Antiemetic drugs - Ch. 84 Flashcards

1
Q

What are antiemetic drugs used for?

A

Used to relieve nausea and vomiting
-More difficult to control nausea

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

What are the brain regions responsible for vomiting?

A

Vomiting centre (VC) -coordinates muscles
Chemoreceptor trigger zone (CTZ) -leads to reflex

-Both in the medulla oblongata

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

What neurotransmitters are involved in the vomitting reflex?

A

Histamine (H1 receptors)
ACh (muscarinic receptors)
5-HT (5-HT3 receptors)
Dopamine (DA2 receptors)
Substance P (neurokinin 1 receptors)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

What are some causes of N&V that antiemetics are used for?

A

Cancer chemotherapy-induced (CINV)
Post op with general anesthesia
motion sickness

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

What is the mechanism of action of 5-HT (serotonin) antagonist antiemetics?

A

Block 5-HT3 (serotonin) receptors in CTZ and VC and GI

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Examples of 5-HT (serotonin) antagonists?

A

Odansetron
Dolasetron
Granisetron
Palonosetron

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What types of N&V are 5-HT (serotonin) antagonists used for?

A

CINV
Post op N and V

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

What is the mechanism of action of dopamine (DA) receptor antagonists?

A

Block DA receptors in the CTZ

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What type of N&V is DA receptor antagonists used for?

A

Severe vomiting
e.g, CINV, radiation therapy

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

What are the other indications that DA receptor antagonists are used for?

A

Antipsychotic (neuroleptic) agents
Prokinetic agents (increase GI motility)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Examples of DA receptor antangonists?

A

Chlorpromazine (antipsychotic)
metoclopramide

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

What is the mechanism of action of anticholinergic agents (ACh blockers)?

A

Block ACh receptors in the inner ear labyrinth
Block transmission of nauseating stimuli to VC
Block transmission of nauseating stimuli from the reticular formation to the VC

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Example of ACh blocker?

A

Scopolamine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

What is Scopolamine used for?

A

Motion sickness
-Patch behind ear

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

What is the mechanism of action of antihistamine agents (H1 receptor antagonists)?

A

Block H1 receptors
Prevent cholinergic stimulation in vestibular and reticular areas

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Example of antihistamine antiemetic?

A

Dimenhydrinate (Gravol)
= diphenhydramine + 8-Chlorotheophylline

Diphenhydramine
Cyclizine

17
Q

What adverse effects are associated with Odansetron?

A

Dysrhythmia (long Q-T)

18
Q

What adverse effects are associated with DA antagonists?

A

Movement disorders

19
Q

What adverse effects are associated with Scopolamine?

A

Typical anticholinergic effects

20
Q

What adverse effects are associated with antihistamines?

A

Sedation
Typical anticholinergic effects

21
Q

What is the mechanism of action of glucocorticoids as antiemetics?

A

Unknown mechanism of action as antiemetic

22
Q

Examples of antiemetics glucocorticoids?

A

methylprednisolone
dexamethasone

23
Q

What are antiemetic glucocorticoid commonly used fro?

A

Suppress cancer chemotherapy N&V

24
Q

Example of substance P/neurokinin1 receptor antagonist?

A

Aprepitant

25
Q

What is the mechanism of action of substance P/neurokinin1 receptor antagonist: Aprepitant?

A

Blocks neurokinin1-type receptors in CTZ

-Prolonged duration of action

26
Q

What is aprepitant used for?

A

Postoperative and CI N and V

27
Q

What are Tetrahydrocanabinoids? (THC)

A

Synthetic derivatives of psychoactive substance in marijuana

28
Q

What antiemetics were withdrawn in Canada?

A

Nabilone
Dronabinol

29
Q

What were Nabilone and dronabinol used for?

A

N&V associated with chemotherapy
-second-line drug

30
Q

How should antiemetic drugs be taken?

A

Prophylactically when appropriate

Chemo= 30 min to 3 hours prior to chemo

Motion sickness:
dimenhydrinate = 1h before travel
Scopolamine patch applied 4h before travel