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4. Pharm III > 1- Parkinson's & Alzheimer's > Flashcards

1- Parkinson's & Alzheimer's Flashcards

1
Q

Parkinson’s disease is characterized by a loss of what neurons?

A

DA neurons in the substantia nigra pars compacta (sx once 70-80% loss)

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2
Q

What disease is characterized by bradykinesia, muscular rigidity, resting tremor, and impairment of postural balance and gait?

A

Parkinson’s disease

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3
Q

What is the MOA for L-dopa?

A

Increase DA levels (replacement therapy)

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4
Q

One L-dopa crosses the BBB it is converted to what?

A

DA

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5
Q

What are the SE of L-dopa?

A

Nausea and vomiting

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6
Q

What is the use for L-dopa?

A

Improvement in PD sx (specifically bradykinesia)

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7
Q

Will the effectiveness of L-dopa increase or decrease over time? Why?

A

Decrease. L-dopa does not affect the progression of the disease and neurons continue to degenerate

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8
Q

Will L-dopa tx the sx in drug induced Parkinson’s?

A

No

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9
Q

How is L-dopa taken?

A

Orally (absorption is delayed by food), need high doses to cross BBB

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10
Q

What is the use of L-dopa/Carbidopa?

A

Decreases peripheral effects of L-dopa (Nausea)

Carbidopa will block conversion of L-dopa to DA peripherally decreasing the dose of L-dopa needed

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11
Q

What are the SEs of L-dopa/Carbidopa?

A

GI (N/V)
CV (postural hypotension, arrhythmias, HTN)
Dyskinesias (tx by reducing L-dopa dose)
Behavioral (depression anxiety, agitation, sleep problems, psychosis - tx w/ atypical antipsycholytics)

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12
Q

What is the On-Off Phenomenon?

A

Fluctuations in clinical response of PD to meds when pt is on successful L-dopa therapy.

On = improved mobility
Off = akinesia (due to falling drug levels)
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13
Q

What drug can be used as a rescue in a Parkinson’s pt w/ “Off”?

A

Apomorphine

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14
Q

How can you prevent the On-Off phenomenon in PD pts?

A

Increase dose frequency and L-dopa absorption w/ diet changes

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15
Q

L-dopa will interact w/ what drugs?

A

MAO-AIs => HTN crisis

Pyridoxine => Increased peripheral metabolism, decreasing L-dopas effectiveness

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16
Q

What is L-dope contraindicated?

A 
Psychosis
Closed Angle glaucoma (increases IOP)
CVD
Active PUD (increased GI bleeding)
Malignant melanoma (L-dopa = melanin precursor)
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17
Q

What is the MOA for MAO Inhibitors (MAOIs)?

A

Inhibits MAO-B in CNS => Inhibits DA metabolism

does not affect peripheral metabolism of DA by MAO-A

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18
Q

What is the drug class for Selegiline?

A

MAOI inhibitor

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19
Q

What is the drug class for Rasagiline?

A

MAOI inhibitor

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20
Q

What is the drug class for Safinaminde?

A

MAOI inhibitor

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21
Q

What are the SEs of MAO-BIs?

A

Insomnia
Severe HTN (if given w/ other MAOIs)
Increase SE of L-dopa
Serotonin syndrome

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22
Q

What medication should you not combine w/ MAO-BIs?

A

Meperidine => can lead to stupor, rigidity, agitation, hyperthermia, possible serotonin syndrome

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23
Q

What is the MOA of COMT inhibitors?

A

Inhibits BA and L-dopa metabolism

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24
Q

What is the MOA of Tolcapone?

A

Inhibits COMT in CNS and periphery (prolongs DA in CNS and prolongs pools of L-dopa for transport

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25
Q

What drug class is Tolcapone?

A

COMT inhibitor

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26
Q

What drug class is Entacapone?

A

COMT inhibitor

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27
Q

What is the MOA of Entacapone?

A

inhibits COMT in periphery only (increases pool of L-dopa for transport into the brain)

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28
Q

What are the SEs of COMT inhibitors?

A

orange color in urine, dyskinesia, confusion, nausea, hypotension, abd pain, sleep disturbances

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29
Q

What is the MOA for DA receptor agonists?

A

Stimulate DA receptors directly (primarily DA D2)

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30
Q

Will DA receptor agonists continue to be effective as PD progresses?

A

Yes because they act directly on receptors

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31
Q

What drug class is Bromocriptine?

A

DA Receptor agonist

32
Q

What is a SE of Bromocriptine?

A

Erythromelalgia (red, painful, swollen, itchy feet)

33
Q

What medication is given to a pt w/ mutation in DCC (can’t synthesize DA)?

A

Bromocriptine

34
Q

What drug class is Ropinirole?

A

Dopamine receptor agonist (purely DA D2)

35
Q

What drug class is Pramipexole?

A

Dopamine receptor agonist (newer)

36
Q

What is a SE of Ropinirole and Pramipexole?

A

Narcolepsy

37
Q

What 2 drugs are used as monotherapy for mild PD?

A

Ropinirole and Pramipexole

38
Q

What is the DOC for restless leg syndrome?

A

Ropinirole

39
Q

What medication is a transdermal patch used for PD and RLS?

A

Rotigotine (DA receptor agonist)

40
Q

What is the use of Apomorphine?

A

Rescue for “off” periods in pts w/ optimized L-dopa therapy

41
Q

How is Apomorphine administered?

A

Injected

42
Q

What are the SEs of Apomorphine?

A

Nausea

*give pt trimethobenzamide (antiemetic) prior to administration

43
Q

Why is Apomorphine not given w/ Odansetron (antiemetic)?

A

Targets 5HT => HTN and LOC

44
Q

Why is Apomorphine not given w/ Prochlorperazine (antiemetic)?

A

Blocks DA D2 receptors

45
Q

What is the MOA for Apomorphine?

A

DA receptor agonist

46
Q

What are the SEs of DA receptor agonists?

A

GI: Anorexia, N/V => take w/ meals
CV: Postural hypotension, cardiac arrhythmias (D/C)
Dyskinesia (reduce dose)
Mental disturbances: confusion, hallucinations, delusions
Erythromelalgia: Bromocriptine
Prolactin: DA agonists decrease release

47
Q

What is the MOA of Amantadine?

A

Increase DA neurotransmission

48
Q

What is the use of Amantadine?

A

Treat early or mild cases of PD (also antiviral for influenza)

49
Q

What is a SE of Amantadine?

A

Livedo reticularis- reddish/blue spotting of skin, restlessness, depression, confusion, hallucination, peripheral edema

50
Q

What are the SE of Amantadine OD?

A

Toxic psychosis and convulsions

51
Q

What is the drug class of Benztropine?

A

Anticholinergic

52
Q

What is the drug class for Trihexyphenidyl?

A

Anticholinergic

53
Q

What is the MOA of anticholinergics?

A

Muscarinic receptor antagonists, restores DA/Ach balance in striatum

54
Q

What is the use of Anticholinergics: benzotropine and trihexyphenidyl?

A

Improves rigidity, tremor, little effect on bradykinesia (use as adjunct therapy in PD)

55
Q

What are the SEs of Anticholinergics: benzotropine and trihexyphenidyl?

A

Constipation, urinary retention, blurred vision, sedation, confusion
* D/C medications slowly

56
Q

Diphenhydramine has what effects?

A

Anticholinergic effects

57
Q

What is the use of Pimavanserin?

A

Atypical antipsychotic for tx of psychosis and delusions/hallucinations associated w/ PD

58
Q

What is the MOA of Pimavanserin?

A

Inverse agonist/antagonist for 5-HT receptors, does not affects DA, adrenergic, cholinergic or histamine receptors

59
Q

How is Pimavanserin metabolized?

A

By CYP3A4

60
Q

What are the SEs of Pimavanserin?

A

GI, prolonged QT interval

61
Q

Is Pimavanserin approved for the tx of dementia associated w/ Alzheimer disease?

A

NO. Increases mortality

62
Q

Neuroprotection (antioxidants), pallidotomy, transplant of fetal neurons or stem cells, gene therapy, and deep brain stimulation are are all alternative txs for what?

A

Parkinson’s Disease

63
Q

The deposition of B-amyloids (inside neurons) and Tau-proteins (outside neurons) resulting in degeneration of cholinergic neurons will lead to what disease?

A

Alzheimer’s

64
Q

What is the class and MOA of Donepazil?

A

Cholinesterase inhibitor, inhibits metabolism of ACh => increased amount of ACh in the nerve terminal

65
Q

What is the class and MOA of Rivastigmine?

A

Cholinesterase inhibitor, inhibits metabolism of ACh => increased amount of ACh in the nerve terminal

66
Q

What is the class and MOA of Glantamine?

A

Cholinesterase inhibitor, inhibits metabolism of ACh => increased amount of ACh in the nerve terminal

67
Q

How are cholinesterase inhibitors metabolized?

A

By CYP450s

68
Q

Do cholinesterase inhibitors cross the BBB?

A

Yes

69
Q

What are the SEs of cholinesterase inhibitors?

A

Peripheral effects: GI (N/V/D, cramps)

70
Q

What is the use of cholinesterase inhibitors?

A

Increase brain activity and improves cognitive function

71
Q

What is the class and MOA for Memantine?

A

NMDA receptor antagonist (channel blocker)

Blocks pathological activation of NMDA receptors => reduces excitotoxic effect of glutamate and slows degeneration

72
Q

What is the use of Memantine?

A

Late stages of Alzheimers disease in combo w/ AChE-Is

73
Q

What are the SEs of Memantine?

A

Agitation, insomnia, urinary incontinence, UTI, diarrhea, competes for renal tubular secretion

74
Q

What should you monitor for pts on Memantine?

A

Monitor dose in pt w/ renal impairment

75
Q

What drug is Memantine C/I with?

A

Meperidine

4. Pharm III (16 decks)

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