Dementia Medications - Kinder Flashcards

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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
Q

uncharged AChE inhibitor

A

tertiary ammonium

CNS distribution

physostigmine, donepezil, tacrine, rivastigmine, galantamine

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26
Q

organophosphates

A

lipid soluble - absorbed skin and conjunctiva
-dangerous to humans

CNS toxicity

covalent and irreversible binding to AChE

27
Q

safe insecticide

A

malathion

organophosphate rapidly metabolized to inactive product in mammals

28
Q

DOA for alcohols

A

reversible bind

weak - short lived

2-10 minutes

hydrogen bonding and electrostatic interactions

29
Q

DOA for carbamate esters

A

2 step hydrolysis

2nd step - covalent bond

30min-6 hours

30
Q

DOA for organophosphates

A

hundreds of hours

aging may occur - break O-P bond - even more stable

31
Q

high AChE in CNS

A

convulsion, coma, resp arrest

32
Q

AChE inhibitor on eye

A

miosis

accomodation

33
Q

AChE inhibitor on heart

A

SA node - negative chronotropy
atria - negative inotropy
AV node - negative dromotropy (increased refractory)
ventricle - small decrease contractions

34
Q

AChE inhibitor on blood vesels

A

artery - dilation
-high dose - constriction

vein - dilation
-high dose -constriction

35
Q

AChE inhibitor on lung

A

bronchoconstriction

bronchosecretion

36
Q

AChE inhibitor on GI

A

increase motility
sphincter relaxation
secretion stimulation

37
Q

AChE inhibitor on urinary bladder

A

contract detrusor
relax trigone and sphincter

go pee

38
Q

AChE inhibitor on glands

A

secretion

39
Q

cardiac effect of AChE inhibitor and dose

A

moderate - mild HTN

toxic - hypotension

40
Q

AChE inhibitor on NMJ

A

increase strength of contraction

fibrillation and fasciculation of muscle fiber - high concentrations

continued inhibition - depolarizing muscle blockade - to nondepolarizing blockade

41
Q

tacrine

A

initial tx of dementia

-but hepatotoxic

42
Q

combine AChE inhibitor with nondepolarizing neuromusc block agent

A

diminish neuromuscular blockade

exception - mivacurium

43
Q

succinylcholine and AChE inhibitor

A

increase serum succinylcholine

prolong neuromuscular blockade

44
Q

AChE inhibitor and cholinergic agonist

A

enhance cholinergic agonist

45
Q

beta blocker and AChE inhibitor

A

enhance bradycardia

46
Q

systemic corticosteroids and AChE inhibitor

A

enhance muscle weakness - pt with MG

47
Q

AChE inhibitor intoxication

A
miosis
salivation
sweating
bronchoconstriction
vomiting
diarrhea
48
Q

route of admin for toxic AChE inhibitor

A

ingestion - GI sx first
percutaneous - sweating and muscle fasciculations

poison with lipid soluble agent - CNS involvement rapid - convulsion, coma, resp paralysis

49
Q

death with AChE inhibitor

A

resp failure

50
Q

diagnosis of AChE inhibitor poisoning

A

measure AChE activity in erythrocytes and plasma

51
Q

antidote for cholinergic poisoning

A

atropine - mAChR antagonist

52
Q

pralidoxome

A

cholinesterase re-activator

to regenerate AChE at NMJ

53
Q

cholinesterase re-activator

A

pralidoxime

remove P group from active site of enzyme

must be given before aging

does not enter CNS - no effect of organophosphate poisoning

54
Q

antidote for organophosphate

A

atropine
pralidoxime
benzo (anticonvulsant)

55
Q

donepezil

A

tx mild to moderate and severe AD dementia

rapid absorption
one daily dosing

56
Q

adverse of donepezil

A
GI
urinary incontinence
vivid dreams
bradycardia
syncope
57
Q

galantamine

A

mild to moderate AD

rapid abosrption - t-1/2 7 hours

58
Q

galantamine ADRs

A

GI, dizzy, weight loss, bradycardia and syncope

59
Q

rivastigmine

A

tx mild to moderate AD
severe AD (transdermal patch)
and parkinsons dementia

60
Q

rivastigmine ADRs

A

GI - less with transdermal

61
Q

memantime

A

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
Q

use of memantine

A

moderate-to severe AD

63
Q

memantine adverse

A

dizzy
confusion, hallucinations
increased agitation and delusions