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Flashcards in Antiemetics Deck (24)
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1

Molecular Targets of the Vomiting Reflex

2

describe the 2 phases of Chemotherapy Induced Nausea and Vomiting (CINV) 

1. Acute phase - universally experienced (within 24 hours)

2. Delayed phase - affects only some patients (days 2-5)

3

Scopolamine is a _____

Scopolamine is a muscarinic antagonist

4

Scopolamine is used for prevention and treatment of _____ 

is it a 1st line agent for CINV?

Scopolamine is used for prevention and treatment of motion sickness 

 NOT a 1st line agent for CINV

5

list H1 antagonists

  • Diphenhydramine
  • Meclizine
  • Cyclizine

6

what do H1 antagonists act on and used for? 

vestibular afferents & brainstem -

motion sickness & postoperative emesis

7

list 5-HTAntagonists

"setron"

Ondan-setron, Grani-setron

8

where are 5-HT3 receptors found? 

Critical sites involved in emesis:

  • Vagal afferents
  • Solitary tract nucleus 
  • CTZ
  • Area Postrema

9

What is the DOC for prophylaxis against immediate CINV?

 

"-setron" (5-HT3 antagonists)

10

5-HTAntagonists are also effective against _____

not effective against ____ and ____

 

5-HTAntagonists are also effective against hyperemesis gravidarum

not effective against delayed CINV and motion sickness

11

Ondansetron AE 

  • Torsades de pointes
  • Headache
  • Constipation
  • Serotonin syndrome 

12

list NK1 antagonists for Substance P 

AprepitantFosaprepitant (parenteral)

13

prophylaxis against delayed CINV 

Aprepitant/Fosaprepitant

14

Aprepitant/Fosaprepitant is given orally in combination with ___ and ___

Aprepitant/Fosaprepitant is given orally in combination with dexamethasone and 5-HT3 antagonist

15

___ undergoes extensive CYP3A4 metabolism

affecting the metabolism of ___ and ___

Aprepitant undergoes extensive CYP3A4 metabolism

affecting the metabolism of warfarin and OCPs

16

list D2 receptor Antagonists at the CTZ

  • Prochlorperazine
  • Promethazine
  • Droperidol

17

D2 receptor antagonists have antihistaminic and anticholinergic properties, effectively treating ____

but not effective in ____ 

D2 receptor antagonists have antihistaminic and anticholinergic properties, effectively treat​ing motion sickness

but not effective in CINV

18

D2 antagonists have a potential for adverse _____

D2 antagonists have a potential for adverse extrapyramidal effects

19

list the benzodiazepines 

-zepam, -zolam

Lorazepam, Alprazolam, Diazepam

20

Lorazepam, Alprazolam, Diazepam MOA

activates GABAA in CNS increasing frequency of Cl- channel opening

no intrinisic antiemetic effects but reduce anticipatory component of nausea and vomiting d/t sedative, amnesic, and anti-anxiety effects

21

Lorazepam, Alprazolam, Diazepam AEs

CNS depression and dependence

22

describe Dronabinol (Δ-9-tetrahydrocannabinol)

  • naturally occurring cannabinoid
  • stimulates CB1 receptors in the brainstem

23

CINV prophylactic agent when other anti-emetic medications are not effective

Dronabinol 

24

Dronabinol AEs

  • Marijuana-like "highs”
  • Prominent central sympathomimetic activity
    • Palpitations, tachycardia, vasodilation, hypotension
    • conjunctival injection (bloodshot eyes)
  • Paranoid reactions/ thinking abnormalities
  • Abrupt withdrawal of dronabinol → an abstinence syndrome (irritability, insomnia, and restlessness)
  • Great caution prescribing to persons with substance abuse Hx