Antiemetics- Fitz

Question 1

When is IPECAC particularly dangerous?

Answer 1

If suspected poison is:
Corrosive
Petroleum distillate
Rapidly-acting convulsant

Question 2

Where is CTZ found? Is it inside the BBB?

Answer 2

CTZ is found in brainstem but it is OUTSIDE of the blood brain barrier

Question 3

Are antiemetics more effective at preventing vomiting or stopping emesis once its started?

Answer 3

Preventing vomiting

Question 4

What are the only truly effective agents for cancer chemotherapy-induced emesis?

Answer 4

5HT3 antagonists = “SETRONS”

Question 5

Which agent is most effective for motion sickness?

Answer 5

Scopolamine

Question 6

How must scopolamine be administered?

Answer 6

As a TRANSDERMAL PATCH

Otherwise has high incidence of anticholinergic side effects

Question 7

MOA of scopolamine?

Answer 7

Antimuscarinic

Inhibits muscarinic receptors in the cerebellum

Rapidly and fully distributes to CNS

Good for MOTION SICKNESS

Must be given as transdermal patch

Question 8

Use for activated charcoal?

Answer 8

Binds toxins

Absorbs many drugs/poisons due to its large surface area

Question 9

Use for polyethylene glycol electrolyte solution?

Answer 9

Cathartic

May hasten removal of toxins and reduce absorption

Question 10

What things should you NOT use activated charcoal for?

Answer 10

Does not bind
Iron
Lithium
Potassium

Binds alcohol and cyanide poorly

Question 11

What kind of drug is IPECAC?

Answer 11

Emetic - local GI irritant effect as well as acting on CTZ

Question 12

Which antiemetic is best used in pregnancy?

Answer 12

?

Question 13

When is an NK1 antagonist used?

Answer 13

Prevention of acute and delay phase of chemotherapy induced nausea and vomitting

Question 14

What is typically given in combination with NK1 antagonist?

Answer 14

5HT3 antagonist and dexamethasone

For chemotherapy induced vomiting

Question 15

What is a specific side effect of NK1 antagonist?

Answer 15

Drug-drug interactions!
Metabolized by CYP3A4

Decreases metabolism/increases toxicity of:
Warfarin
Cisapride!
Some chemotherapy agents

Question 16

What three classes of antiemetics MUST cross BBB to be effective?

Answer 16

H1 receptor antagonists
NK1 receptor antagonists
Cannabinoids

Question 17

What three classes of antiemetics are good for chemotherapy induced emesis?

Answer 17

5HT3 receptor antagonists
NK2 receptor antagonists
Corticosteroids

Question 18

“Setrons” MOA

Answer 18

5HT3 receptor antagonists

Question 19

Droperidol

Answer 19

D2 receptor antagonist

Question 20

Metoclopramide

Answer 20

D2 receptor antagonist

Question 21

Prochlorperazine

Answer 21

D2 receptor antagonist

Question 22

Promethazine

Answer 22

D2 receptor antagonist

Question 23

Thiethylperazine

Answer 23

D2 receptor antagonist

Question 24

Scopolamine

Answer 24

M1 receptor antagonist

Question 25

Dimenhydrinate

Answer 25

H1 receptor antagonist Needs to Cross BBB Motion sickeness

Question 26

Diphenhydramine

Answer 26

H1 receptor antagonist Needs to cross BBB Motion sickness

Question 27

Meclizine

Answer 27

H1 receptor antagonist Needs to cross BBB Motion sickness

Question 28

Aprepitant

Answer 28

NK1 receptor antagonist Needs to cross BBB Chemotherapy

Question 29

Fosaprepitant

Answer 29

NK1 receptor antagonist Needs to cross BBB Chemotherapy

Question 30

Dronabinol

Answer 30

Cannabinoid | Needs to cross BBB

Question 31

Nabilone

Answer 31

Cannabinoid | Needs to cross BBB

Question 32

Dexamethasone

Answer 32

Corticosteroid Unknown MOA for antiemesis Chemotherapy

Question 33

Methylprednisolone

Answer 33

Cortiocosteroid Unknown MOA for antiemesis Chemotherapy

Question 34

Where do opioids generally act as antiemetics?

Answer 34

CTZ (outside BBB)

Question 35

Which two classes primarily act in the CTZ?

Answer 35

D2 receptor antagonists | Opioids

Question 36

Which class of antiemetics act mostly on the GI tract?

Answer 36

5HT3 receptor antagonists

Question 37

Dolasetron

Answer 37

5HT3 receptor antagonist

Question 38

Granisetron

Answer 38

5HT3 receptor antagonist

Question 39

Ondansetron

Answer 39

5HT3 receptor antagonist

Question 40

Palonosetron

Answer 40

5HT3 receptor antagonist