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GI/GU II Exam 1 > Anti-Nausea & Anti-Emetics > Flashcards

Anti-Nausea & Anti-Emetics Flashcards

1
Q

what are the adverse effects of CB

A

euphoria/irritable

vertigo

sedation/drowsy

impaired cognition/memory

alteration of perception of reality

xerostomia

sympathomimetic (increase HR/BP)

appetite stimulation

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2
Q

what are the pharmakokinetics for serotonin receptor inhibitors

A

short 1/2-life

except PALONOsetron & sustained release form of GRANIsetron (SubQ)

==> long 1/2-life = effective for delayed CINV as single dose!

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3
Q

what NV medication is used for diabetic gastroparesis

A

metoclopramide

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4
Q

what drugs are used for CINV high-emetogenic regimen

A

3-drug regimen

  1. NK1 antagonist
  2. 5-HT3 antagonist
  3. corticosteroid (dexamethosome)

give prior to chemo (for acute NV) & 3 days after (for delayed NV)

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5
Q

what are the adverse effects and pharmakokinetics of substance P antagonists

A

Adverse effect: GI/CNS

Pharmacokinetics: NETUpitant/POLApitant have mod-major active metabolites - longer 1/2-life

mild to mod inhibition of few CYP450 enzymes *ALWAYS CHECK FOR DRUG INTERACTIONS*

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6
Q

what is the medication recommendation for CINV- minimal-emetogenic regimen

A

0 drug regimen!

no routine prophylaxis therapy recommended!

provide therapy for breakthrough NV or for anticipatory NV

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7
Q

what is the therapeutic use of H1 antagonists

A

idopathic, mild NV

PONV

NVP (dozylamine/b6)

motion sickness/vertigo (meclizine & cyclizine)

CINV (add-on)

RINV (add-on)

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8
Q

what is the suffix for 5-HT3 receptor antagonists?

list the drugs & mode of deliver

A

“-setron”

dolasetron (po/iv)

granisetron (1. cutaneous-24hr patch, 2. SubQ injection)

ondansetron (1. po/iv, 2. oral film)

palonosetron (1. iv, 2. po & iv combo w/ netupitant (po) & fosnetupitant (iv))

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9
Q

what are the drug recommendations for low-emetogenic regimen CINV

A

1-drug regimen (first 2 listed = MC)

  1. Corticosteroid (Dezamethasone) or
  2. 5-HT3 antagonist or
  3. Metoclopramide or
  4. Prochlorperazine

prior to chemo (for acute NV)

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10
Q

what are the therapeutic uses of CB

A

treatment resistant CINV (bc FDA scheduling)

could be add-on for CINV

appetite stimulation in anorexic pt due to severe dz

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11
Q

which N/V drugs have classic anticholinergic effects

A

H1 antagonists

D2 antagonists

muscarinic receptor blocker (obviously)

=drowsy, dry mouth, constipation, urinary retention, blurred vision

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12
Q

What are the medications changes made for CINV moderate-emetogenic regmin doesnt work

A
  1. increase to 3-drug regimen - add NK1 antagonist or. olanzapine
  2. CB in treatment resistant (after trying 3-drug regimen)
  3. therapy of breakthrough NV for all pts
  4. therapy for anticipatory NV
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13
Q

what is the difference btn acute, chronic and anticipatory NV for CINV

A

acute - <24 hr after chemo

chronic- >24 hr after chemo

anticipatory- occurs BEFORE chemo

*rmr proper therapy focus on prevention*

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14
Q

what is the most cost effective and clinically accepted treatment for NV

A

PREVENTION!

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15
Q

what are the therapeutic uses of D2 antagonists

A

idiopathic, mild NV

PONV (but 5-HT3 is 1st line)

NVP

gastroparesis/dysmotility (metoclopramide)

CINV & RINV (olanzapine used in combo w/ other CINV/RINV agents)

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16
Q

What receptors of the GI tract & heart contribute to the cause of N/V

A

mechanoreceptors

chemoreceptors

5-HT3 receptors

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17
Q

what is Scopolamine used for

A

motion sickness

end-of-life care for excessive secretions

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18
Q

What is the suffix for Neurokinin (NK1) receptor antagonists?

list the drugs and mode of delivery

A

“pitant”

APREpitant - po (prodrug = FOSaprepitant - iv)

NETUpitant- po (produg = FOSnetupitant- iv) –> both combo only w/ palonosteron

ROLApitant (po/iv)

19
Q

list the Histamine (H1) receptor antagonists & their mode of delivery

A
  1. (po/iv/im)
  • Diphenhydramine = nonspecific
  • Dimenhydrinate = metabolized to diphenhydramine
  • Promethazine
  1. Hydroxyzine (HCL salt = po/im & pamoate salts= po)
  2. (po)
  • Meclizine
  • Cyclizine
  • Doxylamine - initial therapy for NVP (w/ B6)__​
20
Q

what are the adjustments in regimen for CINV is the high-emetogenic regimen (3-drug regimen) doesnt work

A
  1. increase to 4-drugs –> add olanzapine (D2 antagonist) or CB for treatment-resistant NV
  2. for breakthrough NV for all pts
  3. for anticipatory NV as needed
21
Q

what is the MOA of NK1 receptor antagnoists

A

block neurokinin1 (substance P) receptor in CTZ/VC

peripheral block located on vagal terminals in gut

=moderate antiemetics

22
Q

what is the MOA for 5-HT3 receptor antagonists

A

block serotonin type-3 receptors @ vagal N terminal –> block signal transduction to CTZ

-block receptor activation after serotonin release from intestinal enterochromaffin cells

=strong anti-emetic agents

23
Q

What are cannabinoid receptor AGONISTS (CB)

list the drugs and modes of deliver

A

=synthetic prep of cannabinol (constituent of cannibis stavia; delta-9THC in marijuana)

FDA scheduled - limits quantity, refill #, lifespan of Rx, etc

Dronabinol (po liquid filled capsule or solution)

Nabilone (po)

24
Q

what are drugs interactions to be aware of when prescribing D2 antagonists

A

other agents that case anticholinergic related side effects

anti-arrhythmics

anti-HTN

25
Q

what is the MOA of CB

A

stimulate CB1 and CB2 receptors in VC/CTZ

–> exert signal transduction via GPCR –> decrease excitability of neurons - minimize 5-HT3 release from vagal afferent terminals

=strome antiemetics –> use for treatment resistant CINV

26
Q

what drug interactions should you look out for when prescribing 5-HT3 receptor antagonists

A

antiarrhythmics

QT-prolonging agents

27
Q

what are the pharmacokinetics and drug interactions for CB

A

pharmacokinetics:

  • Dronabinol - large 1st pass effect & metabolize to ONE active metabolite
  • Nabilone- metabolized to SEVERAL active metabolites (fewer doses needed)

both = short time to onset & long duration (24-36 hrs)

interactions: other CNS depressants, CV agents & sympathomimetics

28
Q

what is the therapeutic use of NK1 receptor antagnoists

A

CINV - most effect in combo w/ glucocorticosteroid & 5-HT3 antagonist

Prophylaxis - PONV *ONLY APREpitant* = 3 hrs before anethesia

29
Q

what are changes/addition in medication for low-emetogenic regimen CINV

A

provide therapy for breakthough NV

anticipatory NV

30
Q

what N/V medication is used for vertigo

A

meclizine

cyclizine

31
Q

which receptors of the vestibular system contribute to N/V

A

H1 & M1 receptors

32
Q

What is the recommended moderate-emetogenic regimen for CINV

A

2-drug regimen

  • 5-HT3 antagonist (palonos- /granis- subQ)
  • corticosteroids (dexamethasone

prior to chemo (for acute NV) & 2 day after (for delayed NV)

33
Q

which receptors make up the chemoreceptor trigger zone (area postrema)

A

chemoreceptors

D2, NK1, 5-HT3 receptors

34
Q

what is the MOA of H1 antagonists

A

block histamine-1 receptros in VC and vestibular system

–> exhibit varying levels of central anticholinergic properties at level of CTZ

=weak antiemetics

35
Q

What are the uses for drugs ending in “-setron”

A

CINV - chemo

RINV- radiation

PONV - post-op

NVP - pregnant

36
Q

which 5-HT3 receptor antagonist is NOT used for N/V

A

Alosetron (po)

indicated for IBS-D ONLY

37
Q

what NV medication is used for NVP (stepped therapy)

A
  1. B6 or H1 antagonist w/ B6 or 5HT3 antagonist
  2. D2 antagonist
  3. steroid or different dopamine antagonist
38
Q

which receptors make up the “vomitting center” of the CNS (nucleus of tractus solitarius)

A

H1, M1, NK1, & 5-HT3 receptors

39
Q

what is the classification and MOA of Scopolamine

A

= muscarinic receptor blocker

=block mAch receptors in neural path from vestibular nuclei in inner ear to brainstem & from reticular formation to VC *significant anticholinergic properties*

=weak antiemetics

40
Q

what N/V medication is used for motion sickness

A

scopolamine (patch)

dimenhydrinate

meclizine

41
Q

What is the MOA for D2 antagonists

A

block dopamine type-2 receptor in CTZ ==> exhibit varying levels of anticholinergic properties

metoclopramide - stimulate Ach actions in GI, enhance GI motility & increase LES tone (used in diabetic gasteroparesis)

=weak-mod antiemetics

42
Q

List the types of Dopamine (D2) receptor antagonists & the mode of delivery for each

A

Phenothiazines

  • Chloropromazine (po/iv/im)
  • Perphenazine (po)
  • Prochlorperazine (1. po/iv/im/pr, 2. pr)

Others:

  • Metoclopramide (1. po, 2. ODT)
  • haloperidol, olanzapine - used for mental health conditions, but could be add-ons
  • trimethobenzamide
43
Q

what are the adverse effects of 5-HT3 receptor antagonists?

which one is most worrisome?

A

few CNS & GI ; serotonin syndrome- thermoregulation issues, neurologic seizures, CV issues/arrhythmia

Most worrisome: dose-dep QT prolongation (Torsade’s) - high risk w/ DOLAsetron –> no longer recommended for CINV prophylaxis

-caution when giving to pts taking antiarrhythmics or pts w/ electrolyte imbalance

GI/GU II Exam 1 (16 decks)

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