Autonomic Parasympathetic Drugs: Acetylcholinesterase Inhibitors

Question 1

Indirect cholinomimetics inhibit

Answer 1

acetylcholinesterase

Question 2

Acetylcholinesterase degrades

Answer 2

acetylcholine (ACh)

Question 3

Acetylcholinesterase inhibitors increase

Answer 3

synaptic concentrations of ACh

Question 4

drug suffix of acetylcholinesterase inhibitors

Answer 4

“-stigmine”

Question 5

Acetylcholinesterase inhibitors enhance effects of

Answer 5

ACh at the NMJ (increase activity of NICOTINIC ACh receptors)

Question 6

Myasthenia gravis (MG)

Answer 6

myasthenia gravis (MG) → antibodies against nicotinic ACh receptors at motor endplate (skeletal muscle NMJ)

Question 7

Myasthenia gravis (MG) causes

Answer 7

progressive proximal weakness, ptosis, diplopia (inactivated nicotinic ACh receptors at motor endplate)

Question 8

Pyridostigmine

Answer 8

acetylcholinesterase inhibitor used as long-term treatment for MG

Question 9

Acetylcholinesterase inhibitors for the treatment of Myasthenia Gravis

Answer 9

acetylcholinesterase inhibitors increase ACh at NMJ endplate to outcompete MG antibodies

Question 10

Neostigmine

Answer 10

acetylcholinesterase inhibitor used as treatment for MG

Question 11

Edrophonium

Answer 11

acetylcholinesterase inhibitor that transiently reverses symptoms of MG

Question 12

Pyridostigmine, Neostigmine and Edrophonium are

Answer 12

quaternary amines and do not penetrate the CNS

Question 13

Edrophonium REVERSES

Answer 13

edrophonium REVERSES muscle weakness in undertreated MG patients (POSITIVE tensilon test)

Question 14

Tensilon test

Answer 14

Tensilon test → edrophonium reverses (positive) or fails to reverse (negative) muscle weakness

Question 15

Edrophonium FAILS to reverse muscle weakness during

Answer 15

edrophonium FAILS to reverse muscle weakness during cholinergic crisis (NEGATIVE tensilon test)

Question 16

Nondepolarizing neuromuscular blocking agents (e.g. tubocurarine, pancuronium, cisatracurium) inhibit

Answer 16

nicotinic ACh receptors at NMJ endplate

Question 17

Nondepolarizing neuromuscular blocking agents include

Answer 17

1. Tubocruraine
2. Pancuronium
3. Cisatracurium

Question 18

Acetylcholinesterase inhibitors (e.g neostigmine) reverse

Answer 18

nondepolarizing neuromuscular blockade

Question 19

Succinylcholine is a

Answer 19

depolarizing neuromuscular blocking agent (nicotinic ACh receptor AGONIST)

Question 20

Initial PHASE-1 of depolarizing blockade is

Answer 20

initial PHASE-1 of depolarizing blockade is IRREVERSIBLE (acetylcholinesterase inhibitors potentiate blockade)

Question 21

Acetylcholinesterase inhibitors can be used to treat

Answer 21

urinary retention (muscarinic activation)

Question 22

Physostigmine is an

Answer 22

acetylcholinesterase inhibitor with CENTRAL effects

Question 23

Atropine overdose

Answer 23

atropine overdose → “mad as a hatter, hot as a hare, blind as a bat” (reversed by physostigmine)

Question 24

Atropine overdose is revered by

Answer 24

physostigmine

Question 25

______ is a naturally occurring form of atropine

Answer 25

1. Belladonna flower

2. Jimson weed

Question 26

Physostigmine reverses

Answer 26

atropine overdose (peripheral and CENTRAL effects)

Question 27

Physostigmine (and organophosphates) enters CNS to

Answer 27

cause central cholinergic effects

Question 28

Acetylcholinesterase inhibitor toxicity

Answer 28

Diarrhea, Urination, Miosis, Bronchospasm, Bradycardia, Lacrimation, Salivation

Question 29

Acetylcholinesterase inhibitor toxicity includes

Answer 29

flaccid paralysis (NMJ nicotinic ACh receptor over-activation)

Question 30

Insecticides

Answer 30

insecticides (parathion, malathion, echothiophate) are organophosphates, a type of acetylcholinesterase inhibitor (also includes nerve agents and herbicides)

Question 31

Organophosphates are a major cause of

Answer 31

acute cholinergic toxicity (DUMBBELS)

Question 32

Pralidoxime reverses

Answer 32

organophosphate toxicity (DUMBBELS)

Question 33

Pralidoxime

Answer 33

pralidoxime regenerates acetylcholinesterase at muscarinic and NICOTINIC receptors (reverses cholinergic toxicity INCLUDING FLACCID PARALYSIS)

Question 34

Atropine reverses

Answer 34

atropine reverses both peripheral and CENTRAL muscarinic toxicity from organophosphate poisoning (pralidoxime is peripheral only)

Question 35

“Aging” of the organophosphate-cholinesterase complex leads to

Answer 35

irreversible binding

Question 36

______ is ineffective once aging of organophosphate- cholinesterase complex has occurred

Answer 36

pralidoxime

Question 37

________ is a acetylcholinesterase inhibitor used to treat Alzheimer’s disease

Answer 37

1. Galantamine
2. Rivastigmine
3. Donepezil

Question 38

Galantamine, Rivastigmine, and Donepezil penetrate the

Answer 38

CNS