Parkinson disease, Huntigton disease drugs, headaches - drugs Flashcards Preview

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Flashcards in Parkinson disease, Huntigton disease drugs, headaches - drugs Deck (54):
1

Huntington disease - mode of inferitence / chromosome and trinucleotide repeat / age

AD trinucleotide repeat disorder (anticipation)
ch 4
CAG
20-50

2

Huntington disease - symptoms / and movment disorders

1. choreiform movements
2. aggression --> athetosis, chorea
3. depression
4. dementia

3

Huntington disease - neurotransmitter alternations

1. increased dopamine
2. decreased GABA
3. decreased Ach

4

Huntington disease - MRI

Atrophy of caudate and putamen with hydrocephalus ex vacuo

5

Huntington disease - Drugs

1. Haloperidol
2. Tetrabenazine
3. reserpine

6

Huntington Drugs - Haloperidol - mechanism of action

D2 receptor antagonist

7

Huntington Drugs - Tetrabenazine - mechanism of action

inhibits vesicular monoamine transporter (VMAT) --> limits dopamine vesicle packagings and release

8

VMAT

vesicular monoamine transporter

9

Huntington Drugs and mechanims of action

1. Haloperidol --> D2 receptor antagonist
2. Tetrabenazine --> VMAT inhibitor
3. reserpine --> VMAT inhibitor

10

Huntington Drugs - vesicular monoamine transporter (VMAT) inhibition --->

limits dopamine vesicle packagings and release

11

Alzheimer disease - histology exp

1. loss of ach neurons
2. senile plaques in gray matter
3. Neurofibrillary tangles

12

Alzheimer disease - drugs and mechanism of action

1. Memantine --> NMDA receptor antagonists
2. Donepezil --> Ache inhibitors
3. galantamine --> Ache inhibitors
4. rivastigmine --> Ache inhibitors
5. tacrine --> Ache inhibitors

13

Alzheimer disease - groups of drugs (no the drugs)

1. NMDA receptor antagonists
2. Ache inhbitors

14

Alzheimer disease - NMDA receptor antagonist - drug

Memantine

15

Memantine - side effects

1. Dizziness
2. confusion
3. hallucinations

16

Memantine - mechanims of action

NMDA receptor antagonists -->HELPS PREVENT EXCITOXICITY (mediated by Ca2+)

17

Alzheimer disease - Ache inhibitors - drugs

1. Donepezil
2. galantamine
3. rivastigmine
4. tacrine

18

Alzheimer disease - Ache inhibitors - side effects

1. nausea
2. dizziness
3. insomnia

19

Parkinson disease - histology

1. Lewy bodies
2. loss of dopaminergic neurons of substantia nigra pars compacta (de-pigmentation)

20

Parkinson disease - symproms

MNEMONIC: TRAP
1. Tremor (pill-rolling tremor at rest)
2. Rigidity (cogwheel)
3. Akinesia (or bradykinesia)
4. Postural instability
5. Shuffling gait

21

Parkinsonism mechanism

loss of dopaminergic neurons and excess cholinergic activity

22

Parkinson disease drug - strategy

1. dopamine agonists
2. increase dopamine availability
3. increase L-DOPA availability
4. prevent dopamine breakdown
5. curb excess cholinergic activity

23

Parkinson disease drug - dopamine agonists (drugs)

1. bromocriptine (ergot)
2. pramipexole (non-ergot)
3. ropinirole (non-ergot)

24

Parkinson disease drug - dopamine agonists - preferred drugs

non ergot:
1. pramipexole
2. ropinirole

25

Parkinson disease drug - increase dopamine availability - drugs and mechanism?

amantadine --> increases dopamine release and decreases dopamine reuptake

26

amantadine - clinical use

1. Parkinson disease
2. antiviral against influenza A and rubella

27

amantadine is also used as an antiviral against

1. influenza A
2. rubella

28

amantadine - toxicity

1. ataxia
2. livedo reticularis

29

Parkinson desease drugs - increase L-DOPA availability - mechanism

agents prevent peripheral (pre-BBB) L-DOPA degradation --> increase L-DOPA entering CNS --> increase central L-DOPA available for conversion to dopamine

30

agents that prevent peripheral (pre-BBB) L-DOPA degradation

1. carbidopa
2. entacapone
3. tolcapone

31

entacapone - mechanism of action

prevent peripheral L-DOPA degradation to 3-0-methyldopa (3-OMD) by inhibiting COMT

32

tolcapone - mechanism of action

1. prevent peripheral L-DOPA degradation to 3-0-methyldopa (3-OMD) by inhibiting peripheral COMT
2. blocks conversion of dopamine to DOPAC by inhibiting central COMT

33

carbidopa - mechanism of action

block peripheral conversion of L-DOPA to dopamine by inhibiting peripheral DOPA decarboxylase --> reduse side effects of peipheral L-DOPA conversion into dopamine (eg. nausea, vomiting)

34

Parkinson disease drug - COMT inhibitors

1. tolcapone (central and peripheral COMT)
2. entacapone (peripheral COMT)

35

Parkinson disease drug - prevenet dopamine breakdown - mechanism

agents act centrally (post-BBB) to block breakdown of dopamine --> increase available dopamine

36

Parkinson disease drug - prevenet dopamine breakdowν drugs

1. selegiline (and rasagilini)
2. Tocpapne

37

tolcapone - mechanism of action

1. prevent peripheral L-DOPA degradation to 3-0-methyldopa (3-OMD) by inhibiting peripheral COMT
2. blocks conversion of dopamine to DOPAC by inhibiting central COMT

38

selegiline - mechanism of action

blocks conversion of dopamine into DOPAC by selectively inhibiting MAO-B

39

MAO-B preferentially metabolizes .... over ...

dopamine
over
norepinephrine and seretonin

40

selegiline - clinical use

adjunctive agen to L-dopa in treatment of Parkinson

41

selegiline - toxicity

May enhance adverse effects of L-DOPA

42

L-dopa to dopamine - enzyme?

DOPA decarboxylase

43

L-dopa to 3-0-methyldopa

COMT

44

L-dopa - clinical use

Parkinson disease

45

L-dopa - toxicity

1. arrhythmias from increased peripheral formation of catecholamines
2. Long term use can lead to dyskenesia following administration (on-off phenomeno), akinesia between doses

46

L-dopa - mechanism of action

unlike dopamine, L-dopa can cross BBB and is converted by dopa decarboxylase in the CNS to dopamine

47

L-dopa to dopamine in the CNS- enzyme?

CNS dopa decarboxylase

48

Parkinson disease drug - curb excess cholinergic activity - drugs and action

Benzotropine (antimuscarinic) --> improves tremor and rigidity but has little effect on bradykinesia

49

memantine - side effects

1. Dizziness
2. confusion
3. hallucinations

50

Parkinson disease - drug that causes livedo reticularis

amantadine

51

Parkinson disease - benzotropine - mechasism of action and uses

antimuscarinic --> improves tremor and rigidity but has little effect on bradykinesia

52

Parkinson disease - peripheral COMT inhibitors

1. entacapone
2. tolcapone

53

Parkinson disease - central COMT inhibitors

tolcapone

54

all Parkinson drugs and mechanism of action (shortly)

1. Bromocriptine (dopamine agonist)
2. Pramipexole (dopamine agonist)
3. ropinirole (dopamine agonist)
4. amantadine (incr dopamine release and inh reuptake)
5. Levodopa (increases dopamine levels in CNS)
6. carbidopa (DOPA decarboxylase inhibitor)
7. entacapone(peripheral COMT inhibitor)
8. tolcapone (central and peripheral COMT inhibitor)
9. selegiline (MAO-B inhibitor) (and rasagilini)
10. benzotropine (antimuscarinic)