Anti-Nausea & Anti-Emetics Flashcards
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
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!
what NV medication is used for diabetic gastroparesis
metoclopramide
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)
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*
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
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)
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))
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)
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
which N/V drugs have classic anticholinergic effects
H1 antagonists
D2 antagonists
muscarinic receptor blocker (obviously)
=drowsy, dry mouth, constipation, urinary retention, blurred vision
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
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*
what is the most cost effective and clinically accepted treatment for NV
PREVENTION!
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)
What receptors of the GI tract & heart contribute to the cause of N/V
mechanoreceptors
chemoreceptors
5-HT3 receptors
what is Scopolamine used for
motion sickness
end-of-life care for excessive secretions
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)
- B6 or H1 antagonist w/ B6 or 5HT3 antagonist
- D2 antagonist
- steroid or different dopamine antagonist
which receptors make up the “vomitting center” of the CNS (nucleus of tractus solitarius)
H1, M1, 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/ DOLAsetron –> no longer recommended for CINV prophylaxis
-caution when giving to pts taking antiarrhythmics or pts w/ electrolyte imbalance
