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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
Q

what is diphenhydramine? is is selective or non-selective?

A

benadryl

non-selective – H1 and H2

26
Q

what is dimenhydramine? is it selective or non-selective?

A

dramamine

selective – H1

27
Q

what is dimenhydramine metabolized to?

A

diphenhydramine

28
Q

what is the initial therapy for NVP?

A

doxylamine

[w/ pyridoxine (B6)]

STAR

29
Q

is the histamine (H1) receptor antagonist class strong, moderate, or weak?

A

weak antiemetic agents

good for PONV

30
Q

what drug classes exhibit varying levels of central anticholinergic properties at level of CTZ?

A
  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
Q

name the classic anticholinergic effects

A
  1. drowsiness (CNS depression)
  2. dry mouth
  3. constipation
  4. urinary retention
  5. blurred vision
  6. decrease BP

1-5 STARcumulative effects w/ other agents inducing anti-cholinergics

32
Q

name the two big therapeutic uses of histamine (H1) receptor antagonists

A
  1. NVP (doxylamine/B6)

2. motion sickness/vertigo (meclizine and cyclizine)

33
Q

name the three big drugs of dopamine (D2) receptor antagonists

A

PHENOTHIAZINES

  1. chlorpromazine
  2. perphenazine
  3. prochlorperazine

others: metoclopramide; anti-psychotics (haloperidol, olanzaprine and trimethobenzamide)

34
Q

is the dopamine (D2) receptor antagonist drug class strong, moderate, or weak?

A

weak-moderate antiemetic agents

35
Q

which dopamine (D2) receptor antagonist also stimulates acetylcholine actions in GI to enhance motility and increase LES tone?

A

metoclopramide

for dysmotility use, no impact on GI secretions

blue

36
Q

what is the big therapeutic use of dopamine (D2) receptor antagonists?

A

gastroparesis / dysmotility

metoclopramide

blue

37
Q

what is the muscarinic (M1) receptor antagonist?

A

scopolamine

38
Q

how long is the transdermal scopolamine patch worn for?

A

72 hours

blue

39
Q

what is scopolamine most commonly used for?

A

motion sickness

also used for end-of-life care for excessive secretions
note: IV glycopyrrolate even stronger, in same class..?

blue

40
Q

what are the two cannabinoid receptor agonists?

A
  1. dronabinol

2. nabilone

41
Q

which cannabinoid receptor antagonist is C-II and therefore more risky?

A

nabilone

dronabinol is C-III

42
Q

who can receive treatment with cannabinoids?

A

treatment-resistant CINV ((STAR))
strong antiemetic agents

stimulates CB1 and CB2 –> decreased excitability of neurons (minimizing serotonin release from vagal afferent terminals)

43
Q

can cannabinoids be used in combination with other drugs?

A

yes

44
Q

describe the pharmacokinetics of dronabinol and nabilone

A

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
Q

what interactions does one need to be mindful of when prescribing cannabinoids?

A

other CNS depressants
cardiovascular agents
sympathomimetics

46
Q

describe the treatment protocol for high-emetogenic CINV

A

(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
Q

describe the treatment protocol for moderate-emetogenic CINV

A

(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
Q

describe the treatment protocol for low-emetogenic CINV

A

(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
Q

describe the treatment protocol for minimal-emetogenic regimen CINV

A

(0 drugs)

  1. no routine prophylaxis therapy recommended

A – provide therapy for breakthrough
B – provide therapy for anticipatory

50
Q

name the drugs for motion sickness

overview card

A

scopolamine (patch)
dimenhydrinate
meclizine

blue

51
Q

name the drugs for vertigo

overview card

A

meclizine
cyclizine

blue

52
Q

name the drugs for diabetic gastroparesis

overview card

A

metoclopramide

blue

53
Q

describe the stepped-therapy protocol for pregnancy-induced N/V

(overview card)

A
  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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