Cholinergic pharm COPY Flashcards
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
Edrophonium
cholinesterase inhibitor - simple alcohol ester
rapidly degraded
soman
cholinesterase inhibitor - organophosphate
oxybutynin
muscarinic antagonist - tertiary amine
sarin
cholinesterase inhibitor - organophosphate
darifenacin
muscarinic antagonist - tertiary amine
mecamylamine
ganglionic blocking drug
methscopolamine
muscarinic antagonist - quaternary amine
hexamethonium
ganglionic blocking drug
rivastigmine
cholinesterase inhibitor - carbamate
lobeline
tert alkaloid (DA cholinoceptor ag)
CNS effects
nicotinic activation predominant
ambenonium
cholinesterase inhibitor - carbamate
propantheline
muscarinic antagonist - quaternary amine
solifenacin
muscarinic antagonist - tertiary amine
darifenacin
muscarinic antagonist - tertiary amine
Direct acting cholinoceptor agonists (types)
esters of choline
alkaloids
isoflurophate
cholinesterase inhibitor - organophosphate
demecarium
cholinesterase inhibitor - carbamate
carbaryl
cholinesterase inhibitor - carbamate
high lipid solubility = rapid CNS effects
common insectoside
donepezil
cholinesterase inhibitor used for alzheimers disease
improves cognition - but doesnt slow or cure the disease
pirenzepine
muscarinic antagonist - tertiary amine
M1 selective
fesoteridine
muscarinic antagonist - tertiary amine
pilocarpine
alkaloid (tert)
CNS activity
muscarinic activation predominant
muscarine
quat alkaloid (cholinomemetic DA)
muscarinic activation predominant
Tropicamide
muscarinic antagonist - tertiary amine
atropine methyl nitrate
muscarinic antagonist - quaternary amine
mepenzolate
muscarinic antagonist - tertiary amine
tolterodine
muscarinic antagonist - tertiary amine
M3 selective - bladder
Atropine
muscarinic antagonist - tertiary amine
non selective - inhibits M1/2/3
anticholinergic agents types
tertiary amines
quaternary amines
ganglionic blocking drugs
cholinesterase regenereators - 2PAM
diisopropylflurophosphate (DFP)
cholinesterase inhibitor - organophosphate
glycopyrrolate
muscarinic antagonist - quaternary amine
acetycholine
direct acting cholinoceptor agonst
ester of choline - quaternary ammonium
rapidly hydrolysed
neostigmine
cholinesterase inhibitor - carbamate
quat amm
nicotine
tert alkyloid
CNS activity
nicotinic activation predominant
methacholine
DA cholinoceptor ag
ester of choline
quat amm
more resistant to hydrolysis than acetycholine
dicyclomine
muscarinic antagonist - tertiary amine
Varenicline
direct nicotinic agonist
used to treat nicotine addiction
physostigmine
cholinesterase inhibitor - carbamate
tert am
carbachol and bethanechol
DA cholinoceptor agonist
ester of choline - quat amm
very resistant to hydroylysis
galantamine
cholinesterase inhibitor used in treatment of alzheimers disease
pralidoxime (2-PAM)
cholinesterase regenerator - it binds to cholinesterase and inhibits it but not as tight as organophosphates so it can be used to knock them off if they havent aged yet
malathion
cholinesterase inhibitor - organophosphate
parathion
cholinesterase inhibitor - organophosphate
tacrine
cholinesterase inhibitor used for treatment of alzheimers disease
copolamine
muscarinic antagonist - tertiary amine
trospium
muscarinic antagonist - tertiary amine
Cevimeline
DA muscarinic agonist
choline ester - quat amm
homatropine
muscarinic antagonist - tertiary amine
trimethaphan
ganglionic blocking drug
lacks CNS effects
pyridostigmine
cholinesterase inhibitor - carbamate
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
ipratropium
muscarinic antagonist - quaternary amine