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Ch 28 Nausea/Vomiting

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1. Anticholinergics - Motion sickness 9. Cannabinoids efficacy - CINV (2nd line agent)


(Scopolamine) - Block muscarinic receptors (inner ear
10. Classification of Chemo - Low: <10%
Antiemetic Use & to vomiting center)
Drugs and Patients - Low-Moderate: 10-30%
MOA
- Moderate: 30-60%
2. Antihistamines - Motion sickness - Moderate-High: 60-90%
(Dimenhydrinate) - Block histamine type 1 receptors (inner - High >90%
Antiemetic Use & ear to vomiting center)
MOA • Acute Emesis
• Anticipatory Emesis
3. Basic Principles of - Consider emetogenic potential of
• Delayed Emesis
Chemotherapy chemotherapy regimen.
Antiemetic - Give appropriate antiemetics to prevent 11. Dopamine Antagonists - EPS
Therapy nausea and vomiting at least 30 minutes adverse effects - QT prolongation/dysrhythmia
before emetogenic chemotherapy. - Anticholinergic effects
- Schedule antiemetics throughout (hypotension/sedation)
anticipated period of nausea and - Promethazine: respiratory
vomiting risk. depression in children <2 yo,
- Always prescribe PRN antiemetics for extravasation
breakthrough nausea and vomiting
12. Dopamine Antagonists - Phenothiazines: BBW: dementia
between scheduled doses.
Agents (drugs) pt with psych = EPS/QT
- Use antiemetic combinations with non
prolongation
overlapping MOA when possible.
- Butyrophenones (haloperidol)
- Consider patient-specific variables
- Metoclopramide (avoid in
when choosing a regimen
elderly/antipsychotics)
- Re-evaluate patients frequently during
and between chemotherapy courses for 13. Dopamine Antagonists - CINV
efficacy and toxicity of antiemetic Agents efficacy - PONV
regimen. - Other
- Consider nonpharmacologic 14. Dopamine Antagonists - IM preferred
interventions, especially in patients with clinical pearls - SC contraindicated
anticipatory nausea and vomiting. (Promethazine) - IV through large bore <25
4. Benzodiazepines - unknown mg/min
(Lorazepam) - Unknown: maybe activate GABA 15. Dopamine Antagonists - Chemotherapy, postoperative,
Antiemetic Use & leading (Prochlorperazine) general
MOA to inhibition of pathways Antiemetic Use & MOA - Block dopamine 2 receptors in
5. Cannabanoids - Chemotherapy the CTZ
(Dronabinol) - Unknown: maybe activate cannabinoid 16. Glucocorticoids - Chemotherapy
Antiemetic Use & receptors in the vomiting center (Dexamethasone) - Unknown: maybe prostaglandin
MOA Antiemetic Use & MOA synthesis
6. Cannabinoids - Temporal disintegration 17. Motion Sickness tx - Most Effective: scopolamine (2-
adverse effects - Dissociation 4 hr to see effects) patch = less
- Depersonalization anticholinergic effects
- Dysphoria - Antihistamines: dimenhydrinate,
- Hypotension cyclizine
- Sedation/drowsiness
18. Nausea/Vomiting drugs - Serotonin Antagonists
7. Cannabinoids - Dronabinol - Glucocorticoids
Agents (drugs) - Nabilone - Substance P/Neurokinin-1
8. Cannabinoids - contraindicated in patents with psych Antagonists
clinical pearls disorders - Dopamine Antagonists
- caution in CV disorders - Cannabanoids
- Abuse potential - Anticholinergics
- Antihistamines
- Benzodiazepines
19. Pregnancy and - 1st line: Nonpharmacologic 27. Substance P/Neurokinin-1 - Chemotherapy
Nausea/Vomiting therapy *avoid iron Antagonists (Aprepitant ) - Block substance
- 1st line pharmacologic: Antiemetic Use & MOA P/Neurokinin 1 receptors in
Doxylamine + Vitamine B (↓ by the brain
70%, safe on fetus)
28. Substance P/Neurokinin - fatigue
- 2nd line: Prochlorperazine,
Inhibitors adverse effects - asthenia
metoclopramide, ondansetron
- hiccups
20. Pregnancy and - Vitamin B6 = pyridoxine - diarrhea
Nausea/Vomiting extra - Delayed release combo = - mild transaminitis
info diclegis - drug interactions (inhibits
- Methylprednisolone is last 3A4 + metabolized by 3A4)
resort: risk of cleft lip/palate if
29. Substance P/Neurokinin - aprepitant
before 10 weeks
Inhibitors Agents (drugs) - fosaprepitant → aprepitant
21. Prevention of ACUTE and - High: 5-HT3 + DEX + NK1 + (prodrug)
Delayed N/V OLZ - rolapitant
- Moderate: 5-HT3 + DEX - netupitant
- Low: 5-HT3 or DEX
30. Substance P/Neurokinin - Fos/Aprepitant: effective
- Minimal: none
Inhibitors clinical pearls against delayed and acute
N/V
5-HT3: serotonin receptor
- Fosaprepitant: only IV to
antagonist
replace 1st dose of 3 does
DEX: dexamethasone
regimen aprepitant
NK1: neurokinin receptor
- Netupitant: combo product
antagonist
(effective for delayed N/V)
OZL: olanzapine
31. Substance P/Neurokinin - CINV: moderate efficacy
22. Serotonin 5HT-3 - Headache, dizziness, diarrhea
Inhibitors Efficacy (combo with glucocorticoids
Receptor Antagonists - Ondansetron: QT prolongation
and 5HT antagonist)
Adverse Effects - Dolasetron: fatal arrhythmia
- PONV
(IV @ high dose)
23. Serotonin 5HT-3 - Ondansetron
Receptor Antagonists - Granistron
Agents (drugs) - Palonosetron
- Dolasetron
24. Serotonin 5HT-3 - Palosetron: effective against
Receptor Antagonists delayed and acute N/V
Clinical Pearls - Zofran better at tx anti
vomiting vs tx anti nausea
25. Serotonin 5HT-3 - Pregnancy
Receptor Antagonists - Viral gastritis
Efficay: High - Cisplatin/other emetic chemo
agents (efficacy increased with
glucocorticoids)
- Radiation therapy
- Anesthesia
26. Serotonin Antagonists - Chemotherapy, postoperative,
(Ondansetron) general
Antiemetic Use & MOA - Block 5HT receptors in vagal
afferent and CTZ