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GI II > Anti Nausea and Anti emetic durigs > Flashcards

Anti Nausea and Anti emetic durigs Flashcards

1
Q

what are the 5 receptors that all play a factor in Nausea/Vomiting

A 
5-HT3Serotonin type-3
H1Histamine type-1
M1Muscarinic type-1
D2Dopamine type-2
NK1Neurokinin-1 (Substance P)
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2
Q

where is the vomiting center and chemoreceptor trigger zone located?

A

Vomiting center: Nucleus of tractus solitarius

Chemoreceptor trigger zone: area postrema

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3
Q

what steroid is used for Nausea and vomiting

A

Glucocorticoidsteroid: Dexamethasone

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4
Q

What antipsycotic is used for nausea and vomitting

A

Benzodiazepines:

Alprazolam/Lorazepam

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5
Q

what are the serotonin 5-HT3 receptor antagonists and what suffix is used

A

Dolasetron
Granisetron
Ondansetron
Palonosetron

“setron”

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6
Q

what is Alosetron only indicated for?

A

Irritable bowel syndrome- diarrhea

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7
Q

what is the mechanism of action pf the serotonin 5-HT3) receptor antagonists?

A

block serotonin type-3 receptors at vagal nerve terminals & blocks signal transmission to CTZ

–blocks serotonin-receptor activation after serotonin release from intestinal enterochromaffin cells

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8
Q

Therapeutic uses of Serotonin receptor antagonists

A 
[multiple etiologies of N/V]
–Chemotherapy-induced N/V (CINV)
–Radiation-induced N/V (RINV)
–Post-operative N/V (PONV)
–N/V of Pregnancy (NVP)
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9
Q

Adverse effects of Serotonin receptor antagonists

A

Serotonin Syndrome (use with other 5-HT-affecting drugs)

Dose-dependent QT prolongation (Torsade’s)
•Extreme caution required when using with other QT-prolonging agents (e.g., antiarrhythmics) or in patients with electrolyte imbalances (e.g., hypokalemia or hypomagnesemia)
•Dolasetron high risk; no longer recommended for CINV prophylaxis

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10
Q

what serotonin antagonist has a much longer half life ta all the others?

A

All agents have short half-lives, except Palonosetron & sustained-release formulation of Granisetron(SQ) (much longer; 24+ hours)

•Long half-life makes Palonosetron & 2 branded-Granisetronagents (Sancuso(patch) & Sustol(SQ injection)) effective for delayed-CINV as a single dose

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11
Q

what are the drugs in the Neurokinin NK1 receptor antagonists?

A 
Aprepitant
Fosaprepitant
Netupitant
Fosnetupitant
Rolapitant

fos means prodrug

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12
Q

what NK1 antagonist must be in a combonation with another drug?

A

Netupitant and Fosnetupitant must be in combination with Palonosetron (serotonin receptor antgonist

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13
Q

what is the indicaftion of NK1 receptor antagonist?

A

Moderate antiemetic agents
Blockade of
Neurokinin1(Substance P) receptors in CTZ/VC
–Peripheral blockade of NK1receptors located on vagal terminals in gut an additional hypothesized action

Chemotherapy-induced N/V (CINV)
–Most effective when used in combination with a glucocorticosteroid and 5-HT3antagonist

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14
Q

what is the only NK1 receptor antagonist used in prophylaxis of post operative N/V

A

only aprepitant

Given up to 3 hours prior to anesthesia induction

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15
Q

what are the adverse effects of NK1 receptor antagonists?

A
  • GI(dyspepsia/constipation/diarrhea)

* CNS(dizziness/fatigue/somnolence)

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16
Q

what two NK1 receptor antagonist have longer half lives than the others

A

Netupitant/Rolapitant

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17
Q

what are all the Histamine H1 receptor antagonists?

A 
Diphenhydramine
Dimenhydrinate
Hydroxyzine
Promethazine
Meclizine
Cyclizine
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18
Q

what is the initial therapy for Nausea and vomiting in pregnancy

A

Doxylamine with Pyridoxine B6

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19
Q

what antiemetic agents do Histamine receptor antagonists block?

A

Weak antiemetic agents

–Originally developed for other indications (antihistamine, motion sickness), but also found useful for N/V (PONV)

20
Q

where do the Histamine H1 receptors block and what other varying levels do they cause

A

block histamine type-1 receptors in VC and vestibular system

•Agents exhibit varying levels of central anticholinergic properties at level of CTZ

21
Q

what are the classic adverse effects of histamine receptor antagonists and what are they identical to?

A
  • Drowsiness (CNS depression)
  • Dry mouth
  • Constipation
  • Urinary Retention
  • Blurred vision
  • Decrease BP

classic anticholinergic effects

22
Q

what are the only indications for meclizine and cyclizine

A

these are Histamine 1 receptor antagonists

Motion sickness and vertigo

23
Q

what are the Dopamine D2 receptor antagonists?

A

Phenothiazine’s:
Chlorpromazine
Perphenazine
Prochlorperazine

Metoclopramide

24
Q

what type of antiemetic agents are dopamine receptor antagonists and what are their mechanism of action

A

Weak-to-Moderate antiemetic agents
–Some agents originally developed/utilized as anti-psychotics

block dopamine type-2 receptors in CTZ
•Agents exhibit varying levels of anticholinergic properties; affect other receptors (histamine, muscarinic, adrenergic receptors (alpha))

25
Q

what are the other indications of Metoclopramide?

A

Metoclopramidealso stimulates acetylcholine (ACh) actions in GI, enhancing GI motility & increases lower esophageal sphincter tone

used for dysmotility

26
Q

what are the adverse effects of Dopamine receptor antagonists and what does tthat mimic

A 
•Drowsiness (CNS depression)
•Dry mouth
•Constipation
•Urinary Retention
•Blurred vision
•Hypotension
–Arrhythmias & Extrapyramidal SE’s (EPS) are possible; usually seen with larger (psychiatric) doses

Classic Anticholinergic effects

27
Q

what are the Therapeutic uses of Dopamine receptor antagonists?

A
  • Idiopathic, mild N/V (e.g., infections, opiates & migraines)
  • Post-operative N/V (PONV)
  • N/V of Pregnancy (NVP)

•Gastroparesis/Dysmotility
–specifically metoclopramide

•Chemotherapy-induced N/V (CINV) & Radiation-induced N/V (RINV)
–As single agents, only weak-moderate antiemetic activity; olanzapine used in combination with other agents for CINV/RINV

28
Q

What is the only Muscarinic M1 receptor antagonist?

A

Scopolamine

29
Q

what is Scopolamine used for, length of use, and what is its mechanism of action

A

•Scopolamine
–TransdermScop(patch; worn for 72 hours)

•Weakantiemetic agents
–Most commonly utilized for motion sickness
–Also utilized in end-of-life care for excessive secretions

  • Blockade of Muscarinic receptors
  • Block acetylcholine-stimulated muscarinic receptors in neural pathways from the vestibular nuclei in inner ear to brain stem and from reticular formation to VC
30
Q

Adverse effects of Muscarinic receptor blockers?

A
  • Drowsiness (CNS depression)
  • Dry mouth
  • Constipation
  • Urinary Retention
  • Blurred vision

Classic Anticholinergic effects

31
Q

what are the drugs that are in the Cannabinoid Agonst

A

Dronabinol

Nabilone

32
Q

what are Cannabinoids and what are their mechanism of action?

A

Synthetic preparations of cannabinol (constituent of cannabis sativa; delta-9-tetrahydrocannabinol (delta-9-THC)in marijuana)

•Strong antiemetic agents
–Reserved for treatment-resistant CINV

•Stimulation of cannabinoid receptors
–Stimulates predominantly-central (CB1) and predominantly-peripheral (CB2) cannabinoid receptors in VC/CTZ

•Exert signal transduction effects through G-protein-coupled receptors, resulting in decreased excitability of neurons
–minimizing serotonin (5-HT3) release from vagal afferent terminals

33
Q

Since Cannabinoids are FDA controlled what are some of its limitations

A

Synthetic cannabinoids are FDA-scheduled (Controlled) medications (due to abuse potential)
–[Limits on quantity/refill #/lifespan of Rx/etc…]

34
Q

What are the Therapeutic uses of Cannabinoids

A

•Chemotherapy-induced N/V (CINV)
–Due to FDA-scheduling, commonly reserved for treatment-resistant clinical scenarios
–Can be used in combination with other agents (add on)

•Appetite stimulation in select (anorexic) patients due to severe disease (e.g., cancer or AIDS)

35
Q

What are some interactions of Cannabinoids

A

Caution in use with other CNS depressant’s & cardiovascular agent’s & sympathomimetic’s

36
Q

what are some of the Adverse effects of Cannabinoids

A 
Adverse Effects (dose-related):
•Euphoria/Irritability (emotional lability)
•Vertigo (dizziness)
•Sedation/Drowsiness
•Impaired cognition/memory
•Alterations in perception of reality (distortions in perception and sense of time; hallucinations)
•Xerostomia (dry mouth)
•Sympathomimetic (increased HR/BP)
•Appetite stimulation
37
Q

Difference between Dronabinol and Nabilone

A

•Dronabinol-a large first-pass effect and metabolized to one active metabolite

•Nabilone is metabolized to several active metabolites
–Both have a short-time to onset of activity and long duration of action (24-36 hours); Nabilone fewer doses/day

38
Q

what are the differences between acute, chronic, and anticipatory N/V and what should proper therapy focus on

A

•Acute N/V
–occurs <24 hours after chemo given

•Chronic N/V
–occurs >24 hours after chemo given

•Anticipatory N/V
–occurs before chemo given, customarily in non-treatment-naïve patients

Proper therapy focuses on the prevention

39
Q

What would be a High Emetogenic Regimen be?

A

•High-Emetogenic Regimen (3-drug regimen)

  1. NK1receptor antagonist
  2. 5-HT3receptor antagonist
  3. Corticosteroid (Dexamethasone)

•Give treatment regimen day of (prior to) chemotherapy (for acute N/V) and for 3 days after chemotherapy (for delayed N/V)

A.May add olanzapine (D2antagonist) (increase to 4-drug regimen)

B.May add cannabinoid in treatment-resistance(increase to 4-drug regimen)

C.Provide therapy for breakthrough N/V for all patients

D.Provide therapy for anticipatory N/V, as needed

40
Q

what would a Moderate Emotogenic regimen be?

A

•Moderate-Emetogenic Regimen (2-drug regimen)

  1. 5-HT3receptor antagonist (palonos/granisSQ)
  2. Corticosteroid (Dexamethasone)

•Give treatment regimen day of (prior to) chemotherapy (for acute N/V) and for 2 days after chemotherapy (for delayed N/V)

A.May add NK1antagonist or olanzapine, if necessary (increase to 3-drug regimen

B.May add cannabinoid in treatment-resistance(increase to 4-drug regimen after going up to 3-drug regimen)

C.Provide therapy for breakthrough N/V for all patients

D.Provide therapy for anticipatory N/V, as needed

41
Q

What would a Low-Emetogenic Regimen be?

A

•Low-Emetogenic Regimen (1-drug regimen)

  1. Corticosteroid (Dexamethasone),or
  2. 5-HT3receptor antagonist, or
  3. Metoclopramide,or
  4. Prochlorperazine,or

•Give treatment regimen day of (prior to) chemotherapy (for acute N/V)

A.Provide therapy for breakthrough N/V for all patients

B.Provide therapy for anticipatory N/V, as needed

42
Q

What would a Minimal Emetogenic Regimen Be?

A

•Minimal-EmetogenicRegimen (0-drug regimen)

1.No routine prophylaxis therapy recommended

A.Provide therapy for breakthrough N/V for all patients

B.Provide therapy for anticipatory N/V, as needed

43
Q

What drug to give during Motion sickness?

A

Scopolamine (patch) or Dimenhydrinate or Meclizine

44
Q

what drug to give for Vertigo

A

Meclizineor Cyclizine

45
Q

what drug to give for Diabetic Gastroparesis

A

Metoclopramide

46
Q

What drug to give for Pregnancy induced stepped therapy N/V

A
  1. Vitamin B6 or Histamine Antagonist (w/ Vit. B6) or5-HT3Antagonist
  2. Dopamine Antagonist
  3. Steroid or Different Dopamine Antagonist

GI II (5 decks)

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