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GI II > Anti-nausea and anti-emetic drugs > Flashcards

Anti-nausea and anti-emetic drugs Flashcards

1
Q

What are the six different families of anti-nausea and anti-emetic drugs?

A

serotonin receptor antagonists, neurokinin receptor antagonists, histamine receptor antagonists, dopamine receptor antagonists, muscarinic receptor antagonists, and cannabinoid receptor agonist

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2
Q

what are the 4 drugs in the serotonin receptor antagonist family?

A

Dolasetron, Granisetron, Ondansetron, and Palonosetron

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3
Q

what are the 5 drugs in the Neurokinin receptor antagonist family?

A

Aprepitant, fosaprepitant, netupitant, fosnetupitant, rolapitant

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4
Q

what are the 6 drugs in the histamine receptor antagonist family?

A

Diphenhydramine, dimenhydrinate, hydroxyzine, promethazine, meclizine, and cyclizine

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5
Q

what are the 4 drugs in the dopamine receptor antagonist family?

A

prochlorperazine, olanzapine, metoclopramide, amisulpride

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6
Q

what is the drug in the muscarinic receptor antagonist family?

A

scopolamine

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7
Q

what are the 2 drugs in the cannabinoid (CB) receptor agonist family?

A

dronabinol and nabilone

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8
Q

what is the MOA of the serotonin (5-HT3) receptor antagonists?

A

they block serotonin type-3 receptors at vagal nerve terminals and block signal transmission to CTZ

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9
Q

what are the therapeutic uses of serotonin (5-HT3) receptor antagonists?

A

there are multiple- this is our go to first line agent

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10
Q

what are the common adverse effects associated with serotonin (5-HT3) receptor antagonists?

A

a few mild to moderate CNS and GI effects

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11
Q

what is the more worrisome adverse effect associated with serotonin (5-HT3) receptor antagonists?

A

dose-dependent QT prolongation (Torsade’s)

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12
Q

which serotonin receptor antagonist has the highest risk of dose dependent QT prolongation and is therefore the most deadly?

A

Dolasetron

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13
Q

what are the pharmacokinetics like of the serotonin receptor antagonists?

A

all agents have short half lives except 2

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14
Q

what 2 serotonin receptor antagonists have longer half lives?

A

Palonosetron and sustained-release formulation of Granisetron

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15
Q

the long half life of Palonosetron and sustained-release formulation of Granisetron make them effective for what?

A

delayed chemotherapy induced nausea and vomiting (CINV) as a single dose

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16
Q

what are the drug interactions associated with serotonin receptor antagonists?

A

interact with antiarrhythmics/ QT- prolonging agents

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17
Q

what is the MOA of neurokinin-1 receptor (substance P) antagonists?

A

blockade of neurokinin (substance P) receptors in CTZ/ VC; peripheral blockade of NK1 receptors located on vagal terminals in gut possibly

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18
Q

what are the therapeutic uses of the neurokinin-1 receptor (substance P) antagonists?

A

chemotherapy-induced N/V; most effective when used in combination with other anti-emetic agents–> so not alone

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19
Q

what are the adverse effects associated with the neurokinin-1 receptor (substance P) antagonists?

A

a few mild to moderate CNS and GI effects

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20
Q

which two drugs in the neurokinin-1 receptor (substance P) antagonist family hace moderate to major active metabolites? and what does this mean?

A

Netupitant/ Rolapitant; they have longer half lives; so your patients feel a prolonged duration of action

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21
Q

if a patient presents with pregnancy, nausea, and vomiting, what is a great first line drug?

A

Doxylamine with pyridoxine (vitamin B6)

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22
Q

what is doxylamine?

A

an antihistamine

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23
Q

what is the MOA of the histamine receptor antagonists?

A

blockade of histamine 1 receptors in VC and vestibular system

24
Q

what are the adverse effects associated with histamine receptor antagonists?

A

classic cholinergic effects

25
Q

what are the classic cholinergic effects? (6)

A

drowsiness(CNS depression), dry mouth, constipation, urinary retention, blurred vision, decreased BP

26
Q

what are the 2 drugs in the histamine receptor antagonist family that are used for motion sickness/vertigo?

A

meclizine and cyclizine

27
Q

what is the MOA of Dopamine receptor antagonists?

A

blockade of dopamine 2 receptors in CTZ

28
Q

what are the MOAs of metoclopramide?

A

it acts as a blockade of dopamine 2 receptors in the CTZ but also stimulates ACh actions in the GI, enhancing GI motility and increases LES tone

29
Q

what is metoclopramide used for?

A

dysmotility use; so in a diabetic patient who isn’t moving their GI things along fast enough

30
Q

what is amisulpride used for?

A

it is newer; it is ONLY used for prevention/treatment of post operative n/v when all other therapies have failed

31
Q

what are the adverse effects for all of the dopamine receptor antagonists?

A

drowsiness

32
Q

what are the adverse effects for prochlorperazine?

A

Dry mouth, constipation, urinary retention, blurred vision

33
Q

what are the adverse effects for amisulpride?

A

hypokalemia, hyperprolactinemia, chills

34
Q

what is scopolamine?

A

A transderm Scop (patch; worn for 72 hours)

35
Q

when is scopolamine most commonly used?

A

for motion sickness; also used in end-of-life care for excessive secretions

36
Q

what is the MOA of muscarinic receptor antagonists?

A

block acetylcholine-stimulated muscarinic receptors in neural pathways from the vestibular nuclei in inner ear to brain stem and from reticular formation to VC; significant anticholinergic properties

37
Q

what are the adverse effects associated with the muscarinic receptor antagonists?

A

the classic anticholinergic effects

38
Q

what are cannabinoids?

A

synthetic preparations of cannabinol (THC in marijuana); synthetic cannabinoids are FDA-scheduled (controlled) medications (abuse potential)

39
Q

what is the MOA of cannabinoids?

A

stimulation of cannabinoid receptors; exert signal transduction effects through G-protein coupled receptors resulting in decreased excitability of neurons- minimizing serotonin release from vagal afferent terminals

40
Q

what are the therapeutic uses of cannabinoids?

A

chemotherapy-induced n/v; due to FDA scheduling, these agents are often reserved for treatment-resistant clinical scenarios; appetite stimulation in select (anorexic) patients due to severe disease (eg cancer or AIDS)

41
Q

chemotherapy-induced n/v: acute n/v timing?

A

occurring less than 24 hours after chemo given

42
Q

chemotherapy-induced n/v: chronic n/v timing?

A

occurring more than 24 hours after chemo is given

43
Q

chemotherapy-induced n/v: anticipatory n/v timing?

A

occurring before chemo given, customarily in non-treatment naive patients

44
Q

a high-emetogenic regimen is how many drugs?

A

4

45
Q

what anti-nausea and anti-emetic drugs are involved in a high-emetogenic regimen?

A
  1. D2 antagonist (olanzapine) 2. NK1 receptor antagonist 3. 5-HT3 receptor antagonist 4. Corticosteroid (dexamethasone)
46
Q

how do you treat a high-emetogenic regimen?

A

give treatment day of (prior to) chemotherapy, then a 3-drug treatment for 3 days after chemotherapy

47
Q

what happens if your treatment for a high-emetogenic regimen is resistant?

A

you can add a cannabinoid (so now 5 drugs)

48
Q

a moderate-emetogenic regimen has how many drugs?

A

3

49
Q

what anti-nausea and anti-emetic drugs are involved in a moderate-emetogenic regimen?

A
  1. NK1 receptor antagonist 2. 5-HT3 receptor antagonist 3. Corticosteroid (dexamethasone)
50
Q

how do you treat a moderate-emetogenic regimen?

A

give treatment regimen day of (prior to) chemotherapy, then 2-drug treatment for 2 days after chemotherapy

51
Q

what happens if your treatment for a moderate-emetogenic regimen is resistant?

A

you can add D2 antagonist (olansapine) (so now 4 drugs)

52
Q

a low-emetogenic regimen has how many drugs?

A

1

53
Q

how do you treat a low-emetogenic regimen?

A

give treatment regimen day of (prior to) chemotherapy; may repeat daily for multi-day anticancer therapy

54
Q

a minimal-emetogenic regimen has how many drugs?

A

0-drug regimen; no routine prophylaxis therapy recommended

55
Q

what 3 drugs can treat motion sickness?

A

scopolamine (patch), dimenhydrinate, or meclizine

56
Q

what 2 drugs can treat vertigo?

A

meclizine or cyclizine

57
Q

what drug can treat diabetic gastroparesis?

A

metoclopramide

GI II (20 decks)

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