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NURS 572 Ch 79

Pharm Ch 79 antiemetics, motion sickness

Name all receptors involved in emetic response *5HT-3 *DA-2 *NK-1 (binds substance P) *Muscarinic *H-1 Histamine
Name major receptors that are activated by vestibular apparatus in motion sickness *H-1 *Muscarinic *BNZ
8 total classes of antiemetics - name first 4 *5HT-3 blockers *DA-2 blockers *anticholinergics (primarily motion sickness) *antihistamines (primarily motion sickness)
8 total classes of antiemetics - name second 4 *glucocorticoids-corticosteroids *canabinoids *BNZs *SP NK-1 blockers (substance P neurokinin-1)
5HT-3 blockers MOA block serotonin-3 receptors in CTZ --- AND --- blocks them in vagal afferent
5HT-3 blockers most commonly in combo with this class of drug used in combination with corticosteroids for the prevention/tx of chemo n/v
ADRs of 5HT-3 blockers HA/dizz/D
name five 5HT-3 blockers in class *odeansetron *granisetron *dolasetron *palonosetron *granisetron patch (new)
what 5HT-3 blocker is only available IV only palonosetron
odansetron class 5HT-3 blocker - oral/IV
granisetron class 5HT-3 blocker - oral/IV ---now transdermal
dolasetron class 5HT-3 blocker - oral/IV
palonosetron class 5HT-3 blocker - IV only
Dopamine Blockers - name 2 classes + 1 drug *phenothiazines *butyrophenones *metoclopramide
DA-2 blockers MOA block DA in CTZ
phenothiazianes DA blockers - name 2 *promethazine *prochloroperazine
DA-2 blockers -phenotiazines ADRs EPS, anticholinergic
DA-2 blockers - butyrophenone ADRs EPS, anticholinergic, QT prolongation
metoclopramide MOA blocks DA-2 receptor in CTZ
different SEs for metoclopramide no EPS, has other prokinetic activity like stimulating GI peristalsis
promethazine class DA-2 blocker - phenothiazine
prochloroperazine class DA-2 blocker - phenothiazine
haloperidol class DA-2 blocker - butyrophenone
droperidol class DA-2 blocker - butyrophenone
cortiocosteroids - when used as anti-emetic - in combo with this class used in combo with 5HT-3 blockers
name 2 corticosteroids (glucocorticosteroids) usedas anti-emetic in combo 5HT-3 *methylprednisolone *dexamethasone
cannabinoids - antiemetic MOA unknown - what are ADRs psychotomimetic effects with low intensity/abuse potential
dronabinol class cannabinoids
nabilone class cannabinoids
BNZs anti-emetic MOA bind BNZ receptor in vomit center to suppress psychological effects. sedation, amenesia
what BNZs effective for antiemesis all in class will work (lorazepam, alprazolam, etc)
MOA of SP-NK-1 blockers blocks substance P at BOTH CTZ and vagal efferent. most useful for delayed CINV (chemo induced n/v)
aprepitant class, admin SP-NK-1 blocker ---oral, IV
aprepitant fun fact CYP3A4 metab is short enough not to cause significant interactions (SP-NK-1 blocking class)
What causes motion sickness acivation of vestiular apparatus --> BNZ + H1 + muscarinic binding which sends impulse to vomit center
scopolamine class, MOA anticholinergic blocks muscarinic transmission of vomit impulse
which form of scopolamine best tolerated with fewests anticholinergic SEs transdermal patch ---but also available oral, inj
antihistamines MOA in motion sickness prevention block H-1 + M receptors so vomit center not activated
demenhydrinate class antihistamine - prevent motion sickness
meclizine class antihistamine - prevent motion sickness
Created by: lorrelaws