Pharm Ch 79 antiemetics, motion sickness
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| Name all receptors involved in emetic response | *5HT-3
*DA-2
*NK-1 (binds substance P)
*Muscarinic
*H-1 Histamine
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| Name major receptors that are activated by vestibular apparatus in motion sickness | *H-1
*Muscarinic
*BNZ
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| 8 total classes of antiemetics - name first 4 | *5HT-3 blockers
*DA-2 blockers
*anticholinergics (primarily motion sickness)
*antihistamines (primarily motion sickness)
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| 8 total classes of antiemetics - name second 4 | *glucocorticoids-corticosteroids
*canabinoids
*BNZs
*SP NK-1 blockers (substance P neurokinin-1)
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| 5HT-3 blockers MOA | block serotonin-3 receptors in CTZ --- AND --- blocks them in vagal afferent
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| 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
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| ADRs of 5HT-3 blockers | HA/dizz/D
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| name five 5HT-3 blockers in class | *odeansetron
*granisetron
*dolasetron
*palonosetron
*granisetron patch (new)
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| what 5HT-3 blocker is only available IV only | palonosetron
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| odansetron class | 5HT-3 blocker - oral/IV
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| granisetron class | 5HT-3 blocker - oral/IV ---now transdermal
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| dolasetron class | 5HT-3 blocker - oral/IV
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| palonosetron class | 5HT-3 blocker - IV only
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| Dopamine Blockers - name 2 classes + 1 drug | *phenothiazines
*butyrophenones
*metoclopramide
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| DA-2 blockers MOA | block DA in CTZ
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| phenothiazianes DA blockers - name 2 | *promethazine
*prochloroperazine
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| DA-2 blockers -phenotiazines ADRs | EPS, anticholinergic
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| DA-2 blockers - butyrophenone ADRs | EPS, anticholinergic, QT prolongation
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| metoclopramide MOA | blocks DA-2 receptor in CTZ
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| different SEs for metoclopramide | no EPS, has other prokinetic activity like stimulating GI peristalsis
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| promethazine class | DA-2 blocker - phenothiazine
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| prochloroperazine class | DA-2 blocker - phenothiazine
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| haloperidol class | DA-2 blocker - butyrophenone
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| droperidol class | DA-2 blocker - butyrophenone
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| cortiocosteroids - when used as anti-emetic - in combo with this class | used in combo with 5HT-3 blockers
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| name 2 corticosteroids (glucocorticosteroids) usedas anti-emetic in combo 5HT-3 | *methylprednisolone
*dexamethasone
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| cannabinoids - antiemetic MOA unknown - what are ADRs | psychotomimetic effects with low intensity/abuse potential
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| dronabinol class | cannabinoids
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| nabilone class | cannabinoids
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| BNZs anti-emetic MOA | bind BNZ receptor in vomit center to suppress psychological effects. sedation, amenesia
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| what BNZs effective for antiemesis | all in class will work (lorazepam, alprazolam, etc)
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| MOA of SP-NK-1 blockers | blocks substance P at BOTH CTZ and vagal efferent. most useful for delayed CINV (chemo induced n/v)
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| aprepitant class, admin | SP-NK-1 blocker ---oral, IV
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| aprepitant fun fact | CYP3A4 metab is short enough not to cause significant interactions (SP-NK-1 blocking class)
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| What causes motion sickness | acivation of vestiular apparatus --> BNZ + H1 + muscarinic binding which sends impulse to vomit center
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| scopolamine class, MOA | anticholinergic blocks muscarinic transmission of vomit impulse
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| which form of scopolamine best tolerated with fewests anticholinergic SEs | transdermal patch ---but also available oral, inj
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| antihistamines MOA in motion sickness prevention | block H-1 + M receptors so vomit center not activated
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| demenhydrinate class | antihistamine - prevent motion sickness
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| meclizine class | antihistamine - prevent motion sickness
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