Cholinergic pharm COPY Flashcards

1
Q

three groups of cholinesterase inhibitors (indirect acting cholinomimetics)

A

carbamates

simple alcohol esters

organophosphate

there are a couple others that dont fit in these three categories

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2
Q

Edrophonium

A

cholinesterase inhibitor - simple alcohol ester

rapidly degraded

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3
Q

soman

A

cholinesterase inhibitor - organophosphate

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4
Q

oxybutynin

A

muscarinic antagonist - tertiary amine

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5
Q

sarin

A

cholinesterase inhibitor - organophosphate

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6
Q

darifenacin

A

muscarinic antagonist - tertiary amine

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7
Q

mecamylamine

A

ganglionic blocking drug

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8
Q

methscopolamine

A

muscarinic antagonist - quaternary amine

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9
Q

hexamethonium

A

ganglionic blocking drug

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10
Q

rivastigmine

A

cholinesterase inhibitor - carbamate

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11
Q

lobeline

A

tert alkaloid (DA cholinoceptor ag)

CNS effects

nicotinic activation predominant

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12
Q

ambenonium

A

cholinesterase inhibitor - carbamate

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13
Q

propantheline

A

muscarinic antagonist - quaternary amine

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14
Q

solifenacin

A

muscarinic antagonist - tertiary amine

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15
Q

darifenacin

A

muscarinic antagonist - tertiary amine

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16
Q

Direct acting cholinoceptor agonists (types)

A

esters of choline

alkaloids

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17
Q

isoflurophate

A

cholinesterase inhibitor - organophosphate

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18
Q

demecarium

A

cholinesterase inhibitor - carbamate

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19
Q

carbaryl

A

cholinesterase inhibitor - carbamate

high lipid solubility = rapid CNS effects

common insectoside

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20
Q

donepezil

A

cholinesterase inhibitor used for alzheimers disease

improves cognition - but doesnt slow or cure the disease

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21
Q

pirenzepine

A

muscarinic antagonist - tertiary amine

M1 selective

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22
Q

fesoteridine

A

muscarinic antagonist - tertiary amine

23
Q

pilocarpine

A

alkaloid (tert)

CNS activity

muscarinic activation predominant

24
Q

muscarine

A

quat alkaloid (cholinomemetic DA)

muscarinic activation predominant

25
Tropicamide
muscarinic antagonist - tertiary amine
26
atropine methyl nitrate
muscarinic antagonist - quaternary amine
27
mepenzolate
muscarinic antagonist - tertiary amine
28
tolterodine
muscarinic antagonist - tertiary amine M3 selective - bladder
29
Atropine
muscarinic antagonist - tertiary amine non selective - inhibits M1/2/3
30
anticholinergic agents types
tertiary amines quaternary amines ganglionic blocking drugs cholinesterase regenereators - 2PAM
31
diisopropylflurophosphate (DFP)
cholinesterase inhibitor - organophosphate
32
glycopyrrolate
muscarinic antagonist - quaternary amine
33
acetycholine
direct acting cholinoceptor agonst ester of choline - quaternary ammonium rapidly hydrolysed
34
neostigmine
cholinesterase inhibitor - carbamate quat amm
35
nicotine
tert alkyloid CNS activity nicotinic activation predominant
36
methacholine
DA cholinoceptor ag ester of choline quat amm more resistant to hydrolysis than acetycholine
37
dicyclomine
muscarinic antagonist - tertiary amine
38
Varenicline
direct nicotinic agonist used to treat nicotine addiction
39
physostigmine
cholinesterase inhibitor - carbamate tert am
40
carbachol and bethanechol
DA cholinoceptor agonist ester of choline - quat amm very resistant to hydroylysis
41
galantamine
cholinesterase inhibitor used in treatment of alzheimers disease
42
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
43
malathion
cholinesterase inhibitor - organophosphate
44
parathion
cholinesterase inhibitor - organophosphate
45
tacrine
cholinesterase inhibitor used for treatment of alzheimers disease
46
copolamine
muscarinic antagonist - tertiary amine
47
trospium
muscarinic antagonist - tertiary amine
48
Cevimeline
DA muscarinic agonist choline ester - quat amm
49
homatropine
muscarinic antagonist - tertiary amine
50
trimethaphan
ganglionic blocking drug lacks CNS effects
51
pyridostigmine
cholinesterase inhibitor - carbamate
52
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
53
ipratropium
muscarinic antagonist - quaternary amine