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Year 2 Psych exam I > Pharm, Dementia, Kinder > Flashcards

Pharm, Dementia, Kinder Flashcards

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1
Q

What are the ACHEI approved for dementia

A

donepezil
galantamine
rivastigmine
Tacrine

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2
Q

adverse effects of ACHEI

A

diffuse

CV, GI, eye, respiratory, urinary, CNS, NMJ

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3
Q

groups of cholinesterase inhibitors

A

alcohols
carbamic acid esters
organophosphates

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4
Q

structure of alcohol cholinesterase

A

quaternary amonium
+ charged
like edrophonium
noncovalent short lied

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5
Q

structure of crbamic acid ester cholinesterase inhibitor

A

quaternary or tertiaty ammonium groups (+ or neutral)

stigmines

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6
Q

binding of carbamic ester acids

A

2 steps

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7
Q

organophosphate structure of cholinesterase inhibitors

A

charged neutral
highly lipid soluble resulting in CNS toxicity
covalent irreversible binding

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8
Q

PK of qauternary charged ACHEI

A

reslativley insoluble in lipids
pareneteral preferred
no CNS

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9
Q

PK tertiary uncharged ACHEI

A

well absorbed all sires, CNS distribution, more toxic than quaternary carbamates

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10
Q

what drugs used for dementia are tertiary and uncharged ACHEI

A

donepezil, tacrine, rivastigmine, galantamine

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11
Q

why are organophosphates dangerous

A

readily abosrbed everywhere

distributed all parts of body

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12
Q

toxic organosphosphate, how do we recover

A

need to make more ACHE

oxime regenerator compound

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13
Q

“aging” process

A

after intial binding of organophosphates the enzyme will break a bond of inhibitor and further strenghten the phosphorus enzyme bond

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14
Q

continued inhibition of ACHE in NMJ

A

depolarizing NMJ blockade to nondepolarizing blockade (like succinylcholine)

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15
Q

uses of aCHEI

A

glaucoma, postoperative atony of bladder or GI
NMJ
alzheimers
dementia

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16
Q

tacrine withdrawn because

A

hepatotoxicity

17
Q

DDI ACHE

A 
nondepolarizing NMJ blockin agents (will diminish blockade)
succinycholine (prolong blockade)
cholinergic agonists (enhance)
beta blockers (bradycardia)
systemic corticosteorids (enhance mm weakness)
18
Q

initial signs ACHE I intoxication

A 
miosis
salivation
sweating
bronchial constriction
vomiting diarrhea
19
Q

poisoning of lipid soluble ACHEI

A

confusion, ataxia, generalized convulsions, coma and respiratory paralysis

20
Q

death by ACHEI

A

respiratory failure

21
Q

Dx mild intoxication ACHE

A

ACHE activity in plasma and RBC

22
Q

antidote for chilergic posisoning

A

atropine mACHR antagonist

23
Q

atropine ineffective against

A

peripheral NMstimulation nACHR

24
Q

pralidozime

A

cholinesterase reactivator to regenerate ACHE

25
Q

does pralidoxie cross bbb

A

no

26
Q

metabolism donepezil

A

CY2D6 and 3A4

27
Q

donepezil used for what alzheimer dementia levels

A

mild to mod and severe

PD and lewy body too (off label)

28
Q

adverse effects donepezil

A

GI especially on intiation

urinary incontinence, viivd dreams, bradycardia, syncope

29
Q

half life donepezil

A

70 hours

daily dosing

30
Q

galantamine used for

A

mild to mod alzheimer dementia

off label severe dementia or PD or lewy body

31
Q

adverse effects galantamine

A

GI, dizziness, weight loss,
bradycardia and syncope
depression fatigue somnolence

32
Q

metabolism rivastigmine

A

esterase hydrolysis

33
Q

rivastigmine used for

A

mild to mod AD
severe AD in transdermal patch
Parkinsons dementia
and lewy body (off label)

34
Q

side effects rivastigmine

A

high incidence nausea vomiting diarrhea in oral form
less with transdermal patch
brady cardia and syncope

35
Q

MOA memantine

A

antagonist NMDA R glutamate

binds Mg site with longer time and so blocks only the excessive stimulation

36
Q

use mematnine

A

mod to severe AD dementia

37
Q

adverse effects memantine

A

well tolerated
fewer side effects
dizziness, confusion, hallucinations
increase agitation and delusional behaviors in some

Year 2 Psych exam I (15 decks)

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