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GI II > Anti-Nausea and Anti-Emetic Pharmacology > Flashcards

Anti-Nausea and Anti-Emetic Pharmacology Flashcards

1
Q

which receptor antagonist is associated with substance p?

A

NK1

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2
Q

what is the poster child of glucocorticosteroids?

A

dexamethasone

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3
Q

what is the poster child of benzodiazepines?

A

alprazolam/lorazepam

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4
Q

which can be used as anti-emetic for anticipatory N/V?

dexamethasone or alprazolam/lorazepam

A

alprazolam/lorazepam

benzodiazepines

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5
Q

-setron

A

5-HT3 / serotonin

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6
Q

-pitant

A

NK1 / neurokinin

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7
Q

which receptor class is an agonist?

A

cannabinoid

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8
Q

which serotonin drug is only indicated for IBS-D?

A

alosetron

[lotronex] (po)

blue

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9
Q

name the five drugs in the serotonin (5-HT3) receptor antagonist class

A
  1. dolasetron
  2. granisetron
  3. ondansetron
  4. palonosetron
  5. alosetron (only for IBS-D)

this class is good b/c v. effective and relatively SE free; can be given in variety of methods (po, iv, patch, subq)

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10
Q

which serotonin drug can be used as either transdermal cutaneous patch or SQ injection?

A

granisetron

  • sancuso (cutaneous patch)
  • sustol (SQ injection)
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11
Q

which serotonin drug is combination-only when given iv?

A

palonosetron

akynzeo

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12
Q

is the serotonin (5-HT3) drug class strong, moderate, or weak?

A

strong antiemetic agents

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13
Q

which drug class has dose-dependent QT prolongation (torsade’s) as a worrisome adverse effect? name the highest risk drug

A

serotonin (5-HT3) receptor antagonists; dolasetron

extreme caution when

  • using w/ other QT-prolonging agents (antiarrhythmics)
  • pts have electrolyte imbalances (hypok or hypomg)

STAR

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14
Q

does the serotonin drug class have a long or short half-life? name the exceptions

A

short half-lives; can be single-dose for delayed-CINV

  1. palonosetron
  2. granisetron [esp. in sustained release form (SQ)]

blue

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15
Q

name the five drugs of the neurokinin (NK1) receptor antagonist class

A
  1. aprepitant
  2. fosaprepitant
  3. netupitant
  4. fosnetupitant
  5. rolapitant
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16
Q

which drugs in the neurokinin (NK1) class are iv?

A 
the prodrugs (fosaprepitant and fosnetupitant)
rolapitant (po/iv)
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17
Q

which drugs in the neurokinin (NK1) class are combo-only?

A

fosnetupitant and netupitant

blue

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18
Q

is the neurokinin (NK1) receptor antagonist class strong, moderate, or weak?

A

moderate antiemetic agents

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19
Q

name the two therapeutic uses of neurokinin drugs

A
  1. CINV (most effective in combo)

2. prophylaxis of PONV only aprepitant

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20
Q

which neurokinin drug is effective for prophylaxis of PONV?

A

aprepitant

pt will have hx of PONV

STAR

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21
Q

aside from GI, what other system can have adverse effects due to neurokinins?

A

CNS – dizziness, fatigue, somnolence

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22
Q

of the neurokinins, what drugs have moderate-major active metabolites and longer half-lives?

A

netupitant and rolapitant

blue

23
Q

neurokinins are mild-moderate [activators or inhibitors] of CYP450 enzymes…

A

inhibitors

so watch for DDIs

24
Q

name the seven drugs in the histamine (H1) receptor antagonists class

A
  1. diphenhydramine
  2. dimenhydramine
  3. hydroxyzine
  4. promethazine
  5. meclizine
  6. cyclizine
  7. doxylamine
25
what is diphenhydramine? is is selective or non-selective?
benadryl | non-selective -- H1 and H2
26
what is dimenhydramine? is it selective or non-selective?
dramamine | selective -- H1
27
what is dimenhydramine metabolized to?
diphenhydramine
28
what is the initial therapy for NVP?
doxylamine [w/ pyridoxine (B6)] **STAR**
29
is the histamine (H1) receptor antagonist class strong, moderate, or weak?
weak antiemetic agents | good for PONV
30
what drug classes exhibit varying levels of central anticholinergic properties at level of CTZ?
1. histamine (H1) receptor antagonists 2. dopamine (D2) receptor antagonists 3. muscarinic (M1) receptor antagonists **STAR** so don't pair w/ other anti-cholin.
31
name the classic anticholinergic effects
1. drowsiness (CNS depression) 2. dry mouth 3. constipation 4. urinary retention 5. blurred vision 6. decrease BP **1-5 STAR**cumulative effects w/ other agents inducing anti-cholinergics
32
name the two big therapeutic uses of histamine (H1) receptor antagonists
1. NVP (doxylamine/B6) | 2. motion sickness/vertigo (meclizine and cyclizine)
33
name the three big drugs of dopamine (D2) receptor antagonists
PHENOTHIAZINES 1. chlorpromazine 2. perphenazine 3. prochlorperazine others: metoclopramide; anti-psychotics (haloperidol, olanzaprine and trimethobenzamide)
34
is the dopamine (D2) receptor antagonist drug class strong, moderate, or weak?
weak-moderate antiemetic agents
35
which dopamine (D2) receptor antagonist also stimulates acetylcholine actions in GI to enhance motility and increase LES tone?
metoclopramide for dysmotility use, no impact on GI secretions **blue**
36
what is the big therapeutic use of dopamine (D2) receptor antagonists?
gastroparesis / dysmotility metoclopramide **blue**
37
what is the muscarinic (M1) receptor antagonist?
scopolamine
38
how long is the transdermal scopolamine patch worn for?
72 hours **blue**
39
what is scopolamine most commonly used for?
motion sickness also used for end-of-life care for excessive secretions note: IV glycopyrrolate even stronger, in same class..? **blue**
40
what are the two cannabinoid receptor agonists?
1. dronabinol | 2. nabilone
41
which cannabinoid receptor antagonist is C-II and therefore more risky?
nabilone dronabinol is C-III
42
who can receive treatment with cannabinoids?
treatment-resistant CINV ((**STAR**)) strong antiemetic agents stimulates CB1 and CB2 --> decreased excitability of neurons (minimizing serotonin release from vagal afferent terminals)
43
can cannabinoids be used in combination with other drugs?
yes
44
describe the pharmacokinetics of dronabinol and nabilone
dronabinol -- large first-pass effect; metabolized to ONE active metabolite nabilone -- metabolized to SEVERAL active metabolites both -- short-time to onset and long duration of action; nabilone has fewer doses/day
45
what interactions does one need to be mindful of when prescribing cannabinoids?
other CNS depressants cardiovascular agents sympathomimetics
46
describe the treatment protocol for high-emetogenic CINV
(3-drugs) 1. NK1 2. 5-HT3 3. dexamethasone (corticosteroid) give treatment day of (prior to) chemo for acute, and for 3 days after for delayed ``` A OR B to increase to 4-drug regimen: A -- olanzapine (D2) B -- cannabinoid C -- therapy for breakthrough D -- therapy for anticipatory ```
47
describe the treatment protocol for moderate-emetogenic CINV
(2 drugs) 1. 5-HT3 2. dexamethasone (corticosteroid) give treatment day of (prior to) chemo for acute, and for 2 days after for delayed A -- olanzapine (D2); to increase to 3 B -- cannabinoid; to increase to 4 C -- therapy for breakthrough D -- therapy for anticipatory
48
describe the treatment protocol for low-emetogenic CINV
(1 drug) any one of the following: 1. dexamethasone (corticosteroid) 2. 5-HT3 3. metoclopramide 4. prochlorperazine give treatment day of (prior to) chemo for acute A -- therapy for breakthrough B -- therapy for anticipatory ABOVE: 1 and 2 most common
49
describe the treatment protocol for minimal-emetogenic regimen CINV
(0 drugs) 1. no routine prophylaxis therapy recommended A -- provide therapy for breakthrough B -- provide therapy for anticipatory
50
name the drugs for motion sickness | overview card
scopolamine (patch) dimenhydrinate meclizine **blue**
51
name the drugs for vertigo | overview card
meclizine cyclizine **blue**
52
name the drugs for diabetic gastroparesis | overview card
metoclopramide **blue**
53
describe the stepped-therapy protocol for pregnancy-induced N/V (overview card)
1. B6 or H1 antagonist w/ B6 or 5-HT3 antagonist 2. D2 antagonist 3. steroid or different dopamine antagonist

GI II (5 decks)

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