Cholinergic pharm COPY COPY Flashcards

1
Q

Direct acting cholinoceptor agonists (types)

A

esters of choline

alkaloids

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2
Q

acetycholine

A

direct acting cholinoceptor agonst

ester of choline - quaternary ammonium

rapidly hydrolysed

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3
Q

methacholine

A

DA cholinoceptor ag

ester of choline

quat amm

more resistant to hydrolysis than acetycholine

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4
Q

carbachol and bethanechol

A

DA cholinoceptor agonist

ester of choline - quat amm

very resistant to hydroylysis

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5
Q

Cevimeline

A

DA muscarinic agonist

choline ester - quat amm

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6
Q

pilocarpine

A

alkaloid (tert)

CNS activity

muscarinic activation predominant

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7
Q

nicotine

A

tert alkyloid

CNS activity

nicotinic activation predominant

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8
Q

lobeline

A

tert alkaloid (DA cholinoceptor ag)

CNS effects

nicotinic activation predominant

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9
Q

muscarine

A

quat alkaloid (cholinomemetic DA)

muscarinic activation predominant

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10
Q

Varenicline

A

direct nicotinic agonist

used to treat nicotine addiction

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11
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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12
Q

neostigmine

A

cholinesterase inhibitor - carbamate

quat amm

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13
Q

physostigmine

A

cholinesterase inhibitor - carbamate

tert am

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14
Q

pyridostigmine

A

cholinesterase inhibitor - carbamate

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15
Q

rivastigmine

A

cholinesterase inhibitor - carbamate

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16
Q

ambenonium

A

cholinesterase inhibitor - carbamate

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17
Q

demecarium

A

cholinesterase inhibitor - carbamate

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18
Q

carbaryl

A

cholinesterase inhibitor - carbamate

high lipid solubility = rapid CNS effects

common insectoside

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19
Q

Edrophonium

A

cholinesterase inhibitor - simple alcohol ester

rapidly degraded

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20
Q

echothiophate

A

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
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21
Q

soman

A

cholinesterase inhibitor - organophosphate

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22
Q

sarin

A

cholinesterase inhibitor - organophosphate

23
Q

parathion

A

cholinesterase inhibitor - organophosphate

24
Q

malathion

A

cholinesterase inhibitor - organophosphate

25
isoflurophate
cholinesterase inhibitor - organophosphate
26
diisopropylflurophosphate (DFP)
cholinesterase inhibitor - organophosphate
27
donepezil
cholinesterase inhibitor used for alzheimers disease improves cognition - but doesnt slow or cure the disease
28
tacrine
cholinesterase inhibitor used for treatment of alzheimers disease
29
galantamine
cholinesterase inhibitor used in treatment of alzheimers disease
30
anticholinergic agents types
tertiary amines quaternary amines ganglionic blocking drugs cholinesterase regenereators - 2PAM
31
Atropine
muscarinic antagonist - tertiary amine non selective - inhibits M1/2/3
32
copolamine
muscarinic antagonist - tertiary amine
33
homatropine
muscarinic antagonist - tertiary amine
34
pirenzepine
muscarinic antagonist - tertiary amine M1 selective
35
Tropicamide
muscarinic antagonist - tertiary amine
36
tolterodine
muscarinic antagonist - tertiary amine M3 selective - bladder
37
dicyclomine
muscarinic antagonist - tertiary amine
38
fesoteridine
muscarinic antagonist - tertiary amine
39
mepenzolate
muscarinic antagonist - tertiary amine
40
solifenacin
muscarinic antagonist - tertiary amine
41
oxybutynin
muscarinic antagonist - tertiary amine
42
darifenacin
muscarinic antagonist - tertiary amine
43
darifenacin
muscarinic antagonist - tertiary amine
44
trospium
muscarinic antagonist - tertiary amine
45
atropine methyl nitrate
muscarinic antagonist - quaternary amine
46
methscopolamine
muscarinic antagonist - quaternary amine
47
ipratropium
muscarinic antagonist - quaternary amine
48
propantheline
muscarinic antagonist - quaternary amine
49
glycopyrrolate
muscarinic antagonist - quaternary amine
50
hexamethonium
ganglionic blocking drug
51
trimethaphan
ganglionic blocking drug lacks CNS effects
52
mecamylamine
ganglionic blocking drug
53
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