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GI II > Anti-Nausa and Anti-Emetic Drugs > Flashcards

Anti-Nausa and Anti-Emetic Drugs Flashcards

1
Q

What are the serotonin receptor antagonists?

A

Dolasetron
Granisetron
Ondansetron
Palonosetron

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2
Q

What is the common suffix for serotonin receptor antagonists?

A

-setron

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3
Q

What specific receptors do serotonin antagonists act on?

A

5-HT3

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4
Q

What is the is the downstream effect of serotonin receptor inhibition?

A

block serotonin type 3 receptors at vagal nerve terminals and block signal transmission to chemoreceptor trigger zone

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5
Q

What is the potential toxic effect of 5HT3 antagonists?

A

dose-dependent QT prolongation

*Dolasetron has highest risk

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6
Q

What 5HT3 antagonists would you use for delayed chemotherapy induced N/V as a single dose?

A

Palonosetron

sustained-release formulation of Granisetron

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7
Q

What are the neurokinin receptor antagonists?

A 
Aprepitant
Fosaprepitant
Netupitant
Fosnetupitant
Rolapitant
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8
Q

What does the prefix “fos” represent?

A

Pro-drug

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9
Q

What is the common suffix of neurokinin receptor antagonists?

A

-pitant

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10
Q

What specific receptors do neurokinin antagonists act on?

A

NK1

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11
Q

What is the anti-emetic classification of 5HT3 antagonists?

A

strong anti-emetics

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12
Q

What is the anti-emetic classification of NK1 antagonists?

A

moderate anti-emetics

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13
Q

What is the downstream effect of NK1 antagonists?

A

blockade of NK1 receptors in the chemoreceptor trigger zone

blockade of NK1 receptors on vagal terminals in gut

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14
Q

Are NK1 antagonists used for chemotherapy induced N/V?

A

Yes but they are most effective in combination with 5HT3 antagonists and glucocorticoid

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15
Q

What is given for prophylaxis post-op N/V?

A

aprepitant

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16
Q

What are the possible adverse effects of NK1 antagonists?

A

GI (dyspepsia/constipation/diarrhea)

CNS (dizziness/fatigue/somnolence)

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17
Q

What do you need to check before giving NK1 antagonists?

A

mild CYP450 inhibition so need to check for drug interactions

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18
Q

What are the histamine receptor antagonists?

A 
Diphenhydramine 
Dimenhydrinate
Hydroxyzine 
Promethazine
Meclizine
Cyclizine
Doxylamine + B6
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19
Q

What is the anti-emetic classification of histamine receptor antagonists?

A

weak anti-emetics

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20
Q

What specific receptors do histamine antagonists act on?

A

H1

21
Q

What is the downstream effects of H1 antagonists?

A

blockade of H1 receptors in vomiting center and vestibular system

anticholinergic properties at the level of the chemoreceptor trigger zone

22
Q

What are the adverse effects of H1 antagonists?

A 
*classic anticholinergic effects*
drowsiness
dry mouth
constipation
urinary retention
blurred vision
23
Q

What is given for N/V of pregnancy?

A

doxylamine + B6

24
Q

What are given for motion sickness/vertigo?

A

meclizine
cyclazine
scopolamine

25
Q

What are the dopamine receptor antagonists?

A

chlorpromazine
perphenazine
prochlorperazine
metoclopramide

26
Q

What is the anti-emetic classification of dopamine antagonists?

A

weak to moderate anti-emetics

27
Q

What specific receptors do dopamine antagonists act on?

A

D2

28
Q

What is the downstream effect of D2 antagonists?

A

blockade of D2 in CTZ

varying levels of anticholinergic properties

29
Q

What is special about the downstream effect of metoclopramide?

A

also stimulates ACh actions in GI

enhances GI motility and increases LES tone

30
Q

What are the adverse effects D2 antagonists?

A 
*classic anticholinergic effects*
drowsiness
dry mouth
constipation
urinary retention
blurred vision

arrythmias and extrapyramidal SE’s are possible with large doses!

31
Q

What is used for gastroparesis/dysmotility?

A

meoclopramide

32
Q

What is the muscarinic receptor antagonist?

A

scopolamine

33
Q

What is the anti-emetic classification of muscarinic receptor antagonists?

A

weak anti-emetic

34
Q

How is scopolamine administered?

A

transdermal via 72 hr patch

35
Q

What specific receptors do muscarinic antagonists act on?

A

M1

36
Q

What is the downstream effect of M1 receptors?

A

block of Ach-stimulated muscarinic receptors in neural pathways from the vestibular nuclei and reticular formation

37
Q

What are the adverse effects M1 antagonists?

A 
*classic anticholinergic effects*
drowsiness
dry mouth
constipation
urinary retention
blurred vision
38
Q

What can be given for end-of-life care for excessive secretions?

A

scopolamine

39
Q

What are the cannabinoid receptor agonists?

A

Dronabinol

Nabilone

40
Q

What is the antiemetic classification of cannabinoid receptor agonists?

A

strong anti-emetic

41
Q

What is the downstream effect of CB agonists?

A

Stimulates CB1 and CB2 receptors in the CTZ

Exert signal transduction effects through GPCRs resulting in decreased excitability of neurons – minimizes 5HT3 release from vagal nerve

42
Q

When would you use CB agonists?

A

Chemo induced N/V for treatment resistant scenarios

43
Q

What is another beneficial effect of CB agonists?

A

appetite stimulation

44
Q

What are some “adverse” effects of CB agonists?

A 
Euphoria ;)
Vertigo
Sedation
Impaired cognition/memory
Altered perception of reality/hallucinations
Xerstomia
Increased HR/BP
45
Q

What is the classic high-emetogenic regimen?

A

NK1 antagonist
5HT3 antagonist
Corticosteroid (dexamethasone)

may increased to 4 drug regimen with D2 antagonist or CB agonist

46
Q

What is the classic moderate-emetogenic regimen?

A

5HT3 antagonist
corticosteroid (dexamethasone)

may increased to 3 drug regiment with NK1 antagonist or CB agonist

47
Q

What is the classic low-emetogenic regimen?

A

corticosteroid OR
5HT3 antagonist OR
metoclopramide OR
prochlorperazine

48
Q

What is the classic minimal-emetogenic regimen?

A

No prophylaxis therapy recommended

49
Q

What is the stepped-therapy for pregnancy N/V?

A
  1. B6 OR H1 antagonist + B6 OR 5HT3 antagonist
  2. D2 antagonist
  3. Steroid or different D2 antagonist

GI II (16 decks)

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