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

1
Q

what do anti N/V medication do

A

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

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2
Q

6 classes of medication MOA

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

2 extra classes on their own for N/V

A

Glucocorticosteroids (Dexamethasone*)

Benzodiazepines (alprazolam, lorazepam)

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4
Q

5 5-HT receptor antagonists

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

5-HT receptor antagonists work how

A

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

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6
Q

5-HT receptor antagonists

used for what

A
any use (first one to go to)
- post-operative, radiation, chemo, preg, infections, vertigo motion sickness
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7
Q

5-HT receptor antagonists

adverse effects you should think about

A
  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)
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8
Q

5-HT receptor antagonists half lives

A

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

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9
Q

5-HT receptor antagonists D-D interactions

A

antiarrhythmics, QT prolonging agents

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10
Q

3 NK1 Receptor Antagonists

A
  1. Aprepitant, Foraorepitant (fos = given as IV and then cleaved to active form)
  2. Netupitant, fosnetupitant
  3. Rolapitant
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11
Q

NK1 Receptor Antagonist used for what

A

Chemotherapy induced N/V only

usually used with other anti-emetic drugs

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12
Q

NK1 Receptor Antagonist adverse effects and in body interactions

A
  1. GI,CNS mild like all other emetic drugs

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

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13
Q

6 H1 receptor Antagonists

A
  1. Diphenhydramine, Dimenhydrinate = in Benadryl
  2. Hydroxyzine
  3. Promethazine
  4. Meclizine
  5. Cyclizine
  6. Doxylamine
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14
Q

H1 receptor Antagonist used when

A
  1. Doxylamine + Pyridoxine (VitB6) = for pregnancy
  2. Meclizine + Cyclizine = motion sickness and vertigo
  3. all other reasons
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15
Q

H1 receptor Antagonist adverse effects

A
  1. Drowsiness
  2. dry mouth
  3. constipation
  4. urinary retention
  5. blurred vision
  6. Decreased BP
    * *** Anti cholinergic effects
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16
Q

4 D2 receptor Antagonists

A
  1. Prochlorperazine
  2. Olanzapine
  3. Metoclopramide
  4. Amisulpride
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17
Q

D2 receptor Antagonist Metoclopramide does what and is used for

A

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

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18
Q

D2 receptor Antagonist Amisulpride used for

A

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

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19
Q

D2 receptor Antagonist adverse effects

A
  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
20
Q

D2 receptor Antagonist Olanzapine used for

A

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

21
Q

1 M1 receptor antagonist

A

Scopolamine

22
Q

M1 receptor antagonist is used how and used for

A

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

23
Q

Scopolamine works how

A

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

24
Q

Scopolamine adverse effects

A
  1. drowsy
  2. dry mouth
  3. constipation
  4. urinary retention
  5. blurred vision
    =classic anti-cholinergic sx
25
Q

2 CB receptor agonists

A
  1. Dronabinol

2. Nabilone

26
Q

CB receptor agonist has what active component

how are they given

A

delta-9-THC

FDA approved for scheduled controlled quantity life span and refills (abuse ability)

27
Q

CB1

A

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

28
Q

CB2

A

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

29
Q

CB receptor agonist MOA detailed

A

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

30
Q

CB receptor agonist used for

A

Chemo induced N/V, when other drugs fail

anorexic or failure to thrive patients

31
Q

metabolism of Dronabinol

A

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

32
Q

metabolism of Nabilone

A

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

33
Q

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

A
  1. HIGH : more then 90% risk
  2. MODERATE : 30%-90% risk
  3. LOW : 10%-30% risk
  4. MINIMAL : less then 10% risk
34
Q

High emetogenic regimen patient undergoing chemotherapy

A
  1. D2 antagonist : Olanzapine
  2. NK1 antagonist : any
  3. 5-HT antagonist : any
  4. Corticosteroid : Dexamethasone
35
Q

High emetogenic regimen is given how

A
  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
36
Q

Moderate emetogenic regimen patient undergoing chemotherapy

A
  1. NK1 antagonist : any
  2. 5-HT antagonist : any
  3. Corticosteroid : Dexamethasone
37
Q

Moderate emetogenic regimen is given how

A
  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
38
Q

Low emetogenic regimen patient undergoing chemotherapy

A

pick 1 drug

  • corticosteroid : dexamethasone
  • 5-HT antagonist
  • Metoclopramide (D2)
  • Prochlorperazine (D2)
39
Q

Low emetogenic regimen

given how

A

day of prior to tx (no take home)

take every day only if multi-day therapy

40
Q

Minimal emetogenic regimen patient undergoing chemotherapy

A

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

41
Q

Anticipatory emesis TX

A

non drug ways

= relaxations, hypnosis, music, muscle relaxations, yoga, acupuncture, anxiolytic therapy

42
Q

TX Pregnancy related emesis in steps

A
  1. VitB6 + Doxylamine, OR 5-HT, OR just H1
  2. then try D2
  3. then try steroid or different D2
43
Q

motion sickness tx

A

Scopolamine patch OR Dimenhydrinate OR Meclizine

44
Q

Diabetic Gastroparesis TX

A

Metoclopramide

45
Q

Acute N/V

Chronic N/V

A
  1. n/v less then 24hrs after chemo given

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

46
Q

Anticipatory n/v happens when

A

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