycardia, blurred vision

34
Q

What does SLUDGE stand for

A
salivation
lacrimation
urination
defication
GI issues
emisis = vomitting
35
Q

Why do we get blurred vision from reversible AchE inhibitors?

A

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

36
Q

Used to diagnose myasthenia gravis

used to treat myastenia gravis

A

edrophonium

neostigmine

37
Q

used to distinguish cholinergic from mysthenic crisis

A

edrophonium

38
Q

Drug used to reverse paralysis by competitive neuromuscular blocking agents

A

edrophonium