Parkinson disease, Huntigton disease drugs, headaches - drugs

Question 1

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

Answer 1

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

Question 2

Huntington disease - symptoms / and movment disorders

Answer 2

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

Question 3

Huntington disease - neurotransmitter alternations

Answer 3

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

Question 4

Huntington disease - MRI

Answer 4

Atrophy of caudate and putamen with hydrocephalus ex vacuo

Question 5

Huntington disease - Drugs

Answer 5

1. Haloperidol
2. Tetrabenazine
3. reserpine

Question 6

Huntington Drugs - Haloperidol - mechanism of action

Answer 6

D2 receptor antagonist

Question 7

Huntington Drugs - Tetrabenazine - mechanism of action

Answer 7

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

Question 8

VMAT

Answer 8

vesicular monoamine transporter

Question 9

Huntington Drugs and mechanims of action

Answer 9

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

Question 10

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

Answer 10

limits dopamine vesicle packagings and release

Question 11

Alzheimer disease - histology exp

Answer 11

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

Question 12

Alzheimer disease - drugs and mechanism of action

Answer 12

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

Question 13

Alzheimer disease - groups of drugs (no the drugs)

Answer 13

1. NMDA receptor antagonists

2. Ache inhbitors

Question 14

Alzheimer disease - NMDA receptor antagonist - drug

Answer 14

Memantine

Question 15

Memantine - side effects

Answer 15

1. Dizziness
2. confusion
3. hallucinations

Question 16

Memantine - mechanims of action

Answer 16

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

Question 17

Alzheimer disease - Ache inhibitors - drugs

Answer 17

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

Question 18

Alzheimer disease - Ache inhibitors - side effects

Answer 18

1. nausea
2. dizziness
3. insomnia

Question 19

Parkinson disease - histology

Answer 19

1. Lewy bodies

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

Question 20

Parkinson disease - symproms

Answer 20

MNEMONIC: TRAP

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

Question 21

Parkinsonism mechanism

Answer 21

loss of dopaminergic neurons and excess cholinergic activity

Question 22

Parkinson disease drug - strategy

Answer 22

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

Question 23

Parkinson disease drug - dopamine agonists (drugs)

Answer 23

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

Question 24

Parkinson disease drug - dopamine agonists - preferred drugs

Answer 24

non ergot:

1. pramipexole
2. ropinirole

Question 25

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

Answer 25

amantadine --> increases dopamine release and decreases dopamine reuptake

Question 26

amantadine - clinical use

Answer 26

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

Question 27

amantadine is also used as an antiviral against

Answer 27

1. influenza A | 2. rubella

Question 28

amantadine - toxicity

Answer 28

1. ataxia | 2. livedo reticularis

Question 29

Parkinson desease drugs - increase L-DOPA availability - mechanism

Answer 29

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

Question 30

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

Answer 30

1. carbidopa 2. entacapone 3. tolcapone

Question 31

entacapone - mechanism of action

Answer 31

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

Question 32

tolcapone - mechanism of action

Answer 32

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

Question 33

carbidopa - mechanism of action

Answer 33

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)

Question 34

Parkinson disease drug - COMT inhibitors

Answer 34

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

Question 35

Parkinson disease drug - prevenet dopamine breakdown - mechanism

Answer 35

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

Question 36

Parkinson disease drug - prevenet dopamine breakdowν drugs

Answer 36

1. selegiline (and rasagilini) | 2. Tocpapne

Question 37

tolcapone - mechanism of action

Answer 37

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

Question 38

selegiline - mechanism of action

Answer 38

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

Question 39

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

Answer 39

dopamine over norepinephrine and seretonin

Question 40

selegiline - clinical use

Answer 40

adjunctive agen to L-dopa in treatment of Parkinson

Question 41

selegiline - toxicity

Answer 41

May enhance adverse effects of L-DOPA

Question 42

L-dopa to dopamine - enzyme?

Answer 42

DOPA decarboxylase

Question 43

L-dopa to 3-0-methyldopa

Answer 43

COMT

Question 44

L-dopa - clinical use

Answer 44

Parkinson disease

Question 45

L-dopa - toxicity

Answer 45

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

Question 46

L-dopa - mechanism of action

Answer 46

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

Question 47

L-dopa to dopamine in the CNS- enzyme?

Answer 47

CNS dopa decarboxylase

Question 48

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

Answer 48

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

Question 49

memantine - side effects

Answer 49

1. Dizziness 2. confusion 3. hallucinations

Question 50

Parkinson disease - drug that causes livedo reticularis

Answer 50

amantadine

Question 51

Parkinson disease - benzotropine - mechasism of action and uses

Answer 51

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

Question 52

Parkinson disease - peripheral COMT inhibitors

Answer 52

1. entacapone | 2. tolcapone

Question 53

Parkinson disease - central COMT inhibitors

Answer 53

tolcapone

Question 54

all Parkinson drugs and mechanism of action (shortly)

Answer 54

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)