Cholinomimetics

Question 1

Two natural Cholinomimetics

Answer 1

(1) Muscarine

(2) Pilocarpine

Question 2

A sialogen that is a cholinomimetic

Answer 2

Pilocarpine

Question 3

4 Synthetic Cholinergic Agents:

Answer 3

(1) Cevimeline
(2) Methacholine
(3) Bethanechol
(4) Carbachol

Question 4

Cholinomimetic that’s susceptible to breakdown by esterases.

Answer 4

Methacholine

Question 5

Cholinomimetic that has strong nicotinic receptor activity.

Answer 5

Carbachol

Question 6

Contraindications to the use of Choline esters.

Answer 6

Peptic ulcers
Asthma
Hyperthyroid
Coronary Insufficiency
Organic obstruction in the bladder of the GI tract

Question 7

Sarin and “Thios” are…

Answer 7

Irreversible acetylcholinesterase inhibitors

Question 8

How do AchE’s age? And what happens when they age?

Answer 8

They age by losing alkyl groups.

They can no longer break down Ach once they’ve aged.

Question 9

Reversible AchE Inhibitors

Answer 9

Edrophonium
Neostigmine
Physostigmine

Question 10

IRReversible AchE Inhibitors

Answer 10

Sarin
Malathion
Parathion
Echothiophate

Question 11

How to AchE inhibitors work chemically?

Answer 11

They covalently bind to the Serine-OH group at the esteratic binding site of the enzyme.

Question 12

Two binding sites of AchE

Answer 12

1) Ionic binding site

2) Esteratic binding site

Question 13

A reversible AchE Inhibitor that binds to the AchE ionic binding site, but not to the esteratic binding site.

Answer 13

Edrophonium

Question 14

Phosphorylation of AchE enzyme causes what?

Answer 14

IRReversible INHIBITION

Question 15

Reactivates phosphorylated AchE

Answer 15

Pralidoxime

BUT it only works if the enzyme hasn’t aged yet.

Question 16

Carbamyl inhibitors of AchE

Answer 16

Stigmines:

Physostigmine
Neostigmine (N+)

Question 17

Neostigmine (N+)

Answer 17

Doesn’t cross the blood brain barrier bc it’s charged.

Question 18

Used to diagnose Myasthenia Gravis

Answer 18

Edrophonium

Question 19

What is myasthenia gravis?

Answer 19

The body attacks the nicotinic receptors on muscle, causing muscle weakness.

Question 20

Irreversible Organophosphate Inhibitors of AchE

Answer 20

All the THIOS!

Echothiophate (N+)
Sarin
Malathion
Parathion

Question 21

Used to reduce intraocular pressure.

Answer 21

Pilocarpine

Echothiophate (N+)

Question 22

Not broken down by insects

Answer 22

Milothion and Parathion

Question 23

Used for pediculosis (lice)

Answer 23

Malathion

Question 24

Respiratory paralysis is caused by….

Answer 24

Too much Ach at the Nm receptor site.