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GI II Final > Pharmacology of Nausea And Vomiting > Flashcards

Pharmacology of Nausea And Vomiting Flashcards

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

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

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?

A

Promethazine

24
Q

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

A

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

25
Q

D2 receptor antagonists

A

Phenothiazines: chlorpromazine, perphenazine, prochlorperazine

Other: metoclopramide

26
Q

Strength and MOA of dopamine receptor antagonists

A

Weak-to-moderate antiemetic agents [originally developed as anti-psychotics]

MOA: block D2 receptors in CTZ, exhibiting varying levels of anticholinergic properties

27
Q

______ is a D2 receptor antagonist with the additional MOA of stimulating ACh actions in GI tract, enhancing motility and increasing lower esophageal sphincter tone

A

Metoclopramide

28
Q

Therapeutic uses of D2 receptor angatonists

A

Idiopathic, mild N/V

Gastroparesis/dysmotility (metoclopramide)

PONV

NVP

CINV and RINV - often as part of combination therapy

29
Q

Adverse effects of dopamine receptor antagonists

A 
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
Q

Potential drug interactions with dopamine receptor antagonists

A

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

Antiarrhythmics (esp. QT-prolonging agents)

Anti-hypertensives

31
Q

Muscarinic (M1) receptor antagonist used for N/V

A

Scopolamine

32
Q

Strength and MOA of M1 receptor blocker Scopolamine

A

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
Q

Adverse effects of muscarinic receptor blockers

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

[note classic anticholinergic effects]

34
Q

Interactions with M1 receptor blockers

A

Other agents that also induce anticholinergic related side effects

35
Q

Cannabinoid receptor agonists utilized for N/V and their controlled status

A

Dronabinol (C-III)

Nabilone (C-II)

36
Q

Strength and MOA of cannabinoid receptor agonists

A

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
Q

Therapeutic uses of cannabinoid receptor agonists

A

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
Q

Adverse effects of cannabinoid receptor agonists

A 
Euphoria/irritability (emotional lability)
Vertigo
Sedation
Impaired cognition/memory
Alterations in perception of reality
Xerostomia
Sympathomimetic (increased HR/BP)
Appetite stimulation
39
Q

Pharmacokinetics of cannabinoids

A

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
Q

Interactions with cannabinoid receptor agonists

A

Caution in use with other CNS depressants, CV agents, and sympathomimetics

41
Q

What organizations provide guidelines on treatment of CINV?

A

National Comprehensive Cancer Network (NCCN)

American Society of Clinical Oncology (ASCO)

42
Q

Typical high-emetogenic regimen for CINV

A

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
Q

Options for supplementing the typical high-emetogenic regimen for CINV

A

May add olanzapine (D2 receptor antagonist)

May add cannabinoid in treatment resistance

44
Q

Typical moderately-emetogenic regimen for CINV

A

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
Q

Options for supplementing typical moderately-emetogenic regimen for CINV

A

May add NK1 antagonist or olanzapine, if necessary

May add cannabinoid in treatment resistance (after going up to 3-drug regimen)

46
Q

Typical low-emetogenic regimen for CINV

A

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
Q

Typical minimal-emetogenic regimen for CINV

A

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
Q

Breakthrough emesis regimen

A

The general principle of breakthrough treatment is to add one agent from a different class to current regimen

49
Q

N/V drugs used for motion sickness

A

Scopolamine
Dimenhydrinate
Meclizine

50
Q

N/V drugs used for vertigo

A

Meclizine

Cyclizine

51
Q

N/V drugs used for diabetic gastroparesis

A

Metoclopramide

52
Q

Drugs used for pregnancy-induced N/V

A
  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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