Anti-Nausea and Emetic Drugs

Question 1

Common causes of N/V

Answer 1

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

Question 2

Categories of emetic potential for chemo

Answer 2

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

Question 3

Vestibular system receptors that project to the vomiting center

Answer 3

H1, M1

Question 4

Area postrema receptors that project to vomiting center

Answer 4

chemoreceptors, D2, NK1, 5-HT3

Question 5

GI receptors/nerves that project to vomiting center

Answer 5

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

Question 6

Classes of anti-N/V drugs

Answer 6

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

Question 7

Suffix for 5-HT3 antagonists

Answer 7

-setron

Question 8

5-HT3 MOA

Answer 8

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

Question 9

Therapeutic uses of 5-HT3 receptor antagonists

Answer 9

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

Question 10

AE 5-HT3 antagonists

Answer 10

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

Question 11

Sxs of serotonin syndrome

Answer 11

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

Question 12

Pharmacokinetics 5-HT3 antagonists

Answer 12

short half-lives (except palonosetron and granisetron)

Question 13

Drug interactions of 5-HT3 antagonists

Answer 13

antiarrhythmics/QT-prolonging agents

Question 14

Suffix for NK1 receptor antagonists

Answer 14

-pitant

Question 15

Aprepitant pro-drug

Answer 15

fosaprepitant

Question 16

Netupitant pro-drug

Answer 16

fosnetupitant

Question 17

NK1 antagonist MOA

Answer 17

moderate antiemetic agents, block NK1 receptors in CTZ/VC

Question 18

Therapeutic uses NK1 antagonist

Answer 18

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

Question 19

AE NK1 antagonists

Answer 19

dyspepsia, constipation, diarrhea, dizziness, fatigue, somnolence

Question 20

Pharmacokinetics NK1

Answer 20

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

Question 21

Important H1 receptor antagonists

Answer 21

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

Question 22

H1 antagonist MOA

Answer 22

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

Question 23

AE H1 antagonist

Answer 23

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

Question 24

Therapeutic uses H1 antagonist

Answer 24

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

Question 25

Phenothiazines- D2 antagonists

Answer 25

chloropromazine, perphenazine, prochlorperazine

Question 26

non-phenothiazine dopamine antagonists

Answer 26

metoclopramide, haloperidol, olanzapine, trimethobenzamide

Question 27

MOA dopamine antagonists

Answer 27

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

Question 28

MOA metoclopramide

Answer 28

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

Question 29

AE D2 antagonists

Answer 29

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

Question 30

Therapeutic uses of D2 antagonists

Answer 30

idiopathic, PONV, NVP, gastroparesis, CINV and RINV

Question 31

D2 antagonist interactions

Answer 31

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

Question 32

Most common M1 blocker

Answer 32

scopolamine

Question 33

MOA M1 blocker

Answer 33

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

Question 34

AE M1 blocker

Answer 34

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

Question 35

common CB agonists

Answer 35

Nabilone, dronabinol

Question 36

FDA schedule dronabinol

Answer 36

C-III

Question 37

FDA schedule nabilone

Answer 37

C-II

Question 38

CB agonist MOA

Answer 38

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

Question 39

Therapeutic uses CB agonists

Answer 39

CINV, appetite stimulation in select patients

Question 40

AE CB agonists

Answer 40

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

Question 41

Pharmacokinetics CB agonists

Answer 41

dronabinol has one active metabolite, nabilone has several active metabolites

Question 42

CB agonist interactions

Answer 42

CNS depressants, CV agents, sympathomimetics

Question 43

acute CINV onset

Answer 43

<24 hours after chemo

Question 44

chronic CINV onset

Answer 44

>24 hours after chemo

Question 45

Anticipatory CINV

Answer 45

before chemo given

Question 46

High emetogenic regimen for CINV

Answer 46

NK1 antagonist, 5-HT3 antagonist, corticosteroid

Question 47

When should high-emetogenic regimens be given

Answer 47

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

Question 48

Potential high-emetogenic regimen changes

Answer 48

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

Question 49

Moderate-emetogenic drug regimen for CINV

Answer 49

5-HT3 antagonist, corticosteroid

Question 50

When should moderate-emetogenic regimen be given?

Answer 50

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

Question 51

Potential moderate-emetogenic regimen changes

Answer 51

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

Question 52

Low-emetogenic drug regimen for CINV

Answer 52

corticosteroid OR 5-HT3 antagonist OR metoclopramide OR prochlorperazine

Question 53

When should low-emetogenic drug regimens be given?

Answer 53

tx day of prior to chemo

Question 54

Potential low-emetogenic regimen changes

Answer 54

breakthrough and anticipatory as needed

Question 55

minimal-emetogenic drug regimen for CINV

Answer 55

NO routine prophylaxis recommended, provide therapy prn

Question 56

General rule for breakthrough emesis regimen

Answer 56

add one agent from a different class to the current regimen

Question 57

Anticipatory emesis regimen

Answer 57

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

Question 58

Drugs for motion sickness

Answer 58

scopolamine, dimenhydrinate, meclizine

Question 59

Drugs for vertigo

Answer 59

meclizine, cyclizine

Question 60

Drugs for diabetic gastroparesis

Answer 60

metoclopramide

Question 61

Drugs for NVP

Answer 61

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