Cholinergic pharm COPY COPY 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
sarin
cholinesterase inhibitor - organophosphate
parathion
cholinesterase inhibitor - organophosphate
malathion
cholinesterase inhibitor - organophosphate
isoflurophate
cholinesterase inhibitor - organophosphate
diisopropylflurophosphate (DFP)
cholinesterase inhibitor - organophosphate
donepezil
cholinesterase inhibitor used for alzheimers disease
improves cognition - but doesnt slow or cure the disease
tacrine
cholinesterase inhibitor used for treatment of alzheimers disease
galantamine
cholinesterase inhibitor used in treatment of alzheimers disease
anticholinergic agents types
tertiary amines
quaternary amines
ganglionic blocking drugs
cholinesterase regenereators - 2PAM
Atropine
muscarinic antagonist - tertiary amine
non selective - inhibits M1/2/3
copolamine
muscarinic antagonist - tertiary amine
homatropine
muscarinic antagonist - tertiary amine
pirenzepine
muscarinic antagonist - tertiary amine
M1 selective
Tropicamide
muscarinic antagonist - tertiary amine
tolterodine
muscarinic antagonist - tertiary amine
M3 selective - bladder
dicyclomine
muscarinic antagonist - tertiary amine
fesoteridine
muscarinic antagonist - tertiary amine
mepenzolate
muscarinic antagonist - tertiary amine
solifenacin
muscarinic antagonist - tertiary amine
oxybutynin
muscarinic antagonist - tertiary amine
darifenacin
muscarinic antagonist - tertiary amine
darifenacin
muscarinic antagonist - tertiary amine
trospium
muscarinic antagonist - tertiary amine
atropine methyl nitrate
muscarinic antagonist - quaternary amine
methscopolamine
muscarinic antagonist - quaternary amine
ipratropium
muscarinic antagonist - quaternary amine
propantheline
muscarinic antagonist - quaternary amine
glycopyrrolate
muscarinic antagonist - quaternary amine
hexamethonium
ganglionic blocking drug
trimethaphan
ganglionic blocking drug
lacks CNS effects
mecamylamine
ganglionic blocking drug
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