Pharm, Dementia, Kinder

Question 1

What are the ACHEI approved for dementia

Answer 1

donepezil
galantamine
rivastigmine
Tacrine

Question 2

adverse effects of ACHEI

Answer 2

diffuse

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

Question 3

groups of cholinesterase inhibitors

Answer 3

alcohols
carbamic acid esters
organophosphates

Question 4

structure of alcohol cholinesterase

Answer 4

quaternary amonium
+ charged
like edrophonium
noncovalent short lied

Question 5

structure of crbamic acid ester cholinesterase inhibitor

Answer 5

quaternary or tertiaty ammonium groups (+ or neutral)

stigmines

Question 6

binding of carbamic ester acids

Answer 6

2 steps

Question 7

organophosphate structure of cholinesterase inhibitors

Answer 7

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

Question 8

PK of qauternary charged ACHEI

Answer 8

reslativley insoluble in lipids
pareneteral preferred
no CNS

Question 9

PK tertiary uncharged ACHEI

Answer 9

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

Question 10

what drugs used for dementia are tertiary and uncharged ACHEI

Answer 10

donepezil, tacrine, rivastigmine, galantamine

Question 11

why are organophosphates dangerous

Answer 11

readily abosrbed everywhere

distributed all parts of body

Question 12

toxic organosphosphate, how do we recover

Answer 12

need to make more ACHE

oxime regenerator compound

Question 13

“aging” process

Answer 13

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

Question 14

continued inhibition of ACHE in NMJ

Answer 14

depolarizing NMJ blockade to nondepolarizing blockade (like succinylcholine)

Question 15

uses of aCHEI

Answer 15

glaucoma, postoperative atony of bladder or GI
NMJ
alzheimers
dementia

Question 16

tacrine withdrawn because

Answer 16

hepatotoxicity

Question 17

DDI ACHE

Answer 17

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

Question 18

initial signs ACHE I intoxication

Answer 18

miosis
salivation
sweating
bronchial constriction
vomiting diarrhea

Question 19

poisoning of lipid soluble ACHEI

Answer 19

confusion, ataxia, generalized convulsions, coma and respiratory paralysis

Question 20

death by ACHEI

Answer 20

respiratory failure

Question 21

Dx mild intoxication ACHE

Answer 21

ACHE activity in plasma and RBC

Question 22

antidote for chilergic posisoning

Answer 22

atropine mACHR antagonist

Question 23

atropine ineffective against

Answer 23

peripheral NMstimulation nACHR

Question 24

pralidozime

Answer 24

cholinesterase reactivator to regenerate ACHE

Question 25

does pralidoxie cross bbb

Answer 25

no

Question 26

metabolism donepezil

Answer 26

CY2D6 and 3A4

Question 27

donepezil used for what alzheimer dementia levels

Answer 27

mild to mod and severe | PD and lewy body too (off label)

Question 28

adverse effects donepezil

Answer 28

GI especially on intiation | urinary incontinence, viivd dreams, bradycardia, syncope

Question 29

half life donepezil

Answer 29

70 hours | daily dosing

Question 30

galantamine used for

Answer 30

mild to mod alzheimer dementia | off label severe dementia or PD or lewy body

Question 31

adverse effects galantamine

Answer 31

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

Question 32

metabolism rivastigmine

Answer 32

esterase hydrolysis

Question 33

rivastigmine used for

Answer 33

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

Question 34

side effects rivastigmine

Answer 34

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

Question 35

MOA memantine

Answer 35

antagonist NMDA R glutamate | binds Mg site with longer time and so blocks only the excessive stimulation

Question 36

use mematnine

Answer 36

mod to severe AD dementia

Question 37

adverse effects memantine

Answer 37

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