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GI II Final > Pharmacology of Nausea And Vomiting > Flashcards

Pharmacology of Nausea And Vomiting Flashcards

(52 cards)

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1
Q

Families of drugs used to tx nausea/vomiting

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

Glucocorticosteroids (e.g., dexamethasone) and Benzodiazepines (e.g., alprazolam/lorazepam) are also commonly utilized

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2
Q

5-HT3 receptor antagonists

A

Dolasetron
Granisetron
Ondansetron
Palonosetron

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3
Q

5-HT3 receptor antagonist NOT utilized for N/V because it is only indicated for IBS-D

A

Alosetron

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4
Q

Strength and MOA of 5-HT3 receptor antagonists for N/V

A

Strong anti-emetic agents

MOA: blockade of 5-HT3 receptors at vagal nerve terminals; blocks signal transmission to CTZ [blocks receptor activation after serotonin release from intestinal enterochromaffin cells]

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5
Q

Therapeutic uses for 5-HT3 receptor antagonists in terms of N/V

A

CINV
RINV
PONV
NVP

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6
Q

Adverse effects of 5-HT3 receptor antagonists

A

CNS - headache
GI - constipation/diarrhea

MOST WORRISOME = dose-dependent QT prolongation and Torsade’s (extreme caution required when using with other QT-prolonging agents or in patients with electrolyte imbalances

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7
Q

Which 5-HT3 receptor antagonist drug is considered highest risk for the AE of QT prolongation and Torsade’s?

A

Dolasetron — no longer recommended for CINV prophylaxis

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8
Q

All 5-HT3 receptor antagonists have short half-lives, except ________ and sustained release formation of ________

A

Palonosetron

Granisetron

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9
Q

Drug interactions with 5-HT3 receptor antagonists

A

QT-prolonging agents

Antiarrhythmics

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10
Q

Neurokinin (NK1) receptor antagonists

A 
Aprepitant
Fosaprepitant
Netupitant
Fosnetupitant
Rolapitant
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11
Q

_______, and its prodrug _______, are NK1 antagonists that are only used in combination with ________

A

Netupitant; Fosnetupitant; Palonosetron (5HT3 receptor antagonist)

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12
Q

Strength and MOA of NK1 receptor antagonists

A

Moderate antiemetic agents

MOA: blockade of NK1 (substance P) receptors in CTZ/VC

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13
Q

Therapeutic uses of NK1 receptor antagonists

A

CINV - most effective when used in combo with glucocorticosteroid and 5-HT3 antagonist

Prophylaxis of PONV — only aprepitant! - given up to 3 hours prior to anesthesia induction

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14
Q

What is the only NK1 receptor antagonist that is utilized for prophylaxis of PONV?

A

Aprepitant

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15
Q

adverse effects of NK1 receptor antagonists

A

GI - dyspepsia, constipation, diarrhea

CNS - dizziness, fatigue, somnolence

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16
Q

Which NK1 receptor antagonists have longer half-lives?

A

Netupitant

Rolapitant

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17
Q

What pharmacokinetic property of NK1 receptor antagonists is important to remember regarding drug interactions?

A

NK1 receptor antagonists exhibit mild-moderate inhibition of a few key CYP450 enzymes

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18
Q

Histamine (H1) receptor antagonists

A 
Diphenhydramine
Dimenhydrinate
Hydroxyzine
Promethazine
Meclizine
Cyclizine
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19
Q

______ is an H1 receptor antagonist administered with _______ as initial therapy for NVP

A

Doxylamine; pyridoxine (B6)

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20
Q

Strength and MOA of histamine receptor antagonists

A

Weak antiemetic agents

MOA: blockade of histamine-1 receptors in VC and vestibular system; agents exhibit varying levels of central anticholinergic properties at level of CTZ

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21
Q

Therapeutic uses of histamine receptor antagonists

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A

Idiopathic, mild N/V

PONV

NVP (doxylamine+B6)

Motion sickness/vertigo (meclizine, cyclizine)

CINV - as add-on therapy only

RINV - as add-on therapy only

22
Q

Adverse effects of histamine receptor antagonists

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A 
Drowsiness (CNS depression)
Dry mouth
Constipation
Urinary retention
Blurred vision
Decreased BP

[note classic anticholinergic effects]

23
Q

IV administration of which histaminen receptor antagonist requires dilution and lower dose than the oral form?

24
Q

What drug interactions should be considered when giving histamine receptor antagonists?

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A

Other agents that induce anti-cholinergic related side effects, as these will become cumulative

25
D2 receptor antagonists
Phenothiazines: chlorpromazine, perphenazine, prochlorperazine Other: metoclopramide
26
Strength and MOA of dopamine receptor antagonists
Weak-to-moderate antiemetic agents [originally developed as anti-psychotics] MOA: block D2 receptors in CTZ, exhibiting varying levels of anticholinergic properties
27
______ is a D2 receptor antagonist with the additional MOA of stimulating ACh actions in GI tract, enhancing motility and increasing lower esophageal sphincter tone
Metoclopramide
28
Therapeutic uses of D2 receptor angatonists
Idiopathic, mild N/V Gastroparesis/dysmotility (metoclopramide) PONV NVP CINV and RINV - often as part of combination therapy
29
Adverse effects of dopamine receptor antagonists
``` Drowsiness (CNS depression) Dry mouth Constipation Urinary retention Blurred vision Hypotension (arrhythmias and extrapyramidal SE’s (EPS) are possible - usually seen with larger (psychiatric) doses) ``` [note classic anticholinergic effects]
30
Potential drug interactions with dopamine receptor antagonists
Other agents that also induce anticholinergic-related side effects (cumulative) Antiarrhythmics (esp. QT-prolonging agents) Anti-hypertensives
31
Muscarinic (M1) receptor antagonist used for N/V
Scopolamine
32
Strength and MOA of M1 receptor blocker Scopolamine
Weak antiemetic agent - most commonly utilized for motion sickness MOA: Blockade of muscarinic receptors in neural pathways from the vestibular nuclei in inner ear to brainstem and from reticular formation to VC — significant anticholinergic properties!
33
Adverse effects of muscarinic receptor blockers
``` Drowsiness (CNS depression) Dry mouth Constipation Urinary retention Blurred vision ``` [note classic anticholinergic effects]
34
Interactions with M1 receptor blockers
Other agents that also induce anticholinergic related side effects
35
Cannabinoid receptor agonists utilized for N/V and their controlled status
Dronabinol (C-III) | Nabilone (C-II)
36
Strength and MOA of cannabinoid receptor agonists
Strong antiemetic agents - reserved for treatment-resistant CINV MOA: stimulation of cannabinoid receptors - stimulates predominantly-central (CB1) and predominantly-peripheral (CB2) cannabinoid receptors in VC/CTZ - exert transduction effects through GPCRs —> decreased excitability of neurons
37
Therapeutic uses of cannabinoid receptor agonists
CINV — d/t FDA scheduling, commonly reserved for treatment-resistant clinical scenarios; can be given in combo with other agents Appetite stimulation in select (anorexic/cachectic) pts due to severe disease (e.g., cancer or AIDS)
38
Adverse effects of cannabinoid receptor agonists
``` Euphoria/irritability (emotional lability) Vertigo Sedation Impaired cognition/memory Alterations in perception of reality Xerostomia Sympathomimetic (increased HR/BP) Appetite stimulation ```
39
Pharmacokinetics of cannabinoids
Dronabinol —a large first-pass effect and metabolized to ONE active metabolite Nabilon — metabolized to SEVERAL active metabolites - so it has longer MOA than Dronabinol Both have short-time to onset of activity and a long duration of action (24-36 hours)
40
Interactions with cannabinoid receptor agonists
Caution in use with other CNS depressants, CV agents, and sympathomimetics
41
What organizations provide guidelines on treatment of CINV?
National Comprehensive Cancer Network (NCCN) American Society of Clinical Oncology (ASCO)
42
Typical high-emetogenic regimen for CINV
3-drug regimen including: 1. NK1 receptor antagonist 2. 5-HT3 receptor antagonist 3. Corticosteroid (dexamethasone) Give regimen on the day of, and prior to, chemotherapy AND for 3 days after chemotherapy
43
Options for supplementing the typical high-emetogenic regimen for CINV
May add olanzapine (D2 receptor antagonist) May add cannabinoid in treatment resistance
44
Typical moderately-emetogenic regimen for CINV
2-drug regimen including: 1. 5-HT3 receptor antagonist 2. Corticosteroid (dexamethasone) Give regimen on the day of, and prior to, chemotherapy AND for 2 days after chemotherapy
45
Options for supplementing typical moderately-emetogenic regimen for CINV
May add NK1 antagonist or olanzapine, if necessary May add cannabinoid in treatment resistance (after going up to 3-drug regimen)
46
Typical low-emetogenic regimen for CINV
1-drug regimen including one of the following: Corticosteroid (dexamethasone) 5-HT3 receptor antagonist Metoclopramide Prochlorperazine Give regimen day of, and prior to, chemotherapy for acute N/V
47
Typical minimal-emetogenic regimen for CINV
0-drug regimen! No routine prophylaxis therapy recommended However, like all CINV drug regimens, therapy must be provided for breakthrough N/V for all patients, and for anticipatory N/V as needed
48
Breakthrough emesis regimen
The general principle of breakthrough treatment is to add one agent from a different class to current regimen
49
N/V drugs used for motion sickness
Scopolamine Dimenhydrinate Meclizine
50
N/V drugs used for vertigo
Meclizine | Cyclizine
51
N/V drugs used for diabetic gastroparesis
Metoclopramide
52
Drugs used for pregnancy-induced N/V
1. Vitamin B6, histamine antagonist+B6, or 5-HT3 antagonist 2. Dopamine antagonist 3. Steroid or different dopamine antagonist

GI II Final (8 decks)

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