Cholinomimetics

Question 1

Metacholine

Answer 1

Direct cholinomimetic
It is a cholinester
3x more resistant to cholinesterases than acetylcholine
Muscarinic effects only (muscarinic agonist)
Causes bronchoconstriction => used in asthma diagnosis

Question 2

Pilocarpine

Answer 2

Direct Cholinomimetic
Alkaloid
Tertiary amine
Selective M effects (M3)
Increased secretion and contraction of SM
Use: xerostomia, glaucoma, sjogren disease

Question 3

Nicotine

Answer 3

Direct cholinomimetic
Alkaloid
Tertiary amine
Selective nicotinic effects
Potent poison
Use: nicotine replacement therapies

Question 4

varenicline

Answer 4

Direct cholinomimetic
Synthetic agonist
Partial Nn receptor agonist
Effects the Nn receptor in the reward pathway
Decreases smoking cravings
Side effects: depression, suicidal thoughts, aggressiveness, anxiety, weight gain

Question 5

Edrophonium

Answer 5

Indirect cholinomimetic
Competitive reversible choniesterase inhibitor
Short duration of action (5-15 min)
Use: myasthenia gravis diagnosis

Question 6

Donepezil

Answer 6

Indirect cholinomimetic
Competitive reversible cholinesterase inhibitor
Use: Alzheimer’s disease

Question 7

Rivastigmine

Answer 7

Indirect cholinomimetic
Non competitive reversible cholinesterase inhibitor
Tertiary amine
Use: transdermal patch in Alzheimer’s disease

Question 8

Neostigmine

Answer 8

Indirect cholinesterase
Non competitive reversible cholinesterase inhibitor
Quaternary amine
Peripheral effects only
Use: paralytic ileum, bladder and stomach atony, suppression of curare effect
Highly bradycardial
0.5-2 hours duration of action

Question 8

Pyridostigmine

Answer 8

Indirect cholinomimetic
Non competitive reversible cholinesterase inhibitor
Quaternary amine
3-6 hours duration of action
Use: per os treatment for myasthenia gravis