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NURS 572 Ch 79
Pharm Ch 79 antiemetics, motion sickness
| Question | Answer |
|---|---|
| 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
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