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GI > Anti- N/V Drugs > Flashcards

Anti- N/V Drugs Flashcards

1
Q

Common causes of N/V

A 
Chemo/Radiation
Postop
Pregnancy
Vestibular
GI obstruction/dysmotility
Metabolic
Infections
Intracranial lesions
Non Chemo meds
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2
Q

Where are receptors that stimulates N/V

A

brain and GI tract

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3
Q

Generally, are single agents or combo of meds used for N/V control?

A

combination with different MOAs (especially with chemo and rad N/V)

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4
Q

What is the typical glucocorticosteroid used for N/V

A

Dexamethasone

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5
Q

What are benzodiazepines used for N/V

A

Alprazolam/Lorazepam

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6
Q

What is unique about N/V meds generally?

A

all antagonist (block receptor function) except cannabinoids

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7
Q

What is the suffix of serotonin antagonists?

A

-setron

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8
Q

What serotonin receptor is antagonized for N/V control?

A

5-HT3

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9
Q

What are the 5-HT3 receptor antagonists used for N/V

A

Dolasetron

Granisetron

Ondansetron

Palonosetron

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10
Q

What is Alosetron indicated for instead of N/V?

A

IBS-diarrhea

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11
Q

What are serotonin antagonists used for?

A

multiple etiologies of N/V:

Chemo and Rad NV
Postop NV
Pregnancy NV

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12
Q

Are serotonin antagonists strong, moderate or weak by themselves?

A

strong antiemetic agents

–>originally developed for chemo induced NV

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13
Q

Where do serotonin antagonists act?

A

type 3 receptors at vagal nerve

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14
Q

What is the most worrisome adverse effect of serotonin antagonists?

A

Dose-Dependent QT prolongation (Torsade’s)
–>occurs when using other QT agents (antiarrhythmics) or with electrolyte imbalances

Dolasetron high risk

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15
Q

What are some adverse effects of serotonin antagonists (minor)?

A

few CNS and GI
–>overall WELL TOLERATED

can have serotonin syndrome if large doses (doesn’t block synthesis, so can have thermoregulation dysfunction, seizures, cardiac sx)

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16
Q

Why is Dolasetron not recommended for chemo NV prophylaxis anymore?

A

high risk for dose-dependent QT prolongation

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17
Q

Serotonin antagonists have short half-lives except which drug?

A

Palonosetron and sustained-release formulations of Granisetron

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18
Q

What drugs are used in delayed chemo NV as a single dose?

A

Palonosetron

Grainsetron (Sancuso and Sustol)

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19
Q

What are drug-drug interactions associated with serotonin antagonists?

A

antiarrhythmics

QT prolonging drugs

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20
Q

What does fos mean in terms of drug names?

A

it is a prodrug (not activate until ingested and transformed)

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21
Q

What suffix is associated with Neurokinin-1 / Substance P receptor antagonists?

A

-pritant

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22
Q

What neurokinin receptor antagonists are used in combination only?

A

Netupitant

Fosnetupitant

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23
Q

Are neurokinin receptor antagonists strong, moderate or weak antiemetic agents?

A

moderate

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24
Q

Where are neurokinin receptors blocked?

A

vagal terminals in gut

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25
Q

When to use neurokinin receptor antagonists

A

chemo N/V IN COMBO with glucocorticosteroid and serotinin antagonist

PROPHYLAXIS of postop NV

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26
Q

What neurokinin is the only drug approved for prophylactic treatment of postop NV?

A

Aprepitant

–>given 3 hours before anesthesia induction

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27
Q

What neurokinin antagonists have moderate-major active metabolites and longer half-lives?

A

Netupitant

Rolapitant

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28
Q

What are common adverse effects of neurokinin antagonists?

A

GI and CNS

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29
Q

What is the initial therapy for pregnancy NV?

A

Doxylamine with pyridoxine (B6)

–> H1 antagonist

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30
Q

What are common antihistamines/ H1 antagonists?

A

Diphenhydramine (Benadryl)

Dimenhydrinate (Dramamine)

Hydroxyzine

Promethazine (Phenergan)

Meclizine

Cyclizine

31
Q

Are H1 antagonists strong, moderate or weak antiemetics?

A

weak

–>use with motion sickness and postop NV

32
Q

Where do antihistamines act (H1 receptors)?

A

in VC and vestibular system

–> ANTICHOLINERGIC properties

33
Q

What are classic anticholinergic effects via H1 receptor antagonists?

A 
Drowsiness (CNS depression)
Dry mouth
Constipation
Urinary Retention
Blurred vision
34
Q

What are possible interactions with H1 antagonists?

A

drugs that also induce anticholinergic side effects

–>cumulative

35
Q

What is the only circumstance you would give Meclizine or Cyclizine?

A

Motion sickness/Vertigo

–> H1 antagonists

36
Q

What are therapeutic uses for H1 antagonists (antihistamines)?

A

idiopathic and mild NV

postop NV

NV pregnancy (doxylamine with B6)

motion sickness/vertigo (meclizine, cyclizine)

not first line, used as add-on with chemo and rad NV

37
Q

Dopamine (D2) receptor antagonist examples

A

Chlorpromazine

Perphenazine

Prochlorperazine

Metoclopramide

others in psych

38
Q

Are D2 receptor antagonists strong, moderate or weak antiemetics?

A

weak to moderate

39
Q

What D2 antagonist to treat GI dysmotility?

A

Metoclopramide

–>stimulates ACh in GI to enhance motility and increase sphincter tone w/o messing with secretions

40
Q

What properties do D2 antagonists display?

A

anticholinergic and affect other receptors (mACh, histamine, alpha)

41
Q

What are adverse effects of D2 antagonists

A

classic anticholinergic effects:

drowsiness, dry mouth, constipation, urinary retention, blurred vision

42
Q

Therapeutic uses of D2 antagonists

A

idiopathic mild NV

postop NV

pregnany NV

GI dysmotility or gastroparesis (metoclopramide)

Chemo and Rad NV
–>use in combo with other agents d/t weak activity by themselves

43
Q

What are D2 antagonist interactions

A

other agents that induce anticholinergic side effects
–>cumulative

antiarrhythmics

antihypertensives

44
Q

What drug is a muscarinic (M1) receptor antagonist

A

Scopolamine (patch worn for 72 hours)

45
Q

What are muscarinic antagonists used for?

A

motion sickness

end-of-life care for excessive secretions

46
Q

Do muscarinic receptor blockers have anticholinergic properties?

A

yes, significant

47
Q

What is the only category of N/V drugs that are agonists?

A

cannabinoid receptor agonists

48
Q

What are the drugs in the category of cannabinoid receptor agonists?

A

Dronabinol (C-III)

Nabilone (C-II)

49
Q

Are cannabinoids highly abused?

A

YES

THC is synthetic and FDA scheduled (class 2 and 3)

50
Q

Are cannabinoids strong, moderate or weak antiemetics?

A

strong

reserved for treatment-resistant chemo NV

51
Q

What are cannabinoids reserved for?

A

treatment-resistant chemo NV

52
Q

How do cannabinoids work?

A

decrease excitability of neurons through G proteins–> minimize serotonin release

53
Q

Which cannabinoid is metabolized to several active metabolites with short onset and fewer doses per day?

A

Nabilone

Dronabinol metab to 1

54
Q

Interactions with cannabinoids

A

CNS depressants
Cardiovascular drugs
Sympathomimetics

55
Q

Define acute NV

A

less than 24 hours after chemo is given

56
Q

Define chronic NV

A

occurs more than 24 hours after chemo is given

57
Q

Define anticipatory NV

A

occurs before chemo is given (ex: second round of tmt)

58
Q

What is proper chemo NV therapy focused on?

A

prevention

59
Q

Describe high-emetogenic regimen for chemo NV

A

3 drug regimen:

Neurokinin antag
Serotonin (5-HT3) antag
Dexamethasone (glucocort)

–>give prior to and for 3 days after chemo

60
Q

What to add to high-emetogenic regimen for chemo NV

A

olanzapine (D2 antagonist)

–>increases to 4 drug regimen

61
Q

What to add to any emetogenic regimen in terms of treatment resistance for chemo NV

A

cannabinoid

–>increases to 4 drug regimen

62
Q

What can you add to any emetogenic regimen for chemo NV

A

therapy for breakthrough and anticipatory NV as needed

63
Q

Describe moderate-emetogenic regimen for chemo NV

A

2 drug regimen:

Serotonin (5-HT3) antag
Dexamethasone (glucocort)

–>give prior to and 2 days after chemo

64
Q

What to add to moderate-emetogenic regimen for chemo NV

A

neurokinin antagonist or olanzapine

—> increase to 3 drug regimen

65
Q

Describe low-emetogenic regimen for chemo NV

A 
1 drug regimen:
Dexamethasone   OR
Serotonin antag     OR
Metoclopramide    OR
Prochlorperazine

given prior to chemo

66
Q

What to add to low-emetogenic regimen for chemo NV

A

only for breakthrough and anticipatory NV

—> used for acute NV

67
Q

Compare dosing time for high, moderate and low-emetogenic regimen for chemo NV

A

High: prior to and 3 days after

Moderate: prior to and 2 days after

Low: prior to chemo

68
Q

Describe minimal-emetogenic regimen for chemo NV

A

0 drug regimen

No routine prophylaxis recommended
—> treat breakthrough and anticipatory NV if arise

69
Q

Describe breakthrough emesis regimen

A

add one agent from different drug class to current regimen

70
Q

Drugs to use for motion sickness

A

Scopolamine patch

Dimenhydrinate

Meclizine

71
Q

Drugs to use for Vertigo

A

Meclizine

Cyclizine

72
Q

Drug to use for diabetic gastroparesis/dysmotility

A

Metoclopramide

73
Q

Drugs to use for pregnancy NV

A

Vitamin B6 OR Histamine Antag with B6 OR Serotonin Antag

Dopamine Antag

Steroid OR different dopamine antag

GI (4 decks)

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