Cholinergic pharm Flashcards
Direct acting cholinoceptor agonists (types)
esters of choline
alkaloids
acetycholine
direct acting cholinoceptor agonst
ester of choline - quaternary ammonium
rapidly hydrolysed
methacholine
DA cholinoceptor ag
ester of choline
quat amm
more resistant to hydrolysis than acetycholine
carbachol and bethanechol
DA cholinoceptor agonist
ester of choline - quat amm
very resistant to hydroylysis
Cevimeline
DA muscarinic agonist
choline ester - quat amm
pilocarpine
alkaloid (tert)
CNS activity
muscarinic activation predominant
nicotine
tert alkyloid
CNS activity
nicotinic activation predominant
lobeline
tert alkaloid (DA cholinoceptor ag)
CNS effects
nicotinic activation predominant
muscarine
quat alkaloid (cholinomemetic DA)
muscarinic activation predominant
Varenicline
direct nicotinic agonist
used to treat nicotine addiction
three groups of cholinesterase inhibitors (indirect acting cholinomimetics)
carbamates
simple alcohol esters
organophosphate
there are a couple others that dont fit in these three categories
neostigmine
cholinesterase inhibitor - carbamate
quat amm
physostigmine
cholinesterase inhibitor - carbamate
tert am
pyridostigmine
cholinesterase inhibitor - carbamate
rivastigmine
cholinesterase inhibitor - carbamate
ambenonium
cholinesterase inhibitor - carbamate
demecarium
cholinesterase inhibitor - carbamate
carbaryl
cholinesterase inhibitor - carbamate
high lipid solubility = rapid CNS effects
common insectoside
Edrophonium
cholinesterase inhibitor - simple alcohol ester
rapidly degraded
echothiophate
cholinesterase inhibitor - organophosphate
- Well absorbed topically - used as insecticides
- Well distributed into CNS
- Phosphorlyated AChE active site - very stable
- Undergoes aging - once aged you can’t get rid of the phos - you just have to make a new enzyme
- Before aging you can use pralidoxime (2-PAM) to restore enzyme function
soman
cholinesterase inhibitor - organophosphate