Dementia Medications - Kinder Flashcards

(63 cards)

1
Q

Donepezil

A

AChE inhibitor

approved for dementia

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2
Q

galantamine

A

AChE inhibitor

approved for dementia

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3
Q

rivastigmine

A

AChE inhibitor

approved for dementia

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4
Q

tacrine

A

AChE inhibitor

approved for dementia

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5
Q

pralidoxome

A

cholinesterase reactivator

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6
Q

prevalence of AD

A

20% over 85yo

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7
Q

AD path

A

tau tangles, amyloid plaques

also - loss of cholinergic neurons
-marked decrase choline acetyltransferase

also possible excess of glutamate

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8
Q

direct acting cholinomimetic

A

bind to and activate mAChR and nAChR

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9
Q

indirect acting cholinomimetic

A

AChE inhibitor

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10
Q

cholinesterases

A

butylcholinesterase
acetylcholinesterase

target of AChE inhibitors - acetylcholinesterase

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11
Q

AChE

A

hydrolysis of ACh to choline and acetate

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12
Q

alcohol AChE inhibitors

A

alcohol group and quaternary ammonium
-positive charge

noncovalent and reversible, short lived
-binding to AChE

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13
Q

edrophonium

A

AChE inhibitor - alcohol

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14
Q

carbamic acid ester AChE inhibitors

A

carbamic acid ester of alcohol
-quaternary or tertiary ammonium group

positive charge or neurtal

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15
Q

neostigmine

A

carbamic acid ester AChE inhibitor

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16
Q

pyridostigmine

A

carbamic acid ester AChE inhibitor

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17
Q

physostigmine

A

carbamic acid ester AChE inhibitor

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18
Q

carbaryl

A

carbamic acid ester AChE inhibitor

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19
Q

binding of carbamic acid ester AChE inhibitor

A

to AChE - two step oricess

covalent bond of carbamoylated enzyme - more resistant to second step hydration

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20
Q

organophosphates

A

covalent and irreversible bind to AChE

charge neutral and highly lipid soluble
-CNS toxicity

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21
Q

echothiophate

A

organophosphate

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22
Q

parathion and malathion

A

organophosphate

insectisides

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23
Q

sarin and soman

A

organophosphate

nerve gas

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24
Q

charged AChE inhibitor

A

quaternary ammonium

no CNS effects

ex/ neostigmine, pyridostigmine, edrohonium, echothiophate, ambenonium

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25
uncharged AChE inhibitor
tertiary ammonium CNS distribution physostigmine, donepezil**, tacrine**, rivastigmine**, galantamine**
26
organophosphates
lipid soluble - absorbed skin and conjunctiva -dangerous to humans CNS toxicity covalent and irreversible binding to AChE
27
safe insecticide
malathion organophosphate rapidly metabolized to inactive product in mammals
28
DOA for alcohols
reversible bind weak - short lived 2-10 minutes hydrogen bonding and electrostatic interactions
29
DOA for carbamate esters
2 step hydrolysis 2nd step - covalent bond 30min-6 hours
30
DOA for organophosphates
hundreds of hours aging may occur - break O-P bond - even more stable
31
high AChE in CNS
convulsion, coma, resp arrest
32
AChE inhibitor on eye
miosis | accomodation
33
AChE inhibitor on heart
SA node - negative chronotropy atria - negative inotropy AV node - negative dromotropy (increased refractory) ventricle - small decrease contractions
34
AChE inhibitor on blood vesels
artery - dilation -high dose - constriction vein - dilation -high dose -constriction
35
AChE inhibitor on lung
bronchoconstriction | bronchosecretion
36
AChE inhibitor on GI
increase motility sphincter relaxation secretion stimulation
37
AChE inhibitor on urinary bladder
contract detrusor relax trigone and sphincter go pee
38
AChE inhibitor on glands
secretion
39
cardiac effect of AChE inhibitor and dose
moderate - mild HTN | toxic - hypotension
40
AChE inhibitor on NMJ
increase strength of contraction fibrillation and fasciculation of muscle fiber - high concentrations continued inhibition - depolarizing muscle blockade - to nondepolarizing blockade
41
tacrine
initial tx of dementia | -but hepatotoxic
42
combine AChE inhibitor with nondepolarizing neuromusc block agent
diminish neuromuscular blockade exception - mivacurium
43
succinylcholine and AChE inhibitor
increase serum succinylcholine prolong neuromuscular blockade
44
AChE inhibitor and cholinergic agonist
enhance cholinergic agonist
45
beta blocker and AChE inhibitor
enhance bradycardia
46
systemic corticosteroids and AChE inhibitor
enhance muscle weakness - pt with MG
47
AChE inhibitor intoxication
``` miosis salivation sweating bronchoconstriction vomiting diarrhea ```
48
route of admin for toxic AChE inhibitor
ingestion - GI sx first percutaneous - sweating and muscle fasciculations poison with lipid soluble agent - CNS involvement rapid - convulsion, coma, resp paralysis
49
death with AChE inhibitor
resp failure
50
diagnosis of AChE inhibitor poisoning
measure AChE activity in erythrocytes and plasma
51
antidote for cholinergic poisoning
atropine - mAChR antagonist
52
pralidoxome
cholinesterase re-activator to regenerate AChE at NMJ
53
cholinesterase re-activator
pralidoxime remove P group from active site of enzyme must be given before aging does not enter CNS - no effect of organophosphate poisoning
54
antidote for organophosphate
atropine pralidoxime benzo (anticonvulsant)
55
donepezil
tx mild to moderate and severe AD dementia rapid absorption one daily dosing
56
adverse of donepezil
``` GI urinary incontinence vivid dreams bradycardia syncope ```
57
galantamine
mild to moderate AD rapid abosrption - t-1/2 7 hours
58
galantamine ADRs
GI, dizzy, weight loss, bradycardia and syncope
59
rivastigmine
tx mild to moderate AD severe AD (transdermal patch) and parkinsons dementia
60
rivastigmine ADRs
GI - less with transdermal
61
memantime
antagonist at NMDA glutamate receptor normally - Mg ion block channel - excess activation - prevent Mg reentering and blocking pore (with AD) - memantine - blocks intrapore Mg site - effective receptor blocker
62
use of memantine
moderate-to severe AD
63
memantine adverse
dizzy confusion, hallucinations increased agitation and delusions