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Adv Pharm I > Exam 2 Neuro > Flashcards

Exam 2 Neuro Flashcards

1
Q

Medications used to treat Alzheimer’s

A

Cholinesterase inhibitors
NMDA receptor antagonist
Combination

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2
Q

Cholinesterase inhibitors

A

Rivastigmine
Donepezil
Galantimine

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3
Q

NMDA receptor antagonist

A

Memantine

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4
Q

Combination Rx for alzheimers

A

Donepezil + memantine

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5
Q

MOA Cholinesterase inhibitors

A

Selectively inhibit cholinesterase (enzyme that hydrolyzes or inactivates Ach) in CNS.
Increase Ach concentrations in cerebral cortex

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6
Q

Benefit of cholinesterase inhibitors

A

May slow deterioration of cognitive function. Preserves memory, learning, attention

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7
Q

Route of administration for donepezil

A

PO, ODT

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8
Q

Route of administration for rivastigmine

A

PO, transdermal patch

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9
Q

Route of administration for galantamine

A

PO

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10
Q

Adverse effects for all cholinesterase inhibitors

A

Diarrhea, nausea/vomiting, bradycardia, dizziness, syncope, urinary incontinence, hypersalivation, sweating

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11
Q

Adverse effect of donepezil

A

Insomnia

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12
Q

Adverse effect of rivastigmine

A

Hepatotoxicity

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13
Q

Adverse effect of galantamine

A

Weight gain

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14
Q

Drug interactions of cholinesterase inhibitors

A

Anticholinergic drugs

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15
Q

Cholinesterase inhibitor adverse effects pneumonic

A

DUMBELS - diarrhea, urination, miosis, bronchospasm, Messi, lacrimation, salivation

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16
Q

Cholinergic crisis s/s - pneumonic

A

SLUDGE - salivation, lacrimation, urination, defecation, gastric upset, emesis

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17
Q

MOA of memantine

A

NMDA receptor antagonist. Attenuates excitotoxic effects of glutamate (neuroprotective)

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18
Q

Adverse effects for memantine

A

Constipation, headache, confusion, dizziness, hallucinations, hypertension

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19
Q

NMDA receptor antagonist characteristics

A

Indicated for moderate to severe disease, can be used in combination with cholinesterase inhibitors

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20
Q

Parkinson’s mortality is due to

A

Immobility - aspiration PNA, clotting disorder

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21
Q

Parkinson’s without treatment

A

Progress to akinetic state 5-10 years

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22
Q

S/s Parkinson’s

A

Severe loss of dopaminergic neurons in substantia negra

Presence of Lewy bodies - creates imbalance of acetylcholine and dopamine

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23
Q

Pharmacologic targets for Parkinson’s disease

A

See slide 2 on page 9; neuro ptt 1

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24
Q

Extrapyramidal symptoms in Parkinson’s

A

Bradykinesia, muscular rigidity, resting tremor, postural instability, tics

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25
Q

Presentation of Parkinson’s disease

A

Extrapyramidal symptoms, speech disturbances, anxiety

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26
Q

Dopaminergic agents used for Parkinson’s disease

A

Levodopa, amantadine

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27
Q

Levodopa MOA

A

Biosynthetic precursor of dopamine. Increases concentration of dopamine in the brain

28
Q

Metabolism of levodopa

A

Metabolized in peripheral tissue by decarboxylase and catechol-O-methyl transferase (COMT). Less than 1% of Rx reaches brain if given as monotherapy. Need decarboxylase inhibitor and COMT inhibitor

29
Q

Characteristic of levodopa

A

ALWAYS given in combination with carbidopa

30
Q

Adverse effects of levodopa

A

N/V (take antacid 30m prior), orthostatic hypotension, sedation, depression, delirium, paranoia, delusions, hallucinations, motor fluctuations

31
Q

New formulation of levodopa (name)

A

Rytary

32
Q

Characteristics of Rytary

A

Minimal reduction in motor fluctuations, less freq. dose, can be opened & sprinkled, not interchangeable with sinemet, EXPENSIVE

33
Q

MOA carbidopa

A

Decarboxylase inhibitor. Inhibits conversion of levodopa to dopamine in peripheral tissues. Increases amount of levodopa that enters brain. Decreases CVS/GI adverse effects

34
Q

Carbidopa negative aspects

A

Wearing off phenomenon. Loss of efficacy over time. Effective for 2-5 years or need higher dose.

35
Q

Carbidopa administration

A

Always given in combination with levodopa (sinemet)

36
Q

Titration of carbidopa

A

Titrate slowly to a minimum of 75 mg daily - reduce incidence of peripheral conversion // reduce AES

37
Q

COMT inhibitors

A

Tolcapone and entacapone

38
Q

COMT inhibitors MOA

A

Inhibits peripheral metabolism of levodopa through inhibition of COMT

39
Q

COMT inhibition used in combo with?

A

Levodopa/carbidopa to enhance effectiveness and **manage wearing off
** Entacapone combined with levodopa/carbidopa

40
Q

Adverse effects of COMT inhibitors

A

Hepatotoxicity (tolcapone) — monitor LFTs, orthostatic hypotension, diarrhea, hallucinations, brown-orange urine discoloration

41
Q

MAO inhibitors

A

Selegiline, rasagiline, safinamide

42
Q

MAO Inhibitors MOA

A

Irreversibly inhibits the MAO enzyme system.
MAO-A: catabolize serotonin and norepinephrine
MAO-B: catabolize dopamine

43
Q

Selective MAO-B

A

At low doses

Selegiline, rasagiline

44
Q

Characteristics of selegiline/rasagiline

A

Neuroprotective - blocks free radical formation with dopamine degradation that cause neuronal degeneration. ***Enhances and prolongs effects of dopamine.

45
Q

Adverse effects of MAO inhibitors

A

Augments levodopa toxicities (dyskinesias, psychiatric symptoms), N/D, orthostatic hypotension, hallucinations, insomnia, serotonin syndrome (in combo w/ serotonergic agents)

46
Q

MAO inhibitors interactions

A

At high doses (should be avoided) - MAO-A can be inhibited.
AVOID foods/drinks high in tyramine (aged cheese, smoked meat, red wine)
Reduction in tyramine catabolism —> hypertensive crisis

47
Q

MAO Inhibitors typically used as?

A

Adjunctive therapy

48
Q

Safinamide

A

MAO-B inhibitor, DA reuptake inhibitor

49
Q

DA receptor agonists MOA

A

Directly activate the dopamine receptors in the brain.

Can also activate other dopamine receptors

50
Q

Advantages of DA-receptor agonists over levodopa

A

Direct action on receptor —> less free radicals released.
Less motor fluctuations, dyskinesias.
Longer half life = longer action

51
Q

Types of DA-receptor agonists

A

Pramipexole, ropinirole, apomorphine, rotigotine

52
Q

Pramipexole characteristics

A

Requires renal adjustment

53
Q

Ropinirole characteristics

A

Metabolized by CYP1A2, cigarette smoking INDUCES CYP1A2

54
Q

Apomorphine characteristics

A

SubQ injection, requires close supervision, infusion related rxn - requires test dose. Profound nausea — requires pretreatment.

55
Q

Rotigotine characteristics

A

Transdermal patch

56
Q

Disadvantages of DA receptor agonists

A

Difficult to use in elderly d/t increased CNS effects. May cause/exacerbate dyskinesias

57
Q

Adverse effects of DA-receptor agonists

A

N/V - reduced with food, anorexia, postural hypotension, sedation, hallucinations, confusion, vivid dreams, impaired impulse control, sleep attacks, behavior (impulse) side effects (gambling/shopping).

58
Q

DA-Receptor agonists caution

A

Patients with hx of psychotic illness

59
Q

Acetylcholine receptor antagonists

A

Benztropine, trihexyphenidyl

60
Q

MOA acetylcholine receptor agonists

A

Competes with Ach at muscarinic receptors. Block dopamine reuptake —> prolongs dopamine effect

61
Q

Which medication helps reduce tremor more than other manifestations?

A

Acetylcholine receptor antagonists (benztropine, trihexyphenidyl)

62
Q

Adverse effects of acetylcholine receptor antagonists

A

Anticholinergic - sedation, depression, CONFUSION. Dry mouth, blurred vision, constipation, urinary retention

63
Q

Which medications have a favorable effect on rigidity and bradykinesia?

A

Acetylcholine receptor antagonists

64
Q

Patients often find which medications difficult to tolerate?

A

Acetylcholine receptor antagonists

65
Q

Many Parkinson’s disease patients have this associated symptom

A

Psychosis

66
Q

Pimavanserin MOA

A

Selectively blocks 5-HT2a and 2c receptors

67
Q

Adverse effects of pimavanserin

A

Worsening hallucinations, QTc prolongation, death; BBW increased mortality in elderly patients with dementia related psychosis

Adv Pharm I (8 decks)

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