Anti-Nausea & Anti-Emetics Flashcards by Priyanka Barad

what are the adverse effects of CB

euphoria/irritable

vertigo

sedation/drowsy

impaired cognition/memory

alteration of perception of reality

xerostomia

sympathomimetic (increase HR/BP)

appetite stimulation

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what are the pharmakokinetics for serotonin receptor inhibitors

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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what NV medication is used for diabetic gastroparesis

metoclopramide

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what drugs are used for CINV high-emetogenic regimen

3-drug regimen

NK₁ antagonist
5-HT₃ antagonist
corticosteroid (dexamethosome)

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

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what are the adverse effects and pharmakokinetics of substance P antagonists

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

0 drug regimen!

no routine prophylaxis therapy recommended!

provide therapy for breakthrough NV or for anticipatory NV

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what is the therapeutic use of H₁ antagonists

idopathic, mild NV

PONV

NVP (dozylamine/b6)

motion sickness/vertigo (meclizine & cyclizine)

CINV (add-on)

RINV (add-on)

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what is the suffix for 5-HT₃ receptor antagonists?

list the drugs & mode of deliver

“-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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what are the drug recommendations for low-emetogenic regimen CINV

1-drug regimen (first 2 listed = MC)

Corticosteroid (Dezamethasone) or
5-HT₃ antagonist or
Metoclopramide or
Prochlorperazine

prior to chemo (for acute NV)

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what are the therapeutic uses of CB

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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which N/V drugs have classic anticholinergic effects

H₁ antagonists

D₂ antagonists

muscarinic receptor blocker (obviously)

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

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

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

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

acute - <24 hr after chemo

chronic- >24 hr after chemo

anticipatory- occurs BEFORE chemo

*rmr proper therapy focus on prevention*

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

PREVENTION!

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what are the therapeutic uses of D₂ antagonists

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

mechanoreceptors

chemoreceptors

5-HT₃ receptors

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what is Scopolamine used for

motion sickness

end-of-life care for excessive secretions

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

list the drugs and mode of delivery

“pitant”

APREpitant - po (prodrug = FOSaprepitant - iv)

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

ROLApitant (po/iv)

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

(po/iv/im)

Diphenhydramine = nonspecific
Dimenhydrinate = metabolized to diphenhydramine
Promethazine

Hydroxyzine (HCL salt = po/im & pamoate salts= po)
(po)

Meclizine
Cyclizine
Doxylamine - initial therapy for NVP (w/ B6)__

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

increase to 4-drugs –> add olanzapine (D₂ antagonist) or CB for treatment-resistant NV
for breakthrough NV for all pts
for anticipatory NV as needed

what is the MOA of NK₁ receptor antagnoists

block neurokinin₁ (substance P) receptor in CTZ/VC

peripheral block located on vagal terminals in gut

=moderate antiemetics

what is the MOA for 5-HT₃ receptor antagonists

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

What are cannabinoid receptor AGONISTS (CB)

list the drugs and modes of deliver

=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)

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

other agents that case anticholinergic related side effects

anti-arrhythmics

anti-HTN

what is the MOA of CB

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_**

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

antiarrhythmics QT-prolonging agents

what are the pharmacokinetics and drug interactions for CB

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

what is the therapeutic use of NK1 receptor antagnoists

_CINV_ - most effect in combo w/ glucocorticosteroid & 5-HT₃ antagonist _Prophylaxis_ - _PONV_ \*ONLY APREpitant\* = 3 hrs before anethesia

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

provide therapy for breakthough NV anticipatory NV

what N/V medication is used for vertigo

meclizine cyclizine

which receptors of the vestibular system contribute to N/V

H₁ & M₁ receptors

What is the recommended **_moderate-emetogenic regimen_** for CINV

**_2-drug regimen_** * 5-HT₃ antagonist (palonos- /granis- subQ) * corticosteroids (dexamethasone _prior_ to chemo (for acute NV) & _2 day after_ (for delayed NV)

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

chemoreceptors D₂, NK₁, 5-HT₃ receptors

what is the MOA of H₁ antagonists

block histamine-1 receptros in VC and vestibular system --\> **exhibit varying levels of central _anticholinergic_ properties at level of CTZ** =weak antiemetics

What are the uses for drugs ending in "-setron"

CINV - chemo RINV- radiation PONV - post-op NVP - pregnant

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

Alosetron (po) indicated for IBS-D ONLY

what NV medication is used for NVP (stepped therapy)

1. B6 _or_ H₁ antagonist w/ B6 _or_ 5HT₃ antagonist 2. D₂ antagonist 3. steroid _or_ different dopamine antagonist

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

H_1,M_1,NK₁, & 5-HT₃ receptors

what is the classification and MOA of Scopolamine

= 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

what N/V medication is used for motion sickness

scopolamine (patch) dimenhydrinate meclizine

What is the MOA for D₂ antagonists

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

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

**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

what are the adverse effects of 5-HT₃ receptor antagonists? which one is most worrisome?

few CNS & GI ; _serotonin syndrome_- thermoregulation issues, neurologic seizures, CV issues/arrhythmia **Most worrisome: _dose-dep QT prolongation (Torsade's)_** - high risk w/ **_DOLA_**setron --\> no longer recommended for CINV prophylaxis -caution when giving to pts taking antiarrhythmics or pts w/ electrolyte imbalance