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Maddy - GI II Exam I - some pharm > Pharm - Anti Nausea/Vomiting > Flashcards

Pharm - Anti Nausea/Vomiting Flashcards

1
Q

list the serotonin (5-HT3) receptor antagonists

A
  • dolasetron
  • granisetron
  • ondansetron
  • palonosetron
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2
Q

-pitant ending indicates what drug

A

neurokinin (NK1) receptor antagonist

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3
Q

-setron ending indicates what drug

A

serotonin (5-HT3) receptor antagonist

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4
Q

list the histamine (H1) receptor antagonists

A
  • diphenydramine
  • dimenhydrinate
  • hydroxyzine
  • promethazine
  • meclizine
  • cyclizine
  • doxylamine
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5
Q

list the dopamine (D2) receptor antagonists

A
  • chlorpromazine
  • perphenazine
  • prochlorperazine
  • metoclopramide
  • haloperidol
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6
Q

list the muscarinic (M1) receptor antagonist

A

scopolamine

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7
Q

list the cannabinoid receptor agonists

A
  • dronabinol

- nabilone

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8
Q

MOA of serotonin (5-HT3) receptor antagonists

A

blocks serotonin type-3 receptors at the vagal nerve terminal and blocks signal transmission to chemoreceptor trigger zone

(blocks serotonin-receptor activation after serotonin release from intestinal enterochromaffin cells)

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9
Q

therapeutic uses of serotonin (5-HT3) receptor antagonists

A
  • chemotherapy induced N/V
  • radiation-induced N/V
  • post-operative N/V
  • N/V of pregnancy
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10
Q

adverse effects of serotonin (5-HT3) receptor antagonists

A
  • headaches
  • constipation/diarrhea (serotonin syndrome)
  • dose-dependent QT prolongation (torsades)
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11
Q

extreme caution should be used when prescribing serotonin (5-HT3) receptor antagonists with _____

A

QT prolonging agents

- antiarrhythmics

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12
Q

what patients should not be prescribed serotonin (5-HT3) receptor antagonists

A

hypokalemic and hypomagnesmic patients

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13
Q

half life of serotonin (5-HT3) receptor antagonists

A

all have short half-lives EXCEPT palonosetron and sustained-release formulation of granisetron

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14
Q

what serotonin (5-HT3) receptor antagonists should be used for delayed chemotherapy induced N/V as a single dose

A
  • palonosetron (long half life)
  • 2 branded-granisetron agents (long half life)
  • sustol
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15
Q

therapeutic uses of neurokinin-1 receptor antagonists

A
  • chemotherapy induced N/V

- prophylaxis of post-operative N/V

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16
Q

what is the only NK1 antagonist that should be used prophylactically for post-operative N/V

A

aprepitant

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17
Q

to treat chemotherapy induced N/V, NK1 antagonists should be used in combination with ____

A

a glucocorticosteroid and 5-HT3 antagonist

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18
Q

adverse effects of NK1 antagonists

A
  • dyspepsia/constipation/diarrhea

- dizziness/fatigue/somnolence

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19
Q

what NK1 antagonists have longer half lives

A
  • netupitant

- rolapitatant

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20
Q

what drug interactions can occur with NK1 antagonists

A

many - it’s a cyp450 inhibitor

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21
Q

MOA of H1 receptor antagonists

A

block histamine type 1 receptors in the vomiting center and vestibular system
- varying levels of anticholinergic properties at the level of chemoreceptor trigger zones

22
Q

therapeutic uses of H1 receptor antagonists

A
  • idiopathic, mild N/V
  • post-operative N/V
  • N/V of pregnancy
  • motion sickness/vertigo
  • chemotherapy induced N/V
  • radiation induced n/V
23
Q

what is the only indication for meclizine and cyclizine (H1 receptor antagonists)

A

motion sickness/vertigo

24
Q

therapeutic use of doxylamine (H1 receptor antagonist) with pyridoxine (B6)

A

N/V of pregnancy

25
Q

adverse effects H1 receptor antagonists

A
  • drowsiness
  • dry mouth
  • constipation
  • urinary retention
  • blurred vision
  • decreased BP

(classic anticholinergic effects)

26
Q

drug interactions with H1 receptor antagonists

A

interactions with other agents that also induce anticholinergic related side effects

27
Q

MOA of dopamine (D2) receptor antagonists

A

block dopamine type 2 receptors in the chemoreceptor trigger zone
- agents exhibit varying levels of anticholinergic properties

28
Q

MOA of metoclopramide, other than the normal MOA of other dopamine (D2) receptor antagonists

A

it also stimulates acetycholine actions in the GI tract –> enhances GI motility and increases lower esophageal sphincter tone
- no impact on GI secretions

29
Q

which dopamine (D2) receptor antagonist can be used to treat diabetic gastroparesis/dysmotility

A

metoclopramide

30
Q

therapeutic uses of dopamine (D2) receptor antagonists

A
  • idiopathic, mild N/V
  • gastroparesis/dysmotility (metoclopramide)
  • post operative N/V
  • N/V of pregnancy
  • chemotherapy induced N/V
  • radiation induced N/V
31
Q

adverse effects of dopamine (D2) receptor antagonists

A
  • drowsiness
  • dry mouth
  • constipation
  • urinary retention
  • blurred vision
  • decreased BP (sometimes arrhythmias)

(classic anticholinergic effects)

32
Q

drug interactions with dopamine (D2) receptor antagonists

A
  • other agents w/ anticholinergic effects
  • antiarrhythmics
  • antihypertensives
33
Q

how is scopolamine administered

A

transderm scop (a patch worn for 72 hours, normally placed behind ear)

34
Q

therapeutic uses for scopolamine

A

motion sickness

- also end of life care for excessive secretions

35
Q

MOA scopolamine

A

block acetycholine-stimulated muscarinic receptors in neural pathways from the vestibular nuclei in the inner ear –> brain stem and from the reticular formation –> vomiting center
- significant anticholinergic properties

36
Q

adverse effects scopolamine

A
  • drowsiness
  • dry mouth
  • constipation
  • urinary retention
  • blurred vision

(classic anticholinergic effects, but does not drop BP)

37
Q

drug interactions scopolamine

A

other agents that induce anticholinergic effects

38
Q

therapeutic uses cannabinoids

A
  • treatment-resistance chemotherapy-induced N/V

- appetite stimulation in anorexic patients due to severe disease (cancer, AIDS)

39
Q

MOA cannabinoids

A

stimulate CB1 and CB2 receptors in the vomiting center/chemoreceptor trigger zone

  • exert signal transduction effects through GPCR –> decreased excitability of neurons
  • minimized serotonin release from vagal afferent terminals
40
Q

adverse effects cannabinoids

A
  • euphoria/irritability
  • vertigo
  • sedation/drowsiness
  • impaired cognition/memory
  • hallucinations
  • xerostomia
  • sympathomimetic (increased HR/BP)
  • appetite sitmulation
41
Q

compare pharmacokinetics of dronabinol and nabilone

A

dronabinol: large first pass effect and metabolized to one active metabolite
nabilone: metabolized to several active metabolites

42
Q

drug interactions with cannabinoids

A

use caution when prescribing with other CNS depressants, cardiovascular agents, and sympathomimetics

43
Q

compare acute, chronic, and anticipatory chemotherapy induced N/V

A

acute: occurs less than 24 hrs after chemo
chronic: occurs more than 24 hrs after chemo
anticipatory: occurs before chemo

44
Q

describe the high-emetogenic regiment (3-drug regimen) for chemotherapy induced N/V

A
  1. NK1 receptor antagonist
  2. 5-HT3 receptor antagonist
  3. Corticosteroid (dexamethasone)

give regimen the day of the chemo (for acute N/V) and for 3 days after chemo (for chronic)

45
Q

what can you add to the high-emetogenic (3 drug regimen) to form the 4 drug regimen

A
  • may add olanzapine (D2 antagonist)

- may add cannabinoid in treatment-resistance

46
Q

describe the moderate-emetogenic regiment (2 drug regimen)

A
  1. 5-HT3 receptor antagonist
  2. Corticosteroid (dexamethasone)

give regimen the day of the chemo (for acute N/V) and for 2 days after chemo (for chronic)

47
Q

what can you add to the moderate-emetogenic (2 drug regimen) to form the 3 drug regimen

A
  • may add NK1 antagonist or olanzapine

- may add cannabinoid in treatment resistance

48
Q

describe the low-emetogenic regiment (1 drug regimen)

A

One of the following:

  1. corticosteroid
  2. 5-HT3 receptor antagonist
  3. metoclopramide
  4. prochlorperazine

give regimen day of (prior to) chemotherapy (for acute N/V)

49
Q

describe the minimal-emetogenic regiment (0 drug regimen)

A
  1. no routine prophylaxis therapy recommended
50
Q

describe the general principle of the breakthrough emesis regiment

A

add one agent from a different drug class to the current regimen

51
Q

describe the stepped-therapy for pregnancy induced N/V

A
  1. vitamin B6 OR histamine antagonist w/ B6 OR 5-HT3
  2. dopamine antagonist
  3. steroid OR different dopamine antagonist

Maddy - GI II Exam I - some pharm (23 decks)

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