3: Muscarinic Receptor Binding And Anti-AChE

Question 0

Bethanechol

Answer 0

Non selective muscarinic agonist
Poorly absorbed by gut
Used in bladder dysfunction

Question 1

Darifenacin

Answer 1

Selective M3 antagonist
Used in treatment of bladder incontinence
M3-> Gq/11 -> exocrine glands, smooth muscle relaxation, oxytinic cells

Question 2

Pilocarpine

Answer 2

Non selective muscarinic agonist
Used in treatment of glaucoma - absorbed across conjunctiva, contracts ciliary mm, facilitating aqueous humour drainage and decreasing intraocular pressure

Question 3

Atropine

Answer 3

Non selective muscarinic antagonist

Question 4

Edrophonium

Answer 4

Short acting anti-acetylcholinesterase
Quaternary ammonium compound
Reversible ionic interacting
Used to diagnose myasthenia gravis

Question 5

Neostigmine

Answer 5

Medium anticholinesterase
Weak covalent interaction whereby AChE is carbamoylated
Hydrolysis occurs slowly
Used intravenously to reverse neuromuscular blockade post surgery, and orally to treat myasthenia gravis

Question 6

Dyflos

Answer 6

Irreversible antiAChE

Question 7

Malathion

Answer 7

Irreversible antiAChE

Question 8

Pralidoxime

Answer 8

Reverses organophosporus inhibition.
Mechanism: removes phosphorylated serine with strong nucleophile/oxine group
Must occur up to a few hours after