Neuro: neurodegenerative drugs Flashcards

1
Q

In parkinson, as dopamine levels _______ ACH levels______

A

dopamine—-decreases

ACH—-increases

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2
Q

do the parkinson drugs stop or reverse the diseaes

A

NO just help with s/s

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3
Q

what is levodopa

-can it penetrate BBB

A
immediate precursor (before) of dopamine 
and is immediately converted to dopamine once it crosses the BBB
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4
Q

what is carbidopa

A

dopamine decarboxylase inhibitor
–diminishes metabolism of levodopa in the periphery (reducing s/e)—-increasing the availability of levodopa to the CNS—therefore more levodopa to cross BBB and become DOPAMINE

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5
Q

what happens when we add carbidopa to levodopa

A

it lowers the amount of levodopa needed by 4-5 fold!

*decreases SE too from peripherally formed dopamine

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6
Q

what happens if we dont add carbidopa to levodopa?

A

the levodopa is converted to dopamine peripherally—-and less will be available to cross BBB and then the effects of the drug are diminished

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7
Q

Mainstay of TX for PD???

A

L-C

*reduces severity of s/s for the first few years of tx

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8
Q

Long term use of Levodopa causes?

A

“wearing off”

flucctations and diskinesias

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9
Q

Peripheral SE from L-C

A

N/V
cardiac arrythmias
hypoT

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10
Q

Central SE from L-C

A

visual/auditory hallucintions, dyskineseas, psych S/s

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11
Q

drug-drug interactions of L-C

A

Vit B6—-pyridoxine diminishes effectiveness

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12
Q

If L-C is given with _______ can cause HTN crisis

A

MAOI

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13
Q

What happens if L-C given with MAOI

A

HTN CRISIS

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14
Q

T1/2 of L-C

A

1-2 hours

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15
Q

where is L-C absopbed

A

small intestine (if taken w/o food)

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16
Q

MAO Type B

—MOA?

A

inhibits MAO type B—-enzyme that b/d dopamine

actions of levodopa are potentiated*** letting dose be reduces

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17
Q

Selegiline and Rasagiline

A

MAO type B

*adjunct tx to L-C

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18
Q

Catechol-O-Methyltransferease Inhibitors (COMT)
MOA–?
which of the drugs is prefered?

A

ENTACAPONE AND TOLCAPONE
MOA—enzyme COMTresp for b/d of dopamine
*entacapone prefered over Tolcapone

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19
Q

Tolcapone–can cause??

A

COMT-Inhib

may cause fulminating hepatic necrosis—–need to monitor liver enzymes

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20
Q

Dopamine rec agonists work where in brain

A

basal ganlia

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21
Q

Which drug causes more movement disturbances and dyskineasias:
-Levodopa OR Dopamine rec agonists?

A

LEVODPA

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22
Q

Bromocriptine
Pramipexole
Ropinirole

A

dopamine rec agonists

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23
Q

Which receptors does Bromocriptine stimulate

A

dopamine
alpha
serotonin

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24
Q

Which patients need to be cautious when using Bromocriptine

A

Hx of MI or Periph vasc disease due to incr risk of vasospasms

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25
Q

what condition can administrtion of bromocriptine worsen?

A

psychiatric conditions

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26
Q

Bromocriptine is a _____ derivative

A

ERGOT–fungus

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27
Q

Amantadine

A

anti-viral

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28
Q

MOA amantadine

A

increases presynaptic dopamine release and improves long term levodopa induces dyskineases

  • tolerance develops quick
  • few SE
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29
Q

IND for amantadine

A

Early onset PD with mild s/s

30
Q

Antimuscarinics for PD MOA

A

blocks excitatory cholinergic effect

31
Q

IND for antimuscarinics in PD

A

Under 70 with TREMOR***

32
Q

does Antimuscarinic agents improve dyskinesisas?

A

NO

33
Q

Trihexyphenidyl and Benztropine

A

Antimuscarinics for PD

34
Q

SE of Trihexyphenidyl and Benztropine

A

constipation, dry mouth, blurred vision, tachycardia urinary retention

35
Q

Contraindicatinos for Trihexyphenidyl and Benztropine

A

BPH and glaucmoma PT

36
Q

Loss of cortical neurons
amyloid deposition (senile plaques)
Neurofibrillary tangles–tau proteins

A

Three distinguishing features of AlzD

37
Q

Donepezil
Galantamine
Memantine
Rivastigmine

A

Anti-AD

38
Q

1st line tx for AD

A

Acetylcholinesterase Inhibitors

**donepezil

39
Q

MOA for Donepezil

SE

A

reversibly inhibits ACHE

  • **ACH levels remain high in junction
  • **incr in stimulation of nicotinic and muscarinic receptrs

SE:
-Nausea
dizziness
insomnia

40
Q

2nd line tx for AD

MOA of drug

A

N-methyl-d-aspartate (NMDA) Antagonist
MEMANTINE
MOA: blocking NMDA–decrease neuronal excitation b glutamate—-helps improve cognition and funct capacty

41
Q

IND for Memantine

A

2nd line tx for AD

*used in mod-severe

42
Q

SE of memantine

A

agitation dizzines HA—CNS

dystonic rxns

43
Q

Tx for acute exacerbation of MS

A

IV corticosteroids HIGH DOSE

44
Q

TX for relapse-remitting/progressive disease of MS

A

B-interferon

45
Q

Tx for insomnia

A

Zolpidem–prefered hypnotic
or
Zalelon: sim to zolpidem.. but fewwer residual efects on psychomotor and cognitive funct
OR
Eszopiclone–good forp to six months
OR
Ramelteon–can be given Long term—for diff falling asleep**

46
Q

Insomina + anxiety tx

A

benzos

Flurazepam or quazepam

47
Q

ramelton or zalepon–good for what type of insomnia

A

ISSUES FALLING asleep

48
Q

are the medications used for insomnia controlled substanes?

A

yes

49
Q

DOA for phenobarb

A

long acting

50
Q

DOA for secobarbital

A

short acting 2-4hrs

51
Q

PT cannot fall asleep but can stay asleep, which barbituate to give?

A

Secobarbital

52
Q

what drugs have replaced barbituates?

A

benzos

53
Q

high doses of barbituates cause?

A

CNS depressing

54
Q

low doses of barbituates cause?

A

decr in Reticular activating system

sedation/sleep

55
Q

MOA for sedative-hypnotic drugs

A

GABA**

regulates chlorine channel

56
Q

whhat receptor does GABA bind to

A

GABA a

57
Q

GABA effects

A

reduces generation of APs and inhibits neuronal activity

58
Q

Barbituates are used as_____ to tx___ and ____

A

sedative
insomnia
anxiety

59
Q

what drug is used in tx neonatal hyperbilirubinemia

A

phenobarbital

60
Q

SE of barbituates

A

sedation, nausea, ***TERATOGENI

  • p-450—can decr other drug levels–not good for combo use with digitalis, phenytoin
  • **dependency
61
Q

Barbituate OD

TX?

A

cardiac and respiratory depression**
tx with mechanical ventilaion
dyalissi
alkalinzation of urine with sodium bicarb

62
Q

which drug MOA

  • **interferes with electrolyte transport across neuroanl cell membranes
  • inhibit neuron activation
  • potentiate GABAa receptor activity
  • increase flow of Cl- ion—cell mem hyperpolorization
A

BARBITUATES

63
Q

anxiolytics

A

anti anxiety drugs

64
Q

Midazolam and Triazolam are ___acting

A

short

65
Q

Benzos are divinded into three groups based on

A

DOA

66
Q
Lorazepam 
temazepam
oxazepam
alprazolam
chlordiazepoxide 
are all \_\_\_\_\_ acting
A

intermediate

67
Q

diazepam
prazepam
clonazepam
flurazepam

A

long acting

68
Q

which benozs are used as anesthetics

A

midazolam

dizepam

69
Q

which drug prolongs effects of benzo

A

cimitidine–antihistamine

70
Q

cimitidine + benzo

A

increase DOA of benzo because it blocks enzyme inhibition