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Pharmacology > Pharm 8.1 - anticholinesterase agents > Flashcards

Pharm 8.1 - anticholinesterase agents Flashcards

1
Q

anticholinesterase agens

A

indirect acting cholinergic drugs by inhibiting the enzyme AChE and hence protect Ach from hydrolysis - inc levels of Ach

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2
Q

two type so ACE agens

A

reversible and irreversible

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3
Q

reversible short acting

A

edrophonium

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4
Q

reversible intermediate actin

A

neostigmine, physostigmine

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5
Q

long acting ACE agent

A

Pyridostigmine, Tacrine, Ambenonium

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6
Q

irreversible

A

insectisides, nerve gas poison, organophosphorous compounds, carbamates

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7
Q

organphosphorus compunds

A

parathion, malathion, diazinon (TIK-20), Echotiopate, Soman, Sarnin, Tabun (nerve gase poisons)

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8
Q

To differentitat muscle weaknes of myastienia gravis from cholinergic crisis

A

edrophonium

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9
Q

Carbamates

A

carbaryl, proppoxur

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10
Q

Acetylcholinesterasae

A

is an enzyme with anionic and esteratic site, hydrolysis of Ach infolves attraction of popitve N+ of Ach at anionic site and acetylatio nof serine leading to acetylated enzyme, acetylated enzyme reacts with water to produce acetic acid and enzyme is free within milliseconds

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11
Q

reversible anticholinesterases work by

A

comining with ChE and carbamylated enzyme (carbamyl binds at anionic site) is slow to hydorlyze and free the enzyme (in 30 mins), increaseing ach that_s left around

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12
Q

Physostigmine

A

naturally occuring alkaloid (nature is basic)

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13
Q

Physostigmine can enter cells bec

A

it is a tertiary amine - uncharged lipid soluble, corsses BBB, aosl good oral abs

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14
Q

Physositgmine duration of action

A

2-4 hrs

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15
Q

Physostigmine actions

A

reversibly inhibits acetylcholinesterase, wide actions, stimulates muscarinic and nicotinic sites of ANS by increasing the concentration of Ach, also stimulates cholinergic sites in the CNS

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16
Q

Physostigmine therapuetic uses

A

glaucoma - to lower IOT and produce mosis, bladder and intestinal atony - increases intestinal bladder motility, antidote in atropine overdoes (bc it can cross BBB)

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17
Q

Neostigmine structure

A

synthetic quarterary amine - charged - poor oral abs

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18
Q

Neostigmine CNS action

A

absent as it does not enter the CNS so no CNS side effects and can’t be used to overcome toxicity of central acting antimuscarinic agents such as atropoine

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19
Q

Neostigmine works by

A

reversibly inhibits acetylcholinesterase in a manner similar to physostigmine

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20
Q

Neostigmine effects

A

skeletal musles, stimulates bladder and GIT, used in paralytic ileus, urinary retention, symptomatic treatment of myasthenia gravis, antidote for tubocurarine and other competitive neuromuscular blocking agens

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21
Q

Neostigmine duration of action

A

0.5 - 2hrs

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22
Q

Pyridostigmine and ambenonium

A

cholinesterase inhibitors in the chronic management of myasthenia gravis

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23
Q

Pyridostigmine duration of action

A

3-6hrs

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24
Q

Amebenonium duration of action

A

4-8hrs

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25
Q

Edrophonium

A

short acting anticholinesterase drug (10-20 minutes)

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26
Q

Edrophonium actions

A

similar to neostigmine, used for diagnosis of myasthenia gravis and also used to differentiate myasthenia from cholinergic crisis

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27
Q

Demecarium structure

A

quarternary amine, structurally related to neostigmine

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28
Q

Demecarium is used to

A

treat chronic open-angle closed angle glaucoma

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29
Q

Edrophonium can be sued to diagnose

A

myasthenia gravis and then can give neostigmine or physostigmine

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30
Q

if patient comes in with weakness

A

give small dose of edrophonium, if myasthenia gravis the patient will impover, but if it is due to increased Ach activty in neuromuscular jn by giving Edrophonium it worsens

31
Q

anticholinesterase drugs used in Alzhimers to inc Ach and help improve memory

A

tacrine, donepezil, rivastigmine, galantamine

32
Q

irreversible anticholinesterases

A

echothiophate

33
Q

Echothiophate action

A

an organophosphate that binds covalently via its phosphate group to the serine -OH group at the active site of acetylcholinesterase leading to permanently inactivation of the enzyme acetylcholinesterase

34
Q

Echothiophate and aging

A

after covalent modification AChE, the phosphorylaated enzyme slowly releases on of its etyl groups

35
Q

Aging makes it impossible for

A

enzyme reactivator such as pralidoxime to break the bond btw the remaining drug and the enzyme

36
Q

how do reactivators work

A

the drug has the organic group and phosphate and they work to break the bond btw drug and enzyme. As long as alky group is attached to the phosphate it can regenerate. But if not then it cant.

37
Q

actions of Echothiophate

A

generalized cholinergic stimulation, paralysis of motor functin (causing breathing difficulties) and convulsions, produces intense mios (basis of therapeutic application)

38
Q

Echothiophate can lead to paralysis due to

A

over stimulation at the NM jn and desensitization

39
Q

Echothiophate therapuetic uses

A

chronic treatment of open angle glaucoma but potential risk of cataracts

40
Q

Edrophonium usues

A

myasthenia gravis, ileus

41
Q

Edrophonium duration of action

A

10 - 20 minutes

42
Q

Neostigmine uses

A

myasthenia gravis, ileus

43
Q

Pyridostigmine uses

A

myasthenia gravis

44
Q

Ambenonium uses

A

myasthenia gravis

45
Q

Demecarium duration of action

A

4-6hrs

46
Q

Echothiphate duration of action

A

100 hours

47
Q

Common adverse effects of AchE inhibitors

A

generalized cholinergic stimulation, salivation, flushing, dec BP, nausea, abdominal pain, diarrhea and bronchospasm, CNS effects like convulsions like Physostigmine (at high doses)

48
Q

organophosphorous compounds

A

parathion, malathion (insecticides)

49
Q

organophosphorus compounds react with

A

esteratic site which is hydrolized extremely slowly with water or not at all, enzyme can also undergo aging

50
Q

Cholinesterase reactivator

A

Pralidoxime

51
Q

the Phosphorylated ChE react very slowly or not at all with

A

water

52
Q

oximes like pralidoxime bind with

A

anionic site of ChE and undergoes reaction to cause hydroylysis of phosphoserine bond, resulting in free enzyme

53
Q

Pralidoxime should be administered

A

as early as possible followed by OP poisoning (not later than 24hrs max, as aging occurs)

54
Q

Edrophonium characteristics

A

short acting

55
Q

Pyridostigmine sturcture

A

quarternary amine

56
Q

Donepezil and tacrine characteristics

A

lipid soluble for CNS entry in treatment of Alzheimers

57
Q

organophosphate caracteristics

A

lipid soluble ireerversible inhibitors to treat glaucoma, as an insectaside, and a nerve gas (sarin)

58
Q

how are organopphosphates irreversible

A

the organophosphate phosphorylates the enzyme and undergoes aging, losing one of the alkylyl groups and becoming totally resistant to hydrolysis

59
Q

reactivators can’t work on

A

carbamates bc they take up the anionic site but they might be helpful for organophoshphates before aging

60
Q

Pralidoxime is a

A

cholinesterase reactivator

61
Q

phosphorylated choline esterates reacts with water

A

very slowly or not at all - no hydrolysis means drug is not able to reverse its effect

62
Q

pralidoxime (PAM) is eneffective in case of

A

physostigmine or neostigmine because they are carbamates that bind the anionic site and so PAM is not able to bind

63
Q

organophosphorous poisoning acute toxicity

A

excessive muscarinic and nicotinic stimulations

64
Q

Dumbbelss - muscaranic effects of organophosphates

A

diarrhea, urination, miosis, bradycardia, bronchoconstriction, exciatation (CNS and muscle), lacrimation, salivation, and sweating

65
Q

Acetylcholinesterasae inhibitors acute toxicity - nicotinic effects

A

skeletal muscle excitation followed by paralysis, CNS stimulation

66
Q

to counteract muscarinic effects give

A

atropine

67
Q

for regeneration of AChE give

A

pralidoxime as soon as possible to avoid aging

68
Q

treat open/wide angle gaucoma with

A

piocarpine, physostigmine

69
Q

treat myasthenia gravis with

A

neostigmine, pyridostigmine

70
Q

treat urinary retention with

A

neostigmine, pyridostigmine

71
Q

treat parlytic ileus/congenital megacolon with

A

neostigmine, pyridostigmine

72
Q

for drug poisoning with atropine, TCA, or phenothiazines use

A

physostigmine

73
Q

for Alzheimers diesease use

A

donepezil, galantamine, rivastigmine, tarcrine

74
Q

for Sjogren’s syndrom use

A

Pilocarpine

Pharmacology (15 decks)

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