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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

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.

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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

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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.

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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.

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5
Q

What are the Anti-histamine and anticholinergic antagonists ?

A

scopolamine, meclizine, and dimenhydrinate.

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6
Q

Scopolamine

A

Muscarinic receptor antagonist.

Blocking the M1 receptors in the CNS.

Prevents motion sickness.

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7
Q

Clinical Applications of Scopolamine

A

Post-operative nauea/vomiting, motion sickness.

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8
Q

Adverse Reactions

A

Exacerbate psychosis and somnolence, and xerostomia `

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9
Q

Meclizine

A

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

Inhibits histamine and anti-cholinergic pathways

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10
Q

Clinical Applications

A

Nausea/vomiting
Pregnancy
motion sickness

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11
Q

Dimenhydrinate

A

MOA: inhibits histamine and anti-cholinergic pathways.

Clinical Applications: chemotherapy-induced nausea/vomiting

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12
Q

H1 anti-histamine agent do not have —-

A

significant action at CTZ

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13
Q

Dopamine receptor antagonists

A

anti-psychotics
strong anti-emetics
D2 receptor antagonists

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14
Q

What are dopamine receptor antagonists?

A 
Prochlorperazine 
promathazine 
droperidol 
metoclopramide 
domperidone
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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

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16
Q

Adverse Reactions of Prochlorperazine + Promethazine

A

Extrapyrimidal effects.

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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

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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.

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19
Q

Metoclopramide

A

D2 receptor antagonist without antipsychotic activity

Enhancing action of acetylcholine at muscarinic nerve endings in the gut

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20
Q

Metoclopramide Clinical Applications

A

Nausea/vomiting and gastric gastroparesis

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21
Q

Adverse Reactions of Metoclopramide

A

Fatigue, somnolence, Extrapyrimidal side effects, headache

22
Q

Contraindications of Metoclopramide

A

Tardive dyskinesia

23
Q

Domperidone

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:

A

Ondansetron, dolasetron, granisetron, palonosetron

25
Q

What are serotonin 5-HT3 receptors antagonists useful for?

A

They are useful acute pahse chemotherapy induced vomiting. Post-operative nausea/vomiting, and radiation induced nausea/vomiting

26
Q

5-HT3 serotonin receptor antagonists are combined with:

A

they are combined with cortico-steroids

27
Q

Ondansetron:

A

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
Q

Ondanserton adverse effects:

A

QT interval prolongation

29
Q

Dolasetron and Granisetron

A

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
Q

Palonosetron

A

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
Q

What is cannabinoid hyperemesis syndrome?

A

hyper-emesis due to chronic cannabis use

32
Q

Dronabilol and nabilone are

A

synthetic analogs of THC that are used as second line agents to CINV

33
Q

Dronabilol MOA and Clinical Applications

A

breakthrough CINV

chemotherapy induced nausea and vomiting

34
Q

Nabilone

A

Inhibits the vomiting center through the stimulation of CB1 subtype of cannabinoid receptors

chemotherapy induced nausea/vomiting.

Breakthrough CINV

35
Q

Benzodiazepines

A

Weak anti-emetics and are used to prevent anxiety or anticipatory nausea/vomiting

36
Q

Alprazolam and Lorazepam

A

MOA: binds to GABA receptors and causes calming effect and lowers level of anxiety

GABA-A receptors.

37
Q

Clinical applications of of Alprazolam and Lorazepam

A

high level of anxiety and anticipatory nausea/vomiting

38
Q

Neurokinin 1 -receptor antagonists

A

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
Q

Aprepitant

A

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
Q

Clinical Application of Apretitant

A

used for CINV and post-operative nausea/vomiting (PONV)

41
Q

What is Fosaprepitant

A

Fosaprepitant is IV formulation of aprepitant.

42
Q

What are apretitant and fosaprepitant inhibitors of:

A

CYP3A4

43
Q

Dose of dexamethasone should be —— when used concurrently as an anti-emetic

A

should be decreased when used concurrently as an anti-emetic

44
Q

Netupitant is—- inhibitor

Rolapitant is —— inhibitor

A

Neutpitant is a CYP-450 inhibitor (dexamethasone should be decreased)

Rolapitant is a —- CYP-2D6 inhibitor, and dexamethasone shoudn’t be decreased

45
Q

Prokinetic Agents Purpose

A

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
Q

Bethanechol

A

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
Q

Neostigmine

A

MOA: Indirect gastric stimulant/inhibits AChE–> increases ACh, stimultes peristalsis via M2 receptors

Clinical Applications: colonic pseudo obstruction.

48
Q

Metoclopramide

A

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
Q

Domperidone

A

same as metoclopramide

50
Q

Motilin and Macrolide Antibiotics

A

Macrolide antibiotics are motilin receptor agonists.

Clinical: IV pre-op to empty gut for gastroparesis

51
Q

Prucalopride and Tegaserod

A

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)

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