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GI II - Week 1 > Anti-Nausea & Anti-Emetic Drugs (Segars) > Flashcards

Anti-Nausea & Anti-Emetic Drugs (Segars) Flashcards

1
Q

What are the receptor categories of NV drugs?

A
    • Serotonin (5-HT3) receptor antagonists
    • Neurokinin (NK1) receptor antagonists
    • Histamine (H1) receptor antagonists
    • Dopamine (D2) receptor antagonists
    • Muscarinic (M1) receptor antagonists
    • Cannabinoid receptor agonists
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2
Q

What is the common ending for all Serotonin (5-HT3) receptor antagonists?

A

-setron

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3
Q

What are the drugs in the category for Serotonin (5-HT3) receptor antagonists?

A
    • Dolasetron
    • Granisetron
    • Ondansetron
    • Palonosetron
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4
Q

Serotonin (5-HT3) receptor antagonists are used for almost ANY etiology of N/V. How are they taken?

A

Orally or IV

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5
Q

This type of Serotonin receptor antagonist drug is ONLY indicated for IBS-D (irritable bowel syndrome - diarrhea).

A

Alosetron

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6
Q

Serotonin receptor antagonists are (WEAK/STRONG) antiemetic agents that were originally developed for CINV.

A

Strong

***However, still don’t use by themselves!

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7
Q

In Serotonin receptor antagonists, they block Serotonin type-3 receptors at the ______ ______ terminals and blocks signal transmission to the CTZ.

A

Vagal Nerve

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8
Q

Serotonin-receptor activation is blocked after Serotonin release from the…

A

Intestinal enterochromaffin cells

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9
Q

What are the main therapeutic uses of Serotonin (5-HT3) receptor antagonists?

A

CINV
RINV
PONV
NVP

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10
Q

What adverse effect can occur if a patient takes a Serotonin (5-HT3) receptor antagonist along with other 5-HT affecting drugs?

A

Serotonin Syndrome

***Too much Serotonin accumulates in body because receptors are blocked!

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11
Q

What is the most worrisome adverse effect of Serotonin (5-HT3) receptor antagonists?

A

Dose-dependent QT prolongation (Torsade’s)

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12
Q

Extreme caution must be taken when a patient is using Serotonin receptor antagonists along with other QT-prolonging agents like ________, or in patients with _______ _______.

A

Antiarrhythmics

Electrolyte imbalances

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13
Q

This type of Serotonin receptor antagonist drug is at very high risk for dose-dependent QT prolongation, and is no longer recommended for CINV prophylaxis.

A

Dolasetron

***Think Dose-Dependent –> Dolasetron (D with D)!

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14
Q

All Serotonin receptor antagonists have short half-lives, except for ________ and sustained-release formulation of ________ (much longer; 24+ hours).

A

Palonosetron

Granisetron

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15
Q

The long half-life of Palonosetron and Granisetron agents make them effective for delayed-CINV as a _______ dose.

A

Single

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16
Q

What is the common ending for all Neurokinin (NK1) receptor antagonists?

A

-pitant

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17
Q

What drugs are considered Neurokinin (NK1) receptor antagonists?

A 
Aprepitant 
Fosaprepitant 
Netupitant
Fosnetupitant
Rolapitant
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18
Q

Which Neurokinin (NK1) receptor antagonists are considered pro-drugs?

A 
Fosaprepitant = pro-drug of Aprepitant
Fosnetupitant = pro-drug of Netupitant
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19
Q

Netupitant can only be used in combination with what other drug?

A

Palonosetron

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20
Q

Neurokinin (NK1) receptor antagonists are (STRONG/MODERATE) antiemetic agents. They block receptors in CTZ and VC. Still don’t use these drugs alone, used in combination.

A

Moderate

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21
Q

Neurokinin receptor antagonists are used for CINV and are most effective when used in combination with what?

A

Glucocorticosteroid and 5-HT3 antagonist

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22
Q

This is the only Neurokinin receptor antagonist used for prophylaxis of PONV. It is given up to 3 hours prior to anesthesia induction. It is given to patients with a history of PONV, not just given to everyone!

A

Aprepitant

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23
Q

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

A

Netupitant

Rolapitant

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24
Q

Neurokinin receptor antagonists can have mild-moderate inhibition of a few key ________ enzymes, so it’s important to know the drug interactions!

A

CYP450

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25
Q

What drugs are considered Histamine (H1) receptor antagonists?

A 
Diphenhydramine 
Dimenhydrinate
Hydroxyzine 
Promethazine 
Meclizine
Cyclizine
Doxylamine
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26
Q

What is the brand name for Diphenhydramine?

A

Benadryl

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27
Q

This Histamine receptor antagonist is metabolized to Diphenhydramine (Benadryl).

A

Dimenhydrinate (Dramamine)

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28
Q

This Histamine (H1) receptor antagonist is the initial therapy for NVP (NV associated with pregnancy).

A

Doxylamine

***Used in combo with Pyridoxine (B6)

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29
Q

Doxylamine is used in combination with what for NVP?

A

Pyridoxine (B6)

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30
Q

Histamine receptor antagonists are (WEAK/MODERATE) antiemetic agents that were originally developed for other indications such as antihistamine and motion sickness, but were also found useful for NV.

A

Weak

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31
Q

Histamine (H1) receptors are blocked in the VC and vestibular system. These drugs exhibit varying levels of central _________ properties at the level of the CTZ.

A

Anticholinergic

32
Q

What are some classic anticholinergic effects?

A
    • Drowsiness (CNS depression)
    • Dry mouth
    • Constipation
    • Urinary retention
    • Blurred vision
33
Q

What are drug interactions you need to watch out for with Histamine receptor antagonists?

A

Other agents that also induce anticholinergic-related side effects –> causes cumulative adverse effects

34
Q

Which Histamine receptor antagonists are used only for motion sickness and vertigo?

A

Meclizine

Cyclizine

35
Q

Dopamine (D2) receptor antagonists contain a subgroup called…

A

Phenothiazines

36
Q

What drugs are considered Phenothiazines (D2 receptor antagonists)?

A

Chlorpromazine
Perphenazine
Prochlorperazine

37
Q

What is the other drug that is a D2 receptor antagonist, but NOT a Phenothiazine?

A

Metoclopramide

38
Q

Dopamine receptor antagonists are weak-to-moderate antiemetic agents, and work by blocking receptors in the CTZ. These agents exhibit varying levels of _________ properties.

A

Anticholinergic

***Remember, Histamine receptor antagonists also have anticholinergic effects!

39
Q

This Dopamine receptor antagonist also stimulates ACh actions in GI, enhancing GI motility and increases lower esophageal sphincter tone.

A

Metoclopramide

***Used for GI dysmotility issues!

40
Q

What are the drug interactions we need to watch out for with Dopamine receptor antagonists?

A

– Other agents that also induce anticholinergic-related side effects (cumulative)

– Antiarrhythmics (QT-prolonging agents)

– Antihypertensives

41
Q

What drug is a Muscarinic (M1) receptor antagonist?

A

Scopolamine

42
Q

How is Scopolamine administered?

A

Patch worn behind the ear for 72 hours

43
Q

Scopolamine is a weak antiemetic agent that is most commonly used for _______ _______.

A

Motion sickness

44
Q

Besides motion sickness, what can Scopolamine also be used for?

A

End-of-life care for excessive secretions

45
Q

The Muscarinic receptor antagonists block ACh-stimulated Muscarinic receptors in neural pathways from the vestibular nuclei in inner ear to brain stem and from reticular formation to VC. This causes significant _________ properties.

A

Anticholinergic

***Important to watch for patient taking other drugs that also induce anticholinergic-related side effects!

46
Q

Which drugs are Cannabinoid receptor agonists?

A

Dronabinol

Nabilone

47
Q

Synthetic Cannabinoids are FDA-scheduled medications for what reason?

A

Due to their abuse potential –> Limits on quantity, refill #, lifespan of Rx, etc.

48
Q

Which of the Cannabinoid receptor agonists has a higher potential for abuse?

A

Nabilone (C-II) has a slightly higher risk than Dronabinol (C-III)

49
Q

Cannabinoids are strong antiemetic agents that can be used as single agents. They are usually reserved for treating what?

A

Treatment-resistant CINV

50
Q

Cannabinoid receptor agonists stimulate predominantly-central (CB1) and predominantly-peripheral (CB2) cannabinoid receptors in VC/CTZ. These exert signal transduction effects through GPCRs, resulting in decreased excitability of neurons. This minimizes ________ release from vagal afferent terminals.

A

Serotonin (5-HT3)

51
Q

Dronabinol has a large first-pass effect and is metabolized to (ONE/MANY) active metabolite(s).

A

One

52
Q

Nabilone is metabolized to (ONE/MANY) active metabolite(s).

A

Many

53
Q

Cannabinoids (Dronabinol and Nabilone) both have a short-time to onset of activity and long duration of action (______ hours). Nabilone requires fewer doses/day.

A

24-36

54
Q

What drug interactions do we need to be careful of with Cannabinoids?

A

Caution in use with other CNS depressants, cardiovascular agents, and sympathomimetics.

55
Q

This type of CINV occurs <24 hours after chemo is given.

A

Acute N/V

56
Q

This type of CINV occurs >24 hours after chemo is given.

A

Chronic N/V

57
Q

This type of CINV occurs before chemo is give, and is customarily in non-treatment-naive patients (have gone through it before).

A

Anticipatory N/V

58
Q

Proper therapy of CINV focuses on the _________ of it!

A

Prevention

59
Q

This organization provides clinical practice guidelines in oncology for antiemesis (CINV).

A

NCCN = National Comprehensive Cancer Network

60
Q

What does the NCCN recommend for a high-emetogenic regimen?

A

3-drug Regimen =

    • NK1 receptor antagonist
    • 5-HT3 receptor antagonist
    • Corticosteroid (Dexamethasone)
61
Q

According to the NCCN, when is the treatment regimen to be given for high-emetogenic chemo?

A
    • Give day of (prior to) chemo for acute N/V

- - Give for 3 days after chemo for delayed N/V

62
Q

According to the NCCN, what other drugs can be added to a high-emetogenic treatment regimen (making it a 4-drug regimen)?

A
    • Olanzapine (D2 antagonist)

- - Cannabinoid in case of treatment-resistance

63
Q

What does the NCCN recommend for a moderate-emetogenic regimen?

A

2-drug Regimen =

    • 5-HT3 receptor antagonist (palonos/granis SQ)
    • Corticosteroid (Dexamethasone)
64
Q

According to the NCCN, when is the treatment regimen to be given for moderate-emetogenic chemo?

A
    • Give day of (prior to) chemo for acute N/V

- - Give for 2 days after chemo for delayed N/V

65
Q

According to the NCCN, what other drugs can be added to a moderate-emetogenic treatment regimen?

A

– NK1 antagonist or Olanzapine (if necessary, makes it 3-drug regimen)

– Cannabinoid in case of treatment-resistance (increase to 4-drug regimen after going up to 3-drug regimen)

66
Q

What does the NCCN recommend for a low-emetogenic regimen?

A

1-drug Regimen =

    • Corticosteroid (Dexamethasone) OR
    • 5-HT receptor antagonist OR
    • Metoclopramide OR
    • Prochlorperazine

***Most likely to see corticosteroid or 5-HT antagonist because they are most widely used!

67
Q

According to the NCCN, when is the treatment regimen to be given for low-emetogenic chemo?

A

– Give day of (prior to) chem for acute N/V

68
Q

What does the NCCN recommend for a minimal-emetogenic regimen?

A

No routine prophylaxis therapy recommended

69
Q

According to the NCCN, what are two therapy requirements for ALL levels of emetogenic regimens (high, moderate, low, and minimal)?

A
    • Provide therapy for breakthrough N/V for all patients.

- - Provide therapy for anticipatory N/V, as needed.

70
Q

What are the drugs mainly used for motion sickness?

A
    • Scopolamine (patch) OR
    • Dimenhydrinate OR
    • Meclizine
71
Q

What are the drugs mainly used for vertigo?

A
    • Meclizine OR

- - Cyclizine

72
Q

What are the drugs mainly used for diabetic gastroparesis?

A

Metoclopramide

73
Q

What drugs are mainly used for pregnancy-induced N/V (stepped therapy)?

A

1) Vitamin B6 OR Histamine Antagonist (w/ Vit. B6) OR 5-HT3 Antagonist
2) Dopamine Antagonist
3) Steroid OR different Dopamine Antagonist

***Stepped therapy = Option #1 is tried first, then if it fails continue on to other options (more cost-effective for patient)!

74
Q

This major take-home point is that targeted therapy of N/V should be utilized by first determining the…

A

Cause!

75
Q

This major take-home point is that multi-class, ________ therapy is most appropriate for moderate to high emetogenic chemo regimens.

A

Combination

76
Q

_________ is more cost-effective and clinically accepted (especially by your patients) then attempting to treat after it develops!

A

Prevention

GI II - Week 1 (4 decks)

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