Antiemetics Flashcards

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1
Q

Where does the signal to vomit come from?

What events happen in order to vomit?

A

Vomiting centre in medulla

  1. Nausea, Salivation, Sweating
  2. Retrograde peristalsis
  3. Deep inspiration
  4. Closure of glottis
  5. Ab muscles contract
  6. Lower oesophageal sphincter relaxes
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2
Q

List 4 things that can trigger the Chemoreceptor Trigger Zone (CTZ) and lead to vomiting?

A
  • Sensory afferents via midbrain
  • Vestibular nuclei
  • Visceral afferents from gut
  • Direct triggers
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3
Q

Where is the CTZ?

A

In the Area Postrema, on the floor of the 4th ventricle

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4
Q

List 2 types of Antiemetic agent acting on the Vestibular Nuclei

What are they usually used for?

A
  • Muscarinic receptor antagonists
  • H1 receptor antagonists
  • Treating motion sickness
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5
Q

What kind of drug is Hyoscine hydrobromide?

This drug’s targets are where?

A

A muscarinic receptor antagonist

(mAChRs are the targets)

  • Vestibular nuclei
  • CTZ
  • All over body as part of ParaS system
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6
Q

List 5 ADRs of Muscarinic receptor antagonists

A
  • Sedation
  • Memory problems
  • Glaucoma
  • Dry mouth
  • Constipation
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7
Q

List 3 people who Hyoscine hydrobromide would be good for?

A
  • Bowel obstruction
  • Motion sickness
  • People who can’t take tablets
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8
Q

The following drugs are what kind of drug?

  • Cyclizine
  • Levomepromazine
  • Cinnirazine
  • Promethazine
  • Dipenhydramine
A

H1 receptor antagonists

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9
Q

Where do H1 receptor antagonists work?

A
  • Vestibular nuclei

- CTZ (inhibition of histaminergic signals from vestibular system)

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10
Q

Lit 4 ADRs of H1 receptor antagonists

A
  • Sedation
  • Excitation
  • Cardiac toxicity
  • Antimuscarinic (Dry mouth, constipation, urinary retention)
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11
Q

For what patient groups are H1 receptor antagonists good and not good?

Give examples

A

Good for;

  • Motion sickness
  • Promethazine (Morning sickness in pregnancy)

Not good for;
- Cyclizine: Elderly women and children (makes them disoriented and confused)

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12
Q

List 2 types of Antiemetic agent acting on the Visceral afferents from the gut

A
  • 5HT3 (Serotonin) antagonists

- SOME D2 receptor antagonists

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13
Q

Where is most of the body’s Serotonin found and what cells is it made by?

What does Serotonin do here?

A
  • 95% found in gut, made by ECL cells
  • Regulates appetite
  • In response to ParaS stimulation, excites Enteric neurones-> Increased gut secretions and motility (except stomach motility)
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14
Q

What do 5HT3 Receptor Antagonists do Peripherally and Centrally?

Who are these drugs good for?

A

Peripherally;
- Reduced GI motility and secretions

Centrally;
- Inhibits CTZ

Almost everyone, often 1st line treatment

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15
Q

What kind of drugs are Ondansetron, Granisetron and Palonosetron?

List 5 ADRs of these drugs

A

5HT3 receptor antagonists

Uncommon;

  • Constipation
  • Headache
  • Elevated liver enzymes
  • Long QT Syndrome
  • Extra-pyramidal effects (Dystonia, Parkinsonism)
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16
Q

What kind of drugs are Metoclopramide and Domperidone?

What are 2 ADRs of this class of drugs?

A

D2 Receptor Antagonists

  • Galactorrhea (via PRL release)
  • Extra-pyramidal effects (Parkinsonism, Dystonia)
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17
Q

How does Metoclopramide work?

A
  • Increases ACh at mAChRs in gut-> Increased gastric emptying via;
  • Increased tone at LOS so it closes
  • Increased tone & amplitude of gastric contractions
  • Decreased tone of Pylorus so it opens
  • Increases GI peristalsis
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18
Q

Suggest 2 patient groups who Metoclopramide is good for?

A
  • GORD

- Ileus (Peristalsis stops, similar presentation to bowel obstruction)

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19
Q

How does Domperidone work?

List 1 patent group who its for
List 2 ADRs

A
  • Similar mechanism to Metoclopramide
  • Good for improving lactation in breastfeeding mothers (due to its ADR)
  • Galactorrhea
  • Sudden cardiac death (Long QT, VTach)
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20
Q

List all 7 of the Antiemetic agents that act on the CTZ

A
  • Muscarinic receptor antagonists
  • H1 receptor antagonists
  • 5HT3 receptor antagonists
  • D2 receptor antagonists (not all)
  • Corticosteoids
  • Cannabinoids
  • NK1 receptor antagonists
21
Q

What kind of drugs are;

  • Prochlorperazine (safe in pregnancy)
  • Chlorpromazine
  • Levomepromazine
  • Halopiderol
A

Antipsychotics: D2 receptor antagonists that work centrally, not peripherally

(Not Metoclopramide or Dompiderone)

22
Q

How do the ‘zine’ Antipsychotics work?

Suggest 2 patient groups that they are good for?

A
  • Act o CTZ
  • May block H1 and Muscarinic receptors
  • Motion sickness
  • Vertigo
23
Q

What does Halopiderol work on?

Suggest 2 patient groups it’s good for

A
  • Acts on CTZ
  • Chemotherapy
  • Palliation
24
Q

List 3 ADRs of the Antipsychotics

A
  • Sedation (especially Halopiderol)
  • Hypotension
  • Extra-pyramidal effects (Dystonia, Parkinsonism)
25
Q

What kind of drugs are Dexamethasone and Methylprednisolone?

What are 3 things they’re good for?

A
  • Corticosteroids (assumed to act on CTZ, possible D2 receptor antagonist properties)
  • Perioperative nausea and vomiting
  • Chemotherapy
  • Palliation
26
Q

What are 3 ADRs of Corticostetoroids?

A
  • Insomnia
  • Increased blood sugar
  • Increased appetite
27
Q

Are synthetic Cannabinoids cannabis?

Which one is used as an Antiemetic?

A

No

Nabilone

28
Q

Nabilone is assumed to act on the CTZ

What is it good for?
What are 2 ADRs

A
  • Chemotherapy but used as last line therapy
  • Dizziness
  • Drowsiness
29
Q

What kind of drugs are Aprepitant, Netupitant and Fosaprepitant?

How do they work?

A
  • NK1 Receptor Antagonists (Neurokenin 1)
  • Prevent action of Substance P at CTZ & Peripheral nerves
  • Boost effects of 5HT3 Receptor Antagonists
  • Anxiolytic and antidepressant properties
30
Q

What are NK1 Receptor Antagonists good for?

List 3 ADRs

A
  • Chemotherapy, especially for delayed emesis
  • Headache
  • Diarrhoea/ Constipation
  • Stevens-Johnson Syndrome
31
Q

Compare the use of Hyoscine hydrobromide and Cinnirazine in treating motion/ travel sickness

A

Hyoscine hydrobromide (Muscarinic Receptor Antagonist);

  • 1st line
  • Stronger sedative effects so good for kids/ passengers

Cinnirazine (H1 Receptor Antagonist);
- Fewer side effects so good for driver

32
Q

Prokinetics such as Metoclopramide and Domperidone are good to use for GORD and Ileus.

Suggest 2 occasions they’re bad to use?

A
  • Obstruction

- Risk of perforation

33
Q

What’s the usual combination of drugs used for vomiting due to bowel obstruction?

A
  • Ondansetron and/ or Cyclizine

- Then add Dexamethasone (if not working)

34
Q

Describe Hyperemesis Gravidarum

Higher risk with multiple pregnancies

A
  • Rapid rise in Beta-HCG stimulates CTZ-> Vomiting
  • Typically weeks 4-16, may continue beyond

(Dehydration, 5% weight loss, Urinary ketones, Electrolyte imbalance)

35
Q

What’s the routine treatment for Hyperemesis Gravidarum

A
  • Promethazine/ Prochlorperazine
  • Then add Metoclopramide
  • Then add Ondansetron

(Ondansetron has some evidence of Cleft lip/ palate if used in Trimester 1, so only if necessary)

36
Q

List 4 patient risk factors for PONV (Post-Op Nausea and Vomiting)

A
  • Female
  • Young
  • Non smoker
  • History of PONV/ motion sickness
37
Q

List 2 surgical risk factors for PONV

A
  • Longer surgery

- Laparoscopic surgery

38
Q

What’s the usual routine of treatment for PONV?

A
  • Ondansetron and/ or Cyclizine

- Then add Dexamethasone

39
Q

What kind of drugs are Codeine, Morphine and Loperamide?

What are they used for?

A
  • Opioid receptor agonists

- Treating diarrhoea

40
Q

Loperamide is specific to MOP receptors in the Myenteric Plexus.

List 3 ways it helps reduce diarrhoea

(Normally 1st line, takes 48 hours for maximal effect)

A
  • Reduces tone of Longitudinal and Circular smooth muscle
  • Reduces Peristalsis but increases segmental contractions
  • Decreases colonic mass movement by suppressing Gastrocolic reflex
41
Q

List ADRs of using Codeine and Morphine to treat diarrhoea

A
  • Paralytic ileus
  • Sedation
  • Addiction
  • Nausea and vomiting
42
Q

Describe the Constipating Diet, used for those with long-term diarrhoea

A
  • Bananas (high k+ and fibre)
  • White rice (binds stool)
  • Limit fruit to 3 portions per day
  • Avoid caffeine, sorbitol, spicy foods, fizzy drinks
43
Q

List diet and lifestyle changes to help constipation

A
  • More water
  • Increase fibre intake (Whole wheat, fruit + veg, nuts)
  • Regular exercise
44
Q

What drugs can be used to help constipation

A

Enemas;

  • Osmotic
  • Stimulants

Laxatives;

  • Osmotic (Lactulose, Macrogol)
  • Stimulant (Senna, Bisacodyl)
  • Bulk forming (Methylcellulose, Ispaghula husk)
  • Stool softeners (Docusate, Arachis oil)
45
Q

Lactulose, Movicol and Cosmocol are what kind of drugs?

How do they differ in their mechanism

A

Osmotic laxatives

  • Lactulose draws fluid into bowel
  • Macrogols retain the fluid they came with (Movicol & Cosmocol)
46
Q

Describe how Docusate Sodium works?

What are 2 effects of Glycerin suppositories

A

Docusate Sodium: Acts as a stimulant and stool softener

Glycerin Suppositories: Cause rectal irritation and lubrication

47
Q

What kind of drugs are Ispaghula husk and Methylcellulose?

A

Bulk forming laxatives

Soften the stool while bulking it up, basically extra fibre

48
Q

What class of drug contains;

  • Docusate Sodium
  • Glycerin Suppositories
  • Arachis oil
  • Liquid paraffin

How do they work?

A
  • Stool softeners
  • Decrease stool surface tension
  • Increase penetration of fluid into stool