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Pharma 2nd semester > A. 34. Drugs used for treatment of neurodegenerative disorders. Nootropic drugs. > Flashcards

A. 34. Drugs used for treatment of neurodegenerative disorders. Nootropic drugs. Flashcards

1
Q

drugs used in Parkinson’s disease

A

“Lets Call iT PARkinson’S DisEase Please”

Levodopa
Carbidopa 
Tolcapone  
pramipexole 
Amantadine
Ropinirole 
Selegiline

Diphenhydramine
Entacapone
Procyclidine

Benztropine, Trihexyphenidyl*

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2
Q

drugs used in Alzheimer disease

A

“Mom! Dona Riva dances at the Gala”

Memantine
Donepezil
Rivastigmine
Galantamine

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3
Q

what is Piracetam?

A

Nootropic agent

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4
Q

what are Nootropics?

A

drugs, supplements, and other substances that may improve cognitive function (memory, creativity, motivation) in healthy individuals

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5
Q

what is the mechanism of Piracetam?

A

binds to the protein SV2A on the synaptic vesicle –> interfere with neurotransmitter release

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6
Q

what is Piracetam’s therapeutic potential?

A

cognition enhancer and in the treatment of schizophrenia, depression, ADHD, and Parkinson’s disease.

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7
Q

how are the drugs for Alzeheimer given?

A

orally

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8
Q

what are Rivastigmine , Galantamine and Donepezil?

A

Acetylcholine-esterase inhibitors (centrally-acting)

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9
Q

1st line agent for Alzheimer’s disease?

A

Rivastigmine
Galantamine
Donepezil

*provide a modest reduction in the rate of loss of cognitive function

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10
Q

side effects of rivastigmine, galantamine, donepezil

A

Nausea, vomiting
Diarrhea
bradycardia

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11
Q

what is Memantine?

A

glutamate NMDA receptor blocker

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12
Q

side effects for memantine

A

“car”
confusion
agitation
restlessness

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13
Q

why is Levodopa given with Carbidopa?

A

cause Carbidopa acts as a peripheral dopa decarboxylase inhibitor (does not cross the BBB)

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14
Q

what is Levodopa and what does it do?

A

it’s a dopamine precursor
enters the brain via LAT
converted by DOPA decarboxylase to dopamine –> ↑ dopamine activity in the brain (↓ bradykinesia)

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15
Q

how are the drugs for Parkinson’s disease given?

A

orally

*diphenhydramine also has IV preparation for acute drug-induced parkinsonism (acute dystonia)

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16
Q

what is the duration of action of Levodopa?

A

6-8 hours

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17
Q

what is Levodopa+carbidopa for?

A

Parkinson’s disease

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18
Q

side effects of Levodopa+carbidopa

A

GI distress- nausea, vomiting anorexia
Dyskinesia (on/off phenomenon)
hypotension, arrhythmias (peripheral effect of dopamine)
psychosis, agitation, anxiety, hallucinations (central effect of dopamine)

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19
Q

what is the mechanism of action of Selegiline?

A

selective MAO-B inhibitor–> ↓ metabolism of dopamine –>↑ dopamine activity in the brain (↓ bradykinesia)

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20
Q

can we see a “cheese effect” when given Selegiline?

A

no

there is no tyramine interaction like in non-selective MAO inhibitors.

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21
Q

does selegiline have a short T1/2?

A

no, long

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22
Q

what type of metabolism is seen with Selegiline?

A

hepatic
form: 1. desmethylselegiline (neuroprotective)
and 2. amphetamine (psychostimulant)

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23
Q

when is selegiline given?

A

as monotherapy for Parkinson’s disease (early stage) or in adjunct to levodopa+carbidopa (advanced stage)

24
Q

side effects of selegiline

A

“Pork DISH”

Psychosis
Dyskinesia 
Insomnia 
Serotonin syndrome (when used with SSRI'S) 
Hypotension
25
Q

name 2 COMT inhibitors

A

Entacapone

Tolcapone

26
Q

where does Entacapone work?

A

periphery

27
Q

where does Tolcapone work?

A

periphery+CNS

28
Q

what is the daily dose of Entacapone?

A

5 times

29
Q

what is the daily dose of Tolcapone?

A

3 times

30
Q

side effects of Entacapone and Tolcapone?

A

sleep disorders

tolcapone: hepatotoxicity

31
Q

when do we use Entacapone or Tolcapone?

A

Parkinson’s disease (adjunct to levodopa/carbidopa)

32
Q

mechanism of COMT inhibitors

A

periphery: inhibition of COMT enhances levodopa uptake and efficacy
CNS: inhibition of COMT enhances dopamine activity

33
Q

what converts Levodopa to 3-OMD (3-O-Methyldopa)?

A

COMT

34
Q

what does 3-OMD do?

A 
partial agonist (antagonist in the presence of a full agonist)
competes with levodopa for transport and activity
35
Q

name the Dopamine agonists

A

Ropinirole
Pramipexole
Bromocriptine
Pergolide

36
Q

what is Ropinirole?

A

D₂ receptor agonist

non-ergot derivative

37
Q

what is pramipexole?

A

D₃ receptor agonist

non-ergot derivative

38
Q

what type of metabolism does Ropinirole go through?

A

hepatic

39
Q

what type of metabolism does pramipexole go through?

A

renal

40
Q

how many times are ropinirole and pramipexole administered?

A

3 times daily

41
Q

does pramipexole have a short T1/2?

A

yes

42
Q

what are bromocriptine and pergolide?

A

partial D₂ receptor agonists

Ergot alkaloid derivatives

43
Q

side effects of dopamine agonists

A 
Dyskinesia
Psychosis
hallucinations
anorexia, nausea 
bromocriptine--> orthostatic hypotension
44
Q

indications for Ropinirole AND pramipexole

A
  1. Parkinson’s disease -monotherapy/adjunct to levodopa
  2. pramipexole: potential antioxidant
  3. Restless leg syndrome (RLS)- first-line treatment!
45
Q

indications for bromocriptine and pergolide

A
  1. Parkinson’s disease -monotherapy/adjunct to levodopa
  2. hyperprolactinemia
  3. acromegaly
46
Q

what is the mechanism of action of Amantadine?

A
  1. Antiviral medication
  2. enhances the effect of endogenous dopamine (↑ the synthesis and inhibiting its uptake)
  3. muscarinic blockade
  4. NMDA blockade
47
Q

how is Amantadine eliminated?

A

by the kidneys

48
Q

when is Amantadine used?

A

for Parkinson’s disease (adjunct to levodopa/carbidopa)

49
Q

side effects of Amantadine

A

Livedo reticularis
Psychosis
Gi disturbances
Ataxia

50
Q

mechanism of action of antimuscarinics

A

muscarinic blockade–> ↓ the excitatory activity of cholinergic neurons in the striatum–> improves tremor and rigidity
*no effect on bradykinesia

51
Q

names the antimuscarinic agents

A 
Procyclidine 
Diphenhydramine 
Benztropine 
Trihexyphenidyl 
"Tri PARKing my mercedes BENZ"
52
Q

is antimuscarinic recommended as monotherapy for early Parkinson’s disease?

A

no

53
Q

what is the other indication for antimuscarinics except for Parkinson’s disease?

A

drug-induced extrapyramidal symptoms

54
Q

side effects of Antimuscarinics

A

“atropine-like effects”:

dry mouth
urinary retention
constipation
hyperthermia
tachycardia
Mydriasis 
blurred vision
toxicity (3 C's)--> cardiotoxicity, convulsions, coma
55
Q

contraindications of antimuscarinics

A

glaucoma

prostatic hyperplasia

Pharma 2nd semester (49 decks)

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