Cholinesterase Inhibitors -Therapeutics

Question 1

What are the types of cholinesterases?

Answer 1

Acetylcholinesterase
Plasma Cholinesterase

Question 2

What substrate specificity does Plasma Cholinesterase have?

Answer 2

-Acetylcholine
-Succinylcholine
-Local anesthetics (procaine)

Question 3

Where do reversible anti-cholinesterase agents bind?

Answer 3

Muscarinic receptors (M1,M2,M3)
-Smooth muscles (M3)
-Exocrine glands (M3)
-Heart (M2)

Question 4

Where do irreversible anti-cholinesterase agents bind?

Answer 4

Nicotinic receptors (Nn,Nm)
-Autonomic Ganglia (Nn)
-Skeletal Muscle (Nm)

Question 5

What is a distinguishing structural feature of Acetylcholinesterase inhibitors?

Answer 5

Quaternary amine
positive charge
-does not cross BBB

Question 6

What can Physostigmine do that other AChE Inhibitors can not?

Answer 6

can cross BBB
-antidote to antimuscarinic poisoning

Question 7

What are some types of Organophosphates?

Answer 7

-Sarin
-Echothiophate
-Malathion (insecticide)

Question 8

What does Pralidoxime do?

Answer 8

-antidote to AChE poisoning
-can hydrolyze the organophosphate if treated before aging occurs
-combine with Atropine to cross BBB

Question 9

What drug treats Alzhemier’s disease?

Answer 9

Reversible anticholinesterase agents
-Donepezil (Aricept)
-Rivastigmine (Exelon) carbamate AChE inhibitor
-Galantamine (Razadyne)
-Memantine (Namenda) NMDA receptor antagonist

Question 10

What are contraindications to the use of parasympathomimetic drugs?

Answer 10

-Asthma and COPD
-Coronoary deficiency
-Peptic Ulcer
-Obstruction of the urinary/GI tract
-Epilepsy