Anti-nausea And Anti-emetic Drugs (Segars) Flashcards Preview

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Flashcards in Anti-nausea And Anti-emetic Drugs (Segars) Deck (27)
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1
Q

List important receptors in nausea and vomiting:

A
5-HT3 
NK1 (neurokinin)
H1
D2
M1
Cannabinoid 

All should be antagonized with the exception of cannabinoids for anti-nausea/vomiting

2
Q

Dolasetron, granisetron, ondansetron, and palonosetron are what type of drugs?

A

5-HT3 antagonists

3
Q

Aprepitant, fosaprepitant, netupitant, and rolapitant are what type of drugs?

A

NK1 antagonists

4
Q

Chlorpromazine, perphenazine, prochlorperazine are these types of drug:

A

D2 antagonists: Phenothiazines

5
Q

Scopolamine is this type of drug

A

M1 antagonist

6
Q

Dronabinol and nabilone are this type of drug

A

Cannabinoid agonist

7
Q

Diphenhydramine, dimenhydrinate, hydroxyzine, promethazine, meclizine, and cyclizine are these types of drug:

A

H1 antagonists

8
Q

What is the MOA of the “-setron’s”?

A

Block 5-HT3 receptors at vagal nerve terminals and block signal transmission to chemoreceptor trigger zone

Also block 5-HT3 receptors activation after 5-HT3 release from intestinal enterochromaffin cells

9
Q

What is the most worrisome adverse effect of 5-HT3 antagonists?

A

Dose-dependent QT prolongation and torsades

Extreme caution required when using with other QT-prolonging agents (antiarrhythmics) –> Dolasetron very high risk so longer recommended by the FDA for prophylaxis of CINV

10
Q

What are interactions with use of 5-HT3 antagonists?

A

Mainly via CYP450 system
QT prolonging agents
Antiarrhythmics

11
Q

What is the MOA of the “-pitants”?

A

Blockade of NK1 (substance P) receptors in chemoreceptor trigger zone/vomiting center

Peripheral blockade of NK1 receptors located on vagal terminals in gut an additional hypothesis

These are moderate antiemetic agents

12
Q

This H1 receptor antagonist is the initial drug of choice for n/v of pregnancy

A

Doxylamine with B6 (pyridoxine)

13
Q

What is the MOA of H1 receptor antagonists?

A

Block H1 receptors in the vomiting center and vestibular system

THESE AGENTS EXHIBIT VARYING LEVELS OF CENTRAL ANTI-CHOLINGERGIC PROPERTIES AT THE LEVEL OF THE CHEMORECEPTOR TRIGGER ZONE

14
Q

List the classic anti-cholinergic effects of H1 receptor antagonists:

A
Drowsiness (CNS depression)
Dry mouth
Constipation
Urinary retention
Blurred vision
Decrease BP
15
Q

Where do D2 receptor antagonists work?

A

In the CTZ

Metoclopramide also stimulates Ach actions in GI, enhancing GI motility and increases lower esophageal sphincter tone

16
Q

What are adverse effects of Dopamine receptor antagonists (the slide with the star)?

A
Classic anti-cholingeric effects:
Drowsiness
Dry mouth
Constipation
Urinary retention 
Blurred vision
Hypotension (arrhythmias are possible. Usually with larger doses)
Extrapyramidal side effects (dyskinesias)
17
Q

This anti-emetic is a transdermal patch most commonly utilized for motion sickness and is a M receptor antagonist

A

Scopolamine

18
Q

What are adverse effects of scopolamine (slide with the star)?

A
Classic anti-cholinergic effects:
Drowsiness
Dry mouth
Constipation
Urinary retention
Blurred vision
19
Q

These drugs are strong anti-emetic agents reserved for chemo-induced n/v and are scheduled drugs

A

Cannabinoids

Dronabinol (C-3)

Nabilone (C-2)

20
Q

What are therapeutic uses of cannabinoids?

A

Chemo-induced N/V

D/t FDA schedule, commonly reserved for tx-resistant clinical scenarios

21
Q

What is the 3-drug regimen (high-emetogenic regimen) for Chemo-induced N/V?

A

1) 5-HT3 receptor antagonist
2) NK1 receptor antagonist
3) Corticosteroid (dexamethasone)

22
Q

What is the 2 drug regimen (moderate-emetogenic regimen) for chemo-induced N/V?

A

1) 5-HT3 receptor antagonist (Palonosetron)

2) corticosteroid (dexamethasone)

23
Q

What is the 1 drug regimen (low-emetogenic regimen) for chemo-induced N/V?

A

Corticosteroid (dexamethasone)

24
Q

What drug for motion sickness?

A

Scopolamine (patch) or Dimenhydrinate (oral)

25
Q

What drug(s) for vertigo?

A

Meclizine or cyclizine

26
Q

What drug for diabetic gastroparesis?

A

Metoclopramide

27
Q

What drugs for pregnancy induced n/v?

A

Stepped-therapy:

1) 5-HT3 antagonist or histamine antagonist
2) dopamine antagonist
3) steroid or different dopamine antagonist