Brainscape's Knowledge GenomeTM


Top Flashcards (Certified)
All Flashcards

Laxatives, Anti-Diarrheals, Anti-Emetics, and Pro-Kinetic Agents 1 and 2 > Anti-emetic Drugs and Prokinetic Drugs > Flashcards

Anti-emetic Drugs and Prokinetic Drugs Flashcards

(51 cards)

Start Studying
1
Q

What are Anti-emetic Drug physiology?

A

High concentrations of M1, H1, and Neurokinin 1 and serotonin (5-HT3) receptors have been identified in vomiting center.

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

How is vomiting controlled?

A

Chemoreceptor trigger zone (CTZ) and vomiting center is where stimuli are integrated.

Stimulation from higher centers, distension of the stomach and GI tract, and vestibular feedback

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

Pathophysiology Aspects of Chemotherapy Induced Nausea and Vomiting

A

Chemotherapy agents act on Entero-chromaffin cell of the GI tract. Which then causes there to be serotonin release. Serotonin binds to the 5-HT3, which then causes vomiting.

Chemotherapy then causes area postrema -> causes there to be substance P release that attaches to NK1.

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

Anti-histamine anticholinergic antagonists

A

weak anti-emetic activity.

work on muscarinic and histamine receptors in the vomiting center and the vestibular system –> stimulates nausea and vomiting.

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

What are the Anti-histamine and anticholinergic antagonists ?

A

scopolamine, meclizine, and dimenhydrinate.

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

Scopolamine

A

Muscarinic receptor antagonist.

Blocking the M1 receptors in the CNS.

Prevents motion sickness.

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

Clinical Applications of Scopolamine

A

Post-operative nauea/vomiting, motion sickness.

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

Adverse Reactions

A

Exacerbate psychosis and somnolence, and xerostomia `

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

Meclizine

A

MOA: H1 antihistaminic agent with minimal anticholinergic properties that causes less sedation.

Inhibits histamine and anti-cholinergic pathways

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

Clinical Applications

A

Nausea/vomiting
Pregnancy
motion sickness

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

Dimenhydrinate

A

MOA: inhibits histamine and anti-cholinergic pathways.

Clinical Applications: chemotherapy-induced nausea/vomiting

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

H1 anti-histamine agent do not have —-

A

significant action at CTZ

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

Dopamine receptor antagonists

A

anti-psychotics
strong anti-emetics
D2 receptor antagonists

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

What are dopamine receptor antagonists?

A 
Prochlorperazine 
promathazine 
droperidol 
metoclopramide 
domperidone
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Prochlorperazine + Promethazine

A

Blocks Dopaminergic D1 and D2 receptors in the brain.

Inhibit peripheral transmission to the vomiting center.

anti-cholinergic and antihistamine activity

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

Adverse Reactions of Prochlorperazine + Promethazine

A

Extrapyrimidal effects.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Promethazine

A

D1 and D2 receptors in the brain, including CTZ –> inhibits peripheral transmission to the vomiting center.

anti-cholinergic and anti-histaminic activity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Droperidol MOA, Clinical Applications, Adverse Reactions, Contraindications

A

Blocks dopaminergic receptors in the CTZ.

Clinical Applications: post-operative nausea/vomiting. Has not been/limited use for chemotherapy induced also.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

Metoclopramide

A

D2 receptor antagonist without antipsychotic activity

Enhancing action of acetylcholine at muscarinic nerve endings in the gut

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Metoclopramide Clinical Applications

A

Nausea/vomiting and gastric gastroparesis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Adverse Reactions of Metoclopramide

Study These Flashcards
A

Fatigue, somnolence, Extrapyrimidal side effects, headache

22
Q

Contraindications of Metoclopramide

Study These Flashcards
A

Tardive dyskinesia

23
Q

Domperidone

Study These Flashcards
A

MOA: D2-receptor antagonist without anti-psychotic activity

Act centrally by blocking dopamine D2 receptor in the CTZ

Clinical Applications: Prevention of GI symptoms.

24
Q

Serotonin 5-HT3 receptor anagonists are:

Study These Flashcards
A

Ondansetron, dolasetron, granisetron, palonosetron

25
What are serotonin 5-HT3 receptors antagonists useful for?
They are useful acute pahse chemotherapy induced vomiting. Post-operative nausea/vomiting, and radiation induced nausea/vomiting
26
5-HT3 serotonin receptor antagonists are combined with:
they are combined with cortico-steroids
27
Ondansetron:
MOA: Blocks serotinin by acting peripherally on vagal nerve terminals and centrally on CTZ. Clinically Applications: chemotherapy induced nausea/vomiting, post-operative nausea/vomiting acute radiation induced nausea/vomiting
28
Ondanserton adverse effects:
QT interval prolongation
29
Dolasetron and Granisetron
Dolasetron + MOA: Peripherally acts on vagal nerve and centrally on CTZ. Clinical Applications: Chemotherapy induced nausea/vomiting QT interval prolongation is the main side effect for dolasetron. For granisetron, it is constipation, headache, fatigue, progressive ileus, ect
30
Palonosetron
Palonosetron is same basically as all serotonin inhibitors. It is useful in prevention of PONV, CINV, increased efficacy in preventing acute and delayed CINV. better than ondansetron and dolasetron. petter than granisetron. Adverse effect: less effect on QT interval
31
What is cannabinoid hyperemesis syndrome?
hyper-emesis due to chronic cannabis use
32
Dronabilol and nabilone are
synthetic analogs of THC that are used as second line agents to CINV
33
Dronabilol MOA and Clinical Applications
breakthrough CINV chemotherapy induced nausea and vomiting
34
Nabilone
Inhibits the vomiting center through the stimulation of CB1 subtype of cannabinoid receptors chemotherapy induced nausea/vomiting. Breakthrough CINV
35
Benzodiazepines
Weak anti-emetics and are used to prevent anxiety or anticipatory nausea/vomiting
36
Alprazolam and Lorazepam
MOA: binds to GABA receptors and causes calming effect and lowers level of anxiety GABA-A receptors.
37
Clinical applications of of Alprazolam and Lorazepam
high level of anxiety and anticipatory nausea/vomiting
38
Neurokinin 1 -receptor antagonists
Substance P is the principal NT that activates neurokinin 1 receptors in the CNS. Acute phase of CINV is thought to be mediated by serotonin and Substance P, where Substance P is believed to be primary mediator of delayed phase. No affinity for serotonin, dopamine, corticosteroid receptors Useful for delayed phase of CNV combined with dexamethasone and a 5-ht3 receptor antagonist , N1 receptor antagonists Standard care for prevention of CINV in both adults and children receiveing highly emetogenic chemotherapy Useful in prophylaxis treatment of chemotherapy induced nausea/vomiting and post-operative nausea. All may be given before chemotherapy Day 1 Apretitant,
39
Aprepitant
MOA: inhibits the neurokinin 1 receptor, augmenting the anti-emetic activity of 5 -HT3 receptor antagonists and corticosteroid to inhibit the acute and delayed phase of chemo induced emesis
40
Clinical Application of Apretitant
used for CINV and post-operative nausea/vomiting (PONV)
41
What is Fosaprepitant
Fosaprepitant is IV formulation of aprepitant.
42
What are apretitant and fosaprepitant inhibitors of:
CYP3A4
43
Dose of dexamethasone should be ------ when used concurrently as an anti-emetic
should be decreased when used concurrently as an anti-emetic
44
Netupitant is---- inhibitor Rolapitant is ------ inhibitor
Neutpitant is a CYP-450 inhibitor (dexamethasone should be decreased) Rolapitant is a ---- CYP-2D6 inhibitor, and dexamethasone shoudn't be decreased
45
Prokinetic Agents Purpose
Promote the GI transit and speed gastric emptying by enhancing coordinated propulsive motility. Release of excitatory neurotransmitters at nerve muscle junction. Used to pre-op the empty gut, gastroparesis, GERD as anti -emetic .
46
Bethanechol
MOA: not hydrolyzed by AChE Strong muscarinic receptor antagonist (M2 and M3) no nicotinic actions. Pharmacological Effects: increase motility, limited distribution to the CNS Clinical Applications: Stimulate GI smooth musclemotor activity
47
Neostigmine
MOA: Indirect gastric stimulant/inhibits AChE--> increases ACh, stimultes peristalsis via M2 receptors Clinical Applications: colonic pseudo obstruction.
48
Metoclopramide
Dopamine has inhibitory effect on motility, resulting from suppresses ACh releaser from myenteric motor neurons. These are D2 receptor antagonists. Accelerate gastric emptying (emergency surgery, ect), dyspepsia, GERD Adverse Effect: tardive dyskinesia
49
Domperidone
same as metoclopramide
50
Motilin and Macrolide Antibiotics
Macrolide antibiotics are motilin receptor agonists. Clinical: IV pre-op to empty gut for gastroparesis
51
Prucalopride and Tegaserod
5-HT4 receptor agonists. Stimulate peristaltic reflex, intestinal secretions, and GI motility Prucalopride is used to treat Chronic Idiopathic Constipation in adults, and OIC in chronic pain patients Tegaserod is for IBS-C

Laxatives, Anti-Diarrheals, Anti-Emetics, and Pro-Kinetic Agents 1 and 2 (5 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2025 Bold Learning Solutions. Terms and Conditions