Anti-Nausea And Anti-Emetic Drugs - Dr. Segars

Question 1

what do anti N/V medication do

Answer 1

block either 5-HT, H1, M1,D2, or Neurokinin1 (substance P) receptors

Question 2

6 classes of medication MOA

Answer 2

1. Serotonin receptor antagonist
2. Neurokinin receptor antagonist
3. Histamine Receptor antagonist
4. Dopamine receptor antagonist
5. Muscarinic receptor antagonist
6. Cannabinoid receptor AGONIST

Question 3

2 extra classes on their own for N/V

Answer 3

Glucocorticosteroids (Dexamethasone*)

Benzodiazepines (alprazolam, lorazepam)

Question 4

5 5-HT receptor antagonists

Answer 4

1. Dolasetron
2. Granisetron
3. Ondansetron
4. Palonosetron
5. Alosetron (only for IBS-D)

Question 5

5-HT receptor antagonists work how

Answer 5

block receptor activation when seratonin is released from intestinal enterochromaffin cells to the vagal nerve terminals

Question 6

5-HT receptor antagonists

used for what

Answer 6

any use (first one to go to)
- post-operative, radiation, chemo, preg, infections, vertigo motion sickness

Question 7

5-HT receptor antagonists

adverse effects you should think about

Answer 7

1. serotonin syndrome : pt taking other serotonin drugs (psychiatry) can get this and feel very bad like the flu
2. Dose-dependent QT prolongations : pt with arrhythmia or MI or heart conditions on QT prolonging drugs, or pt with electrolyte imbalance like hypo-K or Mg, need to be monitored with EKG and can still take this drug (except for Dolesetron)

Question 8

5-HT receptor antagonists half lives

Answer 8

short except Palonosetron and Granisetron have long half-life and = for delayed chemo N/V 1 dose only

Question 9

5-HT receptor antagonists D-D interactions

Answer 9

antiarrhythmics, QT prolonging agents

Question 10

3 NK1 Receptor Antagonists

Answer 10

1. Aprepitant, Foraorepitant (fos = given as IV and then cleaved to active form)
2. Netupitant, fosnetupitant
3. Rolapitant

Question 11

NK1 Receptor Antagonist used for what

Answer 11

Chemotherapy induced N/V only

usually used with other anti-emetic drugs

Question 12

NK1 Receptor Antagonist adverse effects and in body interactions

Answer 12

1. GI,CNS mild like all other emetic drugs

2. Netupitant and Rolapitant = active metabolites still working as anti-emetic so long halflife drug

Question 13

6 H1 receptor Antagonists

Answer 13

1. Diphenhydramine, Dimenhydrinate = in Benadryl
2. Hydroxyzine
3. Promethazine
4. Meclizine
5. Cyclizine
6. Doxylamine

Question 14

H1 receptor Antagonist used when

Answer 14

1. Doxylamine + Pyridoxine (VitB6) = for pregnancy
2. Meclizine + Cyclizine = motion sickness and vertigo
3. all other reasons

Question 15

H1 receptor Antagonist adverse effects

Answer 15

1. Drowsiness
2. dry mouth
3. constipation
4. urinary retention
5. blurred vision
6. Decreased BP
   * *** Anti cholinergic effects

Question 16

4 D2 receptor Antagonists

Answer 16

1. Prochlorperazine
2. Olanzapine
3. Metoclopramide
4. Amisulpride

Question 17

D2 receptor Antagonist Metoclopramide does what and is used for

Answer 17

stimulated ACh in GI = enhance GI motility AND increase LES tone ** common needed in DM pts
= help dymotility, gastroparesis

Question 18

D2 receptor Antagonist Amisulpride used for

Answer 18

prevention and tx os Post-operative N/V by IV = only when all other therapies fail

Question 19

D2 receptor Antagonist adverse effects

Answer 19

1. Drowsiness ALL
2. Prochloroperazine = dry mouth, constipation, urinary retention, blurred vision
3. amisulpride : hypokalemia, chils
4. hypotension if given in psychiatry for disorder like parkinsons

Question 20

D2 receptor Antagonist Olanzapine used for

Answer 20

the high emesis chemo/radiation drug regiment for the D2 drug part (or moderate emesis if you need to add a 4th drug)

Question 21

1 M1 receptor antagonist

Answer 21

Scopolamine

Question 22

M1 receptor antagonist is used how and used for

Answer 22

Transderm scop patch worn for 72hrs
= motion sickness, cruise, no pills just put on skin near brain
= end of life care

Question 23

Scopolamine works how

Answer 23

blocks ACh M1 receptors to vestibular nuclei in inner ear to brain stem and vomiting center= very anti-cholinergic

Question 24

Scopolamine adverse effects

Answer 24

1. drowsy
2. dry mouth
3. constipation
4. urinary retention
5. blurred vision
   =classic anti-cholinergic sx

Question 25

2 CB receptor agonists

Answer 25

1. Dronabinol | 2. Nabilone

Question 26

CB receptor agonist has what active component | how are they given

Answer 26

delta-9-THC | FDA approved for scheduled controlled quantity life span and refills (abuse ability)

Question 27

CB1

Answer 27

CB agonist stimulates this receptor in the central CNS going to Vomiting center

Question 28

CB2

Answer 28

CB agonist stimulates this receptor in the periphery NS going to vomiting center

Question 29

CB receptor agonist MOA detailed

Answer 29

use Gprotein Ri to decrease neuron excitability = lowers 5-HT3 release

Question 30

CB receptor agonist used for

Answer 30

Chemo induced N/V, when other drugs fail | anorexic or failure to thrive patients

Question 31

metabolism of Dronabinol

Answer 31

metabolized to 1 active metabolite, long halflife, short time onset

Question 32

metabolism of Nabilone

Answer 32

metabolized to few active metabolites, longer halflife, short time onset

Question 33

4 categories for emetic potential in pt with chemotherapy and what % for N/V

Answer 33

1. HIGH : more then 90% risk 2. MODERATE : 30%-90% risk 3. LOW : 10%-30% risk 4. MINIMAL : less then 10% risk

Question 34

High emetogenic regimen patient undergoing chemotherapy

Answer 34

1. D2 antagonist : Olanzapine 2. NK1 antagonist : any 3. 5-HT antagonist : any 4. Corticosteroid : Dexamethasone

Question 35

High emetogenic regimen is given how

Answer 35

1. day of prior to tx (all 4) 2. 3 days after chemo take home : NOT with 5-HT* 3. give connabinoid also in this regime if N/V still persists for next therapy cycle

Question 36

Moderate emetogenic regimen patient undergoing chemotherapy

Answer 36

1. NK1 antagonist : any 2. 5-HT antagonist : any 3. Corticosteroid : Dexamethasone

Question 37

Moderate emetogenic regimen is given how

Answer 37

1. day of prior to tx (all 3) 2. 3 days after tx take home : NOT with 5-HT* 3. give D2 antagonist OLANZAPINE if N/V still persists for next cycles

Question 38

Low emetogenic regimen patient undergoing chemotherapy

Answer 38

pick 1 drug - corticosteroid : dexamethasone - 5-HT antagonist - Metoclopramide (D2) - Prochlorperazine (D2)

Question 39

Low emetogenic regimen | given how

Answer 39

day of prior to tx (no take home) | take every day only if multi-day therapy

Question 40

Minimal emetogenic regimen patient undergoing chemotherapy

Answer 40

no routine therapy needed provide drug it patient has N/D during therapy for next cycle (if tx doesnt work give another one)

Question 41

Anticipatory emesis TX

Answer 41

non drug ways | = relaxations, hypnosis, music, muscle relaxations, yoga, acupuncture, anxiolytic therapy

Question 42

TX Pregnancy related emesis in steps

Answer 42

1. VitB6 + Doxylamine, OR 5-HT, OR just H1 2. then try D2 3. then try steroid or different D2

Question 43

motion sickness tx

Answer 43

Scopolamine patch OR Dimenhydrinate OR Meclizine

Question 44

Diabetic Gastroparesis TX

Answer 44

Metoclopramide

Question 45

Acute N/V | Chronic N/V

Answer 45

1. n/v less then 24hrs after chemo given | 2. n/v more then 24hrs after chemo given

Question 46

Anticipatory n/v happens when

Answer 46

before chemo is given, get it every time before they even get to their seat , nervousness