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

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

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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
What drugs are considered Histamine (H1) receptor antagonists?
``` Diphenhydramine Dimenhydrinate Hydroxyzine Promethazine Meclizine Cyclizine Doxylamine ```
26
What is the brand name for Diphenhydramine?
Benadryl
27
This Histamine receptor antagonist is metabolized to Diphenhydramine (Benadryl).
Dimenhydrinate (Dramamine)
28
This Histamine (H1) receptor antagonist is the initial therapy for NVP (NV associated with pregnancy).
Doxylamine ***Used in combo with Pyridoxine (B6)
29
Doxylamine is used in combination with what for NVP?
Pyridoxine (B6)
30
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.
Weak
31
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.
Anticholinergic
32
What are some classic anticholinergic effects?
- - Drowsiness (CNS depression) - - Dry mouth - - Constipation - - Urinary retention - - Blurred vision
33
What are drug interactions you need to watch out for with Histamine receptor antagonists?
Other agents that also induce anticholinergic-related side effects --> causes cumulative adverse effects
34
Which Histamine receptor antagonists are used only for motion sickness and vertigo?
Meclizine | Cyclizine
35
Dopamine (D2) receptor antagonists contain a subgroup called...
Phenothiazines
36
What drugs are considered Phenothiazines (D2 receptor antagonists)?
Chlorpromazine Perphenazine Prochlorperazine
37
What is the other drug that is a D2 receptor antagonist, but NOT a Phenothiazine?
Metoclopramide
38
Dopamine receptor antagonists are weak-to-moderate antiemetic agents, and work by blocking receptors in the CTZ. These agents exhibit varying levels of _________ properties.
Anticholinergic ***Remember, Histamine receptor antagonists also have anticholinergic effects!
39
This Dopamine receptor antagonist also stimulates ACh actions in GI, enhancing GI motility and increases lower esophageal sphincter tone.
Metoclopramide ***Used for GI dysmotility issues!
40
What are the drug interactions we need to watch out for with Dopamine receptor antagonists?
-- Other agents that also induce anticholinergic-related side effects (cumulative) -- Antiarrhythmics (QT-prolonging agents) -- Antihypertensives
41
What drug is a Muscarinic (M1) receptor antagonist?
Scopolamine
42
How is Scopolamine administered?
Patch worn behind the ear for 72 hours
43
Scopolamine is a weak antiemetic agent that is most commonly used for _______ _______.
Motion sickness
44
Besides motion sickness, what can Scopolamine also be used for?
End-of-life care for excessive secretions
45
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.
Anticholinergic ***Important to watch for patient taking other drugs that also induce anticholinergic-related side effects!
46
Which drugs are Cannabinoid receptor agonists?
Dronabinol | Nabilone
47
Synthetic Cannabinoids are FDA-scheduled medications for what reason?
Due to their abuse potential --> Limits on quantity, refill #, lifespan of Rx, etc.
48
Which of the Cannabinoid receptor agonists has a higher potential for abuse?
Nabilone (C-II) has a slightly higher risk than Dronabinol (C-III)
49
Cannabinoids are strong antiemetic agents that can be used as single agents. They are usually reserved for treating what?
Treatment-resistant CINV
50
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.
Serotonin (5-HT3)
51
Dronabinol has a large first-pass effect and is metabolized to (ONE/MANY) active metabolite(s).
One
52
Nabilone is metabolized to (ONE/MANY) active metabolite(s).
Many
53
Cannabinoids (Dronabinol and Nabilone) both have a short-time to onset of activity and long duration of action (______ hours). Nabilone requires fewer doses/day.
24-36
54
What drug interactions do we need to be careful of with Cannabinoids?
Caution in use with other CNS depressants, cardiovascular agents, and sympathomimetics.
55
This type of CINV occurs <24 hours after chemo is given.
Acute N/V
56
This type of CINV occurs >24 hours after chemo is given.
Chronic N/V
57
This type of CINV occurs before chemo is give, and is customarily in non-treatment-naive patients (have gone through it before).
Anticipatory N/V
58
Proper therapy of CINV focuses on the _________ of it!
Prevention
59
This organization provides clinical practice guidelines in oncology for antiemesis (CINV).
NCCN = National Comprehensive Cancer Network
60
What does the NCCN recommend for a high-emetogenic regimen?
3-drug Regimen = - - NK1 receptor antagonist - - 5-HT3 receptor antagonist - - Corticosteroid (Dexamethasone)
61
According to the NCCN, when is the treatment regimen to be given for high-emetogenic chemo?
- - Give day of (prior to) chemo for acute N/V | - - Give for 3 days after chemo for delayed N/V
62
According to the NCCN, what other drugs can be added to a high-emetogenic treatment regimen (making it a 4-drug regimen)?
- - Olanzapine (D2 antagonist) | - - Cannabinoid in case of treatment-resistance
63
What does the NCCN recommend for a moderate-emetogenic regimen?
2-drug Regimen = - - 5-HT3 receptor antagonist (palonos/granis SQ) - - Corticosteroid (Dexamethasone)
64
According to the NCCN, when is the treatment regimen to be given for moderate-emetogenic chemo?
- - Give day of (prior to) chemo for acute N/V | - - Give for 2 days after chemo for delayed N/V
65
According to the NCCN, what other drugs can be added to a moderate-emetogenic treatment regimen?
-- 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
What does the NCCN recommend for a low-emetogenic regimen?
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
According to the NCCN, when is the treatment regimen to be given for low-emetogenic chemo?
-- Give day of (prior to) chem for acute N/V
68
What does the NCCN recommend for a minimal-emetogenic regimen?
No routine prophylaxis therapy recommended
69
According to the NCCN, what are two therapy requirements for ALL levels of emetogenic regimens (high, moderate, low, and minimal)?
- - Provide therapy for breakthrough N/V for all patients. | - - Provide therapy for anticipatory N/V, as needed.
70
What are the drugs mainly used for motion sickness?
- - Scopolamine (patch) OR - - Dimenhydrinate OR - - Meclizine
71
What are the drugs mainly used for vertigo?
- - Meclizine OR | - - Cyclizine
72
What are the drugs mainly used for diabetic gastroparesis?
Metoclopramide
73
What drugs are mainly used for pregnancy-induced N/V (stepped therapy)?
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
This major take-home point is that targeted therapy of N/V should be utilized by first determining the...
Cause!
75
This major take-home point is that multi-class, ________ therapy is most appropriate for moderate to high emetogenic chemo regimens.
Combination
76
_________ is more cost-effective and clinically accepted (especially by your patients) then attempting to treat after it develops!
Prevention

GI II - Week 1 (4 decks)

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