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Therapeutics I > Cholinergic Agonists (cholinesterase inhibitors) > Flashcards

Cholinergic Agonists (cholinesterase inhibitors) Flashcards

1
Q

what are the two types of cholinesterases

A

acetylcholinesterase and plasma cholinesterase

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2
Q

which cholinesterase is located in synapses

A

acetylcholinesterase

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3
Q

AChE has the (highest/lowest) turnover rate of any known mammalian enzyme

A

highest

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4
Q

what are the two main sites of acetylcholinesterase

A

anionic site and esteratic site

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5
Q

what is the critical step in the hydrolysis of acetylcholine

A

reactivated enzyme, reactivated by water

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6
Q

give an example of a reversible anticholinesterase agent

A

edrophonium

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7
Q

give an example of an irreversible anticholinesterase agent

A

organophosphates

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8
Q

name the 3 reversible carbamates (also anticholinesterase agents)

A

physostigmine, neostigmine, pyridostigmine

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9
Q

name 3 organophosphates

A

echothiophate, sarin, malathion

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10
Q

Edrophonium, neostigmine, and pyridostigmine all share what action

A

inhibition of acetylcholinesterase

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11
Q

edrophonium (covalently/noncovalently) binds to acetylcholinesterase

A

noncovalently

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12
Q

Match the clinical use with the following drugs: very short-acting (minutes); diagnosis of Myasthenia Gravis (MG)
(skeletal muscle weakness due to loss of skeletal muscle nicotinic receptors because of
autoimmune disease)
a. edrophonium
b. pyridostigmine
c. neostigmine

A

a. edrophonium

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13
Q

match the clinical use with the following drugs:
Used in treatment of MG, reversal of nondepolarizing neuromuscular blockade,
pretreatment for potential nerve gas exposure (occupy AChE so that nerve gas has
nowhere to go
a. edrophonium
b. pyridostigmine
c. neostigmine

A

b. pyridostigmine

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14
Q

match the clinical use with the following drugs:
Used for MG, reversal of nondepolarizing neuromuscular blockade, post-op urinary retention
a. edrophonium
b. pyridostigmine
c. neostigmine

A

c. neostigmine

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15
Q

“stigmines” as substrates that are more _______ _________ than ACh

A

slowly hydrolyzed

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16
Q

clinical use of physostigmine

A

antidote to antimuscarinic poisoning

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17
Q

T/F most organophosphates are toxic

A

True

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18
Q

action of echothiophate

A

inhibition of acetylcholinesterase: BUT its long-acting and irreversible

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19
Q

what drug? Action: strong nucleophile, will hydrolyze organophosphate if treated before aging occurs- this will regenerate acetylcholinesterase. does not cross the BBB

A

pralidoxime (2-pam)

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20
Q

clinical use of pralidoxime

A

treatment of organophosphate toxicity

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21
Q

2 drugs used for antidotal therapy for acute organophosphate intoxication

A

pralidoxime and atropine

22
Q

Blocks access to muscarinic receptor (antagonist). Can’t block action at nicotinic receptors

A

Atropine

23
Q

Strong nucleophile. Can’t cross BBB

A

pralidoxime

24
Q

Target of pralidoxime

A

neuromuscular junction;
muscle weaknsess-> respiratory-> DEATH

25
Q

what disease causes widening of sulci and thinning of gyri in the brain

A

alzheimers

26
Q

loss of cholinergic neurons in brain

A

alzheimers

27
Q

4 drugs used to treat alzheimers

A

donepezil (aricept), rivastigmine (exelon), galantamine (razadyne), memantine (namenda)

28
Q

just try to hit all the points on the donepezil slide

A

binds to anionic site and blocks ACh binding, reversible, noncovalent, enhances cognitive ability, does not slow progression of disease

29
Q

hit the points on the rivastigmine slide

A

reversible carbamate AChE inhibitor, enhances cognitive ability by increasing cholinergic function, loses effectiveness as disease progresses

30
Q

side effects of rivastigmine

A

nausea, vomiting, anorexia, and weight loss

31
Q

talk about the galantamine (razadyne) slide

A

reversible competitive AChE inhibitor, loses effectiveness as disease progresses, may be a nicotinic receptor agonist, inhibitors of P450 enzymes (3A4, 2D6) will increase galantamine bioavailability

32
Q

talk about memantine (namenda) slide

A

NMDA receptor antagonist. Glutamate regulators to improve cognitive function. Approved for moderate-to-severe disease, favorable adverse effect profile

33
Q

two alzheimers drugs approved for moderate-to-severe alzheimers

A

donepezil and memantine

34
Q

type of inhibition: Edrophonium

A

reversible

35
Q

type of inhibition: neostigmine

A

reversible

36
Q

type of inhibition: Physostigmine

A

reversible

37
Q

type of inhibition: Donepezil

A

reversible

38
Q

type of inhibition: Echothiophate

A

Irreversible

39
Q

Route of administration: Edrophonium

A

IM or IV

40
Q

Route of administration: Neostigmine

A

IM, IV, or oral

41
Q

Route of administration: Physostigmine

A

IM, IV, or local

42
Q

Route of administration: Donepezil

A

oral

43
Q

Route of administration: Echothiophate

A

local

44
Q

clinical use: Edrophonium

A

Diagnostic for MG

45
Q

clinical use: Neostigmine

A

MG, post-op ileus and bladder distention

46
Q

clinical use: physostigmine

A

glaucoma, alzheimers, antidote to anticholinergic overdose

47
Q

clinical use: donepezil

A

alzheimers

48
Q

clinical use: Echothiophate

A

glaucoma

49
Q

cholinergic agonists side effects

A

DUMBBELS: diarrhea, urination, miosis, bradycardia, brochoconstriction, emesis, lacrimation, salivation, +sweating (SNS effect)

50
Q

When to be cautious with cholinergic agonists

A

patients with asthma, coronary insufficiency, or peptic ulcer

Therapeutics I (4 decks)

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