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
Q

isoflurophate

A

cholinesterase inhibitor - organophosphate

26
Q

diisopropylflurophosphate (DFP)

A

cholinesterase inhibitor - organophosphate

27
Q

donepezil

A

cholinesterase inhibitor used for alzheimers disease

improves cognition - but doesnt slow or cure the disease

28
Q

tacrine

A

cholinesterase inhibitor used for treatment of alzheimers disease

29
Q

galantamine

A

cholinesterase inhibitor used in treatment of alzheimers disease

30
Q

anticholinergic agents types

A

tertiary amines

quaternary amines

ganglionic blocking drugs

cholinesterase regenereators - 2PAM

31
Q

Atropine

A

muscarinic antagonist - tertiary amine

non selective - inhibits M1/2/3

32
Q

copolamine

A

muscarinic antagonist - tertiary amine

33
Q

homatropine

A

muscarinic antagonist - tertiary amine

34
Q

pirenzepine

A

muscarinic antagonist - tertiary amine

M1 selective

35
Q

Tropicamide

A

muscarinic antagonist - tertiary amine

36
Q

tolterodine

A

muscarinic antagonist - tertiary amine

M3 selective - bladder

37
Q

dicyclomine

A

muscarinic antagonist - tertiary amine

38
Q

fesoteridine

A

muscarinic antagonist - tertiary amine

39
Q

mepenzolate

A

muscarinic antagonist - tertiary amine

40
Q

solifenacin

A

muscarinic antagonist - tertiary amine

41
Q

oxybutynin

A

muscarinic antagonist - tertiary amine

42
Q

darifenacin

A

muscarinic antagonist - tertiary amine

43
Q

darifenacin

A

muscarinic antagonist - tertiary amine

44
Q

trospium

A

muscarinic antagonist - tertiary amine

45
Q

atropine methyl nitrate

A

muscarinic antagonist - quaternary amine

46
Q

methscopolamine

A

muscarinic antagonist - quaternary amine

47
Q

ipratropium

A

muscarinic antagonist - quaternary amine

48
Q

propantheline

A

muscarinic antagonist - quaternary amine

49
Q

glycopyrrolate

A

muscarinic antagonist - quaternary amine

50
Q

hexamethonium

A

ganglionic blocking drug

51
Q

trimethaphan

A

ganglionic blocking drug

lacks CNS effects

52
Q

mecamylamine

A

ganglionic blocking drug

53
Q

pralidoxime (2-PAM)

A

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