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GI II Exam 1 > Lecture 1: Anti-Nausea/Emetic Drugs > Flashcards

Lecture 1: Anti-Nausea/Emetic Drugs Flashcards

1
Q

What are the 6 families of Nausea/Vomiting Drugs? (S/N/H/D/M/C)

A 
Serotonin Receptor Antagonists (5-HT3)
Neurokinin Receptor Antagonists (NK1)
Histamine Receptor Antagonists (H1)
Dopamine Receptor Antagonists (D2)
Muscarinic Receptor Antagonists (M1)
Cannabinoid Receptor AGONISTS
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2
Q

What are the 4 Serotonin Receptor Antagonists used to treat Nausea and Vomiting? (D/G/O/P)

What are they commonly used for?

A

Dolasetron, Granisetron, Ondansetron, Palonosetron (anything ending in “-setron”)

  • can be used for almost ALL nausea/vomiting (oral and IV administration)
  • STRONG antiemetic drugs (used for Chemo, Radiation, Post-Op, and Pregnancy N/V)
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3
Q

What is Alosetron and what is the only thing it is indicated for?

A
  • serotonin receptor antagonist used only for Irritable Bowel Syndrome Disease
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4
Q

What are two adverse effects to be aware of when using Serotonin Receptor Antagonists?

Which family member is no longer recommended for prophylaxis of Chemo?

A
  1. Serotonin Syndrome (with other 5-HT drugs)
  2. Dose-Dependent QT-prolongation (TORSADE’S)
    • caution when using other QT-prolonging drugs
    • DOLASETRON has high risk –> not recommended

otherwise only few CNS/GI effects - well tolerated

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5
Q

Which two Serotonin Receptor Antagonists drugs have long half-lives?

A

Palonosetron and Granisetron

  • effective for delayed-CINV as SINGLE DOSE
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6
Q

What are the 5 Neurokinin Receptor Antagonists used to treat Nausea and Vomiting? (A/F/N/F/R)

Which ones are prodrugs? Which ones are combination only and with which drug?

A

Aprepitant, Fosaprepitant, Netupitant, Fosnetupitant, Rolapitant (anything ending in “-pitant”)

  • Fosaprepitant and Fosnetupitant are PRODRUGS
  • Netupitant and Fosnetupitant given with PALONOSETRON

all are MODERATE antiemetic agents

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7
Q

What are the therapeutic uses of Neurokinin Receptor Antagonists and what is Aprepitant commonly used for?

A

T: Chemo-induced nausea and vomiting (most effective in combo with 5-HT3 antagonist and glucocorticoid)

  • Aprepitant given as prophylaxis for Post-Op N/V (given 3 hrs. prior to anesthesia induction in pts. with HISTORY OF PONV)
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8
Q

Which two Neurokinin Receptor Antagonists have long half lives?

A

Netupitant and Rolapitant

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9
Q

What are the 6 Histamine Receptor Antagonists used to treat Nausea and Vomiting? (D/D/H/P/M/C)

What is a drug that is commonly used as initial therapy for NVP and what is it given with?

A

Diphenhydramine, Dimenhydrinate, Hydroxyzine, Promethazine, Meclizine, Cyclizine

  • WEAK antiemetic agents; all have varying lvls of central ANTICHOLINERGIC properties (don’t give multiple class with anticholinergic properties)

DOXYLAMINE (with B6) given initially to treat NVP

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10
Q

What are common anticholinergic adverse effects?

A

drowsiness (CNS depression), dry mouth, constipation, urinary retention, blurred vision

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11
Q

What are the only two indications for using meclizine and cyclizine?

A

motion sickness and vertigo

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12
Q

What are the 4 Dopamine Receptor Antagonists used to treat Nausea and Vomiting? (C/P/P/M)

A

Chlorpromazine, Perphenazine, Prochlorperazine (Phenothiazine’s) and Metochlopramide

  • WEAK to MODERATE antiemetic agents
  • all exhibit varying levels of ANTICHOLINERGIC properties (usually dose related)
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13
Q

What does Metochlopramide also stimulate?

A

stimulates ACh actions in the GI and can enhance GI motility, as well as increasing lower esophageal sphincter tone

**commonly used for pts. with dysmotility issues or gastroparesis (delayed gastric emptying))

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14
Q

What is the main Muscarinic Receptor Antagonist used to treat Nausea and Vomiting?

What two things is it commonly used for and how is it administered?

A

Scopolamine (transderm patch that can be worn for 72 hours)

  • WEAK antiemetic agent commonly used for MOTION SICKNESS and end-of-life care for excessive secretions (placed behind ear)
  • exhibits ANTICHOLINERGIC properties
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15
Q

What are the two Cannabinoid Receptor Agonists used to treat Nausea and Vomiting? (D/N)

When are they commonly given?

A

Dronabinol (C-III) and Nabilone (C-II)

  • synthetic preparations of THC; FDA-scheduled medications = limits to quantity/refills/prescriptions
  • STRONG antiemetic agents reserved for TREATMENT-RESISTANT CINV (most aggressive)

can also be given to stimulate appetite in anorexic patients due to severe disease (AIDS/Cancer)

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16
Q

How are Dronabinol and Nabilone metabolized and what drugs should their used be cautioned with?

A

D - large first-pass effect; one active metabolite
N - several active metabolites (fewer doses/day)

both have short onset time and long duration

CAUTION: use with other CNS depressants, cardiovascular agents, and sympathomimetics

17
Q

What is the difference between Acute and Chronic N/V, and Anticipatory N/V?

A

A: occurs < 24 hrs AFTER chemo given
C: occurs > 24 hrs AFTER chemo given

Anticipatory: occurs BEFORE chemo given, customarily in non-treatment-naive pts.

18
Q

What drugs are used to treat:

  1. Motion Sickness (3)
  2. Vertigo (2)
  3. Diabetic Gastroparesis
A
  1. Scopolamine (patch), Dimenhydrinate, Meclizine
  2. Meclizine, Cyclizine
  3. Metoclopramide
19
Q

What are the 3 stepped-therapies of Pregnancy-induced N/V?

A
  1. Vitamin B6 or Histamine Antagonist (w/B6) or Serotonin Antagonist
  2. Dopamine Antagonist
  3. Steroid or Different Dopamine Antagonist
20
Q

What drug combos would you give and when for:

  1. High-Emetogenic Regimen
  2. Moderate-Emetogenic Regimen
  3. Low-Emetogenic Regimen
  4. Minimal-Emetogenic Regimen
A
  1. NK receptor antagonist, 5-HT3 receptor antagonist, and Corticosteroid (DEXAMETHASONE)
    • 3 DRUG REGIMEN
    • given day before chemo and for 3 days after chemo
  2. 5-HT3 receptor antagonist and Dexamethasone
    • 2 DRUG REGIMEN
    • given day before chemo and 2 days after chemo
  3. Dexamethazone, 5-HT3 receptor antagonist, metoclopramide, prochlorperazine
    • 1 DRUG REGIMEN (dexamethazone most common)
    • given day before chemo
  4. no routine prophylaxis therapy recommended
    • 0 DRUG REGIMEN

GI II Exam 1 (12 decks)

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