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Pharmacology > Anti-emetics > Flashcards

Anti-emetics Flashcards

1
Q

What are the main classes of anti-emetics?

A 
H1 receptor antagonist
D2 receptor antagonist
5HT3 receptor antagonist 
Muscarinic receptor antagonist
Neurokinin-1 antagonist
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2
Q

What is the part of the brain that triggers vomiting?

A

Chemoreceptor trigger zone (CTZ)

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3
Q

What are the triggers for the CTZ?

A

Sensory afferents
Direct triggers (drugs/toxins)
Vestibular nuclei
Visceral afferents from gut

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4
Q

What classes act on the vestibular nuclei?

A

Muscarinic receptor antagonist

H1 receptor antagonist

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5
Q

What classes act on the gut?

A

5HT3 receptor antagonists

D2 receptor antagonists

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6
Q

What classes act on the CTZ?

A 
D2 receptor antagonist
5HT3 receptor antagonist 
Muscarinic receptor antagonist
H1 receptor antagonist
Neurokinin-1 receptor antagonist
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7
Q

What is an example of a muscarinic receptor antagonist?

A

Hyoscine hydrobromide

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8
Q

What is the mechanism of muscarinic receptor antagonist?

A

Blocks muscarinic ACh receptors - competitive inhibitor

  • vestibular nuclei
  • CTZ
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9
Q

What is hyoscine hydrobromide used for?

A

People who cant take tablets
Motion sickness
Bowel obstruction

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10
Q

What are the routes for hyoscine hydrobromide?

A

Patch
Oral
Subcutaneous

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11
Q

What are the side effects of hyoscine hydrobromide?

A 
Sedation 
Memory problems
Glaucoma 
Dry mouth 
Constipation
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12
Q

What are examples of H1 receptor antagonists?

A

Cyclizine

Promethazine

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13
Q

What is the mechanism of H1 receptor antagonists?

A

Inhibits histaminergic signals from vestibular system to CTZ

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14
Q

What is Cyclizine used for?

A

Nausea + Vomiting

Motion sickness

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15
Q

What are the routes of administration for Cyclizine?

A

Oral
IV
IM

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16
Q

Who is Cyclizine not ideal for?

A

Small old ladies
Children

Side effects are worse

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17
Q

What is promethazine used for?

A

Motion sickness

Morning sickness

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18
Q

What are the side effects of H1 receptor antagonists?

A 
Sedation 
Excitation 
Dry mouth 
Constipation 
Cardiac toxicity (long QT)
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19
Q

What classes act on visceral afferents in the gut?

A

5HT3 receptor antagonist

D2 receptor antagonist

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20
Q

What is 5HT also known as?

A

Serotonin

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21
Q

What is the effect of serotonin in the gut?

A

Excites enteric neurones

  • smooth muscle contraction
  • increases gut secretions

Regulates appetite

22
Q

What is an example of a 5HT3 receptor antagonist?

A

Ondansetron

23
Q

What is the mechanism of ondansetron?

A

Peripherally

  • reduces GI motility
  • reduces GI secretions

Centrally
- inhibits CTZ

24
Q

What is ondansetron used for?

A

Chemo nausea

Post-operative nausea

25
Q

What are the routes of administration for ondansetron?

A

Oral
PR
IM

26
Q

What are the side effects of ondansetron?

A

Constipation
Headache
Elevated liver enzymes
Long QT syndrome

27
Q

What are examples of D2 receptor antagonists that act in the gut?

A

Metoclopramide

Domperidone

28
Q

What is the mechanism of action for metoclopramide?

A

Increases ACh at muscarinic receptors in the gut

  • promotes gastric emptying
  • increases tone at LOS
  • decreases tone of pylorus
  • increases peristalsis
29
Q

What is metoclopramide used for?

A

Nausea
GORD
Ileus

30
Q

What are routes of administration of metoclopramide?

A

PO
IM
SC

31
Q

What are the side effects of metoclopramide?

A

Galactorrhoea

Extra-pyramidal effects

32
Q

What is the mechanism of domperidone?

A

Increases ACh at muscarinic receptors in the gut

  • promotes gastric emptying
  • increases tone at LOS
  • decreases tone of pylorus
  • increases peristalsis
33
Q

What is domperidone used for?

A

Nausea

34
Q

What is the route of administration for domperidone?

A

Oral

35
Q

What are the side effects of domperidone?

A

Sudden cardiac death (long QT + VT)

Galactorrhoea

36
Q

What classes act on the CTZ?

A

5HT3 receptor antagonists
H1 receptor antagonists
Muscarininc receptor
D2 receptor antagonist

37
Q

What are examples of D2 receptor antagonists that act on the CTZ?

A

Prochlorperazine
Chlorpromazine
Haloperidol

38
Q

What is chlorpromazine used for?

A

Motion sickness

Vertigo

39
Q

When is prochlorperazine used for?

A

Pregnancy

40
Q

What is haloperidol used for?

A

Nausea
Chemo/palliation
Schizophrenia
Delirium

41
Q

What are side effects of D2 receptor antagonists?

A

Extra-pyramidal effects

  • dystonia
  • parkinsonism

Sedation
Hypotension

42
Q

What are examples of neurokinin-1 receptor antagonists?

A

Aprepitant

Fosaprepitant

43
Q

What is the mechanism of action of neurokinin-1 receptor antagonists?

A

Prevents the action of substance P at the CTZ + peripheral nerves

Boosts effects of 5HT3 receptor antagonists

44
Q

What are neurokinin-1 receptor antagonists used for?

A

Chemo nausea

45
Q

What are the side effects of neurokinin-1 receptor antagonists?

A

Headache
Diarrhoea
Stevens-Johnson syndrome

46
Q

What is Stevens-Johnson syndrome?

A

Type of severe skin reaction

47
Q

What is the first line treatment for motion sickness?

A

Hyoscine hydrobromide

48
Q

Which anti-emetics are prokinetics?

A

Domperidone

Metoclopramide

49
Q

What are prokinetics used for?

A

GORD

Ileus

50
Q

When should you not use prokinetics?

A

Obstruction

Risk of perforation

51
Q

What are the anti-emetics used in bowel obstruction?

A

Ondansetron

Cyclizine

52
Q

Which anti-emetics are used in hyperemesis gravidarum?

A

Promethazine OR prochlorperazine

then add - metoclopramide

then add - ondansetron

Pharmacology (27 decks)

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