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GI II > Anti-Nausea and Emetic Drugs > Flashcards

Anti-Nausea and Emetic Drugs Flashcards

1
Q

Common causes of N/V

A

chemo, postop, pregnancy, vestibular dysfx, GI obstruction, infection, intracranial lesions

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2
Q

Categories of emetic potential for chemo

A

High (>90%), Moderate (30-90%), Low (10-30%), Minimal (fewer that 10%)

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3
Q

Vestibular system receptors that project to the vomiting center

A

H1, M1

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4
Q

Area postrema receptors that project to vomiting center

A

chemoreceptors, D2, NK1, 5-HT3

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5
Q

GI receptors/nerves that project to vomiting center

A

mechano/chemoreceptors, 5-HT3 via CN IX or X

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6
Q

Classes of anti-N/V drugs

A

5-HT3 antagonists, NK1 antagonists, H1 antagonists, D2 antagonists, M1 antagonists, Cannabinoid agonist, glucocorticosteroids, benzodiazepines

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7
Q

Suffix for 5-HT3 antagonists

A

-setron

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8
Q

5-HT3 MOA

A

strong antiemetic agents that block 5-HT3 receptors at CNX terminal and blocks signal transmission to CTZ, blocks 5-HT3 receptor activation after serotonin release from intestinal enterochromaffin cells

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9
Q

Therapeutic uses of 5-HT3 receptor antagonists

A

chemo-induced, radiation-induced, post-op, pregnancy N/V

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10
Q

AE 5-HT3 antagonists

A

serotonin syndrome, dose-dependent QT prolongation (especially for pts on antiarrhythmics)

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11
Q

Sxs of serotonin syndrome

A

mental status changes, diaphoresis, tachy, vomiting, diarrhea, muscle rigidity

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12
Q

Pharmacokinetics 5-HT3 antagonists

A

short half-lives (except palonosetron and granisetron)

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13
Q

Drug interactions of 5-HT3 antagonists

A

antiarrhythmics/QT-prolonging agents

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14
Q

Suffix for NK1 receptor antagonists

A

-pitant

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15
Q

Aprepitant pro-drug

A

fosaprepitant

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16
Q

Netupitant pro-drug

A

fosnetupitant

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17
Q

NK1 antagonist MOA

A

moderate antiemetic agents, block NK1 receptors in CTZ/VC

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18
Q

Therapeutic uses NK1 antagonist

A

CINV (most effective in combo with glucocorticosteroid and 5-HT3 antagonist), PONV (aprepitant only)

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19
Q

AE NK1 antagonists

A

dyspepsia, constipation, diarrhea, dizziness, fatigue, somnolence

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20
Q

Pharmacokinetics NK1

A

Netupitant/rolapitant have longer half-lives, inhibition of some CYP450s

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21
Q

Important H1 receptor antagonists

A

diphenhydramine, dimenhydrinate, hydroxyzine, promethazine, meclizine, cyclizine, doxylamine (NVP)

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22
Q

H1 antagonist MOA

A

weak antiemetics that block H1 receptors in VC and vestibular system, exhibit varying levels of anticholinergic properties at level of CTZ

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23
Q

AE H1 antagonist

A

drowsiness, dry mouth, constipation, urinary retention, blurred vision, decrease BP

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24
Q

Therapeutic uses H1 antagonist

A

idiopathic N/V, PONV, NVP (doxylamine), motion sickness (meclizine and cyclizine), CINV, RINV

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25
Q

Phenothiazines- D2 antagonists

A

chloropromazine, perphenazine, prochlorperazine

26
Q

non-phenothiazine dopamine antagonists

A

metoclopramide, haloperidol, olanzapine, trimethobenzamide

27
Q

MOA dopamine antagonists

A

weak to moderate antiemetics that block D2 receptors in CTZ which may exhibit varying levels of anticholinergic properties

28
Q

MOA metoclopramide

A

stimulates ACh actions in GI, enhances motility and increases LES tone

29
Q

AE D2 antagonists

A

drowsiness, dry mouth, constipation, urinary retention, blurred vision, hypotension

30
Q

Therapeutic uses of D2 antagonists

A

idiopathic, PONV, NVP, gastroparesis, CINV and RINV

31
Q

D2 antagonist interactions

A

agents that cause anticholinergic-related side effects, antiarrhythmics, antihypertensives

32
Q

Most common M1 blocker

A

scopolamine

33
Q

MOA M1 blocker

A

weak antiemetic commonly used for motion sickness that blocks ACh-stimulated pathways from vestibular nuclei to brain stem and from reticular formation to VC

34
Q

AE M1 blocker

A

drowsiness, dry mouth, constipation, urinary retention, blurred vision

35
Q

common CB agonists

A

Nabilone, dronabinol

36
Q

FDA schedule dronabinol

A

C-III

37
Q

FDA schedule nabilone

A

C-II

38
Q

CB agonist MOA

A

strong antiemetic reserved for CINV, stimulated CB1 and CB2 receptors in VC/CTZ, decreases excitability of neurons minimizing serotonin release from vagal afferents

39
Q

Therapeutic uses CB agonists

A

CINV, appetite stimulation in select patients

40
Q

AE CB agonists

A

euphoria, irritability, vertigo, sedation, impaired cognition, alterations in perception of reality, xerostomia, sympathomimetic, appetite stimulation

41
Q

Pharmacokinetics CB agonists

A

dronabinol has one active metabolite, nabilone has several active metabolites

42
Q

CB agonist interactions

A

CNS depressants, CV agents, sympathomimetics

43
Q

acute CINV onset

A

<24 hours after chemo

44
Q

chronic CINV onset

A

> 24 hours after chemo

45
Q

Anticipatory CINV

A

before chemo given

46
Q

High emetogenic regimen for CINV

A

NK1 antagonist, 5-HT3 antagonist, corticosteroid

47
Q

When should high-emetogenic regimens be given

A

start day of chemo treatment and continue for 3 days after chemo

48
Q

Potential high-emetogenic regimen changes

A

add olanzapine, add CB tx, provide therapy for breakthrough and anticipatory N/V

49
Q

Moderate-emetogenic drug regimen for CINV

A

5-HT3 antagonist, corticosteroid

50
Q

When should moderate-emetogenic regimen be given?

A

treat day of prior to chemo and continue for 2 days after

51
Q

Potential moderate-emetogenic regimen changes

A

add NK1 antagonist or olanzapine, add CB agonist, breakthrough or anticipatory N/V as needed

52
Q

Low-emetogenic drug regimen for CINV

A

corticosteroid OR 5-HT3 antagonist OR metoclopramide OR prochlorperazine

53
Q

When should low-emetogenic drug regimens be given?

A

tx day of prior to chemo

54
Q

Potential low-emetogenic regimen changes

A

breakthrough and anticipatory as needed

55
Q

minimal-emetogenic drug regimen for CINV

A

NO routine prophylaxis recommended, provide therapy prn

56
Q

General rule for breakthrough emesis regimen

A

add one agent from a different class to the current regimen

57
Q

Anticipatory emesis regimen

A

avoidance of strong smells, behavioral therapy, acupuncture/acupressure, anxiolytic therapy

58
Q

Drugs for motion sickness

A

scopolamine, dimenhydrinate, meclizine

59
Q

Drugs for vertigo

A

meclizine, cyclizine

60
Q

Drugs for diabetic gastroparesis

A

metoclopramide

61
Q

Drugs for NVP

A

vitamin B6 OR histamine antagonist OR 5-HT3; D2 antagonist; steroid

GI II (8 decks)

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