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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
Cannabinoid (CB) receptor Agonist MOA
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
Cannabinoid (CB) receptor Agonist therapeutic uses
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
What are 3 subtypes of Chemo-induced N/V?
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
High-Emetogenic regimen
**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
Moderate-Emetogenic Regimen
**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
Low-Emesitogenic Regimen
**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
Minimal-Emetogenic Regimen
**0-drug regimen** No routine prophylaxis therapy recommended *Provide therapy for breakthrough N/V* *(Any agent from this lecture series)*
32
Pregnancy-Induced N/V stepped therapy
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
What would you prescribe for Motion Sickness?
Scopolamine (patch) or Dimenhydrinate or Meclizine
34
What would you prescribe for vertigo?
Meclizine or Cyclizine
35
What would you prescribe for Diabetic Gastroparesis?
Metoclopramide

GI 2 (19 decks)

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