Cholinergics:Acetylcholinesterase inhibitors

Question 1

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

Answer 1

Acetycholinesterase inhibitors

Question 2

Sites of action of acetylcholinesterase activity

Answer 2

Post-ganglionic parasympathetic neuroeffector junctions

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

Question 3

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

Answer 3

both

Question 4

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

Answer 4

if it can penetrate the CNS but must be lipophilic

Question 5

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

Answer 5

acetylated

removed via hydrolysis

Question 6

Edrophonium is

Answer 6

Non-substrate reversible AchE inhibitors

Question 7

Edrophonium acts by:

Answer 7

reversibly, competitive inhibitors for the substrate binding domain

Question 8

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

Answer 8

covalent

Question 9

Onset of Edrophonium is delayed/rapid onset

Answer 9

rapid onset

Question 10

Duration of action of Edrophonium

Answer 10

and short duration of action (minutes)

Question 11

Administration route of Edrophonium

Answer 11

• not orally active; i.v. administration

Question 12

Uses of Physostigmine

Answer 12

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)

Question 13

Physostigmine is slowly/rapidly reversible

Answer 13

slowly

Question 14

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

Answer 14

CNS effects

Question 15

Neostigmine: type of drug

Answer 15

“Reversible” substrate inhibitors of acetylcholinesterase

Question 16

Neostigmine is rapidly/slowly reversible

Answer 16

slowly

Question 17

Neostigmine has no CNS affects because

Answer 17

it’s a quarternary amines thus positively charged

Question 18

treatment of myasthenia gravis

Answer 18

Neostigmine

Question 19

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

Answer 19

Neostigmine

Question 20

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

Answer 20

(oral)

Question 21

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

Answer 21

Neostigmine

Question 22

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

Answer 22

IV

Question 23

During breakdown of Ach, the Ach is temporararily

__________ and then _______ is removed by hyrdolysis

Answer 23

acetylated

acetate

Question 24

process of Ach breakdown is

Answer 24

rapid

Question 25

Non-substrate reversible AchE inhibitors

Answer 25

Edrophonium

Question 26

Can edrophonium enter CNS?

why or why not?

Answer 26

nope

has charged amine

Question 27

Two types of reversibe AcheE substrate inhibitors

Answer 27

Neostigmine

Physostigmine

Question 28

Difference of delievery between neostigmine and physostigmine?

Answer 28

Neostigmine is quartanary amine so no CNS penetration

Question 29

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

Answer 29

Neostigmine–given orally

Question 30

Reversible Acetylcholinesterase used to treat wide eyed glaucoma

Answer 30

Physostigmine

Question 31

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

Answer 31

Physostigmine

Question 32

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

Answer 32

Ach stays in post cleft longer thus greater muscle contraction.

Question 33

Side affects of reversible AchE inhibitors

Answer 33

SLUDGE, hypotension, bradycardia, blurred vision

Question 34

What does SLUDGE stand for

Answer 34

salivation
lacrimation
urination
defication
GI issues
emisis = vomitting

Question 35

Why do we get blurred vision from reversible AchE inhibitors?

Answer 35

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

Question 36

Used to diagnose myasthenia gravis

used to treat myastenia gravis

Answer 36

edrophonium

neostigmine

Question 37

used to distinguish cholinergic from mysthenic crisis

Answer 37

edrophonium

Question 38

Drug used to reverse paralysis by competitive neuromuscular blocking agents

Answer 38

edrophonium