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GI 2 > Agents for N/V (Segars) > Flashcards

Agents for N/V (Segars) Flashcards

1
Q

Nausea/Vomiting 6 families of drugs (targeting specific receptors)

A

Serotonin (5-HT3) Receptor Antagonist
Neurokinin (NK1) Receptor Antagonist
Histamine (H1) Receptor Antagonist
Dopamine (D2) Receptor Antagonist
Muscarinic (M1) Receptor Antagonist
Cannabinoid (CB) Receptor Agonist **(only agonist)

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2
Q

Serotonin (5-HT3) Receptor Antagonist drug naming convention?

A

Dola_setron_
Grani_setron_
Ondan_setron_
Palono_setron_

the -se- is like Serotonin

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3
Q

Neurokinin (NK1) Receptor Antagonists naming convention?

A

Aprepitant
Fosaprepitant
Netupitant
Fosnetupitant
Rolapitant

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4
Q

5-HT3 Receptor Antagonist MOA

A

blocks serotonin type 3 receptors at vagal nerve terminals

blocks signal transmission to CTZ

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5
Q

5-HT3 Receptor Antagonist used for which patients?

A

lots of people with different types of N/V

  • Chemotherapy-induced N/V (CINV)
  • Radiation-induced N/V (RINV)
  • Post-operative N/V (PONV)
  • N/V of Pregnancy (NVP)
  • Idiopathic, mild N/V (e.g., infections, etc…)
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6
Q

5-HT3 Receptor Antagonist adverse effects?

A

mild: GI, CNS

Worrisome: Dose-dependent QT prolongation (Torsade’s)
use extreme caution!
Dolastetron has higher risk, not used prophylactically anymore (D=death)

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7
Q

5-HT3 Receptor Antagonist pharmacokinetics: half life (short/long)?

A

all have short half lives
except Palonosetron and sustained-release Granisetron formula (can use single dose)

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8
Q

5-HT3 Receptor Antagonist drug interactions

A

Antiarrythmics/QT-prolonging agents

caution!

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9
Q

Neurokinin (NK1) Receptor Antagonist therapeutic uses & administration

A

Chemo-induced N/V

most effective when used in combination with other anti-emetic agents (rarely used alone)

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10
Q

Neurokinin (NK1) Receptor Antagonist pharmacokinetics: half life (short/long)?

A

Netupitant/Rolapitant have longer half lives dt moderate-major active metabolites

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11
Q

Wht drug regimen do you start with for NVP (pregnancy)?

A

Doxylamine (H1 receptor antagonist) w/ pyridoxine B6

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12
Q

H1 Receptor Antagonist adverse effects?

A

Classic Anticholinergic effects:

Drowsiness
Dry mouth
Constipation
Urinary Retention
blurred vision
decrease BP

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13
Q

What would you prescribe for motion sickness/vertigo?

A

meclizine, cyclizine

(H1 receptor antagonists)

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14
Q

What are the 4 Dopamine (D2) Receptor Antagonists

A

Prochlorperazine
Olanzapine
Metoclopramide
Amisulpride

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15
Q

What are the 6 Histamine (H1) receptor antagonists?

A

Diphenhydramine
Dimenhydrinate
Hydroxyzine
Promethazine
Meclizine
Cyclizine

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16
Q

Dopamine Receptor Antagonist MOA

general:

Metoclopramide:

Amisulpride:

A

general: blocks D2 receptors in CTZ

Metoclopramide: stimulates ACh actions in GI, enhancing GI motility (used by diabetics for dysmotility issues) & increases lower esophageal sphincter tone

Amisulpride: only used for prevention/treatment of PONV (post-op)

17
Q

Dopamine Receptor Antagonist adverse effects

A

ALL: drowsiness

Prochlorperazine: dry mouth
constipation
urinary retention
blurred vision

IV route drugs: hypotension

Amisulpride: Hypokalemia, hyperprolactinemia, chills

18
Q

indication for using amisulpride?

A

Post-operative N/V

19
Q

Indication for using Metoclopramide?

A

Gastroparesis/Dysmotility

20
Q

Muscarinic Receptor Antagonist drugs

A

Scopolamine

21
Q

Scopolamine MOA

A

transderm patch used for motion sickness (and end-of-life secretions)

blocks ACh-stimulated muscarinic receptors (anticholinergic properties)

22
Q

Muscarinic Receptor Antagonist adverse effects?

A

Classic Anticholinergic effects:
drowsiness, dry mouth, constipation, urinary retention, blurred vision

23
Q

Name the 2 Cannabinoid (CB) receptor Agonists

A

Dronabinol
Nabilone

24
Q

Cannabinoid (CB) receptor Agonist chemical makeup?

A

synthetic preoparations of cannabinol (THC)

FDA scheduled (controlled) medications dt abuse potential

25
Q

Cannabinoid (CB) receptor Agonist MOA

A

stimulates central (CB1) and peripheral (CB2) cannabinoid receptors in VC/CTZ

signal transduction effects through G-protien coupled receptors resulting in decreased excitability of neurons

minimizes serotonin release from vagal afferent terminals

26
Q

Cannabinoid (CB) receptor Agonist therapeutic uses

A

chemo-induced N/V

usually reserved for treatment-resistant people (dt FDA scheduling)
can be used as add-on with other agents

sometimes used as appetite stimulant (dt severe disease like cancer or AIDS)

27
Q

What are 3 subtypes of Chemo-induced N/V?

A

acute: occurring <24 hrs after chemo
chronic: occurring >24 hrs after chemo
anticipatory: occurring before chemo given, customarily in non-trreatment naive pts

**focus on prevention**

28
Q

High-Emetogenic regimen

A

4 drug regimen

  1. D2antagonist (Olanzapine*)
  2. NK1receptor antagonist* (-pitant)
  3. 5-HT3receptor antagonist (-stron)
  4. Corticosteroid (Dexamethasone*)

Give treatment regimen day of (prior to) chemotherapy, then 3-drug treatment* for 3 days after chemotherapy
Can add cannabinoid, if treatment resistance(5-drugs)

29
Q

Moderate-Emetogenic Regimen

A

3 drug regimen (drop the D2)

  1. NK1receptor antagonist*
  2. 5-HT3receptor antagonist
  3. Corticosteroid (Dexamethasone*)

Give treatment regimen day of (prior to) chemotherapy, then 2-drug treatment* for 2 days after chemotherapy
Can add D2antagonist (olanzapine), if treatment resistance (4-drugs)

30
Q

Low-Emesitogenic Regimen

A

1 drug regimen

  1. Corticosteroid (Dexamethasone),or
  2. 5-HT3receptor antagonist, or
  3. Metoclopramide,or
  4. Prochlorperazine,or

Give treatment regimen day of (prior to) chemotherapy; may repeat daily for multi-day anticancer therapy
Provide therapy for breakthrough N/V

31
Q

Minimal-Emetogenic Regimen

A

0-drug regimen

No routine prophylaxis therapy recommended
Provide therapy for breakthrough N/V (Any agent from this lecture series)

32
Q

Pregnancy-Induced N/V stepped therapy

A
  1. Vitamin B6 or Histamine Antagonist (w;w/o Vit. B6) or 5-HT3 Antagonist
  2. Dopamine Antagonist
  3. Steroid or Different Dopamine Antagonist
33
Q

What would you prescribe for Motion Sickness?

A

Scopolamine (patch) or Dimenhydrinate or Meclizine

34
Q

What would you prescribe for vertigo?

A

Meclizine or Cyclizine

35
Q

What would you prescribe for Diabetic Gastroparesis?

A

Metoclopramide

GI 2 (19 decks)

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