Indirectly Acting Cholinomimetics Cholinesterase Inhibitors

Question 1

Reversible cholinesterase inhibition

Answer 1

Neostigmine

Question 2

Synthetic analog of physostigmine
Poor penetration of BBB
Direct stimulation of Nm receptors

Answer 2

Neostigmine

Question 3

Rx: myasthenia gravis,
reversal of non-depolarizing neuromuscular blockade
Toxicity: muscarinic and nicotinic excess
Contraindication: intestinal obstruction

Answer 3

Neostigmine

Question 4

Reversible cholinesterase inhibition

Answer 4

Edrophonium

Question 5

Structure lacks ester group
Activates Nm receptors directly
Rapid onset, short duration of action

Answer 5

Edrophonium

Question 6

Rx: diagnosis of myasthenia gravis
differential diagnosis of too little or
too much AchE inhibitor in rx of myasthenia gravis
Toxicity: bradycardia, cardiac standstill
Contraindication: intestinal blockade or urinary obstruction

Answer 6

Edrophonium

Question 7

Reversible cholinesterase inhibition

Answer 7

Physostigmine

Question 8

Alkaloid from the calabar bean, Physostigma venosum
Crosses BBB
Duration ~2 hrs

Answer 8

Physostigmine

Question 9

Rx: antidote for muscarinic antagonist poisoning
Toxicity: convulsions, respiratory and CV depression
Contraindications: asthma, CV disease
intestinal obstruction

Answer 9

Physostigmine

Question 10

Inhibits only acetylcholinesterase

Rx for Alzheimer’s Disease

Answer 10

Donepezil